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%).
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.
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].
【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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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 12-50 μg/ ... 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 (LD50) of the extract against Entamoeba histolytica was 33 µg/mLl. Pliny the Elder and Dioscorides ...
At a minimum inhibitory concentration of 25 μM, growth is reduced by 10-fold within 2.5 hours. At concentrations of 50 μM and ...
... plasma concentration increases with age and this may contribute to the tendency for weight gain as people age.[79][80] ... Ghrelin has inhibitory effects on gonadotropin-releasing hormone (GnRH) secretion. It may cause decreased fertility.[63] ... Yokota I, Kitamura S, Hosoda H, Kotani Y, Kangawa K (April 2005). "Concentration of the n-octanoylated active form of ghrelin ... An inverse relationship between the hours of sleep and blood plasma concentrations of ghrelin exists; as the hours of sleep ...
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, ...
The potency of an antagonist is usually defined by its half maximal inhibitory concentration (i.e., IC50 value). This can be ... versus the log concentration of antagonist for a range of antagonist concentrations.[19] The affinity or Ki is where the line ... "the same amount of antagonist blocks higher concentrations of agonist better than lower concentrations of agonist".[26] ... and the lower the concentration of drug that is required to inhibit the maximum biological response. Lower concentrations of ...
7,8-DHF has also been observed to possess in vitro antiestrogenic effects at very high concentrations (Ki = 50 μM). A variety ... Unlike many other flavonoids, 7,8-DHF 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 ...
... half maximal inhibitory concentration). *LD50 (median lethal dose). *Therapeutic index ... The half maximal effective concentration is sometimes also expressed as pEC50 instead of EC50, where: pEC. 50. =. −. log. 10. ⁡ ... Half maximal effective concentration (EC50) refers to the concentration of a drug, antibody or toxicant which induces a ... The inflection point at which the increase in response with increasing ligand concentration begins to slow is the EC50, which ...
"Neomycin sulfate, EP Susceptibility and Minimum Inhibitory Concentration (MIC) Data" (PDF). TOKU-E.. ... more than 50 years after its discovery, its DNA-binding properties were still unknown. Neomycin has been shown to induce ...
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. ...
... 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% ...
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, ...
... half maximal inhibitory concentration). *Draize test. *Indicative limit value. *No-observed-adverse-effect level (NOAEL) ... So, in these cases, the lethal concentration may be given simply as LC50 and qualified by a duration of exposure (e.g., 10 ... lethal concentration, 50%) or LCt50 is a measure of the lethal dose of a toxin, radiation, or pathogen.[1] The value of LD50 ... where C is concentration and t is time. It is often expressed in terms of mg-min/m3. ICt50 is the dose that will cause ...
When the inhibitory signals are prevented, the motor neurons are more easily activated and the victim will have 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 ...
Inhibitory effects of EHNA[edit]. In primary cultures of rat cortical neurons, the inhibition of PDE2A by EHNA potentiates NMDA ... It has also been suggested that PDE2 might play an important role in the regulation of elevated intracellular concentrations of ... It has been reported that higher concentration of cGMP causes inhibition of PDE3, whereas it stimulates PDE2. Interplay between ... intracellular concentrations of cAMP in cardiomyocytes and of cAMP and cGMP in platelets ...
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 ...
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 ...
Nitric oxide (NO) is particularly effective in relaxing the myometrium and in fact has a lower inhibitory concentration 50% (Ki ... and a higher concentration of K+ ions in the intracellular space than in the extracellular space. Subsequently, having K+ ... it is maintained by a Na+/K+ pump that causes a higher concentration of Na+ ions in the extracellular space than in the ... If implantation does not occur, the frequency remains low, but the amplitude increases dramatically to between 50 and 200 mmHg ...
... mM/L of synephrine on rat white fat cells was antagonized by various β-antagonists with the following inhibitory concentrations ... Synephrine has been found in marmalade made from Citrus unshiu (Satsuma mandarin)[14] obtained in Japan, at a concentration of ... This substance is present at very low concentrations in common foodstuffs such as orange juice and other orange (Citrus species ... There was no significant effect on the ileum at synephrine concentrations up to about 2 × 10−4 M, indicating selectivity for ...
... 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 ...
Lower urinary phenethylamine concentrations are also associated with symptoms of inattentiveness in ADHD individuals. ... The 7 repeat variant of dopamine receptor D4 (DRD4-7R) causes increased inhibitory effects induced by dopamine and is ... The symptoms of ADHD arise from a deficiency in certain executive functions (e.g., attentional control, inhibitory control, and ... Urinary and blood plasma phenethylamine concentrations are lower in ADHD individuals relative to controls and the two most ...
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. ... Results showed that prior to beginning substance use, blackout and youth showed greater activation during inhibitory processing ...
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 ...
"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 ...
Malenka RC, Nestler EJ, Hyman SE (2009). "Chapter 5: Excitatory and Inhibitory Amino Acids". In Sydor A, Brown RY (eds.). ... Bleach exposure time and concentration are correlated with destruction of methamphetamine.[133] Methamphetamine in soils has ... inhibition of firing due to increased release of dopamine; (b) reduction of D2 and GABAB receptor-mediated inhibitory responses ... In low to moderate doses, methamphetamine can elevate mood, increase alertness, concentration and energy in fatigued ...
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 ...
"Long-term effects of chronic khat use: impaired inhibitory control". Frontiers in cognition. 12 January 2011. doi:10.3389/fpsyg ... Researchers estimate about 70-80% of Yemenis between 16 and 50 years old chew khat, at least on occasion. Approximately 60-90% ... In 2016, Oslo municipality estimated 50-70% of Somali immigrant males to be habitual users.[79] ...
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.[36] ... 53 (3): 417-50. PMID 11546836.. *^ "CFR - Code of Federal Regulations Title 21: Regulations on OTC products". U.S. Food and ...
Xiong P, Zeng Y, Wu Q, Han Huang DX, Zainal H, Xu X, Wan J, Xu F, Lu J (August 2014). "Combining serum protein concentrations ... GABA is the brain's primary inhibitory neurotransmitter and phosphorylation of GABAA receptors tend to reduce their activity.[ ... BDNF modulates excitatory and inhibitory synaptic transmission by inhibiting GABAA-receptor-mediated post-synaptic currents.[87 ... increasing its ATPase activity which downregulates GABAA receptor surface expression and subsequently attenuates inhibitory ...
SK2 potassium channels mediate inhibitory influence on action potentials and reduce arborization. ... fatigue and problems in concentration. Anxiety can be appropriate, but when experienced regularly the individual may suffer ... 50] Some writers believe that excessive anxiety can lead to an overpotentiation of the limbic system (which includes the ...
... s are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade ... Studies in animal models suggest that ritonavir may have inhibitory effects on the growth of glioma cells.[112] ... 274 (50): 35734-40. doi:10.1074/jbc.274.50.35734. PMID 10585454.. *^ Laurent N, de Boüard S, Guillamo JS, Christov C, Zini R, ... 50] The number of E1, E2, and E3 proteins expressed depends on the organism and cell type, but there are many different E3 ...
... subcutaneous and intravenous routes of administration were also effective at maintaining the desired blood plasma concentration ... Leukemia inhibitory factor (LIF). *Macrophage-stimulating protein (MSP; HLP, HGFLP). *Midkine (NEGF2) ...
Cell viability transiently increased upon the addition of a low concentration, but decreased upon the addition of high ... These two kinases regulate autophagy through inhibitory phosphorylation of the Unc-51-like kinases ULK1 and ULK2 (mammalian ... concentrations. The findings suggest that cannabisin B possesses considerable antiproliferative activity and that it may be ... 50][51] and UVRAG.[52][53] Following the fusion LC3 is retained on the vesicle's inner side and degraded along with the cargo, ...
At high concentrations, it had no effect on spontaneous or potassium evoked amino acid release.[45] ... the main inhibitory neurotransmitter in the central nervous system and decrease voltage-sensitive sodium channels.[2][4] ... Some patients have reported experiencing a loss of concentration, even with very small doses. Lamotrigine has been implicated ... For example, lamotrigine blocked sustained repetitive firing in cultured mouse spinal cord neurons in a concentration-dependent ...
PrP is present in both the pre- and post-synaptic compartments, with the greatest concentration in the pre-synaptic portion.[42 ... "Normal inhibitory avoidance learning and anxiety, but increased locomotor activity in mice devoid of PrP(C)". Brain Res. Mol. ... 6 (6): 435-50. doi:10.1038/nrg1616. PMID 15931169.. *^ Papassotiropoulos A, Wollmer MA, Aguzzi A, Hock C, Nitsch RM, de ... Gerstmann-Sträussler-Scheinker syndrome - usually a change in codon 102 from proline to leucine[50] ...
When a T-cell receptor is activated by contact with a peptide:MHC complex, CD45 dephosphorylates inhibitory tyrosine of ... T cell are less dependent on costimulatory signals and higher antigen concentration than naive T cell.[16] ...
Increased inhibitory effect, compared to thalidomide, was noticed with the groups that had an oxygen atom attached directly to ... In vitro, apremilast reduces PDE4 activity leading to an increase in cyclic-adenosine monophosphate (cAMP) concentrations in ... The improved angiogenesis inhibitory activity could be due to increased solubility or that the positively charged nitrogen has ... Substituents at Z leading to increasing PDE4 inhibitory activity thus followed the order: N(CH3)2 ≤ NH2 < NHC(O)CH3 < CH3 For ...
Taurine is a non-protein sulfur amino acid that is found in high concentrations in human milk. It has been shown to have ... While it is an inhibitory neurotransmitter, its ability to cross the blood brain barrier is limited. There is a lot of ... GABA is a major inhibitory neurotransmitter in the central nervous system. It modulates the activity of several ... of the degradation pathway of the inhibitory neurotransmitter γ-aminobutyric acid, or GABA. The disorder has been identified in ...
... reaches its maximum concentration (tmax) within 1-2 hours.[9] After a 20 mg dose, plasma concentrations reach ... Tranylcypromine analogues with more potent and selective LSD1 inhibitory activity are being researched in the potential ... Tranylcypromine has been found to inhibit CYP46A1 at nanomolar concentrations.[16] The clinical relevance of this effect is ... that tranylcypromine is a high-affinity substrate for CYP2A6 and does not inhibit CYP enzymes at therapeutic concentrations.[9] ...
Among them, the inhibitory activity of semisynthetic sulfated tri mannose C-C-linked dimers (STMCs) to P-selectin was shown by ... In ischemic stroke patients, plasma P-selectin concentration was reported to be highly correlated to plasminogen activator ... P-selectin is located on chromosome 1q21-q24, spans , 50 kb and contains 17 exons in humans.[7] P-selectin is constitutively ...
Brain catecholamine levels are high,[88] and corticotropin-releasing factor (CRF) concentrations are high.[89][90] Together, ... Descending inhibitory inputs from the medial prefrontal cortex (mPFC) regulate the transmission from the BLA to the CeA, which ... Multiple studies described elevated concentrations of the thyroid hormone triiodothyronine in PTSD.[97] This kind of type 2 ... Lindley SE, Carlson EB, Benoit M (May 2004). "Basal and dexamethasone suppressed salivary cortisol concentrations in a ...
These results require relatively high concentrations (at a concentration of 10 μM). Blocking the formation of 5-HETE, by ... Macrophage inhibitory cytokine-1 (MIC-1) stimulates the focal adhesion kinase (FAK) signaling pathway which leads to prostate ... Unfortunately, oral ingestion of zinc is ineffective since high concentrations of zinc into prostate cells is not possible ... doi:10.1186/1475-2891-9-50. PMC 2987772 . PMID 21044319.. *^ "Chemicals in Meat Cooked at High Temperatures and Cancer Risk". ...
Potassium concentration[edit]. Main articles: Potassium § Homeostasis, and Potassium in biology. High potassium concentrations ... Inhibitory neurons using GABA, make compensating changes in the neuronal networks preventing runaway levels of excitation.[61] ... Sodium concentration[edit]. Main article: Renin-angiotensin system. Further information: Sodium in biology, Tubuloglomerular ... High PTH concentrations cause the excretion of phosphate ions via the urine. Since phosphates combine with calcium ions to form ...
The half-life of venlafaxine is about 5 hours, and with once-daily dosing, steady-state concentration is achieved after about 3 ... The results showed that the strongest electron-withdrawing m-trifluoromethyl analogue exhibited the most potent inhibitory ... This results in an increase in the extracellular concentrations of serotonin and norepinephrine and, therefore, an increase in ... Increasing the electron-withdrawing nature of the aromatic ring provides more potent inhibitory effect of norepinephrine uptake ...
... a known inhibitory factor in breast development.[58] Moreover, suppression of PGE2 in breast tissue is relevant because, via ... which keeps prolactin concentrations high, levels of prolactin will quickly drop, the menstrual cycle will resume and hence ... and leukemia inhibitory factor (LIF).[40] These factors regulate cellular growth, proliferation, and differentiation via ... during oral contraceptive use and with lessening of the normal age-associated decline in circulating IGF-1 concentrations in ...
Cells that are attracted by chemokines follow a signal of increasing chemokine concentration towards the source of the ... an important role in mast cell recruitment and activation in the lung.There is also evidence that CXCL8 might be inhibitory of ... Inflammatory: inflammatory chemokines are produced in high concentrations during infection or injury and determine the ... Chemokines released by infected or damaged cells form a concentration gradient. Attracted cells move through the gradient ...
Low concentrations of urate in the blood serum is associated with an increased risk of PD.[48] ... the basal ganglia normally exert a constant inhibitory influence on a wide range of motor systems, preventing them from ... 50-66. ISBN 978-0-7817-7881-7.. *^ Nuytemans K, Theuns J, Cruts M, Van Broeckhoven C (July 2010) [18 May 2010]. "Genetic ... Genes implicated in the development of PD include SNCA, LRRK2, GBA, PRKN, PINK1, PARK7, VPS35, EIF4G1, DNAJC13 and CHCHD2.[50] ...
In low doses, methamphetamine can cause an elevated mood and increase alertness, concentration, and energy in fatigued ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors,[67] however the implications for humans ... thereby increasing the concentration of these neurotransmitters in the cytosol, or intracellular fluid, of the presynaptic ... 5 (6): 50-55. PMC 2695750. PMID 19727285.. *^ Wilens TE, Adler LA, Adams J, Sgambati S, Rotrosen J, Sawtelle R, Utzinger L, ...
A related gene family of GluN3 A and B subunits have an inhibitory effect on receptor activity. Multiple receptor isoforms with ... The excitatory postsynaptic potential (EPSP) produced by activation of an NMDA receptor increases the concentration of Ca2+ in ... However, overactivation of NMDAR increases the cytosolic concentrations of calcium and zinc, which significantly contributes to ... These antagonists can be displaced from the receptor by high concentration of glutamate which can exist under excitotoxic ...
Peak plasma concentrations are seen in about one hour, with peak cerebrospinal fluid concentrations at 1.4-3.8 hours. When ... The strong potency of rivastigmine, provided by its dual inhibitory mechanism, has been postulated to lead to more nausea and ... concentration) as the highest doses of rivastigmine capsules, but with one-third fewer reports of nausea and vomiting.[1] ... with lower peak plasma concentrations and reduced fluctuations.[17] The 9.5 mg/24 h rivastigmine patch provides comparable ...
Thiocyanate concentration in saliva of cystic fibrosis patients. . In: Folia Histochem. Cytobiol.. . 46, Nr. 2, 2008, S. 245-6 ... Combined inhibitory effect of bovine immune whey and peroxidase-generated hypothiocyanite against glucose uptake by ... 50, 1996, S. 227-244. *↑ Wever R, Kast WM, Kasinoedin JH, Boelens R: The peroxidation of thiocyanate catalysed by ...
In the body's tissues, the concentration of calcium ions (Ca2+. ) outside cells is normally about 10000-fold higher than the ... Chiodera P, Coiro V (May 1990). "Inhibitory effect of ethanol on the arginine vasopressin response to insulin-induced ... Neurons were exposed to sustained ethanol concentrations of 50 mM for 3 days in vitro. Western blot and protein analysis were ... Results showed calcium current decreased as concentration of ethanol increased.[24] Similar results have shown to be true in ...
... antibiotics without exceeding total daily dose would help to keep the antibiotics level above minimum inhibitory concentration ... Once daily dosing of aminoglycoside is sufficient to achieve peak plasma concentration for clinical response without kidney ... platelet count , 80,000/mm3 or 50% drop from maximum in chronically thrombocytopenic, or ... 50% of all sepsis cases start as an infection in the lungs. In one third to one-half of cases, the source of infection is ...
... with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ.[2] ...
... of malignant tumors express high concentrations of VEGF. Strategies to inhibit the VEGF pathway include antibodies directed ... Cartilage-Derived Angiogenesis Inhibitory Factor. matrix metalloproteinase inhibitors. angiostatin. inhibit cell proliferation ... This page was last edited on 9 February 2018, at 04:50. ...
Inhibitory concentration required to inhibit HIV replication in H9 lymphocytes growth by 50%. ...
... inhibitory concentration against human protease enzyme plasmin; IA: Inactive. ...
... aureus demonstrated that this molecule was likely responsible for the inhibitory activity, and further proof was provided when ... aureus demonstrated that this molecule was likely responsible for the inhibitory activity, and further proof was provided when ... The dog pathogen, S. schleiferi, expressed the most potent inhibitory activity and was active against all four agr classes ... The dog pathogen, S. schleiferi, expressed the most potent inhibitory activity and was active against all four agr classes ...
... 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 ...
Valeriana; X-ray diffraction; anti-inflammatory activity; inhibitory concentration 50; irradiation; macrophages; nitric oxide; ... inhibitory concentration 50 Remove constraint Subject: inhibitory concentration 50 Start Over ...
Serum Macrophage Inhibitory Cytokine-1 Concentrations Correlate with the Presence of Prostate Cancer Bone Metastases. Katri S. ... Serum concentrations of macrophage inhibitory cytokine 1 (MIC 1) as a predictor of miscarriage. Lancet 2004;363:129-30. ... Concentration in plasma of macrophage inhibitory cytokine-1 and risk of cardiovascular events in women: a nested case-control ... Serum Macrophage Inhibitory Cytokine-1 Concentrations Correlate with the Presence of Prostate Cancer Bone Metastases ...
Half-maximal inhibitory concentration. PBS. Phosphate-buffered saline. SEM. Scanning electron microscopy ...
... half maximal inhibitory concentration; hydroxysafflor yellow A; traditional Chinese medicine ... CYP; Cytochrome P450; DGLL; Detoxification; Drug interactions; GA; GZ; HSYA; IC(50); Liquorice; P-glycoprotein; P-gp; TCM; ...
Concentrations (mg/L). A Value. Inhibitory rate (%). IC50 (mg/L). Concentrations (mg/L). A Value. Inhibitory rate (%). IC50 (mg ... Table 1. Inhibitory effects of 5-FU and GA-CTS/5-FU on proliferation of the SMMC-7721 parental cell line and the SMMC-7721 5-FU ... Table 1. Inhibitory effects of 5-FU and GA-CTS/5-FU on proliferation of the SMMC-7721 parental cell line and the SMMC-7721 5-FU ... The lowest concentration was seen with 5-FU. In other tissues, the levels of 5-FU were lower following treatment with GA-CTS/5- ...
minimal inhibitory concentration. IC50. half maximal inhibitory concentration. HIV. human immunodeficiency virus ...
Inhibitory Concentration 50 * Models, Molecular * Molecular Conformation * Protein Binding / drug effects * Proto-Oncogene ...
... inhibitory concentration of 829 nmol/L. Increased vigilance is required during treatment follow-up. ... Clinical quinine failure was associated with a 50% ... Inhibitory concentration. Study isolate. 3D7. W2. Cutoff value ...
... inhibitory concentration. LD50:. Median lethal dose. PCV:. Packed cell volume. ... This pronounced antimalarial activity observed in the established infection test may be due to inhibitory effect of the extract ... 45-50, 2010. View at Publisher · View at Google Scholar · View at Scopus ... This suggests that LD50 of the extract is greater than 2000 mg/kg. ...
Half maximal inhibitory concentration.. Conflicts of Interest. The authors declare that there are no conflict of interests ... with zone of inhibition diameters ranging within 0-30 mm and minimal inhibitory concentration (MIC) values of 1 : 512-1 : 4096 ... The Iranian Citrus aurantifolia and Citrus aurantium extracts revealed a strong urease inhibitory activity, with IC50 values of ... The 2.5% (v/v) concentration of BJ inhibited the growth of the clinical isolates tested by 50%, while 5% of BJ reduced H. ...
Inhibitory Concentration 50 * Luminescent Proteins / metabolism * Plasmodium falciparum / drug effects * Plasmodium falciparum ...
... half maximal inhibitory concentration. ... CD4i antibodies in the presence of subinhibitory concentrations ... A, Neutralization of SF162, shown as the reciprocal dilution providing 50% reduction in reporter signal. Group assignments are ... The dashed line indicates 50% neutralization cutoff. Group designation indicated below each box plot. Ab, antibody; Ctrl, ...
Half maximal inhibitory concentration (IC50). The obtained absorbance at 540 nm was used to determine the percentage of cell ... Three replications of each experiment were performed and the half maximal inhibitory concentration (IC50) of each extract was ... the fractional inhibitory concentration index (FICI) method should be performed in order to determine the level, if any, of ... Aso K, Kanno S, Tadano T, Satoh S, Ishikawa M: Inhibitory effect of propolis on the growth of human leukemia U937. Biol ...
Rutaceae; alpha-glucosidase; biochemical pathways; enzyme inhibition; inhibitory concentration 50; phenolic compounds; stems. ... inhibitory concentration 50 Text Availability Citation in PubAg Remove constraint Text Availability: Citation in PubAg Start ... Trichilia; bark; cell lines; chemical composition; cytotoxicity; inhibitory concentration 50; leaves; lymphoma; mass ... Gardenia jasminoides; cytotoxicity; ethanol; flowers; hepatoma; inhibitory concentration 50; neoplasm cells; nuclear magnetic ...
... inhibitory concentration for wild-type CCR5-tropic HIV-1.. Type: Poster. Title: Lower than expected Maraviroc concentrations in ... inhibitory concentration for wild-type CCR5-tropic HIV-1.. Lower than expected Maraviroc concentrations in cerebrospinal fluid ... inhibitory concentration for wild-type CCR5-tropic HIV-1.. Authors: Croteau D, Best B, Letendre S, Rossi S, Ellis RJ, Clifford ... Home /Lower than expected Maraviroc concentrations in cerebrospinal fluid still exceed the 50% ...
Urease inhibitory activity of ursane type sulfated saponins from the aerial parts of Zygophyllum fabago Linn.(Short ... Table 1 Urease inhibitory activity of compounds 1-5. Compounds Inhibition at 0.5 mM concentration [%) 1 87.0 2 75.8 3 60.0 4 ... Urease inhibitory activity Sulfated saponins Ursane Molecular docking Introduction Many plants belonging to the genus ... S.v. Urease inhibitory activity of ursane type sulfated saponins from the aerial parts of Zygophyllum fabago Linn.." Retrieved ...
median inhibitory concentration. ID50. median inhibitory dose. IPCS. International Programme on Chemical Safety. ...
... inhibitory concentration. IPA. Ingenuity Pathway Analysis. ISR. integrated stress response. LC50. 50% lethal concentration. ... inhibitory concentration) was calculated from three independent experiments using SigmaPlot (version 12.5) software (Systat ... being the latter accumulated in a concentration-dependent fashion (Table I). In contrast, only the highest concentration of CA ... 3D). Compared with the stronger inhibitory activity of MG-132 (IC50∼70 nm, Fig. 3E), CS was ∼200-fold less potent, suggesting ...
... inhibitory concentration 50; ID, intellectual disability; L-AP4, L-2-amino-4-phosphonobutyric acid; LiCl, lithium chloride; ... Disruption of the interaction between PICK1 and mGlu7 appears to interfere with mGlu7s inhibitory activity via decreased cell ... 1996). Target-cell-specific concentration of a metabotropic glutamate receptor in the presynaptic active zone. Nature 381, 523- ... Further pharmacological experiments confirmed the specific involvement of mGlu7: only a high concentration of L-AP4 depressed ...
Background Mutant prevention concentration (MPC) is an alternative pharmacodynamic parameter that has been used to measure ... C max serum maximum concentration, AUC 24h area under curve over a 24 h time period, MIC minimum inhibitory concentration, MPC ... The concentration range between minimum inhibitory concentration (MIC) and MPC is defined as mutant selection window (MSW). The ... a comparison of minimum inhibitory concentrations and mutant prevention concentrations for ceftiofur, cefquinome, florfenicol, ...
... inhibitory concentration (IC50) of an unlabeled test peptide to the purified DR is a reasonable approximation of the affinity ... Final detergent concentration in the incubation mixture was 0.05% Nonidet P-40. Assays were performed at pH 7.0 with the ... The final concentrations of protease inhibitors (each from Calbiochem) were: 1 mM PMSF, 1.3 nM 1.10 phenanthroline, 73 μM ... Peptide inhibitors were typically tested at concentrations ranging from 120 μg/ml to 1.2 ng/ml. In appropriate stoichiometric ...
CI-1040 had no inhibitory effect on the growth of SNU-423 cells at a concentration of 0.1 μm (Fig. 4C), but it was able to ... inhibitory concentration (IC50) of 0.172 μm. It was ∼70-fold more sensitive than the least sensitive cell line, SNU-387 (IC50 ... inhibitory concentration. p-RPS6 S235/236. ribosomal protein S6 phosphorylated at the serine 235/236 residue. MAPK. mitogen- ... Note that CI-1040 had no significant inhibitory effect on cell growth at 0.1 μm (indicated by a red arrow). D, sorafenib- ...
The EA-AP and En-AP showed less inhibitory activity of mushroom tyrosinase than ascorbic acid at the maximum concentration. In ... inhibitory concentration of melanin secretion and cellular tyrosinase activity in melan-a cells was approximately 31.3 μg/ml of ... melan-a cells were treated with different concentrations of these extracts. The inhibitory effect of EA-AP and En-AP on melanin ... The inhibitory activity (IC50) of mushroom tyrosinase on Asterina pectinifera extracts in mushroom tyrosinase. ...
Inhibitory Concentration 50. Liver Neoplasms / enzymology*, genetics, pathology. Mitogen-Activated Protein Kinase 10 / genetics ... was developed by exposing parental cells to gradually increasing concentrations of adriamycin. The MTT assay was used to ...
  • This is a measurement of the half maximal inhibitory concentration. (
  • ELP-p21 had little effect on proliferation, while the half maximal inhibitory concentration of p21-ELP-Bac was ~30 µM. (
  • NC 2067 retained its anticancer activity in the complex with CDgemini surfactant for different drug-to-carrier mole ratios, with an IC 50 (half-maximal inhibitory concentration) value comparable to that for NC 2067 without the carrier. (
  • However, free-drug concentrations in brain following 40 mg/kg intravenous dose reach levels that exceed reported in vitro half-maximal inhibitory concentration (IC 50 ) values, suggesting that E6201 may be efficacious in inhibiting MEK-driven brain tumors. (
  • The study was conducted to determine the antioxidant capacity, expressed as half maximal inhibitory concentration, IC 50 , of Caesalpinia pulcherrima leaf, flower and seed methanol extracts, and their correlation to their total phenolic, flavonoid and triterpenoid contents. (
  • At concentrations that appear clinically achievable in humans, AF demonstrated potent antiproliferative and proapoptotic effects in canine lymphoid tumor cell lines. (
  • 50 clindamycin was 39 mol/L (the in vitro resistance cutoff or protection against mosquitoes. (
  • Traditionally, the in vitro activity of antimicrobial susceptibility is assessed by minimum inhibitory concentration (MIC) or minimum bactericidal concentration (MBC). (
  • The mutant prevention concentration (MPC) concept is an alternative in vitro measurement of drug susceptibility against the infecting pathogen, representing the drug concentration that prevents a population of more than 10 10 colony forming unit (CFU)/mL bacteria from first mutation. (
  • Auranofin appears to inhibit the growth and initiate apoptosis in canine lymphoma cells in vitro at clinically achievable concentrations. (
  • Mitochondrial inhibition in vitro occurred at a CPC concentration that may be relevant to human exposures. (
  • MIC50/90 is the lowest concentration required to inhibit 50%/90% of the isolates tested. (
  • Because of the difficulties in counting actual organisms in a dose, infective doses may be expressed in terms of biological assay, such as the number of LD 50 's to some test animal. (
  • Correlation data revealed a strong negative correlation between the IC 50 and the total phenolic, flavonoid and triterpenoid contents of the extracts, with statistically significant negative correlations observed between the flavonoids of leaf (r=-0.997) and flower¬ (r=-0.998) with reducing power assay, and triterpenoids of flower (r=-1.000) with 2,2-diphenyl-1-picrylhydrazyl scavenging assay. (
  • Expression microarrays were utilized to estimate the EMT status as a binary phenotype, and the transcriptional responses of 46 ovarian cancer cell lines to cisplatin were measured at dosages equivalent to 50% growth inhibition. (
  • EA-AP and En-AP induced significant inhibition of melanin production and cellular tyrosinase activity. (
  • The average daily pSTAT and time above 50% inhibition were calculated at clinical plasma drug exposures in immune cells. (
  • The drugs inhibitory concentration at 90% inhibition. (
  • Both 1 and 2 were found to have moderate inhibitory activity against the transcription factor AP-1 (IC₅₀ = 5.2 and 6.0 μM, respectively). (
  • In terms of IC 50 values, the crude extract (65,48 μg/mL) exhibited moderate inhibitory activity which was as half potent as that of its ethyl acetate fraction (32,94 μg/mL). (
  • The 50% inhibitory concentration (LD50) of the extract against Entamoeba histolytica was 33 µg/mLl. (
  • 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. (
  • In addition, the compounds were not toxic to nonmalignant fibroblast cells at the IC50 concentrations. (
  • Focusing the immune response toward selected determinants could be of value in the case of various chronic viral diseases and cancer, where T cells directed against the immunodominant epitopes might have been inactivated and T cells specific for subdominant epitopes might have escaped T cell tolerance ( 44 , 45 , 46 , 47 , 48 , 49 , 50 ). (
  • D ) Effect of MS0015203 (0 to 10 μM) on cAMP concentrations in wild-type Neuro2A cells (N2A) and Neuro2A cells in which GPR171 is knocked down (N2A + KDV). (
  • METHODS: A MDR human HCC cell line, SMMC-7721/ADM, was developed by exposing parental cells to gradually increasing concentrations of adriamycin. (
  • These cells were further exposed to stepwise increased concentrations of TPT, up to 950 n m TPT. (
  • From this time point on, the cells were exposed to this concentration of drug weekly for 1 h. (
  • A TAMR/MCF-7 cells xenograft model was established to investigate the inhibitory effect of SAHA on tumor growth in vivo. (
  • Local high concentrations of Cx were shown to impede the proliferation of cancer cells directly, while chemoprevention has been demonstrated with low Cx doses. (
  • Background- Because complement-mediated vascular injury participates in atherosclerosis and C-reactive protein (CRP) can activate the complement cascade, we sought to determine whether CRP affects the expression of the protective complement-inhibitory factors on the cell surface of endothelial cells (ECs). (
  • When grown as spheroids, the IC 50 of STA-1474 for BACA cells was approximately two-fold higher than when grown as a monolayer (0.348 μM vs . 0.168 μM), whereas CLAC spheroids were relatively drug resistant. (
  • Peter Anderson (Abstract 96LB) led the iPrEx pharmacology effort to measure plasma and intracellular concentrations of FTC and tenofovir (TFV). (
  • In toxicology , the median lethal dose , LD 50 (abbreviation for " lethal dose , 50%"), LC 50 (lethal concentration, 50%) or LCt 50 is a measure of the lethal dose of a toxin , radiation , or pathogen . (
  • The median infective dose (ID 50 ) is the number of organisms received by a person or test animal qualified by the route of administration (e.g., 1,200 org/man per oral). (
  • Among the viruses neutralized, the median 50% inhibitory concentration was 0.001 μg/ml. (
  • median inhibitory concentration [IC 50 ], 0.1 μM in cellular phosphorylation assays). (
  • This appears to arise because TAF is able to achieve higher intracellular concentrations of TFV-diphosphate (the pharmacologically-active moiety) at lower plasma TFV concentrations. (
  • As expected, plasma TFV concentrations after oral dosing were much higher, 30-fold for AUC, than rectal. (
  • In addition, the enzyme extract (En-AP) of A. pectinifera, to which protease was added, was processed. (
  • A study was carried out in the comparative analysis of ethanolic extract (50%) of clove & clove oil as natural antimicrobial agents on some food spoilage bacteria. (
  • The antibacterial activity of clove oil & its extract (50% ethanol) was tested against ten bacteria (seven Gram positive & three Gram negative) & seven fungi by agar well diffusion assays. (
  • The 50% inhibitory concentration (IC 50 ) of each extract was calculated by PROBIT analysis. (
  • We don't see, however, how lower plasma concentrations explains the greater increase in fasting lipids seen with TAF. (
  • The dog pathogen, Staphylococcus schleiferi , expressed the most potent inhibitory activity and was active against all four agr classes found in S. aureus . (
  • Subsequent cloning and heterologous expression of the S. schleiferi AIP in S. aureus demonstrated that this molecule was likely responsible for the inhibitory activity, and further proof was provided when pure synthetic S. schleiferi AIP was able to completely abolish agr induction of an S. aureus reporter strain. (
  • Further fractionation by size exclusion chromatography lead to four fractions for each of 30DCM and 100DCM, with the highest antiproliferative activity on cancer but not normal cell lines being observed in fraction# 3 of 30DCM (IC 50 value of 4.09 - 14.7 μg/ml). (
  • The more enriched propolis fractions typically revealed a higher antiproliferative activity (lower IC 50 value). (
  • CA treatment induces the expression of proteins involved in the unfolded protein response in a concentration dependent manner reflecting ER stress, whereas CS directly inhibits chymotrypsin-like activity of the 20S proteasome. (
  • Urease inhibitory activity of ursane type sulfated saponins from the aerial parts of Zygophyllum fabago Linn. (
  • The urease inhibitory effects of these compounds have been investigated for the first time as well as their molecular docking studies have also been carried out to check the structure-activity relationship. (
  • In view of this broad inhibitory spectrum, the precise mechanisms underlying the anti-tumor activity remain elusive. (
  • Mutant prevention concentration (MPC) is an alternative pharmacodynamic parameter that has been used to measure antimicrobial activity and represents the propensities of antimicrobial agents to select resistant mutants. (
  • EA-AP and En-AP among A. pectinifera extracts showed strong inhibitory activity against the cell-free mushroom tyrosinase activity. (
  • These results showed that EA-AP and En-AP inhibited melanogenesis by reducing tyrosinase activity and melanin production via subsequent downregulation of tyrosinase-related proteins. (
  • The most promising leishmanicidal activity was observed with diethyl ether fraction of the roots of Rhynchostylis retusa with IC 50 values of 56.04 and 18.4 μg/mL against promastigotes and intracellular amastigotes respectively. (
  • In all three cases, there was overlap of the antiestrogenic activity with the mitochondrial inhibitory activity. (
  • The antiestrogenic activity of CPC, BAK, rotenone, and triclosan may be related to their mitochondrial inhibitory activity. (
  • The cultures were evaluated for antiprotozoal activity based on their 50 percent inhibitory concentration. (
  • The CMNSXXI researchers reported that the chloroform fraction achieved the highest inhibitory activity against Entamoeba histolytica and Giardia lamblia . (
  • The cell viability (%) and IC 50 values were calculated. (
  • The [IC.sub.50] values of these compounds could not be found due to paucity of the samples. (
  • P = .018) to 50% inhibitory concentration values. (
  • MPC 50 / MPC 90 values were 4/64、8/64、4/32、16/256 μg/mL, respectively. (
  • Against early stage gametocytes IC 50 values ranging between 60 nM and 7.5 μM were obtained. (
  • The IC 50 values of ursolic acid against G. lamblia and T. vaginalis were 8.12 μg/mL and 5.51 μg/mL, respectively. (
  • Lower than expected Maraviroc concentrations in cerebrospinal fluid still exceed the 50% inhibitory concentration for wild-type CCR5-tropic HIV-1. (
  • 50 isolate and these 2 controls are shown in the Table. (
  • BAK, another antimicrobial QUATS that is structurally similar to CPC, and the pesticide rotenone, a known complex 1 inhibitor, also showed mitochondrial inhibitory and antiestrogenic effects. (
  • Treatment of tumor-stromal fibroblasts with STA-1474 resulted in a dose-dependent decrease in their relative cell viability with a low IC 50 of 0.28 μM. (
  • As significant decreases in relative cell viability can be achieved with nanomolar concentrations of STA-1474, investigation into the clinical efficacy of this drug in canine lung cancer patients is warranted. (
  • TFV-diphosphate concentrations were detectable in rectal tissue and were greater after 7 days of rectal application that after the single application. (
  • Zygophyllum fabago extracts may also contain antiviral photosensitizers but the activities were only seen at high concentrations (Hudson et al. (
  • [1] The value of LD 50 for a substance is the dose required to kill half the members of a tested population after a specified test duration. (
  • The related quantities LD 50 /30 or LD 50 /60 are used to refer to a dose that without treatment will be lethal to 50% of the population within (respectively) 30 or 60 days. (
  • ICt 50 is the dose that will cause incapacitation rather than death. (
  • The IC 50 was much lower for all triphenylphosphonium derivatives when compared to betulinic acid. (
  • Combined inhibitory effects on daunorubicin transport were observed when cepharanthin was used together with cyclosporin A, a potent immunosuppressive agent and P-glycoprotein modulator. (
  • It's either the initial or steady state concentration of the drug in the blood plasma. (
  • This is the peak concentration of a drug after administration. (
  • This is the lowest concentration a drug reaches before a second administration of the drug occurs. (
  • Typically measured in hours, it is the time required for the concentration of the drug in your blood to be reduced by ½. (
  • In other words, it is a measure of how much drug must be taken before 50% of the particular biochemical function is inhibited. (
  • The human prostate cell line, PC‑3, was exposed to docetaxel, the concentrations of which were increased in a stepwise manner in the medium to select the drug‑resistant cell line, PC‑3/DTX. (
  • Clinical data have demonstrated that, in addition to the ~50% of patients who fail to respond to docetaxel inherently, in most patients who initially respond to the drug, disease progression will recur within 1 year from the start of treatment, indicating the generation of acquired chemoresistance ( 5 ). (
  • In 2011, the U.S. Food and Drug Administration approved alternative methods to LD 50 for testing the cosmetic drug Botox without animal tests. (
  • Concerns regarding the applicability of most rodent cancer models to human patients include immune status, lack of clonal heterogeneity, tumor location (orthotopic versus heterotopic), relative tumor burden, differences in drug distribution/metabolism, and differences in "achievable" drug concentrations. (
  • MTT reduction, a measure of cell proliferation, diminished as a function of increasing drug concentration and exposure time in the HT-29 cell line studies. (
  • For example, all infections in the active arm of the primary analysis were associated with undetectable (91%) or low (9%) drug concentrations. (
  • Neomycin had also an inhibitory effect on the DMPP-induced increase in cytosolic Ca ++ concentration ([Ca ++ ] i ). (
  • The inhibitory effect of neomycin on the DMPP-induced [Ca ++ ] i increase was apparent when the neomycin treatment was performed simultaneously with DMPP, suggesting a direct action on the nicotinic receptor. (
  • The results of this study suggest that EEAML has a possible neurotoxic effect in concentrations equal to or greater than 5 mg/ml. (
  • 13 The effect of CRP on the expression of complement-inhibitory factors is unknown. (
  • Because complement-inhibitory proteins protect the endothelium from complement-mediated injury and CRP is proatherogenic, in part because of its ability to activate complement, we hypothesized that the detrimental effect of CRP may involve the downregulation of these protective proteins. (
  • These results indicate that cepharanthin can reverse multidrug resistance, and proper combination with other P-glycoprotein modulators could potentiate its inhibitory effect on expelling the anticancer drugs out of the cell via P-glycoprotein. (
  • A drugs effective concentration at 50% of the max effect. (
  • 12 It has recently been shown that SU5416 inhibits cellular phosphorylation of both wild-type FLT3 and FLT3-ITD mutants (IC 50 , 0.1-0.25 μM). (
  • Preincubation for 24 h with high glucose and insulin (high Glc/Ins) reduced insulin-stimulated GLUT4 translocation by 50%, without affecting GLUT4 expression. (
  • A comparable measurement is LCt 50 , which relates to lethal dosage from exposure, where C is concentration and t is time. (
  • LD 50 figures are frequently used as a general indicator of a substance's acute toxicity . (
  • A lower LD 50 is indicative of increased toxicity. (
  • As a measure of toxicity, LD 50 is somewhat unreliable and results may vary greatly between testing facilities due to factors such as the genetic characteristics of the sample population, animal species tested, environmental factors and mode of administration. (
  • In the action of EA-AP and En-AP on melanogenesis, they reduced the expression of melanogenic genes and proteins including tyrosinase, tyrosinase-related protein-1 (TRP-1) and dopachrome tautomerase (Dct). (
  • Methods and Results- Human coronary artery or human saphenous vein ECs were incubated with CRP (0 to 100 μg/mL, 0 to 72 hours), and the expression of the complement-inhibitory proteins decay-accelerating factor (DAF), membrane cofactor protein (CD46), and CD59 were measured by flow cytometry. (
  • The increased expression of complement-inhibitory proteins was functionally effective, resulting in significant reduction of complement-mediated lysis of antibody-coated human saphenous vein ECs. (
  • 50 μl samples of N=139 unfrozen individual normal platelet poor citrated plasmas and of N=11 unfrozen normal citrated plasma pools were supplemented with the clinically relevant concentration of 0 to 19.6 mg/l of gentamicin on microtiter plates. (
  • The overall results suggest that EA-AP and En-AP among A. pectinifera extracts may be promising candidates for the treatment of hyperpigmentation disorder and useful for self-tanning cosmetic products. (
  • 9 Due to a high degree of sequence homology among different receptor tyrosine kinases (RTKs), the related receptor c-kit is inhibited by SU5416 to a significant degree (IC 50 , 0.1 μM). (
  • 50 roquine (472 nmol/L, threshold 100 nmol/L). The IC for transmission ( 3 ). (
  • Our findings support the need for additional research on the mitochondrial inhibitory and antiestrogenic effects of QUATS, including CPC and BAK. (
  • 3 With rare exceptions in cases of hematopoietic cell transplantation, 4 the overall response rates for novel agents including retinoids, histone deacetylase (HDAC) inhibitors, and pralatrexate range from 30% to 50% and are generally not durable. (
  • The total concentrations in brain were higher than in plasma, resulting in a brain-to-plasma AUC ratio (Kp) of 2.66 in wild-type mice. (
  • The results showed that the mutant strain NB327 was exposed to EEAML (5 mg/ml) concentration, it showed a significant decrease in average locomotion, resulting in 13 undulations in 30 s. (
  • It can lower the water's surface tension from 72 mN/m to 27 mN/m at a concentration as low as 20 μM. (
  • Macrophage-inhibitory cytokine-1 (MIC-1) is a divergent member of the transforming growth factor β superfamily. (
  • Macrophage-inhibitory cytokine-1 (MIC-1), also known as PLAB, prostate-derived factor, GDF-15, and NAG-1, is a divergent member of the transforming growth factor β superfamily ( 1 , 2 ). (
  • some may be killed by much less, while others survive doses far higher than the LD 50 . (
  • 50 copies/mL) at 4--6 months after treatment initiation. (
  • After treatment at this concentration, one colony was picked. (
  • 50 copies/ml without treatment. (