Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Substances that reduce the growth or reproduction of BACTERIA.
A group of antibiotics that contain 6-aminopenicillanic acid with a side chain attached to the 6-amino group. The penicillin nucleus is the chief structural requirement for biological activity. The side-chain structure determines many of the antibacterial and pharmacological characteristics. (Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1065)
One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.
The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.
Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.
Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.
Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.
Nonsusceptibility of an organism to the action of penicillins.
A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.
A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid.
The action of a drug in promoting or enhancing the effectiveness of another drug.
Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.
Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.
A cephalosporin antibiotic.
The ability of bacteria to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.
Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.
A beta-lactamase preferentially cleaving penicillins. (Dorland, 28th ed) EC 3.5.2.-.
Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS.
A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.
An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea.
A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection.
Bacteria which retain the crystal violet stain when treated by Gram's method.
A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.
Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.
A cephalosporin antibiotic.
An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.
Any liquid or solid preparation made specifically for the growth, storage, or transport of microorganisms or other types of cells. The variety of media that exist allow for the culturing of specific microorganisms and cell types, such as differential media, selective media, test media, and defined media. Solid media consist of liquid media that have been solidified with an agent such as AGAR or GELATIN.
Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.
Four-membered cyclic AMIDES, best known for the PENICILLINS based on a bicyclo-thiazolidine, as well as the CEPHALOSPORINS based on a bicyclo-thiazine, and including monocyclic MONOBACTAMS. The BETA-LACTAMASES hydrolyze the beta lactam ring, accounting for BETA-LACTAM RESISTANCE of infective bacteria.
Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)
A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.
An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.
Oils which evaporate readily. The volatile oils occur in aromatic plants, to which they give odor and other characteristics. Most volatile oils consist of a mixture of two or more TERPENES or of a mixture of an eleoptene (the more volatile constituent of a volatile oil) with a stearopten (the more solid constituent). The synonym essential oils refers to the essence of a plant, as its perfume or scent, and not to its indispensability.
The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
Semisynthetic wide-spectrum cephalosporin with prolonged action, probably due to beta-lactamase resistance. It is used also as the nafate.
Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method.
Semisynthetic broad-spectrum cephalosporin.
Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.
A family of gram-negative, facultatively anaerobic, rod-shaped bacteria that do not form endospores. Its organisms are distributed worldwide with some being saprophytes and others being plant and animal parasites. Many species are of considerable economic importance due to their pathogenic effects on agriculture and livestock.
Enzymes found in many bacteria which catalyze the hydrolysis of the amide bond in the beta-lactam ring. Well known antibiotics destroyed by these enzymes are penicillins and cephalosporins.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections.
A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.
A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208)
A genus of gram-positive, facultatively anaerobic, coccoid bacteria. Its organisms occur singly, in pairs, and in tetrads and characteristically divide in more than one plane to form irregular clusters. Natural populations of Staphylococcus are found on the skin and mucous membranes of warm-blooded animals. Some species are opportunistic pathogens of humans and animals.
A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.
Substances that are destructive to protozoans.
A species of gram-negative, aerobic bacteria primarily found in purulent venereal discharges. It is the causative agent of GONORRHEA.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.
Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It has been proposed especially against Pseudomonas infections.
A kingdom of eukaryotic, heterotrophic organisms that live parasitically as saprobes, including MUSHROOMS; YEASTS; smuts, molds, etc. They reproduce either sexually or asexually, and have life cycles that range from simple to complex. Filamentous fungi, commonly known as molds, refer to those that grow as multicellular colonies.
A group of QUINOLONES with at least one fluorine atom and a piperazinyl group.
An imidazole antifungal agent that is used topically and by intravenous infusion.
A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.
Naturally occurring family of beta-lactam cephalosporin-type antibiotics having a 7-methoxy group and possessing marked resistance to the action of beta-lactamases from gram-positive and gram-negative organisms.
A unicellular budding fungus which is the principal pathogenic species causing CANDIDIASIS (moniliasis).
Closely congeneric derivatives of the polycyclic naphthacenecarboxamide. (Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1117)
A strain of Staphylococcus aureus that is non-susceptible to the action of METHICILLIN. The mechanism of resistance usually involves modification of normal or the presence of acquired PENICILLIN BINDING PROTEINS.
A broad-spectrum antimicrobial carboxyfluoroquinoline.
A sweet viscous liquid food, produced in the honey sacs of various bees from nectar collected from flowers. The nectar is ripened into honey by inversion of its sucrose sugar into fructose and glucose. It is somewhat acidic and has mild antiseptic properties, being sometimes used in the treatment of burns and lacerations.
An antibiotic first isolated from cultures of Streptomyces venequelae in 1947 but now produced synthetically. It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered. It acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra Pharmacopoeia, 29th ed, p106)
A genus of yeast-like mitosporic Saccharomycetales fungi characterized by producing yeast cells, mycelia, pseudomycelia, and blastophores. It is commonly part of the normal flora of the skin, mouth, intestinal tract, and vagina, but can cause a variety of infections, including CANDIDIASIS; ONYCHOMYCOSIS; vulvovaginal candidiasis (CANDIDIASIS, VULVOVAGINAL), and thrush (see CANDIDIASIS, ORAL). (From Dorland, 28th ed)
A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES rimosus and used in a wide variety of clinical conditions.
Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.
Cyclic AMIDES formed from aminocarboxylic acids by the elimination of water. Lactims are the enol forms of lactams.
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.
Infections with bacteria of the genus STAPHYLOCOCCUS.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.
A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.
An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.
A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS. It has also been proposed as a radiation sensitizer for hypoxic cells. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985, p133), this substance may reasonably be anticipated to be a carcinogen (Merck, 11th ed).
Nonsusceptibility of bacteria to the action of VANCOMYCIN, an inhibitor of cell wall synthesis.
Five membered rings containing a NITROGEN atom.
Plants whose roots, leaves, seeds, bark, or other constituent parts possess therapeutic, tonic, purgative, curative or other pharmacologic attributes, when administered to man or animals.
A broad-spectrum cephalosporin antibiotic with a very long half-life and high penetrability to meninges, eyes and inner ears.
The outer layer of the woody parts of plants.
A gram-positive organism found in the upper respiratory tract, inflammatory exudates, and various body fluids of normal and/or diseased humans and, rarely, domestic animals.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in the intestines of humans and a wide variety of animals, as well as in manure, soil, and polluted waters. Its species are pathogenic, causing urinary tract infections and are also considered secondary invaders, causing septic lesions at other sites of the body.
Semisynthetic, broad-spectrum antibacterial derived from CEPHALORIDINE and used especially for Pseudomonas and other gram-negative infections in debilitated patients.
A method where a culturing surface inoculated with microbe is exposed to small disks containing known amounts of a chemical agent resulting in a zone of inhibition (usually in millimeters) of growth of the microbe corresponding to the susceptibility of the strain to the agent.
A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A semisynthetic cephamycin antibiotic resistant to beta-lactamase.
An antibiotic derived from penicillin similar to CARBENICILLIN in action.
Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.
A mitosporic Oxygenales fungal genus causing various diseases of the skin and hair. The species Microsporum canis produces TINEA CAPITIS and tinea corporis, which usually are acquired from domestic cats and dogs. Teleomorphs includes Arthroderma (Nannizzia). (Alexopoulos et al., Introductory Mycology, 4th edition, p305)
The ability of fungi to resist or to become tolerant to chemotherapeutic agents, antifungal agents, or antibiotics. This resistance may be acquired through gene mutation.
A genus of gram-negative, facultatively anaerobic, rod-shaped bacteria whose organisms arrange singly, in pairs, or short chains. This genus is commonly found in the intestinal tract and is an opportunistic pathogen that can give rise to bacteremia, pneumonia, urinary tract and several other types of human infection.
A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.
A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
A building block of penicillin, devoid of significant antibacterial activity. (From Merck Index, 11th ed)
Proteins found in any species of bacterium.
A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.
Encrustations, formed from microbes (bacteria, algae, fungi, plankton, or protozoa) embedding in extracellular polymers, that adhere to surfaces such as teeth (DENTAL DEPOSITS); PROSTHESES AND IMPLANTS; and catheters. Biofilms are prevented from forming by treating surfaces with DENTIFRICES; DISINFECTANTS; ANTI-INFECTIVE AGENTS; and antifouling agents.
A genus of gram-positive, coccoid bacteria whose organisms occur in pairs or chains. No endospores are produced. Many species exist as commensals or parasites on man or animals with some being highly pathogenic. A few species are saprophytes and occur in the natural environment.
Amphoteric macrolide antifungal antibiotic from Streptomyces natalensis or S. chattanoogensis. It is used for a variety of fungal infections, mainly topically.
Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.
A complex sulfated polymer of galactose units, extracted from Gelidium cartilagineum, Gracilaria confervoides, and related red algae. It is used as a gel in the preparation of solid culture media for microorganisms, as a bulk laxative, in making emulsions, and as a supporting medium for immunodiffusion and immunoelectrophoresis.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
A species of gram-positive, coccoid bacteria commonly isolated from clinical specimens and the human intestinal tract. Most strains are nonhemolytic.
A fluorinated cytosine analog that is used as an antifungal agent.
Gram-negative, non-motile, capsulated, gas-producing rods found widely in nature and associated with urinary and respiratory infections in humans.
An antibiotic complex produced by Streptomyces kitasatoensis. The complex consists of a mixture of at least eight biologically active components, A1 and A3 to A9. Leucomycins have both antibacterial and antimycoplasmal activities.
Gram-negative bacteria occurring in the lower intestinal tracts of man and other animals. It is the most common species of anaerobic bacteria isolated from human soft tissue infections.
A genus of gram-positive, anaerobic bacteria whose organisms divide in three perpendicular planes and occur in packets of eight or more cells. It has been isolated from soil, grains, and clinical specimens.
Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.
An amidinopenicillanic acid derivative with broad spectrum antibacterial action.
One of the PENICILLINS which is resistant to PENICILLINASE but susceptible to a penicillin-binding protein. It is inactivated by gastric acid so administered by injection.
A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.
A seven-membered aromatic ring compound. It is structurally related to a number of naturally occurring antifungal compounds (ANTIFUNGAL AGENTS).
An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.
A species of HAEMOPHILUS found on the mucous membranes of humans and a variety of animals. The species is further divided into biotypes I through VIII.
Ability of a microbe to survive under given conditions. This can also be related to a colony's ability to replicate.
Compounds with a core of 10 carbons generally formed via the mevalonate pathway from the combination of 3,3-dimethylallyl pyrophosphate and isopentenyl pyrophosphate. They are cyclized and oxidized in a variety of ways. Due to the low molecular weight many of them exist in the form of essential oils (OILS, VOLATILE).
A mitosporic fungal genus and an anamorphic form of Arthroderma. Various species attack the skin, nails, and hair.
The rate dynamics in chemical or physical systems.
Basic lipopeptide antibiotic group obtained from Bacillus polymyxa. They affect the cell membrane by detergent action and may cause neuromuscular and kidney damage. At least eleven different members of the polymyxin group have been identified, each designated by a letter.
A methylsulfonyl analog of CHLORAMPHENICOL. It is an antibiotic and immunosuppressive agent.
Derivatives of acetamide that are used as solvents, as mild irritants, and in organic synthesis.
A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.
Acute infectious disease characterized by primary invasion of the urogenital tract. The etiologic agent, NEISSERIA GONORRHOEAE, was isolated by Neisser in 1879.
Beta-lactam antibiotics that differ from PENICILLINS in having the thiazolidine sulfur atom replaced by carbon, the sulfur then becoming the first atom in the side chain. They are unstable chemically, but have a very broad antibacterial spectrum. Thienamycin and its more stable derivatives are proposed for use in combinations with enzyme inhibitors.
An antifungal agent used in the treatment of TINEA infections.
Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.
2-Hydroxy-N-phenylbenzamides. N-phenyl substituted salicylamides. Derivatives have been used as fungicides, anti-mildew agents and topical antifungal agents. In concentrated form may cause irritation of skin and mucous membranes.
A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.
Drugs used in the treatment of tuberculosis. They are divided into two main classes: "first-line" agents, those with the greatest efficacy and acceptable degrees of toxicity used successfully in the great majority of cases; and "second-line" drugs used in drug-resistant cases or those in which some other patient-related condition has compromised the effectiveness of primary therapy.
Infections by bacteria, general or unspecified.
Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)
Elements of limited time intervals, contributing to particular results or situations.
A compound used to treat histomoniasis in poultry.
Antiprotozoal and antimicrobial agent used mainly in veterinary practice.
Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity.
A serotype of SALMONELLA ENTERICA that causes mild PARATYPHOID FEVER in humans.
Loss of epithelial tissue from the surface of the cornea due to progressive erosion and necrosis of the tissue; usually caused by bacterial, fungal, or viral infection.
The sumac plant family in the order Sapindales, subclass Rosidae, class Magnoliopsida. They are tropical and subtropical trees, shrubs, and woody vines that have resin ducts in the bark. The sap of many of the species is irritating to the skin.
A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
Macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.
A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Gyrase binds to DNA as a heterotetramer consisting of two A and two B subunits. In the presence of ATP, gyrase is able to convert the relaxed circular DNA duplex into a superhelix. In the absence of ATP, supercoiled DNA is relaxed by DNA gyrase.
Enumeration by direct count of viable, isolated bacterial, archaeal, or fungal CELLS or SPORES capable of growth on solid CULTURE MEDIA. The method is used routinely by environmental microbiologists for quantifying organisms in AIR; FOOD; and WATER; by clinicians for measuring patients' microbial load; and in antimicrobial drug testing.
Therapy with two or more separate preparations given for a combined effect.
The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion.
A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.
Analog of KANAMYCIN with antitubercular as well as broad-spectrum antimicrobial properties.
Established cell cultures that have the potential to propagate indefinitely.
Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.
The ability of fungi to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance phenotype may be attributed to multiple gene mutations.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.
A serotype of SALMONELLA ENTERICA which is the etiologic agent of TYPHOID FEVER.
Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.
Non-susceptibility of a microbe to the action of METHICILLIN, a semi-synthetic penicillin derivative.
A plant genus of the family EUPHORBIACEAE. The common name of dragon's blood is also used for DRACAENA and Daemonorops (ARECACEAE). Croton tiglium is the source of CROTON OIL.
Nonsusceptibility of bacteria to the action of the beta-lactam antibiotics. Mechanisms responsible for beta-lactam resistance may be degradation of antibiotics by BETA-LACTAMASES, failure of antibiotics to penetrate, or low-affinity binding of antibiotics to targets.
The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.
Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.
A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients.
The L-isomer of Ofloxacin.
Substances used on humans and other animals that destroy harmful microorganisms or inhibit their activity. They are distinguished from DISINFECTANTS, which are used on inanimate objects.
Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.
Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA.
An alkaloid derived from the bark of the cinchona tree. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona that have been used for that purpose since before 1633. Quinine is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Quinine is also useful in some muscular disorders, especially nocturnal leg cramps and myotonia congenita, because of its direct effects on muscle membrane and sodium channels. The mechanisms of its antimalarial effects are not well understood.
A plant genus of the family LAMIACEAE that contains eudesmane sesquiterpenes and antimicrobial abietane diterpenoids.
A plant genus of the family RHAMNACEAE. Members contain nummularogenin (a spirostane) and is the source of an edible fruit.
An antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by inhibiting the initiation and elongation processes during protein synthesis.
A semisynthetic ampicillin-derived acylureido penicillin.
An imidazole derivative with a broad spectrum of antimycotic activity. It inhibits biosynthesis of the sterol ergostol, an important component of fungal CELL MEMBRANES. Its action leads to increased membrane permeability and apparent disruption of enzyme systems bound to the membrane.
A genus of mitosporic fungi containing about 100 species and eleven different teleomorphs in the family Trichocomaceae.
Bacterial proteins that share the property of binding irreversibly to PENICILLINS and other ANTIBACTERIAL AGENTS derived from LACTAMS. The penicillin-binding proteins are primarily enzymes involved in CELL WALL biosynthesis including MURAMOYLPENTAPEPTIDE CARBOXYPEPTIDASE; PEPTIDE SYNTHASES; TRANSPEPTIDASES; and HEXOSYLTRANSFERASES.
Use of plants or herbs to treat diseases or to alleviate pain.
Six-carbon alicyclic hydrocarbons.
A genus of gram-positive, coccoid bacteria consisting of organisms causing variable hemolysis that are normal flora of the intestinal tract. Previously thought to be a member of the genus STREPTOCOCCUS, it is now recognized as a separate genus.
A species of ACTINOMYCES found in the oral cavity of man and hamsters. It has been isolated from actinomycotic lesions in swine, cats, and dogs and has been identified as a causative agent of animal diseases.
A genus of gram-negative bacteria of the family MORAXELLACEAE, found in soil and water and of uncertain pathogenicity.
A genus of gram-negative, anaerobic, rod-shaped bacteria. Its organisms are normal inhabitants of the oral, respiratory, intestinal, and urogenital cavities of humans, animals, and insects. Some species may be pathogenic.
Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.
QUINOLONES containing a 4-oxo (a carbonyl in the para position to the nitrogen). They inhibit the A subunit of DNA GYRASE and are used as antimicrobials. Second generation 4-quinolones are also substituted with a 1-piperazinyl group at the 7-position and a fluorine at the 6-position.
Enzyme which catalyzes the peptide cross-linking of nascent CELL WALL; PEPTIDOGLYCAN.
The mallow family of the order Malvales, subclass Dilleniidae, class Magnoliopsida. Members include GOSSYPIUM, okra (ABELMOSCHUS), HIBISCUS, and CACAO. The common names of hollyhock and mallow are used for several genera of Malvaceae.
Acyltransferases that use AMINO ACYL TRNA as the amino acid donor in formation of a peptide bond. There are ribosomal and non-ribosomal peptidyltransferases.
Clavulanic acid and its salts and esters. The acid is a suicide inhibitor of bacterial beta-lactamase enzymes from Streptomyces clavuligerus. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.
The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity.
Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.

Basic homopolyamino acids, histones and protamines are potent antagonists of angiogenin binding to ribonuclease inhibitor. (1/4054)

A radio-ribonuclease inhibitor assay based on the interaction of 125I-angiogenin with ribonuclease inhibitor (RI) was used to detect pancreatic-type ribonucleases and potential modulators of their action. We show that highly basic proteins including the homopolypeptides poly-arginine, poly-lysine and poly-ornithine, core histones, spermatid-specific S1 protein and the protamines HP3 and Z3 were strong inhibitors of angiogenin binding to RI. A minimum size of poly-arginine and poly-lysine was required for efficient inhibition. The inhibition likely resulted from direct association of the basic proteins with the acidic inhibitor, as RI bound to poly-lysine and protamines while 125I-angiogenin did not. Antagonists of the angiogenin-RI interaction are potential regulators of either angiogenin-triggered angiogenesis and/or intracellular RI function, depending on their preferential target.  (+info)

Overexpression of the multidrug resistance-associated protein (MRP1) in human heavy metal-selected tumor cells. (2/4054)

Cellular and molecular mechanisms involved in the resistance to cytotoxic heavy metals remain largely to be characterized in mammalian cells. To this end, we have analyzed a metal-resistant variant of the human lung cancer GLC4 cell line that we have selected by a step-wise procedure in potassium antimony tartrate. Antimony-selected cells, termed GLC4/Sb30 cells, poorly accumulated antimony through an enhanced cellular efflux of metal, thus suggesting up-regulation of a membrane export system in these cells. Indeed, GLC4/Sb30 cells were found to display a functional overexpression of the multidrug resistance-associated protein MRP1, a drug export pump, as demonstrated by Western blotting, reverse transcriptase-polymerase chain reaction and calcein accumulation assays. Moreover, MK571, a potent inhibitor of MRP1 activity, was found to markedly down-modulate resistance of GLC4/Sb30 cells to antimony and to decrease cellular export of the metal. Taken together, our data support the conclusion that overexpression of functional MRP1 likely represents one major mechanism by which human cells can escape the cytotoxic effects of heavy metals.  (+info)

Nitric oxide inhibits cardiac energy production via inhibition of mitochondrial creatine kinase. (3/4054)

Nitric oxide biosynthesis in cardiac muscle leads to a decreased oxygen consumption and lower ATP synthesis. It is suggested that this effect of nitric oxide is mainly due to the inhibition of the mitochondrial respiratory chain enzyme, cytochrome c oxidase. However, this work demonstrates that nitric oxide is able to inhibit soluble mitochondrial creatine kinase (CK), mitochondrial CK bound in purified mitochondria, CK in situ in skinned fibres as well as the functional activity of mitochondrial CK in situ in skinned fibres. Since mitochondrial isoenzyme is functionally coupled to oxidative phosphorylation, its inhibition also leads to decreased sensitivity of mitochondrial respiration to ADP and thus decreases ATP synthesis and oxygen consumption under physiological ADP concentrations.  (+info)

Alternative oxidase inhibitors potentiate the activity of atovaquone against Plasmodium falciparum. (4/4054)

Recent evidence suggests that the malaria parasite Plasmodium falciparum utilizes a branched respiratory pathway including both a cytochrome chain and an alternative oxidase. This branched respiratory pathway model has been used as a basis for examining the mechanism of action of two antimalarial agents, atovaquone and proguanil. In polarographic assays, atovaquone immediately reduced the parasite oxygen consumption rate in a concentration-dependent manner. This is consistent with its previously described role as an inhibitor of the cytochrome bc1 complex. Atovaquone maximally inhibited the rate of P. falciparum oxygen consumption by 73% +/- 10%. At all atovaquone concentrations tested, the addition of the alternative oxidase inhibitor, salicylhydroxamic acid, resulted in a further decrease in the rate of parasite oxygen consumption. At the highest concentrations of atovaquone tested, the activities of salicylhydroxamic acid and atovaquone appear to overlap, suggesting that at these concentrations, atovaquone partially inhibits the alternative oxidase as well as the cytochrome chain. Drug interaction studies with atovaquone and salicylhydroxamic acid indicate atovaquone's activity against P. falciparum in vitro is potentiated by this alternative oxidase inhibitor, with a sum fractional inhibitory concentration of 0.6. Propyl gallate, another alternative oxidase inhibitor, also potentiated atovaquone's activity, with a sum fractional inhibitory concentration of 0.7. Proguanil, which potentiates atovaquone activity in vitro and in vivo, had a small effect on parasite oxygen consumption in polarographic assays when used alone or in the presence of atovaquone or salicylhydroxamic acid. This suggests that proguanil does not potentiate atovaquone by direct inhibition of either branch of the parasite respiratory chain.  (+info)

Inhibitory effect of sulfur-containing compounds in Scorodocarpus borneensis Becc. on the aggregation of rabbit platelets. (5/4054)

The inhibitory effects of three pure compounds isolated from wood garlic, 2,4,5-trithiahexane (I), 2,4,5,7-tetrathiaoctane (II), and 2,4,5,7-tetrathiaoctane 2,2-dioxide (III), on rabbit platelet aggregation induced by collagen, arachidonic acid, U46619, ADP (adenosine 5'-diphosphate), PAF (platelet aggregating factor), and thrombin were studied in vitro. The anti-aggregating activity of 2,4,5,7-tetrathiaoctane 4,4-dioxide (IV) was also measured with collagen and arachidonic acid. I, II, III, and IV inhibited the platelet aggregation induced by all tested agonists. I, II, and III exhibited a stronger inhibitory effect against the thrombin-induced aggregation of GFP (gel-filtered platelets) than against the aggregation induced by the other agonists. Notably, the IC50 value for III was 4 microM, which is approximately 2.5 times stronger than MATS (methyl allyl trisulfide), a major anti-platelet compound isolated from garlic. In inhibiting collagen-induced aggregation, II was as potent as MATS and aspirin, with a marked disaggregation effect on the secondary aggregation by arachidonic acid, at the rate of 47.05%/min at a concentration of 10(-4) M. I, II, and III also suppressed U46619-induced aggregation. These results suggest that sulfur-containing compounds in wood garlic not only inhibit arachidonic acid metabolism but also suppress aggregation in association with the function of the platelet plasma membrane.  (+info)

A three-dimensional construction of the active site (region 507-749) of human neutral endopeptidase (EC. (6/4054)

A three-dimensional model of the 507-749 region of neutral endopeptidase-24.11 (NEP; E.C. was constructed integrating the results of secondary structure predictions and sequence homologies with the bacterial endopeptidase thermolysin. Additional data were extracted from the structure of two other metalloproteases, astacin and stromelysin. The resulting model accounts for the main biological properties of NEP and has been used to describe the environment close to the zinc atom defining the catalytic site. The analysis of several thiol inhibitors, complexed in the model active site, revealed the presence of a large hydrophobic pocket at the S1' subsite level. This is supported by the nature of the constitutive amino acids. The computed energies of bound inhibitors correspond with the relative affinities of the stereoisomers of benzofused macrocycle derivatives of thiorphan. The model could be used to facilitate the design of new NEP inhibitors, as illustrated in the paper.  (+info)

Molecular recognition of fatty acids by peroxisome proliferator-activated receptors. (7/4054)

The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors for fatty acids (FAs) that regulate glucose and lipid homeostasis. We report the crystal structure of the PPAR delta ligand-binding domain (LBD) bound to either the FA eicosapentaenoic acid (EPA) or the synthetic fibrate GW2433. The carboxylic acids of EPA and GW2433 interact directly with the activation function 2 (AF-2) helix. The hydrophobic tail of EPA adopts two distinct conformations within the large hydrophobic cavity. GW2433 occupies essentially the same space as EPA bound in both conformations. These structures provide molecular insight into the propensity for PPARs to interact with a variety of synthetic and natural compounds, including FAs that vary in both chain length and degree of saturation.  (+info)

Inhibition of gene expression by anti-sense C-5 propyne oligonucleotides detected by a reporter enzyme. (8/4054)

Using a reporter plasmid containing the luciferase gene under the control of the insulin-like growth factor 1 (IGF-1) promoter region [including its 5' untranslated region (UTR)], we demonstrate that a 17-mer oligophosphorothioate containing C-5 propyne pyrimidines is able to inhibit luciferase gene expression in the nanomolar concentration range when the anti-sense oligonucleotide is targeted either to a coding sequence in the luciferase gene or to the 5' UTR of the gene for IGF-1. Inhibition was obtained independently of whether the plasmid and the anti-sense oligonucleotide were co-transfected or transfected separately into hepatocarcinoma cells. However, the efficiency of inhibition by the anti-sense oligonucleotides was 10-fold greater in the first case. The unmodified oligophosphorothioate targeted to the 5' UTR of IGF-1 did not inhibit luciferase gene expression at a 100-fold higher concentration unless its length was increased from 17 to 21 nt, in which case an inhibition of gene expression was obtained and an IC50 of 200 nM was observed.  (+info)

Pingyangmycin is an anticancer drug known as bleomycin A5 (A5), discovered in the Pingyang County of Zhejiang Province of China. Bleomycin (BLM) is a mixture of mainly two compounds (A2 and B2), which is on the World Health Organizations list of essential medicines. Both BLM and A5 are hydrophilic molecules that depend on transporters or endocytosis receptors to get inside of cells. Once inside, the anticancer activities rely on their abilities to produce DNA breaks, thus leading to cell death. Interestingly, the half maximal inhibitory concentration (IC50) of BLMs in different cancer cell lines varies from nM to μM ranges. Different cellular uptake, DNA repair rate, and/or increased drug detoxification might be some of the reasons; however, the molecules and signaling pathways responsible for these processes are largely unknown. In the current study, we purified the A2 and B2 from the BLM and tested the cytotoxicities and the molecular mechanisms of each individual compound or in combination with six
In last decades, biologically active natural compound (R)-goniothalamin and its derivatives received great attention from researchers. The reason for this interest is the wide range of biological properties of goniothalamin; including anti-microbial, antiprotozoan, anti-inflammatory, cytotoxic and anti-proliferative activities. The present study sets out the asymmetric large scale synthesis of α,β- unsaturated lactone derivative (R)-(+)-6-(2-Methylnaphthalen-1-yl)-5,6-dihydro-2Hpyran- 2-one. In recent studies, this linker modified analog of goniothalamin was shown to be cytotoxic against PC-3 (prostate cancer) and MCF-7 (human breast cancer) cell lines with half maximal inhibitory concentration values of 0.13 μM and 2.6 μM, respectively. The preparation of the target compound consists of three steps. First, asymmetric synthesis of homoallylic alcohol using (R)-Tol-BINAP AgF catalyst complex was performed with allyltrimethoysilane. After that, treating the chiral homoallylic alcohol ...
ABSTRACT The present study aims to investigate the cytotoxic effect of the major aflatoxins (B1, B2, G2 and G2) and also aflatoxin combination, using a simple, rapid and cheap cytotoxicity test like MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay in three in vitro models (human umbilical vein endothelial cells [HUVEC], human lung fibroblasts [HFL] and A2780 cell line) and to extrapolate the data to in vivo situation using a prediction model. A difference in cell sensitivity has been observed for B1 and B1 + B2, in the following order A2789 > HFL > HUVEC, while for B2, G1, G2, Mix (B1 + B2 + G1 + G2) the order was HFL > A2789 > HUVEC when comparing the IC50 (half maximal inhibitory concentration) values. We confirm that in vitro cytotoxicity test MTT assay is able to predict in vivo toxicity, at least for aflatoxins using the prediction model. The values of LD50 (lethal dose 50%) calculated from experiments are different for each cell line. This fact may indicate that ...
BioAssay record AID 64221 submitted by ChEMBL: In vitro minimum inhibition concentration against Escherichia coli D21f2, LPS mutant; Range is from 25-50.
Cadmium (Cd) is harmful for humans and animals, especially for the reproductive system. However, the mechanism of its toxicity has not been elucidated, and how to alleviate its toxicity is very important. This study aimed to explore the role and mechanism of action of sulforaphane (SFN) in protecting mouse Leydigs (TM3) cells from cadmium (Cd)-induced damage. The half-maximal inhibitory concentration (IC50) of Cd and the safe doses of SFN were determined using a methyl thiazolyl tetrazolium (MTT) assay. The testosterone secretion from TM3 cells was measured using the enzyme-linked immunosorbent assay. The intracellular oxidative stress was evaluated using corresponding kits. The cell apoptosis was detected using flow cytometry. The mRNA expression of genes associated with NF-E2-related factor 2 (Nrf2)/antioxidant response element (ARE) signaling was detected using reverse transcriptionâ »polymerase chain reaction, including Nrf2, heme oxygenase I (HO-1), glutathione peroxidase (GSH-Px), ...
In this study we (i) calculated half-maximal inhibitory concentrations (IC.sub.50) by motility tests against O. felineus adults and newly excysted metacercarie ...
WK23 is an inhibitor based on four aromatic groups and able to efficiently fill the binding pockets of MDM2/MDMX, its median inhibitory concentration (IC50) values to MDM2/MDMX are 1.17 and 36 uM, respectively
1 FPL 63547, in its active diacid form, was a potent inhibitor of rabbit lung angiotensin converting enzyme (ACE) in vitro (IC50… Expand ...
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Purpose: The PI3K/AKT/mTOR pathway is one of the most highly activated cellular signaling pathways in advanced ovarian cancer. Although several PI3K/AKT/mTOR inhibitors have been developed to treat various types of cancer, the antitumor efficacy of many of these compounds against ovarian cancer has remained unclear.. Methods: Here, we tested and compared a panel of 16 PI3K/AKT/mTOR inhibitors (XL765, Miltefosine, Rapamycin, CCI-779, RAD001, FK506, XL147, GSK2110183, IPI-145, GSK2141795, BYL719, GSK458, CAL-101, XL765 analogue SAR245409, Triciribine, and GDC0941) that have entered clinical trials for antitumor activity against ovarian cancer, as well as the front line drug, paclitaxel. Antitumor efficacy was measured in both ovarian cancer cell lines and patient-derived ovarian primary tumor cell lines in vitro and in vivo.. Results: We identified the PI3K/mTOR dual inhibitor GSK458 as a potent inhibitor of proliferation in all cell lines tested at half maximal inhibitory concentrations (IC50) of ...
A8326 AZD-5438 AZD5438 is a potent small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with half maximal inhibitory concentration IC50 of 16 nmol/L, 6 nmol/L and 20 nmol/L respectively. AZD5438 has also been found to potently inhibit the human cyclin E/CDK2 complex, the cyclin B1/CDK1 complex and the cyclin A/CDK2 complex with IC50 of 0.006 μM, 0.016 μM and 0.045 μM respectively. In previous studies, AZD5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with IC50 ranging from 0.2 μmol/L to 1.7 μmol/L, in which the phosphorylation of a few proteins, including CDK substrates pRb, nucleolin, protein phosphatase 1a and RNA polymerase II COOH-terminal domain, and cell cycling at G2-M, S and G1 phases were inhibited. ...
Curcumin (1) and ten derivatives (2-11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.
IL-12, a heterodimeric cytokine, consists of two disulfide-linked subunits, p40 and p35. We investigated the role of p40 in ligand binding and signal transduction by expressing this subunit alone in COS cells. Culture media of the transfected COS cells exhibited specific dose-dependent binding to KIT225/K6 cells, a human T cell line that expresses IL-12R. Analysis of the culture media by SDS-PAGE and Western blotting demonstrated the presence of 40-kDa monomers and 80-kDa disulfide-linked homodimers. The two p40 species were purified and identified by N-terminal sequencing and proteolytic peptide mapping. Characterization of the p40 proteins for binding and bioactivity showed that both the p40 monomer and dimer inhibited 125I-labeled IL-12 binding to IL-12R, but the 80-kDa species, having a 50% inhibitory concentration (IC50) of 20 to 70 ng/ml, was at least 20-fold more effective than the monomer. Although neither the monomer nor the dimer stimulated human PHA-blast proliferation, the 80-kDa ...
BioAssay record AID 594378 submitted by ChEMBL: Cell cycle arrest in human K562 cells assessed as accumulation at G0-G1 phase at IC100 after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 43.40%).
ICカードケース / タータンチェックSANS-SERIFバッグの特徴は、イギリス・ロンドンバスで実際に使用された、タイベック製のデスティネーションサイン(バスの前面で回転して変わる行き先案内表示)を素材にし、京都の鞄職人よる縫製技術によって、1つずつ手作業で丁寧に縫い上げる、全てデザインが異なる一点物のバッグです。従来モデルのスタイルを継承しながら、京都府産学公連携として京都精華大学テキスタイル学科とのコラボレーションによって製品化したプロダクトです。金蘭の端切れや廃棄される洋服のタータンチェックやデニム生地をアップサイクルしたICカードケースです。相反する印象の素材同士がうまく融合した独特のテイストのプロダクトです。裏地はベルベットを使用
Dengue is a major mosquito-borne disease currently with no effective antiviral or vaccine available. Effort to find antivirals for it has focused on bioflavonoids, a plant-derived polyphenolic compounds with many potential health benefits. In the present study, antiviral activity of four types of bioflavonoid against dengue virus type -2 (DENV-2) in Vero cell was evaluated. Anti-dengue activity of these compounds was determined at different stages of DENV-2 infection and replication cycle. DENV replication was measured by Foci Forming Unit Reduction Assay (FFURA) and quantitative RT-PCR. Selectivity Index value (SI) was determined as the ratio of cytotoxic concentration 50 (CC50) to inhibitory concentration 50 (IC50) for each compound. The half maximal inhibitory concentration (IC50) of quercetin against dengue virus was 35.7 μg mL-1 when it was used after virus adsorption to the cells. The IC50 decreased to 28.9 μg mL-1 when the cells were treated continuously for 5 h before virus infection and up to
Betulinic acid (BA) is a novel antineoplastic agent under evaluation for tumor therapy. Because of the selective cytotoxic effects of BA in tumor cells (including gliomas), the combination of this agent with conservative therapies (such as radiotherapy and chemotherapy) may be useful. Previously, the combination of BA with irradiation under hypoxic conditions had never been studied. In this study, the effects of 3 to 30 μM BA on cytotoxicity, migration, the protein expression of PARP, survivin and HIF-1α, as well as radiosensitivity under normoxic and hypoxic conditions were analyzed in the human malignant glioma cell lines U251MG and U343MG. Cytotoxicity and radiosensitivity were analyzed with clonogenic survival assays, migration was analyzed with Boyden chamber assays (or scratch assays) and protein expression was examined with Western blot analyses. Under normoxic conditions, a half maximal inhibitory concentration (IC50) of 23 μM was observed in U251MG cells and 24 μM was observed in U343MG
The study was carried out to evaluate the antioxidant activity and α-amylase activity inhibitory potential of Sarotherodon galillaeus muscle protein hydrolysates. Sarotherodon galillaeus muscle protein isolate was hydrolysed with three digestive proteases namely trypsin, chymotrypsin and pepsin. Degree of hydrolysis was determined. The antioxidative potential of the hydrolysates was investigated using DPPH radical scavenging, ferric reducing power, hydrogen peroxide scavenging and metal chelating activity. The ability of the hydrolysates to inhibit the activity of sugar-hydrolysing enzyme was also evaluated. Highest degree of hydrolysis was obtained with pepsin (55.86%) followed by trypsin (47.11%) and chymotrypsin (42.36%) after 6 hrs of hydrolysis. The half maximal inhibitory concentration (IC50) of hydrolysates produced by trypsin, chymotrypsin and pepsin for DPPH radical scavenging activity were 1.26 ± 0.95, 0.98 ± 0.07 and 1.18 ± 0.34 mg/ml respectively. Trypsin-produced hydrolysates ...
Microalgae are at the start of the food chain, and many are known producers of a significant amount of lipids with essential fatty acids. However, the bioactivity of microalgal lipids for anti-inflammatory and antithrombotic activities have rarely been investigated. Therefore, for a sustainable source of the above bioactive lipids, the present study was undertaken. The total lipids of microalga Chlorococcum sp., isolated from the Irish coast, were fractionated into neutral-, glyco-, and phospho-lipids, and were tested in vitro for their anti-inflammatory and antithrombotic activities. All tested lipid fractions showed strong anti-platelet-activating factor (PAF) and antithrombin activities in human platelets (half maximal inhibitory concentration (IC50) values ranging ~25-200 µg of lipid) with the highest activities in glyco- and phospho-lipid fractions. The structural analysis of the bioactive lipid fraction-2 revealed the presence of specific sulfoquinovosyl diacylglycerols (SQDG) bioactive ...
Background and purpose: Artemisia is one of the well-known herbal medicinal plants for antimicrobial, insecticidal, antioxidant, and antimalarial activities. The antiproliferative effects of dichloromethane extracts of Artemisia biennis (A. biennis) and A. ciniformis and the petroleum ether extract of A. ciniformis have been demonstrated previously on human cancerous cell lines. In the current study, further fractionation was carried out on the aforementioned extracts and their cytotoxic effects were evaluated on three human cancer cell lines; B16/F10, PC3, and MCF7. F1 to F16, F1 to F11, and F1 to F10 were resulted from the fractionation of dichloromethane extracts of A. biennis, A. ciniformis, and petroleum ether extract of A. ciniformis, respectively. Experimental approach: The cytotoxic effects of 16 (F1-F16), 11 (F1-F11) and 10 (F1-F10) fractions, on B16/F10, PC3, and MCF7 cell lines were assessed using resazurin to measure viability and propidium iodide staining (sub G1) and flow ...
The bioactive lipid intermediate palmitoyl CoA (PCoA) can inhibit mitochondrial ADP/ATP transport, though the physiological relevance of this regulation remains unclear. We questioned whether myocardial ischemia provides a pathological setting in which PCoA regulation of ADP/ATP transport would be beneficial, and secondly, whether the chronically elevated lipid content within the diabetic heart could make mitochondria less sensitive to the effects of PCoA. PCoA acutely decreased ADP-stimulated state 3 respiration and increased the apparent Km for ADP twofold. The half maximal inhibitory concentration (IC50 ) of PCoA in control mitochondria was 22 µM. This inhibitory effect of PCoA on respiration was blunted in diabetic mitochondria, with no significant difference in the Km for ADP in the presence of PCoA, and an increase in the IC50 to 32 µM PCoA. The competitive inhibition by PCoA was localised to the phosphorylation apparatus, particularly the ADP/ATP carrier (AAC). During ischemia, the AAC imports
Artemisinin is the frontline fast-acting anti-malarial against P. falciparum. Emergence and spread of resistant parasite in eastern-India poses a threat to national malaria control programs. Therefore, the objective of our study is to evaluate the artesunate-sulfadoxine-pyrimethamine efficacy in Central India. 180 monoclonal P. falciparum-infected patients received standard ASSP therapy during August 2015-January 2017, soon after diagnosis and monitored over next 42-days. Artemisinin-resistance was assessed through in-vivo parasite clearance half-life (PC1/2), ex-vivo ring-stage survivability (RSA), and genome analysis of kelch13 and other candidate gene (pfcrt, pfmdr1, pfatpase 6, pfdhfr and pfdhps). ...
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity. - Mechanism of Action & Protocol.
InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32) ...
The Quantitative Structure-Activity Relationship of a series of novel Thiazoline derivatives with anticancer activity has been studied by using the density functional theory by B3LYP/ 6-31G. Descriptors of quantum mechanics of 21 thiazoline derivatives with known activity were obtained. Multiple linear regressions were employed to model the relationships between molecular descriptors and biological activity of molecules using stepwise method. The most model shows not only significant statistical quality, but also predictive ability, with the square of adjusted correlation coefficient (R2=0.945) and standard error (SE=0.586). We find that the anticancer activity expressed that as half maximal inhibitory concentration (IC50), closely relates to the highest occupied molecular orbital, dipole moment, softness, hardness, ionization energy, electron affinity. Accordingly can be offered a quantitative model, and interpret the activity of the compounds relying on the multivariate statistical analysis. This
Masitinib is a selective tyrosine kinase inhibitor with potent activity against the juxta membrane domain of c-Kit. Masitinib is also thought to promote survival via modulation of immunostimulation-mediated anticancer effects and modulation of the tumor microenvironment. The objective of this study was to evaluate the efficacy and safety of masitinib with respect to dacarbazine in the treatment of non-resectable or metastatic stage 3 or stage 4 melanoma carrying a mutation in the juxta membrane domain of c-Kit. Following a protocol amendment, the dacarbarzine treatment group was closed and recruitment restricted to masitinib treatment of chemo-naïve (first-line) patients ...
Sapacitabine cancer drug molecule (nucleoside analogue). Stylized skeletal formula (chemical structure): Atoms are shown as color-coded circles: hydrogen (hidden), carbon (grey), nitrogen (blue), oxygen (red). - Stock Image F018/3177
AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375, respectively.
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Sigma-Aldrich offers abstracts and full-text articles by [Marta Leirós, Eva Alonso, Mostafa E Rateb, Wael E Houssen, Rainer Ebel, Marcel Jaspars, Amparo Alfonso, Luis M Botana].
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【市場調査レポート】タッチパネル用コントローラーICの世界市場2017-2021 | 発行日:2017年4月12日 | 商品コード:IRTNTR12538 | 発行/調査会社:Technavio | Global Touch Controller IC Market 2017-2021 | キーワード:グローバル、電子、タッチパネルコントローラーIC、タッチスクリーン [市場規模/動向/予測など世界の産業分析レポート販売のマーケットレポート.jp]
Masitinib is a selective, oral tyrosine kinase inhibitor with neuroprotective capability demonstrated via numerous preclinical studies. Two of masitinibs main cellular targets are the mast cell and microglia cell. It is well-established that mast cells play a prominent role in neuroinflammatory processes. Microglia, resident immune cells of the central nervous system (CNS), also constitute an important source of neuroinflammatory mediators and may have fundamental roles in numerous neurodegenerative disorders. The development of masitinib in ALS is therefore based on the pharmacological action of masitinib in microglia cells and mast cells, thereby slowing microglial-related disease progression, reducing neuro-inflammation, and modulating the neuronal microenvironment in both central and peripheral nervous systems. This is a multicenter, double-blind, randomized, placebo-controlled, parallel-group (two ascending dose titrations of masitinib and matching placebo), comparative study of oral ...
Anticancer bisdioxopiperazines, including ICRF-154, razoxane (Raz, ICRF-159) and ICRF-193, are a family of anticancer agents developed in the UK, especially targeting metastases of neoplasms. Two other bisdioxopiperazine derivatives, probimane (Pro) and MST-16, were synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Cytotoxic activities and mechanisms of Raz (+)-steroisomer (ICRF-187, dexrazoxane), Pro and MST-16 against tumor cells were evaluated by MTT colorimetry, flow cytometry and karyotyping. Pro was cytotoxic to human tumor cell lines in vitro (IC50|50 μM for 48 h). Four human tumor cell lines (SCG-7901, K562, A549 and HL60) were susceptible to Pro at low inhibitory concentrations (IC50 values | 10 μM for 48 h). Although the IC50 against HeLa cell line of vincristine (VCR, 4.56 μM), doxorubicin (Dox, 1.12 μM) and 5-fluoruouracil (5-Fu, 0.232 μM) are lower than Pro (5.12 μM), ICRF-187 (129 μM) and MST-16 (26.4 μM), VCR, Dox and 5-Fu shows
Anticancer bisdioxopiperazines, including ICRF-154, razoxane (Raz, ICRF-159) and ICRF-193, are a family of anticancer agents developed in the UK, especially targeting metastases of neoplasms. Two other bisdioxopiperazine derivatives, probimane (Pro) and MST-16, were synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Cytotoxic activities and mechanisms of Raz (+)-steroisomer (ICRF-187, dexrazoxane), Pro and MST-16 against tumor cells were evaluated by MTT colorimetry, flow cytometry and karyotyping. Pro was cytotoxic to human tumor cell lines in vitro (IC50|50 μM for 48 h). Four human tumor cell lines (SCG-7901, K562, A549 and HL60) were susceptible to Pro at low inhibitory concentrations (IC50 values | 10 μM for 48 h). Although the IC50 against HeLa cell line of vincristine (VCR, 4.56 μM), doxorubicin (Dox, 1.12 μM) and 5-fluoruouracil (5-Fu, 0.232 μM) are lower than Pro (5.12 μM), ICRF-187 (129 μM) and MST-16 (26.4 μM), VCR, Dox and 5-Fu shows
Class I PI3Ks can form an allosteric or specificity pocket (adjacent to the adenine pocket) only in the presence of propeller-like inhibitors (29). The half-maximal inhibitory concentrations (IC50s) for the propeller-like PI3K inhibitors (e.g., PIK-39) (fig. S9) are generally much worse for Vps34 than other PI3Ks. This is probably due to increased rigidity of the Vps34 pocket arising from a bulky residue substituted in the P loop (Phe612-Hs, Phe673-Dm) that packs against the aromatic hinge residue unique to Vps34 (Phe684-Hs, Tyr746-Dm). These differences effectively close off a corner of the adenine-binding pocket, giving it a more constrained appearance.. Currently there is no high-affinity, specific inhibitor of Vps34. We determined the structure of a complex of Vps34 with 3-methyladenine (3-MA) (Fig. 4, B and C), which is often used as a specific inhibitor of autophagy. We also determined the structures of Vps34 in complexes with three multi-targeted inhibitors: (i) PIK-90, (ii) PIK-93, ...
Scorpion venom-derived peptidyl toxins are valuable pharmacological tools for investigating the structure-function relationship of ion channels. Here, we report the purification, sequencing and functional characterization of a new K(+) channel blocker (MeuKTX) from the venom of the scorpion Mesobuthus eupeus. Effects of MeuKTX on ten cloned potassium channels in Xenopus oocytes were evaluated using two-electrode voltage-clamp recordings. MeuKTX is the orthologue of BmKTX (α-KTx3.6), a known Kv1.3 blocker from the scorpion Mesobuthus martensii, and classified as α-KTx3.13. MeuKTX potently blocks rKv1.1, rKv1.2 and hKv1.3 channels with 50% inhibitory concentration (IC(50)) of 203.15 ± 4.06 pM, 8.92 ± 2.3 nM and 171 ± 8.56 pM, respectively, but does not affect rKv1.4, rKv1.5, hKv3.1, rKv4.3, and hERG channels even at 2 μM concentration. At this high concentration, MeuKTX is also active on rKv1.6 and Shaker IR. Our results also demonstrate that MeuKTX and BmKTX have the same channel spectrum ...
Oxidative damage to the vascular endothelium may play an important role in the pathogenesis of atherosclerosis and aging, and may account in part for reduced vascular prostacyclin (PGI2) synthesis associated with both conditions. Using H2O2 to induce injury, we investigated the effects of oxidative damage on PGI2 synthesis in cultured endothelial cells (EC). Preincubation of EC with H2O2 produced a dose-dependent inhibition (inhibitory concentration [IC50] = 35 microM) of PGI2 formation from arachidonate. The maximum dose-related effect occurred within 1 min after exposure although appreciable H2O2 remained after 30 min (30% of original). In addition, H2O2 produced both a time- and dose-dependent injury leading to cell disruption, lactate dehydrogenase release, and 51Cr release from prelabeled cells. However, in dramatic contrast to H2O2 effects on PGI2 synthesis, loss of cellular integrity required doses in excess of 0.5 mM and incubation times in excess of 1 h. The superoxide-generating ...
immune Uncategorized Col4a2, Masitinib ( AB1010) interactions where the biological aftereffect of an publicity depends upon an individuals genotype are widely held to become ubiquitous-and rightly thus considering epidemiologists have got long abandoned the paradigm of ascribing disease to either character or nurture (if indeed they ever considered etiology in unifactoral conditions) and today seek to comprehend the joint actions of both character and nurture. gene-environment connections in individual observational research stands in sharpened contrast towards the wide-spread proof for gene-environment relationship from experimental research in model microorganisms (2). This discrepancy is certainly a puzzle. Masitinib ( AB1010) Will there be something fundamentally different about the biology of individual complicated attributes? Are there limitations to how gene-environment interactions have been analyzed in humans? Or both? Stenzel et al. (3) discuss two important methodological ...
Silibinin has limited in vitro antiproliferative activity in 4T1 cells 4T1-luc tumor cells were seeded in triplicates in 96-well plates at a concentration of 10
To discover leads for next-generation chemoprotective antimalarial drugs, we tested more than 500,000 compounds for their ability to inhibit liver-stage development of luciferase-expressing Plasmodium spp. parasites (681 compounds showed a half-maximal inhibitory concentration of less than 1 micromolar). Cluster analysis identified potent and previously unreported scaffold families as well as other series previously associated with chemoprophylaxis. Further testing through multiple phenotypic assays that predict stage-specific and multispecies antimalarial activity distinguished compound classes that are likely to provide symptomatic relief by reducing asexual blood-stage parasitemia from those which are likely to only prevent malaria. Target identification by using functional assays, in vitro evolution, or metabolic profiling revealed 58 mitochondrial inhibitors but also many chemotypes possibly with previously unidentified mechanisms of action.
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Overview: Also known as: AB-1010 Pharmaceutical Company:AB Sciences Route and Dose of Administration: Oral (4.5mg/kg/day or 4.5-6 mg/kg/day) Type: Immunomodulator...
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It was initially hard for me to know how to get started and contribute in this project and I think there are others how feel the same way, so Im describing here how I approached it. Its not the only way or even the correct way but just an experience Ive had so far.. ...
Each year the government adds an addional amount of money to our school budget for children who are eligible for free school meals, for Children in Care and for those who are members of service families. This is know as the Pupil Premium.. With the introduction of Universal Infant Free School Meals, parents who are on certain benefits, such as Income Support, are still encouraged to apply for Free School Meals, to enable their children to qualify for the Pupil Premium.. At Millbrook School, this money is particularly used to in the staffing line of the budget to enable more support to be given to the qualifying children, whether this be in general or specific programmes of study. A more detailed report on the expenditure can be found below along with our policy. ...
Results: All the evaluations were performed in triplicates and results were noted down. It was observed that aqueous extract of C. sativus fruits showed a maximum DPPH radical scavenging activity (p,0.0001), half-maximal inhibitory concentration (IC50) at a concentration of 122.67 μg/ml. The ethyl acetate fraction of C. sativus fruits exhibited maximum hyaluronidase (p,0.0001), MMP-1/collagenase (p,0.04), and tyrosinase (p,0.04) inhibitory activity, IC50 at a concentration of 59.54, 45.79, and 24.46 μg/ml, respectively. The elastase (p,0.0001) inhibitory activity by n-butanol fraction of C. sativus fruits extract was maximum, IC50 at a concentration of 52.76 μg/ml. ...
TY - JOUR. T1 - A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogues. AU - Dimmock, J. R.. AU - Padmanilayam, M. P.. AU - Puthucode, R. N.. AU - Nazarali, A. J.. AU - Motaganahalli, N. L.. AU - Zello, G. A.. AU - Quail, J. W.. AU - Oloo, E. O.. AU - Kraatz, H. B.. AU - Prisciak, J. S.. AU - Allen, T. M.. AU - Santos, C. L.. AU - Balzarini, J.. AU - De Clercq, E.. AU - Manavathu, E. K.. PY - 2001/2/15. Y1 - 2001/2/15. N2 - A series of 3,5-bis(arylidene)-4-piperidones 1 and related N-acryloyl analogues 2 were prepared as candidate cytotoxic agents with a view to discerning those structural features which contributed to bioactivity. A number of the compounds were markedly cytotoxic toward murine P388 and L1210 leukemic cells and also to human Molt 4/C8 and CEM neoplasms. Approximately 40% of the IC50 values generated were lower than the figures obtained for melphalan. In virtually all cases, the N-acyl compounds ...
A new study reviews the potential for curcumin and nanosystems to treat COVID-19. Curcumin has been characterized and studied thoroughly, as a natural molecule with medicinal properties. Its tolerability and safety have been well documented, with a maximum dose of 12 g/day. Curcumin inhibits viral enzymes due to its ability to inhibit the virus itself, as well as to modulate inflammatory pathways. It regulates viral transcription and regulation, binds with high potency to the viral main protease (Mpro) enzyme that is key to replication, and inhibits viral attachment and entry into the host cell. It may also disrupt viral structures. It has been reported to inhibit the 3C-like protease (3CLpro) more effectively than other natural products, including quercetin, or drugs like chloroquine and hydroxychloroquine. It also inhibits papain-like protease (PLpro) with a 50% inhibitory concentration (IC50) of 5.7 µM that surpasses quercetin and other natural products. Modeling studies have shown that ...
As expected, the soluble CD4 positive control inhibited CXCR4 (50% inhibitory concentration [IC(50)] 3.7 μg/ml) and CCR5 (IC(50) 0.03 μg/ml) tropic HIV-1 infectivity. Free melittin doses ,2 μM were not cytotoxic and were highly effective in reducing HIV-1 infectivity for both CXCR4 and CCR5 strains in TZM-bl reporter cells, while VK2 vaginal cell viability was adversely affected at all free melittin doses tested. However, VK2 cell viability was not affected at any dose of melittin-loaded nanoparticles. Melittin nanoparticles safely and significantly decreased CXCR4 (IC(50) 2.4 μM and IC(90) 6.9 μM) and CCR5 (IC(50) 3.6 μM and IC(90) 11.4 μM) strain infectivity of TZM-bl reporter cells. Furthermore, melittin nanoparticles captured more HIV-1 than blank nanoparticles.. ...
Pharmaceuticals 2016, 9, 78 19 of 33 aptamers, exhibited cross-protection against infections of H1N1, H5N1, H7N7, and H7N9 influenza viruses, with a 50% inhibitory concentration (IC50) around 10 nM. The association of the viral polymerase, bound to the cap, and eIF4GI may be involved in the preferential translation of viral mRNAs during influenza infection. In addition, the interaction of NS1, bound to a conserved 5untranslated region (UTR) element of the viral mRNA, with eIF4GI and PABP1 could promote the formation of a closed loop between the 5′ and 3′ ends of the viral mRNA; (4) RIG-I is a cytosolic receptor for non-self RNA that mediates immune responses against viral infections through IFNα/β production. Mitochondrial antiviral-signaling (MAVS) protein. Table 6 shows information on the aptamers described against influenza virus. Vaccination is a powerful approach to diminish the effects of influenza epidemics, but the use of antiviral drugs can also be very useful, particularly in ...
Exploration of Scaffolds from Natural Products with Antiplasmodial Activities, Currently Registered Antimalarial Drugs and Public Malarial Screen Data. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
The present invention relates to a mast cell inhibitor, a pharmaceutical composition and a method for the treatment of patients afflicted with Parkinsons disease, wherein said patients are treated with a tyrosine kinase inhibitor or mast cell inhibitor, in particular masitinib, or a compound selected from imatinib, cromolyn sodium, midostaurin, BLU-285, bosutinib, ibrutinib, LAS189386, DP-2618, fostamatinib, dasatinib, sunitinib, axitinib, pazopanib, and toceranib or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.
Novel anti-HIV-1 agents derived from betulinic acid have been greatly concerned. 3D-QSAR and molecular docking studies were applied to rationalize the structural requirements responsible for the anti-HIV activity of these compounds. The CoMFA and CoMSIA models resulted from 28 molecules gave rcv² values of 0.599 and 0
In an interview with |em|Targeted Oncology|/em|, Jorge E. Cortes, MD, discussed the results from the QuANTUM-R trial, as well as some other studies investigating the use of quizartinib in different patient populations in AML.
The selective activity of genes is affected by displacements (morpho-genetic movements) of cells, their spatial location. They are provided by the ability of cells to actively move and adhere (selective formation of contacts with each other, in which glycocalyx plays an important role). Neighboring cells exert physical, chemical, and other influences on the cells that migrated and came into contact with them, selectively activating and inactivating the genes of their nuclei. Morphogenetic movement of cells is one of the mechanisms of selective activation of genes ...
Laurie Arliss, professor of speech communication, has worked with the Exploratory Program for more than a dozen years and has taught at IC since 1984. Her...
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This is also known as the minimum inhibitory concentration (MIC). The antiviral effects of surfactin distinguish this ... Fortunately, these results were seen at high concentrations of about 40 μM to 60 μM. These concentrations also exhibited the ... the bacterium needs to be treated with a high concentration. In fact, surfactin needs to be in concentrations between 12 and 50 ... It can lower the water's surface tension from 72 mN/m to 27 mN/m at a concentration as low as 20 μM. Surfactin accomplishes ...
... inhibitory concentration for HIV". AIDS. 19 (9): 949-52. doi:10.1097/01.aids.0000171409.38490.48. PMID 15905676. S2CID 3162858 ... June 2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% ...
... inhibitory concentration (LD50) of the extract against Entamoeba histolytica was 33 µg/mLl. Pliny the Elder and Dioscorides ...
... has also been observed to possess in vitro antiestrogenic effects at very high concentrations (Ki = 50 μM). A ... Unlike many other flavonoids, tropoflavin does not show any inhibitory activity on 17β-hydroxysteroid dehydrogenase. ... 39 (3): 638-50. doi:10.1038/npp.2013.243. PMC 3895241. PMID 24022672. Yang YJ, Li YK, Wang W, Wan JG, Yu B, Wang MZ, Hu B (2014 ...
At a minimum inhibitory concentration of 25 μM, growth is reduced by 10-fold within 2.5 hours. At concentrations of 50 μM and ...
Concentration-dependent antibiotics, such as gentamicin and amikacin, are best suited for RLP because they have higher efficacy ... Concentration-dependent effects of tiludronate on equine articular cartilage explants incubated with and without interleukin-1β ... Horses must be sedated, because movement can force blood past the tourniquet and reduce the concentration of drug below the ... Regional limb perfusion allows drug dose to be reduced while maintaining therapeutic concentrations at the site of interest, ...
... inhibitory concentration (IC50) was determined as 91 nM. Shiomi, Kazuo; Qian, Wen-Hong; Lin, Xin-Yu; Shimakura, Kuniyoshi; ... AETX I is part of the sea anemone sodium channel inhibitory subfamily 1 and binds to the neurotoxin receptor site 3 of voltage- ... The LD50 of AETX K is not known so far, but its 50% ...
However, at similar concentrations it was found to inhibit swarming and (probably consequently) biofilm formation of Bacillus ... Huang YT, Onose J, Abe N, Yoshikawa K (2009). "In vitro inhibitory effects of pulvinic acid derivatives isolated from Chinese ... It has strong antioxidant properties, and a nonspecific inhibitory effect on cytochrome P450 enzymes. A total synthesis was ... It was found antibiotically inactive against an array of bacteria and fungi using the disk diffusion assay at 50 μg. ...
"Neomycin sulfate, EP Susceptibility and Minimum Inhibitory Concentration (MIC) Data" (PDF). TOKU-E. Archived (PDF) from the ... The following represents minimum inhibitory concentration (MIC) susceptibility data for a few medically significant gram- ... However, more than 50 years after its discovery, its DNA-binding properties were still unknown. Neomycin has been shown to ... 50 (3): 218-20. doi:10.1097/00000542-197903000-00010. PMID 219730. S2CID 13551808. Mehta R, Champney WS (September 2003). " ...
The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological ... is the fixed concentration of agonist and EC50 is the concentration of agonist that results in half maximal activation of the ... is fixed substrate concentration and Km is the Michaelis constant i.e. concentration of substrate at which enzyme activity is ... substrate and enzyme concentrations) the Ki is an absolute value. Ki is the inhibition constant for a drug; the concentration ...
... half maximal inhibitory concentration) of 85 pM. In this study, a negative effect was also found. There have been ... Margatoxin irreversibly inhibits the proliferation of human T-cells in a concentration of 20 μM. At lower concentrations, this ... In contrast to when the plasma concentration of margatoxin is higher than 10nM, the transient hyperactivity occurs in pigs. It ... 33 (50): 15061-70. doi:10.1021/bi00254a015. PMID 7999764. Garcia-Calvo M, Leonard RJ, Novick J, Stevens SP, Schmalhofer W, ...
"Cefpodoxime, Free Acid Susceptibility and Minimum Inhibitory Concentration (MIC) Data" (PDF). "Pharmaceuticals Manufacturer, ... It has well established pharmacokinetic profile with absorption of 50%. It is indicated in community acquired pneumonia, ... POSTPOD-50 (Cefpodoxime 50mg/5ml) (by Laafon Galaxy Pharmaceuticals) Fischer J, Ganellin CR (2006). Analogue-based Drug ...
When the inhibitory signals are prevented, the motor neurons are more easily activated and the victim has spastic muscle ... In persons killed by strychnine, the highest concentrations are found in the blood, liver, kidney and stomach wall. The usual ... Strychnine is an antagonist of glycine; it binds noncovalently to the same receptor, preventing the inhibitory effects of ... In the presence of an inhibitory neurotransmitter, such as glycine, a greater quantity of excitatory neurotransmitters must ...
Unlike the former, when piperacillin-tazobactam concentrations exceed minimum inhibitory concentrations (MIC) of a pathogen by ... shown to consist of a strong association with the duration of time the concentration exceeds minimum inhibitory concentrations ... while for organisms with higher minimum inhibitory concentrations, ~4.5g of piperacillin-tazobactam was administered every 6 ... of the plasma concentrations. The concentration of piperacillin-tazobactam is especially lower in fatty tissue, making up less ...
... at a concentration of 1 μM, had almost identical potency to that of the same concentration of β-phenethylamine in stimulating ... admixture with an equal amount of gramine markedly enhanced this inhibitory effect. Tyramine N-Methyltyramine Candicine N,N- ... This researcher found a mean concentration of hordenine in raw barley around 0.7 μg/g; in green malts (i.e. barley that had ... In contrast to tyramine, hordenine did not produce contraction of isolated rat vas deferens, but a 25 μM concentration of the ...
The drugs have low concentration in the brain due to low biological half-life. It is difficult to measure the plasma ... Once attached, conformational changes occur which stabilize the receptors and inhibitory signals are produced Synthetic ... Alprazolam has high oral bioavailability (84-91%) in which its maximum plasma concentration (Cmax) is reached after 1 to 2 ... one male and a female have their serum concentration of 8.1 and 10.2 μg/L respectively after 5 minutes, down to 4.6 and 6.1 μg/ ...
At such high concentrations, the nutrients become inhibitory, even though they have no such effect at the normal concentrations ... 2. High cell density (High cell concentration)[1] In a batch culture, to achieve very high cell concentrations, e.g. 50-100 g ... To cultivate the mutant on a low concentration of the required nutrient, it is fed to the batch culture at a controlled rate. ... Keeping the concentration of this compound as low as possible (while still allowing for sufficient cell growth) permits ...
The growth of M. plumbeus varied with different gas concentrations. Growth in N2 was 80% of that in air. Growth also occurred ... This study also revealed that thymol has effective inhibitory action against M. plumbeus. In nature, M. plumbeus can be found ... Growth on cheddar cheese in an atmosphere of: 20% CO2 and 5% O2 was 50% of that in air; 20% CO2 and 1% O2 was 40% of that in ... Growth on Czapek Yeast Extract Agar (CYA) and Malt Extract Agar (MEA) produces colonies at least 50 mm in diameter, often ...
SO2NHCH3 substituent diminishes COX-2 inhibitory activity as noted with a very high inhibitory concentration-50 (see structures ... Some of these analogs retained COX-2 inhibitory activity, whereas many others did not. However, when the ability of all these ... Schönthal AH, Chen TC, Hofman FM, Louie SG, Petasis NA (February 2008). "Celecoxib analogs that lack COX-2 inhibitory function ... which celecoxib does not inhibit at therapeutic concentrations) inhibits the production of prostaglandins and the production of ...
This increasing inhibitory effect is seen in dosages up to 1500 mg per day; at higher doses, the inhibitory effect of AMPT ... AMPT's effect on dopamine concentration and transport is reversible and short-lived. If methamphetamine is administered while ... Although it is not well understood, this relationship allows for AMPT's inhibitory property, which blocks tyrosine hydroxylase ... A relationship between cytoplasmic dopamine concentration and VMAT activity was established using cocaine, methamphetamines, ...
... is absorbed from the gut to at least 88% and reaches highest concentrations in the blood plasma after one to four ... thereby increasing inhibitory GABAergic neurotransmission. ... The terminal half-life is 50 to 60 hours. The safety and ... Cenobamate induces the enzymes CYP3A4 and CYP2B6 and can therefore decrease blood concentrations of drugs that are metabolized ... potentially increasing concentrations of drugs metabolized by this enzyme (for example omeprazole). Cenobamate is a voltage- ...
Nitric oxide (NO) is particularly effective in relaxing the myometrium and in fact has a lower inhibitory concentration 50% (Ki ... compounds can be added to the organ bath in increasing concentrations to create a cumulative concentration-response curve (CCRC ... The concentration of prostaglandins in the blood plasma and amniotic fluid increases during labor. These inflammatory mediators ... and a higher concentration of K+ ions in the intracellular space than in the extracellular space. Subsequently, having K+ ...
... did not produce significant and irregular contractions until a concentration of 1:2500had been reached, implying an inhibitory ... mM/L of synephrine on rat white fat cells was antagonized by various β-antagonists with the following inhibitory concentrations ... However, the potency of synephrine at these receptors is relatively low (i.e. relatively large concentrations of the drug are ... This substance is present at very low concentrations in common foodstuffs such as orange juice and other orange (Citrus species ...
... half maximal effective or inhibitory concentration, respectively, of a drug), and TCID50 (50% tissue culture infectious dose of ... the concentration of a test substance that produces an effect of interest in half of the test units. Examples include LD50 (the ... so it is easier to measure the concentration of the test substance that produces a 50% response. Reed, L.J.; Muench, H. (1938 ... See article above for overview of 50% endpoints and comparison with other methods of calculating 50% endpoints. The Reed-Muench ...
A 2018 meta-analysis found that the largest differences between fibromyalgia patients and healthy subjects were for inhibitory ... Kimura, Shigemi; Toyoura, Makiko; Toyota, Yuko; Takaoka, Yutaka (15 December 2020). "Serum concentrations of insulin-like ... About 75% of fibromyalgia patients report significant problems with concentration, memory, and multitasking. ... 50 (1): 56-66. doi:10.1590/S0482-50042010000100006. PMID 21125141. Derry S, Wiffen PJ, Häuser W, Mücke M, Tölle TR, Bell RF, ...
The minimum inhibitory concentrations (MICs) of pathogens isolated in clinical field trials conducted in the United States ... It has broad-spectrum, concentration dependent, bactericidal activity; however, its efficacy is not as good as enrofloxacin or ... Difloxacin is rapidly and almost completely absorbed after oral administration, and approximately 50% is bound to circulating ...
In addition, GAD and GABA-AT are responsible in regulating the concentration of GABA. GABA's feature is that it does not ... mostly inhibitory neurotransmitter in the central nervous system, into succinic semialdehyde. The active enzyme is a homodimer ... The quantification of GABA concentration during cell activity needs to have high spatial and temporal resolution. As before, ... high performance liquid chromatography (HPLC) was used in quantifying GABA concentration levels. In present time, GABA is now ...
"Doxycycline hyclate Susceptibility and Minimum Inhibitory Concentration (MIC) Data" (PDF). Retrieved 16 April 2017 ... It reaches highest concentrations in the blood plasma after one to two hours and has a high plasma protein binding rate of ... Very high concentrations are found in the gallbladder, liver, kidneys, lung, breast milk, bone and genitals; low ones in saliva ... In addition, food has less effect on absorption than on absorption of earlier drugs with doxycycline serum concentrations being ...
As the extracellular concentration of 5-HT is regulated by the activity of the 5-HT transporter (5-HTT), the gene SLC6A4 ... Activation during correct inhibitory-responses relative to go-responses in the left and middle frontal gyri at baseline ... A rapid increase in blood alcohol concentration (BAC) is most consistently associated with the likelihood of a blackout. ... Wetherill, Reagan R; Castro, Norma; Squeglia, Lindsay M; Tapert, Susan F (2013). "Atypical neural activity during inhibitory ...
The inhibitory effect of myricetin on T cells, which was described in this study, was explained as being mediated via ... At higher and higher concentrations of myricetin, the rate of DNA damage has been shown to decrease. A current hypothesis for ... Myricetin's pro-oxidative capabilities can also be seen in its ability to act as an inhibitory agent against glutathione ... Myricetin produced epithelial layer contractile reflexes in separate rat aortic rings at a concentration of 50 M. This ...
Glycinergic and GABAergic inhibitory neurons make up half of all inspiratory neurons. Exposure of the pre-Bötzinger complex to ... Calcium-sensitive dyes have shown that internal concentrations of calcium increase during bursts. The activation of different ... The inhibitory connections discovered indicate their ability to connect different classes of neurons, their importance in ... In addition to the inhibitory synaptic regulation of respiratory rhythm within the pre-Bötzinger complex, there is also an ...
In high enough concentrations, coniine can be dangerous to humans and livestock. With its high potency, the ingestion of ... Coniine acts directly on the central nervous system through inhibitory action on nicotinic acetylcholine receptors. ... Poison hemlock is most poisonous in the spring when the concentration of γ-coniceine (the precursor to other toxins) is at its ... up to 50 centimetres (20 inches) long and 40 cm (16 in) broad. Hemlock's flower is small and white; they are loosely clustered ...
Yoo, Jae-Myung; Park, Eun Seok; Kim, Mee Ree; Sok, Dai-Eun (2013-04-01). "Inhibitory effect of N-Acyl dopamines on IgE-mediated ... NADA is an endogenous arachidonic acid based lipid found in the brain of rats, with especially high concentrations in the ... Furthermore, NADA also displays inhibitory activity in HIV-1 replication assays. Finally, NADA can prevent the degranulation ... It activates the TRPV1 channel with an EC50 of approximately of 50 nM which makes it the putative endogenous TRPV1 agonist. In ...
... gastrin Inhibitory factors:gastric inhibitory peptide (GIP), secretin, somatostatin, glucagon, calcitonin Gastrinoma ... Plasma gastrin concentration is elevated in virtually all individuals with mucolipidosis type IV (mean 1507 pg/mL; range 400- ... i.e. during the gastric phase) Inhibitory factor: acidity (pH below 3) - a negative feedback mechanism, exerted via the release ... Stimulatory factor: bombesin or gastrin-releasing peptide (GRP) Inhibitory factor: somatostatin - acts on somatostatin-2 ...
The fly was presented uniformly moving gratings while the calcium concentration in the dendritic tips of the tangential cells ... provide evidence for a mechanism primarily based on inhibitory signals from SAC's based on an oversampled serial block-face ... Optical measurements of Ca2+ concentration showed that they respond strongly to the centrifugal motion (the outward motion from ... Further evidence suggests that starburst cells release inhibitory neurotransmitters, GABA onto each other in a delayed and ...
Zhao L, Samuels T, Winckler S, Korgaonkar C, Tompkins V, Horne MC, Quelle DE (January 2003). "Cyclin G1 has growth inhibitory ... Concentrations of p16INK4a increase dramatically as tissue ages. p16INK4a, along with senescence-associated beta-galactosidase ... "The nuclear protein p34SEI-1 regulates the kinase activity of cyclin-dependent kinase 4 in a concentration-dependent manner". ... 50 (1): 45-51. doi:10.1016/j.oraloncology.2013.10.007. PMC 3942323. PMID 24211084. Hwang H, Tse C, Rodriguez S, Gown A, Churg A ...
CREB2 generates an inhibitory environment by increasing expression of leaky potassium channels, which helps to stabilize peak ... highlighting importantly that her model could account for normal growth despite local variations in morphogen concentration. ... Fascinatingly, CycA is only expressed in 40-50 neurons in the fly brain, intermingled with circadian clock neurons suggesting ...
These results require relatively high concentrations (at a concentration of 10 μM). Blocking the formation of 5-HETE, by ... X-linked inhibitor of apoptosis (XIAP) is hypothesized to promote cancer cell survival and growth, the Macrophage inhibitory ... Unfortunately, oral ingestion of zinc is ineffective since high concentrations of zinc into prostate cells is not possible ... Senapati S, Rachagani S, Chaudhary K, Johansson SL, Singh RK, Batra SK (March 2010). "Overexpression of macrophage inhibitory ...
The primary function of the basal ganglia appears to be action selection: they send inhibitory signals to all parts of the ... salt concentration in the bloodstream, blood glucose levels, blood oxygen level, and others. The ability of an animal to ... The basal ganglia are the central site at which decisions are made: the basal ganglia exert a sustained inhibitory control over ... The functions of these synapses are very diverse: some are excitatory (exciting the target cell); others are inhibitory; others ...
Its concentration in soil may be as high as 2 μg/L, and its concentration in natural aquatic environments may be as high at 88 ... Inhibitory and toxic effects of extracellular self-DNA in litter: a mechanism for negative plant-soil feedbacks? New ... Inhibitory effects of extracellular self-DNA: a general biological process? New Phytologist 206: 127-132. Veresoglou, SD, ... In this context, direct comparisons of eDNA concentrations with biomass and stock assessment metrics, such as catch per unit ...
... require salt concentrations in excess of 2 mol/L (or about 10%, three times the ocean salinity which is around 35g/ ... Haloarchaea can grow at an aw close to 0.75, yet a water activity (aw) lower than 0.90 is inhibitory to most microbes. The ... The concentration gradient generated from this process can then be used to synthesize ATP. Many haloarchaea also possess ... Retaining these salts is referred to as the "salt-in" method where the cell accumulates a high internal concentration of ...
Geometric mean concentration (GMC) of anti-S IgG (BAU/ml) was reported. Before the 1st injection, anti-S IgG level of the all ... Neutralizing antibody levels were evaluated by plaque reduction neutralization test with inhibitory dilution greater than 50% ( ... At day 42, anti-S IgG concentration of the vaccine group reached 1254.7 BAU/ml, while that of placebo group remained unchanged ... At day 35, GMT of groups Nanocovax 25 mcg, 50 mcg, 75 mcg were 20.9, 22.5 and 33.6, respectively. At day 42, their respective ...
Men have a higher concentration of androgens while women have a higher concentration of estrogens. To date, wound healing ... "Macrophage Migration Inhibitory Factor Is Induced by Thrombin and Factor Xa in Endothelial Cells". Journal of Biological ... amygdala and a decreased concentration in females' amygdala. In this case, stress causes females' emotion regulation to drop, ... Gross measures of body strength suggest that women are approximately 50-60% as strong as men in the upper body, and 60-70% as ...
However, DAT, the primary way dopamine is transported out of the cell, can work to decrease dopamine concentration in the ... This suggests that in schizophrenia, the alpha-2 adrenergic receptor, a presynaptic inhibitory receptor, may be less sensitive ... At the same time, higher levels of 5-HT are maintained in the synapse increasing the concentrations of the latter ... This thwarts the absorption of these chemicals into the presynaptic terminal and allows a large concentration of dopamine, ...
... is expressed within the non-permissive cells and is a key inhibitory factor of HIV-1 replication and infectivity. ... Additionally, it has been shown that there is a dose response between intracellular APOBEC3G concentration and degree of viral ... 418 (6898): 646-50. Bibcode:2002Natur.418..646S. doi:10.1038/nature00939. PMID 12167863. S2CID 4403228. Takaori A (December ...
PGMS concentration and f-actin content are inversely correlated; when PGMS becomes enriched at the tip of a neurite, its f- ... Nogo-A is a type of neurite outgrowth inhibitory component that is present in the central nervous system myelin membranes ( ... This is achieved by a high concentration of voltage-gated sodium channels in the initial segment where the action potential is ... The resulting increase in intracellular calcium concentration causes synaptic vesicles (tiny containers enclosed by a lipid ...
Concentrations of yohimbine in the commercial products ranged from < 0.1 to 489 ppm, compared with 7089 ppm in the authentic ... One possible explanation for this finding is the existence of powerful and multiple inhibitory controls on sexual behavior in ... Yohimbine interacts with serotonin and dopamine receptors in high concentrations. Yohimbine has been studied as a way to ... 53 (3): 417-50. PMID 11546836. "CFR - Code of Federal Regulations Title 21: Regulations on OTC products". U.S. Food and Drug ...
Thompson R, Johnson A (1951). "The inhibitory action of saliva on the diphtheria bacillus: hydrogen peroxide, the inhibitory ... Only supraphysiologic concentrations of exogenous H2O2 (0.34% w/v, 100 mM) were sufficient to inactivate BV-associated bacteria ... The inhibitory substances produced by vaginal Lactobacillus is a primary factor in protecting the vaginal microbiota, with ... with inhibitory activity ranging from narrow (closely related Lactobacillus species) to broad (diverse groups of bacteria, ...
Guanylurea concentrations above 200 μg/L have been measured in a German river, which are amongst the highest reported for ... Activation of AMPK was required for metformin's inhibitory effect on liver glucose production. AMPK is an enzyme that plays an ... Peak plasma concentrations (Cmax) are reached within 1-3 hours of taking immediate-release metformin and 4-8 hours with ... Blood or plasma metformin concentrations are usually in a range of 1-4 mg/L in persons receiving therapeutic doses, 40-120 mg/L ...
Basket cells in CA3 receive excitatory input from the pyramidal cells and then give an inhibitory feedback to the pyramidal ... This may be a consequence of the concentration of excitable glutamate receptors in the hippocampus. Hyperexcitability can lead ... Other cells in smaller proportion are inhibitory interneurons, and these often show place-related variations in their firing ... These events are associated with bursts of spike activity lasting 50 to 100 milliseconds in pyramidal cells of CA3 and CA1. ...
... and that A-beta fiber signals acting on inhibitory cells in the dorsal horn can reduce the intensity of pain signals sent to ... and difficulties in concentration and attention… - Harold Merskey 2000 Although pain is considered to be aversive and ... Pain is the main reason for visiting an emergency department in more than 50% of cases, and is present in 30% of family ...
It can be found in the soil, ground water, air, and in small concentrations in food. Arsenic has many applications such as in ... prevents inhibitory effects of triphenyltin (TPT) on the key enzymes of the human sex steroid hormone metabolism". J. Steroid ... Substances, such a xenobiotics that target and act as agonists of PPARα, typically act to reduce overall serum concentrations ... Substances that target and act as agonists of PPARγ/RXR complex typically act to increase overall serum concentrations of ...
These inhibitory effects are thought to be responsible for the "memory blanks" that can occur at levels as low as 0.03% blood ... The concentration of alcohol in blood is measured via blood alcohol content (BAC). The amount and circumstances of consumption ... "Blood Alcohol Concentration (BAC)". Carleton College: Wellness Center. Archived from the original on 14 September 2009. Feige B ... Extreme levels of consumption can cause alcohol poisoning and death; in fact, a concentration in the blood stream of 0.36% will ...
The removal of the inhibitory RuBP, CA1P, and the other inhibitory substrate analogs by activase requires the consumption of ... The pH and the concentration of magnesium ions in the fluid compartment (in plants, the stroma of the chloroplast) increases in ... Rubisco side activities can lead to useless or inhibitory by-products. Important inhibitory by-products include xylulose 1,5- ... After the CA1P is released from RuBisCO, it is rapidly converted to a non-inhibitory form by a light-activated CA1P-phosphatase ...
Concentrations in the cerebrospinal fluid and in breast milk are 1 to 10% of blood plasma concentrations. The vast majority of ... In animals, sodium valproate raises cerebral and cerebellar levels of the inhibitory synaptic neurotransmitter, GABA, possibly ... Protein binding is saturable: it decreases with increasing valproate concentration, low albumin concentrations, the patient's ... In general, serum or plasma valproic acid concentrations are in a range of 20-100 mg/L during controlled therapy, but may reach ...
... occurs at high concentrations within mitochondrial fluid which greatly exceed the plasma concentration of melatonin. ... A possible mechanism by which melatonin may regulate weight gain is through its inhibitory effect on leptin. Leptin acts as a ... Melatonin concentrations differ not only among plant species, but also between varieties of the same species depending on the ... Notably high melatonin concentrations have been measured in popular beverages such as coffee, tea, wine, and beer, and crops ...
... concentration in human milk during lactation". Journal of Clinical Laboratory Analysis. 16 (6): 304-7. doi:10.1002/jcla.10055. ... "Lactoferricin-Related Peptides with Inhibitory Effects on ACE-Dependent Vasoconstriction". Journal of Agricultural and Food ... concentration in non-symptomatic cats with feline coronavirus (FCoV) infection". Journal of Feline Medicine & Surgery. 9 (4): ... 109 (4): 1039-50. doi:10.1016/0016-5085(95)90561-8. PMID 7557068. Danielsen, E. Michael (1992). "Folding of intestinal brush ...
TFPI contributes significantly to the inhibition of Xa in vivo, despite being present at concentrations of only 2.5 nM. The ... 1989). "Functional significance of the Kunitz-type inhibitory domains of lipoprotein-associated coagulation inhibitor". Nature ... 55 (1): 37-50. doi:10.1016/0049-3848(89)90454-4. PMID 2781520. Girard TJ, Warren LA, Novotny WF, et al. ( ... cDNA coding for the lipoprotein-associated coagulation inhibitor shows that it consists of three tandem Kunitz-type inhibitory ...
NAGly has been the focus of research on the immune system because of its antinociceptive effects and inhibitory action on ... NaGly was identified as a novel insulin secretagogue and was shown to increase intracellular calcium concentration through ... 64 (7): 1147-50. doi:10.1016/S0006-2952(02)01301-1. PMID 12234618. Bradshaw HB, Rimmerman N, Hu SS, Benton VM, Stuart JM, ...
The study was undertaken to test the inhibitory potential on cholesterogenesis of organosulfur compounds derived from garlic. ... Inhibitory Concentration 50 * L-Lactate Dehydrogenase / drug effects * L-Lactate Dehydrogenase / metabolism ... at low concentrations (, or =0.5 mmol/L), and abolished the synthesis at high concentrations (, or =1.0 mmol/L). Diallyl ... Judging from maximal inhibition and IC50 (concentration required for 50% of maximal inhibition), SAC, SEC, and SPC are equally ...
The results of these in vitro drug screening assays are commonly expressed as inhibitory concentration 50% (IC50): the ... concentration of the tested agent that inhibits the proliferation of the cancer cell population to 50% of the theoretically ... Cheburator Software for Automatically Calculating Drug Inhibitory Concentrations from In Vitro Screening Assays. Figure 2. ... Absolute IC50 is defined as the concentration of tested compound which results in 50% inhibition of cell growth as defined by ...
... the median inhibitory concentration [IC] IC50 and IC90) are calculated, and the ratio of the IC50 of the test and reference ... which subsequently results in a higher trough concentration. The result is a lopinavir blood concentration curve that is 100- ... Indinavir concentrations and antiviral effect. Pharmacotherapy 1999;19:708--12.. * Montaner JS, Reiss P, Cooper D, et al. ... Ritonavir increases plasma concentrations of other PIs by ,2 mechanisms, including inhibition of gastrointestinal cytochrome ...
Different concentrations (0.1, 0.2, 0.3, 0.4, and 0.5 mg/ml) of extract and fractions were subjected to α-amylase and α- ... Objective: The objective of the present study was to provide an in-vitro evidence for the potential inhibitory activity of ... Results: Fraction 2 of A. caudatum and fraction 4 of C. argentea has shown highest α-amylase and α-glucosidase inhibitory ... In-vitro α-amylase and α-glucosidase inhibitory activity of Adiantum caudatum Linn. and Celosia argentea Linn. extracts and ...
... inhibitory concentration of 2.7 μM. Thus, TRZ does not appear to undergo measurable blood-brain barrier efflux transport by P- ... After single i.p. injections of TRZ or KET in separate groups of control mice, brain concentrations of TRZ exceeded those in ... On the basis of single time points, brain concentrations of TRZ, or brain/serum ratios, were similar in P-gp-deficient animals ... Coadministration of KET with TRZ increased TRZ concentrations in serum, liver, and brain, both in controls and in P-gp- ...
Half inhibitory concentration. Drugs were added to the cells 4 hours after plating and incubated for 48 hours. For Acaca ... For DNA transfections, final concentration of 5 μg per reaction was used. For RNA transfections, final concentration of 100 ... Cells were then incubated with primary antibodies overnight at 4°C at a concentration of 1:100 in 1% BSA PBS. Anti-Ki67 (Dako) ... The ACC inhibitor TOFA (25 μmol/L) was added together with the indicated concentrations of cerulenin, 4 hours after cell ...
To determine the half maximal inhibitory concentration (IC50) values of heterologous (i.e., L-histidine) L-leucine transport ... We determined the half maximal inhibitory concentrations (IC50s) of L-leucine by homologues competition for all constructs ... Competitor concentrations of 250 µM ((A); 4F2hc-LAT1), 100 µM ((B); LAT1), 2500 µM ((C); 4F2hc-LAT2), and 500 µM ((D); LAT2) ... Competitor concentrations of 250 µM ((A); 4F2hc-LAT1), 100 µM ((B); LAT1), 2500 µM ((C); 4F2hc-LAT2), and 500 µM ((D); LAT2) ...
... inhibitory concentrations , 10 μM for CYP 3A4, 2D6, 1A2, and 2C19.. The therapeutic index for this in vivo model is defined as ... inhibitory concentration , 100 times the efficacious dose in the hERG patch-clamp assay.14 If the compound has a favorable ... with multiple compound concentrations against promastigotes and axenic amastigotes to enable us to determine the concentration ... efficacy concentration for parasites. Compounds with an in vitro therapeutic index ≥ 5, and metabolic stability , 20 minutes in ...
... half maximal inhibitory concentration. LD50: amount of agent to kill 50% of a test population ... Peak plasma concentrations of SM exceeded active in vitro concentrations of SM (higher than 2000 ng/mL). Dose increase resulted ... At equimolar concentrations, on average, SM is 9 times more potent than SS and 19 times more potent than the mono-and-di ... The absolute concentrations of these drugs to obtain similar efficacy as BEC and SM are in the order of 6 - 40 times higher [6 ...
Thus, with its pan-CoV fusion and entry inhibitory activity by targeting two sites in S protein, desirable half-life, and ... exhibited improved fusion inhibitory activity and SI (>1000). S-20-1 could effectively inhibit infection by pseudotyped and ... S-20 with potent membrane fusion inhibitory activity, but moderate selectivity index (SI). After modification, one derivative, ... fusion inhibitory peptides, respectively. However, neither nAb- nor peptide-based drugs can be used orally. In this study, we ...
Trovafloxacin, moxifloxacin, and gatifloxacin yield low minimum inhibitory concentrations (MICs) against most groups of ... In high concentrations, ticarcillin, piperacillin, and mezlocillin have good activity against gram-negative enteric bacilli and ... However, up to 50% of Bacteroides isolates are resistant to moxifloxacin. [48, 49] The use of the quinolones is restricted in ... The emergence of erythromycin-resistant organisms during therapy has been documented and reached up to 50% in recent studies. [ ...
Inhibitory Concentration 50. 1. 2009. 451. 0.090. Why? Proto-Oncogene Proteins. 1. 2022. 4689. 0.090. Why? ...
A number of studies have shown that CDDO-Me displayed a remarkable concentration-dependent inhibitory effect on the ... The half inhibitory concentration (IC50) was defined as the CDDO-Me concentration required for decreasing the cells to 50% of ... half maximal inhibitory concentration; SD, standard deviation; MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium ... The working solution of CDDO-Me was freshly diluted to the desired concentrations with culture medium. The final concentration ...
The synthesized ZnO NPs were subjected for antibacterial activity by minimum inhibitory concentration (MIC), which was ... oryzae (MF579736.1) (concentration in μg/ml) (a- Trail 1, b- Trail 2, and c- Trail 3). Table S1: Place of collection of ... The petri plates were swabbed with Xoo cultures whose concentration was adjusted to 108 CFU/mL. The agar petri plates were made ... The microtiter plates were incubated for 60 min at 28 °C. MICs determine the lowest concentration of the drug that prevents the ...
Of these ions, low pH and high UO22+, Mn2+, Al3+, Cd2+, Zn2+, Co2+, and Ni2+ are both (a) selectively inhibitory of a ... Rhodanobacter abundance is positively correlated with low pH and high concentrations of uranium and 13 other ions and we sought ... a Rhodanobacter isolate from a contaminated well, and (b) reach toxic concentrations (for the Pseudomonas isolate) in the ... USA that has large gradients of pH and widely varying concentrations of uranium, nitrate, and many other inorganic ions. In the ...
Inhibitory concentration. IL-21, IL-6, IL-8:. Interleukins. LD50:. Lethal dose ... Inhibitory effect of caffeic acid on cancer cell proliferation by oxidative mechanism in human HT-1080 fibrosarcoma cell line. ... This pro-oxidant effect leads to deleterious effects on DNA, proteins and lipids [128]. Further, at higher concentrations ... The inhibitory effects of phenolic and terpenoid compounds from Baccharis trimera in Siha cells: differences in their activity ...
... inhibitory concentration 50; mortality; necrosis; patients; phospholipase A2; plant anatomy; polyphenols; proteinases; snake ... 1. Hyaluronidase, phospholipase A2 and protease inhibitory activity of plants used in traditional treatment of snakebite- ...
... inhibitory concentration was 0.001 μg/ml. All 33 lineage members targeted a quaternary epitope focused on V2. While all known ... inhibitory concentration was 0.001 μg/ml. Furthermore, our results highlight the ongoing evolution within a single antibody ... It neutralized 57% of diverse clade viral isolates and 70% of clade C isolates with remarkable potency: the median 50% ...
Minimum Inhibitory Concentration (MIC). In this study, a total of 200 Fusarium and 67 Aspergillus isolates (47 A. flavus, 11 A ... Minimum inhibitory concentration (μg/ml) of antifungal agents against Fusarium spp. (n=200). ... Determination of Minimum Inhibitory Concentration (MIC). The MICs of seven different antifungal agents, namely, amphotericin B ... Minimum inhibitory concentration (μg/ml) of antifungal agents against Aspergillus spp. ...
Phenytoin concentration in people with epilepsy: a comparative study in serum and saliva. Alvarado, A., García, G., Morales, A. ... 50, 3, e02101284.. Research output: Contribution to journal › Article › peer-review ...
Half maximal inhibitory concentration (IC50) was estimated using nonlinear regression analysis. Mean ± SD of technical ... Half maximal inhibitory concentration (IC50) values were determined by nonlinear regression analysis using Prism software. ... Antibodies EBOV-1171 and EBOV-1176 potently neutralized rVSV/EBOV-GP with half maximal inhibitory concentration (IC50) values ... The mAb concentration ranged from 1 to 60 μg/mL for GP binding assays, and from 2 to 100 μg/mL for in vitro functional assays. ...
... we calculated the half maximal inhibitory concentration (IC50) [16, 17]. The IC50 values of sorafenib in normoxia and hypoxia ... B, C SMMC-7721 cell was treated with sorafenib at serial concentrations and CT-707 at different concentrations (2 μM, 3 μM, 4 ... SMMC-7721 and Bel-7402 cells were treated with various concentrations of CT-707 in the first 24 h and then with various doses ... Cells were treated with serial concentrations of sorafenib for 72 h, and then SRB staining assay was used to detect the ...
Ellagic-acid at 100microM concentrations was not more inhibitory than at 50microM. When ellagic-acid was added during BaP ... The inhibition of BaP metabolism by mouse lung explants was indicated by a concentration dependent decrease in the amount of ... Unmetabolized trans BaP was increased 7.2 to 20.3 percent, depending on ellagic-acid concentration while total metabolites were ... Explants were cultured for 16 hours in the presence or absence of 10 to 100 micromolar (microM) concentrations of the naturally ...
... inhibitory growth concentration was calculated with the probit procedure.. Validity criteria fulfilled:. not specified. ... TEST CONCENTRATIONS. - Spacing factor for test concentrations: No data. - Range finding study: Yes, at least 2 tests. Duration: ... Nominal and measured concentrations:. 5 different concentrations. No more data.. Details on test conditions:. TEST SYSTEM. - ... TEST CONCENTRATIONS: the toxicant concentrations were chosen as to cause an inhibition of the acetoclastic activity ranging ...
Minimal inhibitory concentration (MIC) and Minimal bactericidal concentration. The minimum inhibitory (MIC) and minimum ... The Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) of these oils, alone and in combination ... AITC exhibited lower inhibitory (MIC = 50ppm) and bactericidal concentrations (MBC = 200ppm) against E. coli O157:H7 growth ... H7 at concentrations of 12.5ppm AITC + 12.5ppm GO (Table 1). This effect can allow the use of lower concentrations of each ...
NH3 in the concentration range of 50-10000 ppm showed a slight inhibitory effect on biogas dry reforming. The decline rate of ... The results showed that low concentration of H2S in biogas could cause serious deactivation of catalyst. Characterization ... biogas conversion efficiency increased with the increase of NH3 concentration. This was related to the reduction of oxygen ...
... inhibitory concentrations , 10 μM for CYP 3A4, 2D6, 1A2, and 2C19.. The therapeutic index for this in vivo model is defined as ... inhibitory concentration , 100 times the efficacious dose in the hERG patch-clamp assay.14 If the compound has a favorable ... with multiple compound concentrations against promastigotes and axenic amastigotes to enable us to determine the concentration ... efficacy concentration for parasites. Compounds with an in vitro therapeutic index ≥ 5, and metabolic stability , 20 minutes in ...
  • More important, antibacterial evaluation showed that oximes 3c-e are highly potent against Klebsiella pneumoniae, with minimum inhibitory concentration (MIC) values of 0.06, 0.08, and 0.034 µM, respectively, whereas ketone 2c and oxime 4c are more active against Staphylococcus aureus than ciprofloxacin (MIC values: 0.7, 0.38, and 1.6 µM, respectively). (
  • Nine essential oils were tested for their antifungal potential by the method of assessing the minimum inhibitory concentration. (
  • Materials and Methods: N-hexane, ethylacetate, methanol and aqueous extracts of metabolites from the M. bellicosus were assayed for anti-Salmonella activity using the agar dilution method in the determination of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). (
  • To determine the minimum inhibitory concentration of the extract of cashew leaves ( Anacardium occidentale ) on the fungi isolates of groundnut seed. (
  • We confirmed that it does so in a concentration-dependent manner with a low micromolar half-maximal inhibitory concentration (IC 50 = 3 μM) in our protein-based ELISA-type setup, while chloroquine, siramesine, and suramin showed no inhibitory activity in this assay. (
  • Absolute IC 50 is defined as the concentration of tested compound which results in 50% inhibition of cell growth as defined by assay controls (pink lines). (
  • Different concentrations (0.1, 0.2, 0.3, 0.4, and 0.5 mg/ml) of extract and fractions were subjected to α-amylase and α-glucosidase inhibitory assay. (
  • Guided by TNF-α secretion inhibitory activity assay, four taraxastane-type triterpenoids, including two new ones, 22-oxo-20-taraxasten-3β, 30-diol (1) and 22α-hydroxy-20-taraxasten-30β, 30-triol (2), have been obtained from an active fraction of the petroleum ether-soluble extract of the the medicinal and edible plant Cirsium setosum. (
  • A neuraminidase inhibition assay was used to determine the Inhibitory Concentration 50 (IC 50 ) values for all influenza A and B isolates. (
  • These compounds showed immunosuppressant effect in the T-cell proliferation assay with IC 50 values between 31.2 to 2.7 μg/mL, while the IC 50 values for ROS inhibition, representing anti-inflammatory effect, were in the range of 25.6 to 2.0 μg/mL. (
  • After washing and blocking with PBST+5% BSA, detection was performed using Human Anti-Nivolumab Antibody, clone AbD30255 (HCA299) at a concentration of 2 μg/ml and an HRP labeled anti-DYKDDDDK tag antibody in HISPEC Assay Diluent ( BUF049A ) followed by QuantaBlu Fluorogenic Peroxidase Substrate. (
  • After washing and blocking with PBST+5% BSA, detection was performed using Human Anti-Nivolumab Antibody, clone AbD30255 (HCA299) titrated to the given concentrations in PBST followed by an HRP labeled anti-DYKDDDDK tag antibody in HISPEC Assay Diluent ( BUF049A ) and QuantaBlu Fluorogenic Peroxidase Substrate. (
  • Detection was performed using HRP conjugated Human Anti-Nivolumab Antibody ( HCA301 ) at a concentration of 2 µg/ml in HISPEC Assay Diluent ( BUF049A ) and QuantaBlu Fluorogenic Peroxidase Substrate. (
  • that both TM5275 and TM5441 inhibited EC branching within a 3D Matrigel assay at concentrations where that they had small influence on EC apoptosis. (
  • Caspase 3/7 activity assay Cells had been plated as referred to for cell viability and treated with raising concentrations of TM5275 or TM5441 for 48 hours. (
  • 50 clindamycin was 39 mol/L (the in vitro resistance cutoff or protection against mosquitoes. (
  • In-vitro α-amylase and α-glucosidase inhibitory activity of Adiantum caudatum Linn. (
  • The objective of the present study was to provide an in-vitro evidence for the potential inhibitory activity of extracts and fractions of Adiantum caudatum Linn. (
  • In this study, we determined phenolic profiles, antioxidant activity and in vitro inhibitory potential against key enzymes relevant for hyperglycemia of hydro ethanolic extract , acetonic fraction and ethyl acetate fraction. (
  • It was this program, 8 and the co-incidental discovery in 1972 of the macrolide maytansine from Maytenus ovatus , which displayed exceptionally high inhibitory activity in vitro against certain human carcinomas, 9 that catapulted the natural product chemistry of the Celastraceae into the limelight. (
  • In vitro antibacterial activity was determined by disc diffusion and it was concentration dependent. (
  • Classes were generated using rank-sum technique and the top five hits (Olmesartan, Verteporfin, Saprisartan, Atorvastatin and Lapatinib) were tested experimentally to determine the inhibitory effects on growth of HeLa cells in vitro . (
  • Conclusion: This in vitro study suggests that the Hemodyne analyzer and modified Thrombelastograph might be clinically useful methods to monitor the platelet inhibitory effects of agents such as abciximab. (
  • In vitro, human gastric carcinoma SGC-7901 cells were treated with N-desulfated heparin in different concentration (0.1 mg/mL, 1 mg/mL, N-desulfated heparin group), and treated with medium (control group). (
  • IMSEAR at SEARO: Detection of various types of resistance patterns and their correlation with minimal inhibitory concentrations against clindamycin among methicillin-resistant Staphylococcus aureus isolates. (
  • This study was done to determine the various clindamycin resistance patterns in MRSA isolates and to compare them with minimal inhibitory concentration (MIC) of clindamycin. (
  • Results: Of the 50 isolates, 34 were sensitive to both clindamycin and erythromycin. (
  • The minimum inhibitory concentrations were determined of imipenem, meropenem and ertapenem for Klebsiella isolates. (
  • If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. (
  • Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20? (
  • However, in complex mixtures of inhibitory compounds, it is challenging to determine which specific compounds cause changes in abundance and prevent some microorganisms from growing. (
  • Of these ions, low pH and high UO 2 2+ , Mn 2+ , Al 3+ , Cd 2+ , Zn 2+ , Co 2+ , and Ni 2+ are both (a) selectively inhibitory of a Pseudomonas isolate from an uncontaminated well vs. a Rhodanobacter isolate from a contaminated well, and (b) reach toxic concentrations (for the Pseudomonas isolate) in the Rhodanobacter -dominated wells. (
  • The liquid was flushed with nitrogen gas and the flasks were sealed with a rubber septum and a screw cap and placed in reciprocating shaker at 30°C. Catechol was added to each flask to provide toxic concentrations to be investigated. (
  • Simulations predicted sustained high, potentially toxic concentrations with 10 g, 30 g and 50 g Osteoset® T for CLCr values below 10, 20 and 30 mL/min, respectively. (
  • The bioassays on Aedes aegypti larvae and pupae were done by immersion test at different EO concentrations which ranged from 500.00 to 0.003 mg mL-1 (v/v). The results on the larvae and pupae indicated LC99.9 of (0.01 and 1.38 mg mL-1) for EO in dormancy, and (0.08 and 2.63 mg mL-1) for EO during budding, respectively. (
  • The absorbance was measured at 540 and 405 nm using multiplate reader and the percentage of α- amylase and α- glucosidase inhibitory activity and IC₅₀ values of extract and fractions were calculated. (
  • S-20 with potent membrane fusion inhibitory activity, but moderate selectivity index (SI). (
  • Thus, with its pan-CoV fusion and entry inhibitory activity by targeting two sites in S protein, desirable half-life, and promising oral bioavailability, S-20-1 is a potential candidate for further development as a novel therapeutic and prophylactic drug against infection by SARS-CoV-2 and its variants, as well as future emerging and reemerging CoVs. (
  • While GST activity was inhibited by all these compounds, acrolein was the most inhibitory. (
  • Concentrations inhibiting 50 percent of the activity (I50) ranged from around 10(- 3) to 10(-4) molar. (
  • These effects were accompanied with the inhibitory effect against YAP activity by CT-707. (
  • The compound concentration that caused 50% and 80% inhibition of the methanogenic activity was determined by graphic method. (
  • The inhibitory activity against α-amylase, α-glucosidase was carried out. (
  • These results suggest that Bridelia ferruginea has effective enzyme inhibitory activity useful for the management of postprandial hyperglycemia. (
  • A compound with antioxidant activity combined with inhibitory activities against α-glucosidase and α-amylase may be a more effective anti-diabetic agent. (
  • β -Sitosterol-3- O - β -D-glucopyranoside exhibited high cytotoxic activity (IC 50 = 1.279 μg/mL) against HCT-116 cell line. (
  • For the α -amylase inhibition activity, even at lower concentrations (0.025 mg/mL), there were statistically significant differences (P (
  • Although it is commonly stated that paracetamol acts centrally, recent data imply an inhibitory effect on the activity of peripheral prostaglandin-synthesising cyclooxygenase enzymes. (
  • Instead, several data published during the past few years suggest a tissue-dependent inhibitory effect of paracetamol on the activity of both central and peripheral cyclooxygenase enzymes. (
  • Due to our interest in the chemical space of organic dyes to identify potential small-molecule inhibitors (SMIs) for protein-protein interactions (PPIs), we initiated a screen of such compounds to assess their inhibitory activity against the interaction between SARS-CoV-2 spike protein and its cognate receptor ACE2, which is the first critical step initiating the viral attachment and entry of this coronavirus responsible for the ongoing COVID-19 pandemic. (
  • This PPI inhibitory activity of methylene blue could contribute to its antiviral activity against SARS-CoV-2 even in the absence of light by blocking its attachment to ACE2-expressing cells and making this inexpensive and widely available drug potentially useful in the prevention and treatment of COVID-19 as an oral or inhaled medication. (
  • X-ray crystallographic structures have become an important tool in modern drug experimental analysis of few drugs was carried out to test discovery process and insights can be obtained on the the inhibitory activity against carcinoma of cervix, HeLa protein-ligand interactions and biological function of cells. (
  • The Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) of these oils, alone and in combination, against E. coli O157:H7 were determined. (
  • This patient has cellulitis and should receive a beta lactam antibiotic, which will have the best coverage and lowest minimal inhibitory concentration for the likely organism, beta hemolytic streptococci. (
  • Roughly 50 billion cells undergo apoptosis each day in humans. (
  • In humans, 50% inhibitory concentrations of ODSH for these anti-inflammatory activities can be achieved in the blood without anticoagulation. (
  • The receptor-binding domain (RBD) in S1 subunit and heptad repeat 1 (HR1) domain in S2 subunit of SARS-CoV-2 spike (S) protein are the targets of neutralizing antibodies (nAbs) and pan-coronavirus (CoV) fusion inhibitory peptides, respectively. (
  • Judging from maximal inhibition and IC50 (concentration required for 50% of maximal inhibition), SAC, SEC, and SPC are equally potent in inhibiting cholesterol synthesis. (
  • Therefore, the IC50 (50% inhibition concentration) of SOD or SOD-like materials can be determined using colorimetric methods. (
  • As nitrogen donors, they contribute to the synthesis of excitatory glutamate and inhibitory gamma-aminobutyric acid (GABA) (Yudkoff et al,, 2005). (
  • The inhibitory effect of resveratrol on poxviruses is independent of VACV N1 protein, a potential resveratrol binding target. (
  • Resveratrol (Res) exerts inhibitory effects on breast cancer cell lines and animal models, while its efficacy against individual breast cancer cases remains unknown. (
  • The results showed that SE, TanⅡA, and SAS are able to improve biochemical level in high altitude hypoxia mouse model, increase in Ca 2+ concentration, and decrease in MMP, inhibit apoptosis in CoCl 2 -induced PC12 cell hypoxia model by activating Akt signaling pathway, protecting neurons, thus improving the oxygen carrying capacity of brain tissue. (
  • Apoptosis is the most well known processes by compounds were prepared as 3mg/ml concentration which cell death is mediated by at least 14 members of stock solutions in dimethyl sulfoxide (DMSO). (
  • Ciprofloxacin maximum serum concentrations and area under the curve are shown in the chart for the 250 mg to 1000 mg dose range. (
  • Serum concentrations increase proportionately with doses up to 1000 mg. (
  • Ethyl Acetate extract has shown better results with 93% inhibition at 100 µg concentration as compared to other solvent extracts. (
  • The study was undertaken to test the inhibitory potential on cholesterogenesis of organosulfur compounds derived from garlic. (
  • Among water-soluble compounds, S-allyl cysteine (SAC), S-ethyl cysteine (SEC), and S-propyl cysteine (SPC) inhibited [2-14C]acetate incorporation into cholesterol in a concentration-dependent manner, achieving 42 to 55% maximal inhibition. (
  • Clinical qui- nine failure was associated with a 50% inhibitory concentra- performance liquid chromatography) taken immediately tion of 829 nmol/L. Increased vigilance is required during before the fourth drug dose was low (7 mg/L). The patient treatment follow-up. (
  • A 500 mg oral dose given every 12 hours has been shown to produce an area under the serum concentration time curve (AUC) equivalent to that produced by an intravenous infusion of 400 mg ciprofloxacin given over 60 minutes every 12 hours. (
  • Influence of gastric inhibitory polypeptide on pentagastrin-stimulated gastric acid secretion in patients with type 2 diabetes and healthy controls. (
  • Flunixin persists in inflammatory tissues and is associated with anti-inflammatory properties which extend well beyond the period associated with detectable plasma drug concentration. (
  • The inhibitory activities of the extracts were compared to ciprofloxacin (256µg/ml). (
  • Results: At 4000 µg/ml, N-hexane extract inhibited the growth of Salmonella Typhi, S. Paratyphi A, B and C while ethylacetate extract was able to inhibit S. Paratyphi A and C. Methanolic and aqueous extracts at the same concentration were unable to inhibit these strains of Salmonella. (
  • Disc containing 20 mg concentration of all the extracts of OS and AM showed maximum inhibitory effect on the growth of S. enterica serovar Typhimurium and E. coli O26. (
  • Absolute IC 50 values are shown on this plot, but software can also estimate relative IC 50 in linear and nonlinear regression analysis. (
  • Finasteride and 13-cis retinoic acid were poor inhibitors of the enzyme with 50% inhibitory concentration values greater than 500 nM. (
  • 50 isolate and these 2 controls are shown in the Table. (
  • However, salts do not have a significant inhibitory effect on enterobacteria. (
  • This study shows the inhibitory effect of emodin on poly I:C-induced RAW 264.7 via calcium-STAT pathway. (
  • This review attempts to relate data on paracetamol's inhibitory action on peripheral cyclooxygenase enzymes to the published literature on its anti-inflammatory action and its hitherto underestimated side-effects elicited by cyclooxygenase inhibition. (
  • In the present review attempts have been undertaken to relate the data on the cyclooxygenase inhibitory potency of paracetamol to the published literature on its anti-inflammatory action and, more importantly, side-effects possibly related to inhibition of cyclooxygenase enzymes. (
  • For tests, TM5441 (20, 50 or 100 mg/kg) was dissolved in DMSO and included into individual portions of peanut butter and honey. (
  • The corneal infection of fungal etiology is very common and comprising at least 50% of all culture positive cases in India [ 2 ]. (
  • Unlike heparin, ODSH does not interact with heparin-platelet factor-4 antibodies present in patients with heparin-induced thrombocytopenia and even suppresses platelet activation in the presence of activating concentrations of heparin. (
  • Emodin restored the cell viability in poly I:C-induced RAW 264.7 at concentrations of up to 50 μM. (
  • Les concentrations minimales inhibitrices ont été déterminées pour l'imipénème, le méropénème et l'ertapénem pour les isolats de Klebsiella . (
  • Relative IC 50 is defined as the concentration of tested compound which results in half of the maximum inhibition of cell growth attainable for that particular compound (orange lines). (
  • The required amount of inhibitory compound was added to each flask to provide the toxic concentration to be investigated. (
  • The inhibitory effects of O. onites essential oil, against C. spp. (
  • The current 2-year study was conducted to investigate the effects of different kinds and concentrations of allelochemicals, p-hydroxybenzoic acid (H), cinnamic acid (C), phthalic acid (P), and their mixtures (M) on peanut root growth and productivity in response to CC obstacle. (
  • GIP-(3-42) does not antagonize insulinotropic effects of GIP at physiological concentrations. (
  • On the basis of single time points, brain concentrations of TRZ, or brain/serum ratios, were similar in P-gp-deficient animals compared with controls, whereas P-gp-deficient animals had significantly higher KET brain concentrations and brain/serum ratios. (
  • It was observed that proliferation of HeLa cells could be significantly inhibited by Atorvastatin in a concentration dependent manner. (
  • Method: Granular sludge (1 g of VSS) was transferred to the serum vials containing 100 mL of the basal medium and acetate was added from concentrated stock solution to obtain a final concentration of 2 g COD/L (readjusted by addition of acetate). (
  • The action mechanism of EOs in both periods was determined by autobiographic method evaluating the inhibitory potential on the acetylcholinesterase enzyme, indicating greater inhibition of the EO enzyme during dormancy (0.039 mg mL-1) when compared to the EO during budding (0.156 mg mL-1). (
  • No pharmacokinetic (PK) observations with patients treated with Osteoset® T have been published so far, despite well known concentration-related potential toxicity of aminoglycosides. (
  • Movement cytometry Cells had been plated in triplicate in 6-well plates at a denseness of 120,000 cells per well and treated with 50 M TM5275 or TM5441 the very next day for eight hours (BromodeoxyUridine (BrdU) incorporation) or 24 and 48 hours (mitochondrial depolarization). (
  • or =1.0 mmol/L). Diallyl sulfide, dipropyl sulfide, and methyl allyl sulfide slightly inhibited [2-14C]acetate incorporation into cholesterol only at high concentrations. (
  • Rhodanobacter abundance is positively correlated with low pH and high concentrations of uranium and 13 other ions and we sought to determine which of these ions are selective pressures that favor the growth of Rhodanobacter over other taxa. (
  • Anxiety was more relevant than depression in the group of women with fibromyalgia, the perception of pain was very high and cognitive impairment was more evident in executive functions, especially planning and inhibitory control. (
  • Only concentrations have been described in patients implanted with a tobramycin-laden polymer carrier material (Simplex™ P Bone Cement with Tobramycin) showing high tobramycin levels at the operative site but low systemic absorption [ 2 ]. (
  • VetaMeg 50 mg/mL is recommended for the alleviation of inflammation and pain associatedwith musculoskeletal disorders in the horse. (
  • VetaMeg 50 mg/mL is also indicated for the controlof inflammation in endotoxemia. (
  • Antibody concentration after reconstitution 0.8 mg/ml. (
  • A microtiter plate was coated overnight with Human Anti-Nivolumab Antibody, clone AbD30255 (HCA299) at a concentration of 1 µg/ml. (
  • After washing and blocking with PBST+5% BSA, a pre-incubated mixture of nivolumab (0.3 µg/ml), spiked with increasing concentrations of Human Anti-Nivolumab Antibody, clone AbD30255 (HCA299) was added. (
  • Generally, the non-polar fractions showed higher enzyme inhibitory activities compared to the polar fractions. (
  • In this study, we examined how vaccination impacts SIV replication in RMs expressing the MHC-I allele Mamu-B*17 Approximately 21% of Mamu-B*17+ and 50% of Mamu-B*08+ RMs control chronic-phase viremia after SIVmac239 infection. (
  • Four patients who already had 50% reduction on ketogenic diet alone achieved an additional 20-30% reduction. (
  • The simple two-point method uses 2 data points bracketing 50% inhibition of proliferation (green lines) to estimate the IC 50 . (
  • In the third method, the software uses all data points to build nonlinear regression model and estimate IC 50 (blue lines). (
  • After single i.p. injections of TRZ or KET in separate groups of control mice, brain concentrations of TRZ exceeded those in serum [brain/serum area under the concentration curve (AUC) ratio, 5.0], whereas brain/serum AUC ratios for KET were approximately 0.5. (
  • AUC, area under the concentration curve. (
  • La ansiedad fue más relevante que la depresión en el grupo de mujeres con fibromialgia, la percepción del dolor fue muy alta y el deterioro cognitivo fue más evidente en las funciones ejecutivas, especialmente en la planificación y el control inhibitorio. (
  • VetaMeg 50 mg/mL is indicated for the control of pyrexia associated with bovine respiratorydisease, endotoxemia and acute bovine mastitis. (