Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA.
The agent of South American trypanosomiasis or CHAGAS DISEASE. Its vertebrate hosts are man and various domestic and wild animals. Insects of several species are vectors.
A hemoflagellate subspecies of parasitic protozoa that causes nagana in domestic and game animals in Africa. It apparently does not infect humans. It is transmitted by bites of tsetse flies (Glossina).
Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.
A disease endemic among people and animals in Central Africa. It is caused by various species of trypanosomes, particularly T. gambiense and T. rhodesiense. Its second host is the TSETSE FLY. Involvement of the central nervous system produces "African sleeping sickness." Nagana is a rapidly fatal trypanosomiasis of horses and other animals.
An effective trypanocidal agent.
A hemoflagellate subspecies of parasitic protozoa that causes Rhodesian sleeping sickness in humans. It is carried by Glossina pallidipes, G. morsitans and occasionally other species of game-attacking tsetse flies.
A genus of flagellate protozoans found in the blood and lymph of vertebrates and invertebrates, both hosts being required to complete the life cycle.
Infection with protozoa of the genus TRYPANOSOMA.
A homologous group of cyclic GLUCANS consisting of alpha-1,4 bound glucose units obtained by the action of cyclodextrin glucanotransferase on starch or similar substrates. The enzyme is produced by certain species of Bacillus. Cyclodextrins form inclusion complexes with a wide variety of substances.
A method that is derived from western blotting (BLOTTING, WESTERN) and is used to detect protein-protein interactions. The blotted proteins are probed with a non-antibody protein which can then be tagged with a labeled antibody.
Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.
Cyclic GLUCANS consisting of six (6) glucopyranose units linked by 1,4-glycosidic bonds.
Cyclic GLUCANS consisting of eight (8) glucopyranose units linked by 1,4-glycosidic bonds.
The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Enzymes that catalyze the transfer of glucose from a nucleoside diphosphate glucose to an acceptor molecule which is frequently another carbohydrate. EC 2.4.1.-.
A nitrofuran thiazine that has been used against TRYPANOSOMIASIS.
Enzymes which reduce nitro groups (NITRO COMPOUNDS) and other nitrogenous compounds.
A hemoflagellate subspecies of parasitic protozoa that causes Gambian or West African sleeping sickness in humans. The vector host is usually the tsetse fly (Glossina).
Arsenical used in trypanosomiases. It may cause fatal encephalopathy and other undesirable side effects.
A class of annelid worms with few setae per segment. It includes the earthworms such as Lumbricus and Eisenia.
A serine protease that catalyses the release of an N-terminal dipeptide. Several biologically-active peptides have been identified as dipeptidyl peptidase 4 substrates including INCRETINS; NEUROPEPTIDES; and CHEMOKINES. The protein is also found bound to ADENOSINE DEAMINASE on the T-CELL surface and is believed to play a role in T-cell activation.
A subclass of peptide hydrolases that depend on a CYSTEINE residue for their activity.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
A technique of measuring the dielectric properties of materials, which vary over a range of frequencies depending on the physical properties of the material. The technique involves measuring, over a range of frequencies, ELECTRICAL IMPEDANCE and phase shift of an electric field as it passes through the material.
Infection of the mucous membranes of the mouth by a fungus of the genus CANDIDA. (Dorland, 27th ed)
Pathological processes involving the PHARYNX.
Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.
The middle portion of the pharynx that lies posterior to the mouth, inferior to the SOFT PALATE, and superior to the base of the tongue and EPIGLOTTIS. It has a digestive function as food passes from the mouth into the oropharynx before entering ESOPHAGUS.
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)
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.
A unicellular budding fungus which is the principal pathogenic species causing CANDIDIASIS (moniliasis).
A pulmonary disease in humans occurring in immunodeficient or malnourished patients or infants, characterized by DYSPNEA, tachypnea, and HYPOXEMIA. Pneumocystis pneumonia is a frequently seen opportunistic infection in AIDS. It is caused by the fungus PNEUMOCYSTIS JIROVECII. The disease is also found in other MAMMALS where it is caused by related species of Pneumocystis.
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 genus of ascomycetous FUNGI, family Pneumocystidaceae, order Pneumocystidales. It includes various host-specific species causing PNEUMOCYSTIS PNEUMONIA in humans and other MAMMALS.
The prototype species of PNEUMOCYSTIS infecting the laboratory rat, Rattus norvegicus (RATS). It was formerly called Pneumocystis carinii f. sp. carinii. Other species of Pneumocystis can also infect rats.
Infections with species in the genus PNEUMOCYSTIS, a fungus causing interstitial plasma cell pneumonia (PNEUMONIA, PNEUMOCYSTIS) and other infections in humans and other MAMMALS. Immunocompromised patients, especially those with AIDS, are particularly susceptible to these infections. Extrapulmonary sites are rare but seen occasionally.
This drug combination has proved to be an effective therapeutic agent with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.
A sulfone active against a wide range of bacteria but mainly employed for its actions against MYCOBACTERIUM LEPRAE. Its mechanism of action is probably similar to that of the SULFONAMIDES which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with PYRIMETHAMINE in the treatment of malaria. (From Martindale, The Extra Pharmacopoeia, 30th ed, p157-8)
The custard-apple plant family of the order Magnoliales, subclass Magnoliidae, class Magnoliopsida. Some members provide large pulpy fruits and commercial timber. Leaves and wood are often fragrant. Leaves are simple, with smooth margins, and alternately arranged in two rows along the stems.
Dibenzoquinolines derived in plants from (S)-reticuline (BENZYLISOQUINOLINES).
Infections with unicellular organisms formerly members of the subkingdom Protozoa.
A genus of flagellate protozoa comprising several species that are pathogenic for humans. Organisms of this genus have an amastigote and a promastigote stage in their life cycles. As a result of enzymatic studies this single genus has been divided into two subgenera: Leishmania leishmania and Leishmania viannia. Species within the Leishmania leishmania subgenus include: L. aethiopica, L. arabica, L. donovani, L. enrietti, L. gerbilli, L. hertigi, L. infantum, L. major, L. mexicana, and L. tropica. The following species are those that compose the Leishmania viannia subgenus: L. braziliensis, L. guyanensis, L. lainsoni, L. naiffi, and L. shawi.
An order of flagellate protozoa. Characteristics include the presence of one or two flagella arising from a depression in the cell body and a single mitochondrion that extends the length of the body.
Countries in the process of change with economic growth, that is, an increase in production, per capita consumption, and income. The process of economic growth involves better utilization of natural and human resources, which results in a change in the social, political, and economic structures.
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)
Techniques for using whole blood samples collected on filter paper for a variety of clinical laboratory tests.
The quantity of measurable virus in a body fluid. Change in viral load, measured in plasma, is sometimes used as a SURROGATE MARKER in disease progression.
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
Removal of moisture from a substance (chemical, food, tissue, etc.).

The anti-influenza virus drug rimantadine has trypanocidal activity. (1/682)

We report here that bloodstream forms of the African trypanosome, Trypanosoma brucei, are sensitive to the anti-influenza virus drug rimantadine (50% inhibitory concentration of 1.26 micrograms ml-1 at pH 7.4). The activity is pH dependent and is consistent with a mechanism involving inhibition of the ability to regulate internal pH. Rimantadine is also toxic to the trypanosomatid parasites Trypanosoma cruzi and Leishmania major.  (+info)

Structure-based design of submicromolar, biologically active inhibitors of trypanosomatid glyceraldehyde-3-phosphate dehydrogenase. (2/682)

The bloodstream stage of Trypanosoma brucei and probably the intracellular (amastigote) stage of Trypanosoma cruzi derive all of their energy from glycolysis. Inhibiting glycolytic enzymes may be a novel approach for the development of antitrypanosomatid drugs provided that sufficient parasite versus host selectivity can be obtained. Guided by the crystal structures of human, T. brucei, and Leishmania mexicana glyceraldehyde-3-phosphate dehydrogenase, we designed adenosine analogs as tight binding inhibitors that occupy the pocket on the enzyme that accommodates the adenosyl moiety of the NAD+ cosubstrate. Although adenosine is a very poor inhibitor, IC50 approximately 50 mM, addition of substituents to the 2' position of ribose and the N6-position of adenosine led to disubstituted nucleosides with micromolar to submicromolar potency in glyceraldehyde-3-phosphate dehydrogenase assays, an improvement of 5 orders of magnitude over the lead. The designed compounds do not inhibit the human glycolytic enzyme when tested up to their solubility limit (approximately 40 microM). When tested against cultured bloodstream T. brucei and intracellular T. cruzi, N6-(1-naphthalenemethyl)-2'-(3-chlorobenzamido)adenosine inhibited growth in the low micromolar range. Within minutes after adding this compound to bloodstream T. brucei, production of glucose-derived pyruvate ceased, parasite motility was lost, and a mixture of grossly deformed and lysed parasites was observed. These studies underscore the feasibility of using structure-based drug design to transform a mediocre lead compound into a potent enzyme inhibitor. They also suggest that energy production can be blocked in trypanosomatids with a tight binding competitive inhibitor of an enzyme in the glycolytic pathway.  (+info)

Treatment of experimental leishmaniasis with the immunomodulators imiquimod and S-28463: efficacy and mode of action. (3/682)

There is a need for new, effective, and less toxic treatments for leishmaniasis, an infectious disease caused by Leishmania protozoa and is a major cause of suffering and morbidity in much of the developing world. Imiquimod, an immune-response modifier, has recently been approved by the Food and Drug Administration for the treatment of genital warts caused by human papillomaviruses. Imiquimod initiates a local immune reaction, including the stimulation of macrophages, resulting in resolution of human papillomavirus infection and regression of the viral lesion. Since imiquimod activates a number of immune cells, including macrophages, which are the only host cells of Leishmania species, an investigation was done to determine whether it induces leishmanicidal properties in infected macrophages in vitro and in vivo in a mouse model. Imiquimod and a related compound, S-28463, effectively stimulated leishmanicidal activity in macrophages; moreover, imiquimod stimulated signal transduction associated with inducing nitric oxide synthesis in macrophages.  (+info)

Infection-associated decline of cape buffalo blood catalase augments serum trypanocidal activity. (4/682)

Clearance of trypanosomes from the blood of infected Cape buffalo was associated with the development of two responses: (i) complement-dependent and clone-specific lytic activity and (ii) complement-independent trypanocidal activity that was not restricted by trypanosome clone or species. This latter activity was mediated by H2O2 and required the presence of xanthine oxidase in serum but not the addition of purine substrates. Expression of the xanthine oxidase-dependent trypanocidal activity in Cape buffalo serum was coincident with, and required, a decline in its H2O2 catabolic activity. The H2O2 catabolic activity of Cape buffalo serum was due solely to catalase and declined by eightfold around the time that trypanosomes were cleared from the blood, accompanied by a fivefold drop in erythrocyte-associated catalase activity. The Cape buffalo did not develop subsequent parasitemic waves. Clearance of parasitemia in similarly infected cattle was also associated with development of trypanosome clone-specific lytic activity, but not with the acquisition of H2O2-dependent trypanocidal activity in serum, and the cattle supported recurring parasitemia. The lack of trypanocidal activity in pre- and postinfection cattle sera was due to their low content of xanthine oxidase and sustained catalase activity. These data strongly suggest that an infection-induced serum oxidative response, the efficacy of which is amplified by a decline in blood catalase, contributes to suppression of recurring parasitemia in Cape buffalo.  (+info)

Platelet-activating factor induces nitric oxide synthesis in Trypanosoma cruzi-infected macrophages and mediates resistance to parasite infection in mice. (5/682)

Trypanosoma cruzi replicates in nucleated cells and is susceptible to being killed by gamma interferon-activated macrophages through a mechanism dependent upon NO biosynthesis. In the present study, the role of platelet-activating factor (PAF) in the induction of NO synthesis and in the activation of the trypanocidal activity of macrophages was investigated. In vitro, PAF induced NO secretion by T. cruzi-infected macrophages and the secreted NO inhibited intracellular parasite growth. The addition of a PAF antagonist, WEB 2170, inhibited both NO biosynthesis and trypanocidal activity. The inducible NO synthase/L-arginine pathway mediated trypanocidal activity, since it was inhibited by treatment with L-N-monomethyl arginine (L-NMMA), an L-arginine analog. PAF-mediated NO production in infected macrophages appears to be dependent on tumor necrosis alpha (TNF-alpha) production, since the addition of a neutralizing anti-TNF-alpha monoclonal antibody mAb inhibited NO synthesis. To test the role of PAF in mediating resistance or susceptibility to T. cruzi infection, infected mice were treated with WEB 2170, a PAF antagonist. These animals had higher parasitemia and earlier mortality than did vehicle-treated mice. Taken together, our results suggest that PAF belongs to a group of mediators that coordinate the mechanisms of resistance to infections with intracellular parasites.  (+info)

A nucleoside transporter from Trypanosoma brucei involved in drug resistance. (6/682)

Drug resistance of pathogens is an increasing problem whose underlying mechanisms are not fully understood. Cellular uptake of the major drugs against Trypanosoma brucei spp., the causative agents of sleeping sickness, is thought to occur through an unusual, so far unidentified adenosine transporter. Saccharomyces cerevisiae was used in a functional screen to clone a gene (TbAT1) from Trypanosoma brucei brucei that encodes a nucleoside transporter. When expressed in yeast, TbAT1 enabled adenosine uptake and conferred susceptibility to melaminophenyl arsenicals. Drug-resistant trypanosomes harbor a defective TbAT1 variant. The molecular identification of the entry route of trypanocides opens the way to approaches for diagnosis and treatment of drug-resistant sleeping sickness.  (+info)

Antitrypanosomal activity of fluoroquinolones. (7/682)

Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei. All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective concentrations in the low micromolar range. In general, trypanosomes were more susceptible than L1210 leukemia cells. Consistent with the notion that they target type II topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.  (+info)

Differential effects of adenine nucleotide analogues on shape change and aggregation induced by adnosine 5-diphosphate (ADP) in human platelets. (8/682)

Adenosine 5'-diphosphate (ADP) induces human blood platelets to aggregate and change shape, and it has been suggested that these two responses are mediated by more than one subtype of ADP receptor. The structure-activity relationships for several analogues of adenine nucleotides in causing aggregation and shape change were measured and compared in washed platelets using an aggregometer. ADP and its analogues 2-methylthioadenosine 5'-diphosphate (2-methylthio-ADP), adenosine 5'(alpha,beta-methylene)diphosphonate (AMPCP), S(P)-adenosine 5'-O-(1-thiodiphosphate) (AD-P alphaS) and adenosine 5'-O-(2-thiodiphosphate) (ADPbetaS) were used as agonists. Adenosine 5'-triphosphate (ATP) and its analogues, P1, P5-diadenosine pentaphosphate (ApsA), adenosine (5'-(alpha,beta-methylene)triphosphonate (AMPCPP), 2-methylthioadenosine 5'-triphosphate (2-methylthio-ATP) and uridine 5'-triphosphate (UTP), as well as the trypanocidal drug suramin, were used as antagonists. In general, the structure-activity relationships for both responses were similar, but for some analogues differences were observed. ADPalphaS and ADPbetaS were much more potent agonists relative to ADP for shape change than for aggregation and indeed ADPalphaS antagonized ADP-induced aggregation with an apparent pK(B) value of 5.5+/-0.1. 2-Methylthio-ATP also had different effects in aggregation and shape change, being a much higher affinity antagonist of aggregation than of shape change with an apparent pK(B) value of 7.0+/-0.2 for aggregation and 5.2+/-0.2 for shape change. These results support the suggestion that these two responses are mediated by multiple ADP receptors on human platelets, and are consistent with shape change being mediated via one receptor (the P2Y1 receptor) with aggregation requiring the activation of two receptors (the P2Y1 and another P2Y receptor).  (+info)

AMBROZIN, Alessandra R. P. et al. New Pyrone and Quinoline Alkaloid from Almeidea rubra and their Trypanocidal Activity. J. Mex. Chem. Soc [online]. 2005, vol.49, n.2, pp.196-201. ISSN 1870-249X.. The investigation of the ethyl acetate fraction of methanol extract from leaves of Almeidea rubra A. St.-Hil. (Rutaceae) afforded two new compounds 4-methoxy-6-[2-(methylamino)phenyl]-2H-pyran-2-oneand rel-(7R,8R)-8-[(E)-3-hydroxy-3-methyl-1-butenyl]-4,8-dimethoxy-5,6,7,8-tetrahydrofuro[2,3-b]quinoline-7-yl acetate, along with the known compounds arborinine, N-methyl-1-hydroxy-3-methoxyacridone, skimmianine, kokusagine, isodutaduprine, isoskimmianine, and isokokusagine. Their structures were established based on their spectral data, and for the new compounds these data are described herein. Additionally, these compounds were assayed on the tripomastigote forms of Trypanosoma cruzi showing moderate trypanocidal activity.. Keywords : Almeidea rubra; Rutaceae; alkaloids; trypanocidal activity. ...
Buy, download and read Experimental Chemotherapy V4 ebook online in PDF format for iPhone, iPad, Android, Computer and Mobile readers. Author: R Schnitzer. ISBN: 9780323143301. Publisher: Elsevier Science. Experimental Chemotherapy, Volume IV: Chemotherapy of Neoplastic Diseases, Part I focuses on the use of chemotherapy to counteract neoplastic ailments. The book first discusses the chemotherapy of neo
Cianni, Lorenzo; Lemke, Carina; Gilberg, Erik; Feldmann, Christian; Rosini, Fabiana; Rocho, Fernanda dos Reis; Ribeiro, Jean F. R.; Tezuka, Daiane Y.; Lopes, Carla D.; de Albuquerque, Sergio; Bajorath, Juergen; Laufer, Stefan; Leitao, Andrei; Guetschow, Michael; Montanari, Carlos A. ...
The proteasome inhibitor and anti-cancer drug bortezomib was tested for in vitro activity against bloodstream forms of Trypanosoma brucei. The concentrations of bortezomib required to reduce the growth rate by 50% and to kill all trypanosomes were 3.3 nM and 10 nM, respectively. In addition, bortezomib was 10 times more toxic to trypanosomes than to human HL-60 cells. Moreover, exposure of trypanosomes to 10 nM bortezomib for 16 h was enough to kill 90% of the parasites following incubation in fresh medium. However, proteasomal peptidase activities of trypanosomes exposed to bortezomib were only inhibited by 10% and 30% indicating that the proteasome is not the main target of the drug. The results suggest that bortezomib may be useful as drug for the treatment of human African trypanosomiasis.
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors having a reactive group (known as warhead) are subject to continuous studies to discover novel antichagasic compounds. Here, we evaluated
Ethanium Definition Ethanium is a trypanocidal agent and possible antiviral agent that are widely used in experimental cell biology and biochemistry. Ethid
One of the most promising new targets for trypanocidal drugs to emerge in recent years is the cyclic AMP (cAMP) phosphodiesterase (PDE) activity encoded by TbrPDEB1 and TbrPDEB2. These genes were genetically confirmed as essential, and a high-affinity inhibitor, CpdA, displays potent antitrypanosomal activity. To identify effectors of the elevated cAMP levels resulting from CpdA action and, consequently, potential sites for adaptations giving resistance to PDE inhibitors, resistance to the drug was induced. Selection of mutagenized trypanosomes resulted in resistance to CpdA as well as cross-resistance to membrane-permeable cAMP analogues but not to currently used trypanocidal drugs. Resistance was not due to changes in cAMP levels or in PDEB genes. A second approach, a genome-wide RNA interference (RNAi) library screen, returned four genes giving resistance to CpdA upon knockdown. Validation by independent RNAi strategies confirmed resistance to CpdA and suggested a role for the identified cAMP ...
The Scientific World Journal is a peer-reviewed, Open Access journal that publishes original research, reviews, and clinical studies covering a wide range of subjects in science, technology, and medicine. The journal is divided into 81 subject areas.
A dose-dependent trypanocidal activity of propolis extract was observed in vitro. All trypomastigotes were killed 1 h after incubation with 10 μg mL−1 of the extract. In vivo, the concentrations of 100, 200, 300 and 400 mg kg−1 administered orally for 10 consecutive days showed no curative effect, and the rats died from the disease. However, rats treated with the two highest concentrations of propolis extract showed higher longevity than the other groups ...
This study is for people who have advanced cancer for which standard chemotherapy did not work or for which there are no reliably, effective treatments.. AQ4N is an experimental chemotherapy that is thought to target tumor areas with low oxygen content and low blood supply; tumor areas that are usually the most resistant to standard chemotherapy and radiation treatment. AQ4N may be beneficial in cancer treatment by interfering with a protein that is required for cells to grow and divide, causing tumors to die or to delay their growth.. All patients in this study will receive AQ4N. The dose will be increased for each new patient or group of patients until the maximum tolerated dose is reached. ...
Treatment of stomach cancer with an experimental chemotherapy drug after surgery improved survival rates for Japanese patients, a new study found. The results o
Recently, the World Health Organization approved the nifurtimox-eflornithine combination therapy for the treatment of human African trypanosomiasis, renewing interest in nitroheterocycle therapies for this and associated diseases. In this study, we h
Chemotherapy against human African trypanosomiasis relies on four drugs that cause frequent and occasionally severe side-effects. Because human African trypanosomiasis is a disease of poor people in Africa, the traditional market-driven pathways to drug development are not available. One potentially …
BioAssay record AID 523194 submitted by ChEMBL: Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in mouse peritoneal macrophages assessed as endocytic index after 4 day.
It has been more than 25 years since it was first reported that nifurtimox and benznidazole promote superoxide production in trypanosomes. However, there has been no direct evidence of an association between the drug-induced free radicals and trypanocidal activity. Here, we identify a superoxide dismutase required to protect Trypanosoma brucei from drug-generated superoxide.. ...
BioAssay record AID 378804 submitted by ChEMBL: Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 infected in african green monkey Vero cells assessed as growth inhibition of trypomastigotes by beta-galactosidase reporter gene assay.
A Preliminary Trypanocidal Study of Natural and Synthetic Supplementation of Zinc and Magnesium in Combination with Diminazene Aceturate in Wistar Rats
In this study, we were able to achieve a 4-fold reduction in the amount of benznidazole required to significantly reduce blood and tissue parasite burdens by combining the low-dose benznidazole with a recombinant vaccine candidate, Tc24 C4, formulated with a synthetic Toll-like 4 receptor agonist, E6020, in a squalene oil-in-water emulsion. Additionally, vaccination induced a robust parasite-speci...
Study of the in Vitro Antiplasmodial, Antileishmanial and Antitrypanosomal Activities of Medicinal Plants from Saudi Arabia. . 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.
TY - JOUR. T1 - Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. AU - Sola, Irene. AU - Artigas, Albert. AU - Taylor, Martin C.. AU - Gbedema, Stephen Y.. AU - Pérez, Belén. AU - Clos, M. Victòria. AU - Wright, Colin W.. AU - Kelly, John M.. AU - Muñoz-Torrero, Diego. PY - 2014/12/1. Y1 - 2014/12/1. N2 - © 2014 Elsevier Ltd. All rights reserved. We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.. AB - © 2014 Elsevier Ltd. All rights reserved. ...
The most common adverse reactions in patients taking benznidazole were stomach pain, rash, decreased weight, headache, nausea, vomiting, abnormal white blood cell count, urticaria (hives), pruritus (itching) and decreased appetite. Benznidazole is associated with serious risks including serious skin reactions, nervous system effects and bone marrow depression. Based on findings from animal studies, benznidazole could cause fetal harm when administered to a pregnant woman.. Benznidazole was approved using the Accelerated Approval pathway. The Accelerated Approval pathway allows the FDA to approve drugs for serious conditions where there is unmet medical need and adequate and well-controlled trials establish that the drug has an effect on a surrogate endpoint that is reasonably likely to predict a clinical benefit to patients. Further study is required to verify and describe the anticipated clinical benefit of benznidazole.. The FDA granted benznidazole priority review and orphan product ...
Two enzyme-linked immunosorbent assays (ELISA) for the determination of homidium in serum of treated cattle have been developed and evaluated. One is a direct competition (Assay 1) and the other an indirect competition assay (Assay 2). Both assays are highly sensitive with a limit of detection of 0.1 ng homidium per mL serum. Homidium levels were measurable in serum of cattle for over 2 months following administration of a single intramuscular (i.m.) dose at 1 mg/kg bodyweight. The level of sensitivity afforded by these assays makes them potentially useful tools in the pharmacokinetic evaluation of homidium and for invetigating drug resistance or causes of drug failure. Assay 2 was chosen as being most suitable for further studies ...
Alves, Renata Tom et al. Trypanocidal activity of Brazilian plants against epimastigote forms from Y and Bolivia strains of Trypanosoma cruzi. Rev. bras. farmacogn., June 2012, vol.22, no.3, p.528-534. ISSN 0102- ...
by Moraes CB, White KL, Braillard S, Perez C, Goo J, Gaspar L, Shackleford DM, Cordeiro-da-Silva A, Thompson RC, Freitas-Junior L, Charman SA, Chatelain E.
Aqueous and methanol leaf extracts of V. sinaiticum were investigated for the presence of secondary metabolites and their in vitro activity against Trypanosoma congolence..
The goal of this clinical research study is to find out if switching from a standard chemotherapy combination to a more intensive experimental combination, based on imaging scans, will improve response to treatment in patients with Hodgkin lymphoma (HL). The safety of this experimental chemotherapy combination will also be studied.
Sigma-Aldrich offers abstracts and full-text articles by [S T de Macedo-Silva, G Visbal, J A Urbina, W de Souza, J C F Rodrigues].
Recent studies have shown that Benznidazole (BZL), known for its antiparasitic action on Trypanosoma cruzi, modulates pro-inflammatory cytokines and nitric oxide (NO) release in activated macrophages by blocking NF-κB through inhibition of IKK in vitro. As so far, little is known about the mechanism by which BZL provokes the inhibition of inflammatory response in sepsis in vivo, we aimed to deline ...
Raputia praetermissa (Engler) Emmerich is a tree found only in the Forest Reserve Adolpho Ducke, Amazonas, Brazil. The genus Raputia was originally described by Engler and many species were included in this genus, but in 1978, Emmerich proposed three new genera Neoraputia, Raputiarana e Sigmathantus in order to accommodate six species, four belonging to the genus Raputia, which is assigned into the tribe Cuspariae, and two that had not been described yet. From our knowledge no previous phytochemical work has been reported on Raputia. Therefore, this study describes phytochemical and chemosystematic investigation and the search of compounds with trypanocidal and leishmanicidal activity from roots of R. praetermissa. The phytochemical work involved crude extract preparation, followed by fractionation and isolation of compounds thorough different chromatography methods. Spectroscopic analyses permitted the identification of them and the results showed the presence of new substances in addition to ...
The disease has an acute and chronic stage. The acute stage is not associated with symptoms in 95% of cases. Symptoms that do appear can include fever or swelling around the site where the parasite entered the body. While the acute stage does not often cause significant morbidity, children and immunosuppressed individuals have a higher risk of mortality.. The disease enters into the chronic stage post-infection, which can be a few weeks or longer after the acute stage. Many infected people remain asymptomatic for life. However, chronic infection can lead to serious complications and potentially death in an estimated 20-30% of infected individuals, usually 10-30 years after the initial infection. Complications include cardiovascular, gastrointestinal and neurological diseases.. ...
Literature References: Ergosterol biosynthesis inhibitor. Prepn: A. Hubele, P. Riebli, GB 2098607 (1982 to Ciba-Geigy). Properties and antifungal activity: W. Ruess et al., Brighton Crop Prot. Conf. - Pests Dis. 1988, 543. Field studies: A. J. Leadbeater et al., ibid. 917; A. B. Bassi, Jr. et al., Br. Crop Prot. Counc. Monogr. 57, 91 (1994). Uptake and translocation in crops: H. Dahmen, T. Staub, Plant Dis. 76, 523 (1992). ...
by Papadopoulou MV, Bloomer WD, Rosenzweig HS, Chatelain E, Kaiser M, Wilkinson SR, McKenzie C, and Ioset JR. Journal of Medicinal Chemistry, May 2012
Hargrove, John W., Ouifki, Rachid, Kajanguri, Damian, Vale, Glyn A. and Torr, Stephen J. (2012) Modeling the control of Trypanosomiasis using Trypanocides or insecticide-treated livestock. PLOS Neglected Tropical Diseases, 6 (5):e1615. ISSN 1935-2727 (Print), 1935-2735 (Online) (doi:10.1371/journal.pntd.0001615) ...
The nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one of a limited number of treatments targeting Trypanosoma brucei, the causative agent of human African trypanosomiasis. The mode of action of this prodrug involves an initial activation reaction catalysed by a type I nitroreductase (NTR), an enzyme found predominantly in prokaryotes, leading to the formation of a cytotoxic unsaturated open chain nitrile metabolite. Here, we evaluate the trypanocidal activity of a library of other 5-nitrofurans against bloodstream form T. brucei as a preliminary step in the identification of additional nitroaromatic compounds that could potentially partner eflornithine. Biochemical screening against purified enzyme revealed that all 5-nitrofurans were effective substrates for TbNTR with the preferred compounds having apparent k(cat)/K(M) values approximately 50-fold greater than nifurtimox. For several compounds, in vitro reduction by this nitroreductase ...
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Introduction Women with Chagas disease receiving treatment with nifurtimox are discouraged from breast feeding. Many patients who would receive treatment with nifurtimox live in extreme poverty, have limited access to resources such as clean water and baby formula and may not have safe alternatives to breast milk.. Aim We aimed to estimate, using limited available pharmacokinetics data, potential infant exposure to nifurtimox through breast milk.. Methods Original nifurtimox plasma concentrations were obtained from published studies. Pharmacokinetic parameters were estimated using non-linear mixed-effect modelling with NONMEM V.VI. A total of 1000 nifurtimox plasma-concentration profiles were simulated and used to calculate the amount of drug that an infant would be exposed to, if breast fed 150 ml/kg/day.. Results Breast milk concentrations on the basis of peak plasma levels (1361 ng/ml) and milk-plasma ratio were estimated. We calculated infant nifurtimox exposure of a breastfed infant of a ...
TY - JOUR. T1 - In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationships. AU - Iwatsuki, Masato. AU - Otoguro, Kazuhiko. AU - Ishiyama, Aki. AU - Namatame, Miyuki. AU - Nishihara-Tukashima, Aki. AU - Hashida, Junko. AU - Nakashima, Takuji. AU - Masuma, Rokuro. AU - Takahashi, Yoko. AU - Yamada, Haruki. AU - Ömura, Satoshi. N1 - Funding Information: This work was supported, in part, by funds from the Drugs for Neglected Diseases initiative (DNDi), Quality Assurance Framework of Higher Education from the Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT), and the All Kitasato Project Study (AKPS). We are grateful to Ms H Sekiguchi and Mr T Furusawa for their technical assistance.. PY - 2010/10. Y1 - 2010/10. KW - Antitrypanosomal. KW - low-molecular-weight antibiotics. KW - structure/activity relationships. UR - http://www.scopus.com/inward/record.url?scp=78049283272&partnerID=8YFLogxK. UR - ...
Chagas disease (CD) is a neglected disease caused by the parasite Trypanosoma cruzi, which affects underdeveloped countries. The current drugs of choice are nifurtimox and benznidazole, but both have severe adverse effects and less effectivity in chronic infections; therefore, the need to discover new drugs is essential. A computer-guided drug repositioning method was applied to identify potential FDA drugs (approved and withdrawn) as cruzain (Cz) inhibitors and trypanocidal effects were confirmed by in vitro and in vivo studies. 3180 FDA drugs were virtually screened using a structure-based approach. From a first molecular docking analysis, a set of 33 compounds with the best binding energies were selected. Subsequent consensus affinity binding, ligand amino acid contact clustering analysis, and ranked position were used to choose four known pharmacological compounds to be tested in vitro. Mouse blood samples infected with trypomastigotes from INC-5 and NINOA strains were used to test the trypanocidal
This study evaluates the effectiveness of fexinidazole administered to patients with g-HAT at all stages of the disease. The aim of the present study is to provide additional information on the effectiveness and safety of fexinidazole and to assess its use under conditions as close as possible to those in real life, both in patients treated on an out-patient basis and in the hospital setting, depending on clinical ...
Leishmaniasis and trypanosomiasis are protozoan diseases caused respectively by the kinetoplastid protozoan Leishmania parasites transmitted by the female phlebotomine sa..
Unfortunately, one century after its discovery (Chagas 1909), Chagas disease still affects millions of poor people in several Latin American countries...
New formulation for weight-adjusted treatment of pediatric Chagas patients age 0-18 targets most vulnerable patient group / Submission based on results of CHICO (CHagas disease In Children treated with NifurtimOx) phase III clinical study of nifurtimox in pediatric patients with Chagas disease as well as pre-clinical data / Fight against Neglected Tropical Diseases part of Bayers Sustainability Strategy
New formulation for weight-adjusted treatment of pediatric Chagas patients age 0-18 targets most vulnerable patient group / Submission based on results of CHICO (CHagas disease In Children treated with NifurtimOx) phase III clinical study of nifurtimox in pediatric patients with Chagas disease as well as pre-clinical data / Fight against Neglected Tropical Diseases part of Bayers Sustainability Strategy
Chronic chagasic cardiomyopathy (CCC) develops years after acute infection by Trypanosoma cruzi and does not improve after trypanocidal therapy, despite reduction of parasite burden. During disease, the heart undergoes oxidative stress, a potential causative factor for arrhythmias and contractile dysfunction. Here we tested whether antioxidants/ cardioprotective drugs could improve cardiac function in established Chagas heart disease. We chose a model that resembles B1-B2 stage of human CCC, treated mice with resveratrol and performed electrocardiography and echocardiography studies. Resveratrol reduced the prolonged PR and QTc intervals, increased heart rates and reversed sinus arrhythmia, atrial and atrioventricular conduction disorders; restored a normal left ventricular ejection fraction, improved stroke volume and cardiac output. Resveratrol activated the AMPK-pathway and reduced both ROS production and heart parasite burden, without interfering with vascularization or myocarditis ...
In most instances of acute T cruzi infection, a specific diagnosis is not made because of the nonspecific nature of the signs and symptoms and because most cases occur in poor people who have limited ... more
Accepted 22 April 2009. Code Number: oc09127 ABSTRACT. Treatments for Chagas disease have been administered since the first attempts by Mayer & Rocha Lima (1912, 1914) and up to the drugs currently in use (nifurtimox and benznidazole), along with potential drugs such as allopurinol and first, second and third-generation antifungal agents (imidazoles and triazoles), in separate form. Several diseases such as tuberculosis, leprosy and AIDS only came under control after they were treated with associations of drugs with different mechanisms of action. This not only boosts the action of the different compounds, but also may avoid the development of parasite resistance .To this end, over the short term, we propose experimental studies on laboratory animals and clinical trials with the following associations: (i) nifurtimox (8 mg/kg/day) + benznidazole (5 mg/kg/day) x 60 consecutive days; (ii) nifurtimox (8 mg/kg/day) or benznidazole (5 mg/kg/day) + allopurinol (8-10 mg/kg/day) x 60 days and (iii) ...
Title: Perspectives for New Drugs Against Trypanosomiasis and Leishmaniasis. VOLUME: 2 ISSUE: 5. Author(s):Michael P. Barrett and Ian H. Gilbert. Affiliation:University of Glasgow,Institute of Biomedical and Life Sciences, Division of Infection&Immunity, The Joseph Black Building, Glasgow, G12 8QQ, U.K.. Keywords:trypanosomiasis, leishmaniasis, phenanthridinium compound, trypanocidal drugs, megazol. Abstract: Diseases caused by pathogenic trypanosomatids cause great suffering throughout the developing world. New drugs for these diseases are urgently needed. Recent technological advances have permitted the identification and validation of numerous drug targets in these organisms. However, efforts to develop inhibitors of these targets, that may then be taken forward for development into new drugs, have been comparatively scarce. In this review we discuss the design, synthesis and evaluation of inhibitors of two drug targets in trypanosomatids, 6- phosphogluconate dehydrogenase, the third enzyme ...
Benznidazole is an antiprotozoal medicine. It is used treat an infection called American trypanosomiasis (Chagas disease) in children 2 to 12 years of age.
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The heart is the most commonly affected organ in persons with chronic Chagas disease.{ref55}{ref56}{ref57}{ref58} Autopsy may reveal marked bilateral ventricular enlargement, often involving the right... more
Definition : Molecular assay reagents intended to identify Trypanosoma cruzi, a species of protozoon of the suborder Trypanosomatina, by detecting specific genetic information of the deoxyribonucleic acid (DNA) of the target parasite. Trypanosoma cruzi parasites cause Chagas disease (American trypanosomiasis) in humans, characterized by an erythematous nodule (i.e., chagoma) appearing within a few days at the site of the inoculation. These parasites are transmitted to humans via insects, either from other humans or from animals (e.g., cats, dogs, rodents).. Entry Terms : Trypanosoma cruzi Reagents, Identification , Trypanosoma cruzi Detection/Identification Reagents , Trypanosoma Species Reagents, Identification , American Trypanosomiasis Diagnostic Reagents , Sleeping Sickness Diagnostic Reagents , Trypanosomosis Diagnostic Reagents , Trypanosoma Species Detection/Identification Reagents , Chagas Disease Diagnostic Reagents , Reagents, Molecular Assay, Infection, Parasite, ...
Author Summary Chagas disease (American trypanosomiasis) is caused by the protozoan parasite Trypanosoma cruzi and represents a major public health problem in Latin America. Furthermore, growing human population movements extend the disease distribution to regions outside the South American continent. Accurate diagnosis is crucial in patient care and in preventing transmission through blood transfusion, organ transplantation, or vertical transmission from mother to child. Routine diagnosis of Trypanosoma cruzi infection generally is based on detection of the hosts antibodies against the parasite. However, antibody detection tests are liable to specificity problems and are of limited use in assessing treatment outcome and congenital infections. The introduction of the polymerase chain reaction (PCR) to amplify specific DNA sequences opened promising diagnostic perspectives. Despite its reported high sensitivity and specificity, broad use of the PCR technique in diagnosis of Chagas disease is hampered by
Bark used as expectorant and for asthma.. • In Africa, bark root used for pulmonary problems; leaf for leprosy, and flower for kidney ailments and as diuretic.. • In West Nigeria, leaves and stems soaked and boiled in water, used for skin rashes. (see source study). • In India, reported Mawasi tribal use of flowers for diarrhea. (see source study). Scientific studies on the benefits and uses of the monkey tail. • Antimicrobial:. Studies of leaf extracts isolated gallic acid, corilagin and geranin responsible for antimicrobial activity.. • Trypanocidal/ antiprotozoal agent:. Aqueous extract of Acalypha hispida leaves suggest trypanocidal effect.. • Anti-ulcer / Anti-tumor:. Studies yielded geraniin and dehydroellagitannins which suggest diverse biological properties including anti-ulcer and anti-tumor effects, antibacterial activity against helicobacter pylori and antifungal activity.. • Phytochemicals:. Phytochemical studies yield phenolics, flavonoids, hydroxyanthraquinones and ...
Background and Objectives: There is urgent need of search for alternative compounds for chemotherapy of African trypanosomiasis, a disease of major economic and public health importance. The current study investigated the phytochemical composition and in vitro antitrypanosomal activity of aqueous and methanolic leaf extracts of Clutia abyssinica (C. abyssinica) against Trypanosoma congolense (T. congolense) isolated from natural infection of cattle. Materials and Methods: The aqueous and methanol extracts were screened for various secondary metabolites using standard methods. The in vitro antitrypanosomal assay was carried out by monitoring the extract concentrations of 4, 2, 1, 0.4 and 0.2 mg mL-1 for cessation or reduction in motility of trypanosomes followed by inoculation of incubation mixtures to healthy mice and monitoring development of infection for 21 days. Results: Phytochemical screening revealed presence of alkaloids, anthraquinones, flavonoids, glycosides, phenolic compounds, ...
The dissociation of histone proteins a-d from the chromatin ofTrypanosoma brucei brucei procyclic culture forms was investigated by removing the proteins f
During the chronic stage of Chagas disease a 160 kDa antigen appears in the blood of patients and remains detectable many years after the onset of the disease. This antigen is secreted by the trypomastigote form of the parasite while it is undetectable in the epimastigote form. We report here that the chronic 160 kDa exoantigen is encoded by a gene family (CEA 160 family). We describe the cloning and partial nucleotide sequence of a gene (CEA 160-1) belonging to the CEA160 family. Comparison of the gene sequence with other sequences present in the databases revealed homologies with several Trypanosoma cruzi surface antigens. Highest amino acid identity (59%) was with members of a family containing epitopes that mimic nervous tissues (Van Voorhis et al. 1993). Another related group (18-22% amino acid identity) comprises proteins of 85 or 160 kDa sharing an amino acid motif that is conserved among bacterial neuraminidases (Fouts et al. 1991; Pollevick et al. 1991; Kahn et al. 1991; Takle & Cross, ...
The human and veterinary disease complex known as African trypanosomiasis continues to inflict significant global morbidity, mortality, and economic hardship. Drug resistance and toxic side effects of old drugs call for novel and unorthodox strategies for new and safe treatment options. We designed methyltriazenyl purine prodrugs to be rapidly and selectively internalized by the parasite, after which they disintegrate into a nontoxic and naturally occurring purine nucleobase, a simple triazene-stabilizing group, and the active toxin: a methyldiazonium cation capable of damaging DNA by alkylation. We identified 2-(3-acetyl-3-methyltriazen-1-yl)-6-hydroxypurine (compound 1) as a new lead compound, which showed submicromolar potency against Trypanosoma brucei, with a selectivity index of >500, and it demonstrated a curative effect in animal models of acute trypanosomiasis. We investigated the mechanism of action of this lead compound and showed that this molecule has significantly higher ...
It was during his training at the NCI, from 1977 to 1980, that Dr. Schilsky made his decision to specialize in GI cancers. I was mentored by Bruce A. Chabner, MD, who was Head of the Clinical Pharmacology Branch at the NCI, and I was interested in learning more about how drugs worked and doing research in pharmacology and drug development. If you were interested in new drug development, GI cancers offered a good patient population to enroll in phase I and phase II trials to investigate new drugs, because there were so few standard-of-care treatment options for patients at that time, said Dr. Schilsky. It was also during his fellowship at the NCI that he made his first major contribution to the treatment of cancer, which changed the standard of care for patients prescribed the then experimental chemotherapy drug cisplatin. After receiving a call from a patient with ovarian cancer enrolled in a clinical study of the drug, complaining that she was shaking all over, Dr. Schilsky ordered blood ...
Abstract This paper considers the practical problem in experimental chemotherapy where several treatment groups are compared with a control group in a multivariate covariance analysis and the observed data of mice are subjected to multiple comparison test. Mice infected with 50 cercariae of Schistosoma mansoni in unequal group sizes are challenged with some doses of Zingiber officinale extracts, Cremophore and Praziquantel. Data are available for the number of male and female parasites, weights of liver and intestine, and egg per gramme liver and intestine tissues. Proposed herein are multiple testing procedures such as, Tukey, Scheffe and Bonferroni based on two-sample statistics, each comparing an individual treatment with the control, for determining which treatments are more effective than the control. Newman-Keul s test corrobarates exactly with Bonferroni test s result, in the further analysis. ...
Coconut oil was victimized during that era of erroneous dogma that demonized saturated fats, including butter, and created the unhealthy trans-fatty acid hydrogenated unsaturated fat industry, which included margarine. Saturated fats have been resurrected from the trash bin of forbidden foods over the past decade or so with proven health merits.. Now that the fog of junk science dogma has lifted, more and more health conscious folks are finding saturated fats, especially coconut oil, are beyond just safe. They are healthy and medicinal. Several published but unpublicized studies have been conducted and are in progress regarding palm or coconut oils medicinal properties.. One of the most profound studies that you probably havent read or heard about involves cancer. It was conducted by Australian researchers and published in the January 2014 journal Chemotherapy under experimental chemotherapy. It was an in vitro (test tube, petri dish) study on human colon or colorectal cancer ...
Division of Molecular Biotherapy [Y. I., M. N., K. K., S. T., E. I., Y. S.] and Division of Experimental Chemotherapy [T. T.], Cancer Chemotherapy Center, and Department of Molecular Diagnosis [Y. M.], Cancer Institute, Japanese Foundation for Cancer Research, Tokyo 170-8455, and Institute of Molecular and Cellular Biosciences, University of Tokyo, Tokyo 113-0032 [T. T.], ...
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In a rodent model of chronic ChHD, the administration of carvedilol did not change ventricular remodeling and function or interstitial and perivascular fibrosis; additionally, total mortality was unchanged, even though early mortality (up to 100 days with infection) was reduced with carvedilol (62). However, carvedilol was effective in attenuating oxidative damage in ChHD patients after 6 months of treatment in a prospective, case-control, nonrandomized, open-label study (63). Also, a study with 9 patients with ChHD-HF tested the effects of metoprolol (titrated up to 25 mg) and found improvement in functional status, increase in LVEF, and reduction in LV end-diastolic diameter (64). Retrospective analyses have suggested a beneficial effect of β-blockers in patients with ChHD-HF. In a cohort of 231 consecutive patients with ChHD-HF, β-blocker therapy had a protective effect (65). A retrospective analysis of the REMADHE trial (A Long-Term Prospective Randomized Controlled Study Using Repetitive ...
Opens the Highlight Feature Bar and highlights feature annotations from the FEATURES table of the record. The Highlight Feature Bar can be used to navigate to and highlight other features and provides links to display the highlighted region separately. Links in the FEATURES table will also highlight the corresponding region of the sequence. More... ...
Multilocus sequence typing (MLST) is a powerful and highly discriminatory method for analysing pathogen population structure and epidemiology. Trypanosoma cruzi, the protozoan agent of American trypanosomiasis (Chagas disease), has remarkable genetic and ecological diversity. A standardised MLST protocol that is suitable for assignment of T. cruzi isolates to genetic lineage and for higher resolution diversity studies has not been developed ...
Analogues structuraux des porphyrines et des Salens, des ligands de type dipyrrométhène bis-phénol ont été étudiés dans notre groupe, notamment sous forme de complexes pour la catalyse doxydation. Lactivité catalytique de ces complexes étant faible, il a été proposé de remplacer les phénols par des triazoles. Lobjet de cette thèse était détudier et de valoriser une nouvelle famille de ligands dipyrrométhène bis-triazole.Plusieurs voies de synthèse ont dabord été étudiées et optimisées pour accéder à ces nouveaux ligands. Nous nous sommes attachés ensuite à valoriser ces nouveaux ligands selon plusieurs axes.Un de ces ligands a été testé en reconnaissance danions, ainsi que les dérivés monotriazolium et bis-triazolium. Les triazoliums ont également permis laccès à des métallocomplexes carbéniques, qui ont été étudiés.Par ailleurs, les métallocomplexes des dipyrrométhène bis-triazole ont été préparés et caractérisés, y compris par ...
1GY8: High-Resolution Crystal Structure of Trypanosoma Brucei Udp-Galactose 4-Epimerase: A Potential Target for Structure-Based Development of Novel Trypanocides
A doen a de Chagas afeta cerca de 6 a 7 millh es de pessoas no mundo, principalmente Am rica Latina. A busca de alternativas terap uticas para esta enfermidade tem grande relev ncia para a sociedade, j que as op es atuais s o limitadas, sendo dispon vel apenas o benznidazol (BZD) e nifurtimox. Os derivados nitroheteroc clicos s o considerados compostos bioativos com n mero crescente de estudos na comunidade cient fica contra seu agente etiol gico, o Trypanosoma cruzi. Neste sentido, o presente trabalho tem por objetivo a identifica o de derivados do 5-nitrofurano com atividade frente a diferentes cepas do T. cruzi, assim como estudar poss veis modo de a o desta classe de compostos. Esta investiga o envolve estudos computacionais com o prop sito de construir modelos quantitativos de rela es estrutura-atividade (QSAR multivariado) que possam auxiliar na previs o de novas estruturas com perfil farmacol gico otimizado. No presente trabalho foram realizadas as etapas de planejamento, s ntese e ...
Publikations-Datenbank der Fraunhofer Wissenschaftler und Institute: Aufsätze, Studien, Forschungsberichte, Konferenzbeiträge, Tagungsbände, Patente und Gebrauchsmuster
An experimental study was designed to investigate the efficacy of BMAP-27, a compound of the cathelicidin family, in neutralizing… Expand ...
It is also a trypanocidal agent. When administered orally, it is metabolized to salicylamide, which exerts analgesic, ...
... (melaminylthioarsenate) is a trypanocidal agent. In the U.S., it is marketed under the trade names Immiticide ( ...
A natural compound with trypanocidal activity". International Journal of Antimicrobial Agents. 37 (6): 536-43. doi:10.1016/j. ... Antimicrobial Agents and Chemotherapy. 57 (11): 5307-14. doi:10.1128/AAC.00595-13. PMC 3811247. PMID 23939901. Raszeja, W.; ...
... is a trypanocidal agent for veterinary use. Hawking F, Sen AB (December 1960). "The trypanocidal action of ...
... is a triazene trypanocidal agent used in veterinary medicine. It consists of a single Ethidium bromide ...
Eradication of infectious diseases#Human African Trypanosomiasis Trypanocidal agent "US Fraunhofer Center receives Grant from ...
... he tested benzopurpurine dyes supplied by Bayer Pharmaceutical as trypanocidal agents for destruction of the parasite ...
A novel class of anti-hepatitis C agents with potential to bind CD81". J. Med. Chem. Journal of Medicinal Chemistry. 46 (14): ... I. Papanastasiou; A. Tsotinis; N. Kolocouris; S. R. Prathalingam; J. M. Kelly (2008). "Design, synthesis, and trypanocidal ...
A trypanocidal agent is an antiprotozoal agent that acts upon trypanosome parasites. Examples include: Aminoquinuride ... Trypanosomiasis vaccine Trypanocidal+Agents at the US National Library of Medicine Medical Subject Headings (MeSH) MeSH list of ... agents 82014344 GOBLE, F. C. (January 1950). "Chemotherapy of experimental trypanosomiasis; trypanocidal activity of certain ... "Assessment of the occurrence of trypanocidal drug resistance in trypanosomes of naturally infected cattle in the Adamaoua ...
Trypanocidal Activity of a Selection of Naturally Occurring Compounds (1991) A New Triterpenoid Ester from Croton megalocarpus ... and other flavonoids as the active hypoglycaemic agents of Bridelia ferruginea (1989) 9-Methoxychelerythrine as a True Natural ...
A causative agent for eye keratitis infection". Spectrochimica Acta Part A: Molecular Spectroscopy. 153: 714-21. Bibcode: ... Review (2017). "Leishmanicidal and Trypanocidal Activity of Metal Complexes with 1,2,4-Triazolo[1,5-a]pyrimidines: Insights on ... Hemphill A, Mueller J, Esposito M (2006). "Nitazoxanide, a broad-spectrum thiazolide anti-infective agent for the treatment of ... Antiparasitics target the parasitic agents of the infections by destroying them or inhibiting their growth; they are usually ...
Other agents associated with lower toxicity levels are used during stage 1 of the disease. The approval of the nifurtimox- ... Keiser J.; Ericsson O; Burri C (2000). "Investigations of the metabolites of the trypanocidal drug melarsoprol". Clinical ... This is commonly associated with pharmacologic agents that have active metabolites. One such metabolite, Mel Ox, reaches ... Infectious Disease and Antimicrobial Agents". www.antimicrobe.org. Archived from the original on 2016-11-28. Retrieved 2016-11- ...
The effects of betulinic acid as an anticancer agent in breast cancer is found to be cannabinoid receptor dependent. Betulinic ... "Ursolic acid as a trypanocidal constituent in rosemary". Biological & Pharmaceutical Bulletin. 25 (11): 1485-7. doi:10.1248/bpb ... Novel 3,28-Disubstituted Betulinic Acid Derivatives as Potent Anti-HIV Agents Aims/Hypothesis Out-licensing. iptechex ... as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase. It is found in the bark ...
Ulrich P, Cerami A (January 1984). "Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships ... a macrophage-deactivating agent" (Free full text). Journal of Immunology. 160 (11): 5588-95. PMID 9605164. Hauber I, Bevec D, ...
MRI contrast agent commonly contain gadolinium. Lithium carbonate has been used to treat the manic phase of bipolar disorder. ... March 2018). "In vitro leishmanicidal and trypanocidal evaluation and magnetic properties of 7-amino-1,2,4-triazolo[1,5-a] ...
... trypanocidal agents MeSH D27.505.954.122.388 - antiviral agents MeSH D27.505.954.122.388.077 - anti-retroviral agents MeSH ... tocolytic agents MeSH D27.505.954.016 - anti-allergic agents MeSH D27.505.954.122 - anti-infective agents MeSH D27.505.954.122. ... tranquilizing agents MeSH D27.505.696.277.950.015 - anti-anxiety agents MeSH D27.505.696.277.950.025 - antimanic agents MeSH ... fertility agents MeSH D27.505.696.875.552.344 - fertility agents, female MeSH D27.505.696.875.552.510 - fertility agents, male ...
Research has also shown that the venom of P. paulista contains an antimicrobial agent, Mastoparan, that inhibits all ... Trypanocidal activity of mastoparan from Polybia paulista wasp venom by interaction with TcGAPDH. Toxicon. Leite, Natália Bueno ...
Trypanosoma agents. Distribution. Glossina vectors. Sleeping sickness - chronic form. humans. T. brucei gambiense. Western ... The removal of trypanosomosis will eliminate the need for constant prophylactic treatments of the cattle with trypanocidal ... such as trypanocidal drugs, impregnated treated targets (ITT), insecticide-treated cattle (ITC), aerial spraying (Sequential ... and keeping cattle is only feasible when the animals are kept under constant prophylactic treatment with trypanocidal drugs, ...
A trypanocidal agent is an antiprotozoal agent that acts upon trypanosome parasites. Examples include: Aminoquinuride ... Trypanosomiasis vaccine Trypanocidal+Agents at the US National Library of Medicine Medical Subject Headings (MeSH) MeSH list of ... agents 82014344 GOBLE, F. C. (January 1950). "Chemotherapy of experimental trypanosomiasis; trypanocidal activity of certain ... "Assessment of the occurrence of trypanocidal drug resistance in trypanosomes of naturally infected cattle in the Adamaoua ...
Antimicrob Agents Chemother 54:4246-52. 2010. The trypanocidal agents nifurtimox and benznidazole both function as prodrugs and ... trypanocidal agents. Summary. Summary: Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA. ... You are here: Research Topics , chemicals and drugs , .. , .. , antiparasitic agents , antiprotozoal agents , trypanocidal ... Antimicrob Agents Chemother 57:4151-63. 2013. ..Thus, these preliminary studies confirm VNI as a very promising trypanocidal ...
biological evaluation of β-lapachone and nor-β-lapachone complexes with 2-hydroxypropyl-β-cyclodextrin as trypanocidal agents." ... If you are a legal copyright holder or a designated agent for such and you believe a post on this website falls outside the ... Additionally, the biological activities of βLAP, NβL, ICβLAP, and ICNβL were investigated through trypanocidal assays with T. ... biological evaluation of β-lapachone and nor-β-lapachone complexes with 2-hydroxypropyl-β-cyclodextrin as trypanocidal agents. ...
Evaluating 5-nitrofurans as trypanocidal agents. Antimicrob Agents Chemother. Full text not available from this repository. ... The anti-parasitic activity of the most potent agents was demonstrated to be NTR dependent as parasites having reduced levels ... Here, we evaluate the trypanocidal activity of a library of other 5-nitrofurans against bloodstream form T. brucei as a ... the causative agent of human African trypanosomiasis. The mode of action of this prodrug involves an initial activation ...
Nitrofurazone is a topical antibacterial agent indicated as an adjunctive therapy for second and third degree burns when ... resistance to other agents is a real or potential problem. Nitrofurazone is also indicated in skin grafting when bacterial ...
Agents Chemother.Year: 2010, 54, 4246-4252.20679506. Hu L. Q.,; Wu X. H.,; Han J. Y.,; Chen L.,; Vass S. O.,; Browne P.,; Hall ... Trypanocidal Studies The trypanocidal activity over a 72 h period was determined using the Alamar Blue viability, as described ... Agents Chemother.Year: 2010, 54, 2893-2900.20439607. Wilkinson S. R.,; Taylor M. C.,; Horn D.,; Kelly J. M.,; Cheeseman I.,A ... Agents Chemother.Year: 2010, 54, 1193-1199.20028822. Bot C.,; Hall B. S.,; Bashir N.,; Taylor M. C.,; Helsby N. A.,; Wilkinson ...
Trypanocidal Agents / chemistry * Trypanocidal Agents / economics * Trypanocidal Agents / pharmacology* * Trypanosoma brucei ... Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei Chem Biol Drug Des. 2006 May;67(5):355-63. doi: ... several other drugs suspected but never validated as trypanocidal, and 17 novel trypanocidal drugs. ... One potentially rapid and cost-effective approach to identifying and developing new trypanocidal drugs would be high throughput ...
Quinol derivatives as potential trypanocidal agents. Amy Capes, Stephen Patterson, Susan Wyllie, Irene Hallyburton, Iain T. ... title = "Quinol derivatives as potential trypanocidal agents",. abstract = "Quinols have been developed as a class of potential ... Quinol derivatives as potential trypanocidal agents. / Capes, Amy; Patterson, Stephen; Wyllie, Susan; Hallyburton, Irene; ... Quinol derivatives as potential trypanocidal agents. In: Bioorganic & Medicinal Chemistry. 2012 ; Vol. 20, No. 4. pp. 1607-1615 ...
Mapping the S1 and S1 subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents. Author: ... Mapping the S1 and S1 subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents. DSpace ...
Antimicrob Agents Chemother 44: 2954-2961.. *Pomel S, Biot C, Bories C, Loiseau PM (2013) Antiprotozoal activity of ferroquine ... Determination of trypanocidal activity of test samples. Compounds were tested for their activity against bloodstream forms of T ... Loiseau PM, Lubert P, Wolf JG (2000) Contribution of dithiol ligands to in vitro and in vivo trypanocidal activities of ... Antileishmanial and Trypanocidal Activities of Extracts and Aporphine Alkaloids Isolated from Monodora Genus (Annonaceae) Joël ...
Antifungal Agents. Anti-Infective Agents. Trypanocidal Agents. Antiprotozoal Agents. Antiparasitic Agents. 14-alpha Demethylase ...
Antifungal Agents. Anti-Infective Agents. 14-alpha Demethylase Inhibitors. Cytochrome P-450 Enzyme Inhibitors. Enzyme ... Cytokines (except erythropoietin), interferon, or lymphocyte replacement therapy unless patient already taking these agents for ...
Antifungal Agents. Anti-Infective Agents. Antiprotozoal Agents. Antiparasitic Agents. Trypanocidal Agents. To Top ... Concomitant therapy with other investigational agents or participation in another clinical trial ...
Antifungal Agents. Anti-Infective Agents. Antiprotozoal Agents. Antiparasitic Agents. Trypanocidal Agents. To Top ... and efficacy of biweekly administration of 1 of 3 doses of aerosol pentamidine when used as a prophylactic agent in patients ...
Antifungal Agents. Anti-Infective Agents. Antiprotozoal Agents. Antiparasitic Agents. Trypanocidal Agents. To Top ... and effectiveness of long-term biweekly administration of 1 of 2 doses of aerosol pentamidine when used as a prophylactic agent ...
Efficacy of trypanocidal agents in field conditions in working equidae in The Gambia: A prospective clinical study. Status. ... A prospective clinical study using one of three randomised trypanocidal agents. Villages in the Central River District will be ... 2) To improve knowledge of expected clinical response to trypanocidal agents in equidae. 3) To identify incidence of different ... such that a minimum of 50 animals are treated with each of the trypanocidal compounds. Assessment of clinical and ...
Evaluating 5-nitrofurans as trypanocidal agents.. Bot C, Hall BS, Alvarez G, Di Maio R, González M, Cerecetto H, Wilkinson SR. ... 3-Trifluoromethylquinoxaline N,N-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and ... Antimicrob Agents Chemother. 2013 Apr;57(4):1638-47. doi: 10.1128/AAC.02046-12. Epub 2013 Jan 18. ... Design, synthesis and biological evaluation of new potent 5-nitrofuryl derivatives as anti-Trypanosoma cruzi agents. Studies of ...
Trypanocidal Agents/therapeutic use , Trypanocidal Agents/pharmacology , Nitroimidazoles/therapeutic use , In Vitro Techniques/ ... Full text: Available Index: LILACS (Americas) Main subject: Trypanocidal Agents / Nitroimidazoles Language: English Journal: ... Full text: Available Index: LILACS (Americas) Main subject: Trypanocidal Agents / Nitroimidazoles Language: English Journal: ... In vitro genotoxicity of nitroimidazoles as a tool in the search of new trypanocidal agent ...
Trypanosoma cruzi is the causative agent of Chagas disease. The major protease, cruzain, is a target for the development of ... Trypanocidal Agents Grant support * AI35707-1/AI/NIAID NIH HHS/United States ... Trypanosoma cruzi is the causative agent of Chagas disease. The major protease, cruzain, is a target for the development of ...
It is also a trypanocidal agent. When administered orally, it is metabolized to salicylamide, which exerts analgesic, ...
Pharmacological Actions : Trypanocidal Agents. [+] Curcumin has trypanocidal properties.Jun 01, 1998. Click here to read the ...
0 (Nitroimidazoles); 0 (Triazoles); 0 (Trypanocidal Agents); 6TK1G07BHZ (posaconazole); YC42NRJ1ZD (benzonidazole). [Em] M s de ...
0/Reactive Oxygen Species; 0/Trypanocidal Agents; 96-26-4/Dihydroxyacetone; EC 2.7.1.-/Phosphotransferases (Alcohol Group ... Title: Antimicrobial agents and chemotherapy Volume: 51 ISSN: 0066-4804 ISO Abbreviation: Antimicrob. Agents Chemother. ... Nlm Unique ID: 0315061 Medline TA: Antimicrob Agents Chemother Country: United States ... we consider DHA a starting point for a rational design of new trypanocidal drugs.. ...
Trypanocidal drug that acts on circulating trypomastigotes, as well as intracellular amastigotes. The mechanism of action may ... Antiprotozoal agents. Class Summary. These agents are used to treat infections caused by the protozoan T cruzi. ... Trypanocidal drugs for chronic asymptomatic Trypanosoma cruzi infection. Cochrane Database Syst Rev. 2014 May 27. CD003463. [ ... The genome sequence of Trypanosoma cruzi, etiologic agent of Chagas disease. Science. 2005 Jul 15. 309(5733):409-15. [Medline] ...
Activity against drug-resistant Trypanosoma cruzi strains," International Journal of Antimicrobial Agents, vol. 21, no. 1, pp. ... G. Berkelhammer and G. Asato, "2-Amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole: a new antimicrobial agent," Science ... From this perspective, the aim of this work is to present new nitro analogs of megazol with trypanocidal activity designed ... B. Enanga, M. R. Ariyanayagam, M. L. Stewart, and M. P. Barrett, "Activity of megazol, a trypanocidal nitroimidazole, is ...
The trypanocidal activity of cynaropicrin was also evaluated against Trypanosoma cruzi (the causative agent of Chagas disease ... Indeed, most natural agents do not induce a high level of toxicity and target multiple signaling pathways involved in cell ... Cynaropicrin: A Comprehensive Research Review and Therapeutic Potential As an Anti-Hepatitis C Virus Agent. Mahmoud F. Elsebai1 ... Photoaging is the main causative agent for the increased risk for skin cancer and the appearance of damaged skin. Aging of the ...
Novel African trypanocidal agents: membrane rigidifying peptides.. John M Harrington. et al. ... Trypanocidal activity is conferred by peptide hydrophobicity and charge distribution and results from increased rigidity of the ...
Aryl phosphoramidates of 5-phosho erythronohydroxamic acid, a new class of potent trypanocidal agents. J. Med. Chem. 53, 6071- ...
Trypanocidal Agents (administration & dosage) *Trypanosomiasis (drug therapy, prevention & control, transmission, veterinary) * ...
Antimicrob Agents Chemother. 2018 Jan 25;62(2). pii: e01936-17. doi: 10.1128/AAC.01936-17. Print 2018 Feb. ... In Vitro and In Vivo Studies of the Trypanocidal Effect of Novel Quinolines. ... Antimicrob Agents Chemother. 2016 Oct 21;60(11):6844-6852. doi: 10.1128/AAC.01545-16. Print 2016 Nov. ... Antimicrob Agents Chemother. 2016 May 23;60(6):3794-801. doi: 10.1128/AAC.01787-15. Print 2016 Jun. ...
  • The nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one of a limited number of treatments targeting Trypanosoma brucei, the causative agent of human African trypanosomiasis. (surrey.ac.uk)
  • A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro. (biomedsearch.com)
  • In this study, we have synthesized a series of novel 5-nitro-2-furancarboxylamides that show potent trypanocidal activity, ∼1000-fold more potent than nifurtimox against in vitro Trypanosoma brucei with very low cytotoxicity against human HeLa cells. (biomedsearch.com)
  • In the search for agents from tropical medicinal plants to treat these two neglected tropical diseases, serially extracted petroleum ether, dichloromethane and methanol extracts of the leaves of Monodora crispata and Monodora brevipes , and eleven aporphines alkaloids isolated from the dried powdered leaves of the two plants were evaluated against Leishmania donovani promastigotes and Trypanosoma brucei brucei trypomastigotes. (omicsonline.org)
  • OBJECTIVES To evaluate whether the genotoxic effect of 3 was abolished in the seven nitroimidazoles (4-10) analogs using the in vitro alkaline comet assay (CA) and the in vitro cytokinesis -block micronucleus assay (CBMN) in whole human blood cells (WHBC) and correlate this effect with their trypanocidal activity using bloodstream trypomastigote forms of Trypanosoma cruzi . (bvsalud.org)
  • Trypanosoma cruzi is the causative agent of Chagas' disease. (nih.gov)
  • Dibenzylideneacetones Are Potent Trypanocidal Compounds That Affect the Trypanosoma cruzi Redox System. (semanticscholar.org)
  • It has been estimated that around 20 million people are infected and over 40 million individuals are facing the risk of infection by the hemoflagellates protozoan Trypanosoma cruzi , the responsible agent of Chagas' disease. (intechopen.com)
  • The similarity between the membrane sterol requirements of pathogenic fungi and those of the parasitic protozoon Trypanosoma cruzi , the causative agent of Chagas human cardiopathy, has led to repurposing anti-fungal azole inhibitors of sterol 14α-demethylase (CYP51) for the treatment of Chagas Disease. (plos.org)
  • Aqueous and methanol leaf extracts of V. sinaiticum were investigated for the presence of secondary metabolites and their in vitro activity against Trypanosoma congolence, the main causative agent of African animal trypanosomosis in Sub-Saharan Africa and Ethiopia. (omicsonline.org)
  • The trypanocidal acitivity toward Trypanosoma cruzi, the agent causing Chagas Disease, was evaluated for complexes 2-5 and their free ligands, in both amastigotes (intracellular) and epimastigotes cell forms, and also the cytotoxicity in LLC-MK2 monkey kidney epithelial healthy, non-infected cells. (usp.br)
  • The protozoan hemoflagellate Trypanosoma cruzi (T. cruzi) is the etiologic agent of the zoonotic Chagas' disease that affects approximately six to seven million people in Central and South America, causing dilated cardiomyopathy and megavisceral disease. (intechopen.com)
  • The pathogenic protozoan Trypanosoma cruzi ( T. cruzi ) is the causative agent of Chagas' disease, and more than 150 species of mammals are affected by this unicellular parasite, including humans. (intechopen.com)
  • The enzyme cruzain is the major cysteine protease from Trypanosoma cruzi , the etiologic agent of American trypanosomiasis or Chagas' disease, and has been selected as an attractive target for the development of novel trypanocidal drugs. (scielo.br)
  • Here, we evaluate the trypanocidal activity of a library of other 5-nitrofurans against bloodstream form T. brucei as a preliminary step in the identification of additional nitroaromatic compounds that could potentially partner eflornithine. (surrey.ac.uk)
  • The anti-parasitic activity of the most potent agents was demonstrated to be NTR dependent as parasites having reduced levels of the enzyme displayed resistance to the compounds while parasites over expressing TbNTR showed hypersensitivity. (surrey.ac.uk)
  • Phase 2 It is aimed to treat and provide follow-up care and investigation of at least 150 infected donkeys and horses during 2012-2013, such that a minimum of 50 animals are treated with each of the trypanocidal compounds. (thedonkeysanctuary.org.uk)
  • The class of nitroimidazoles includes compounds that are important antiparasitic agents, which have a broad spectrum of action and high biological activity. (scielo.br)
  • About 90 plants were identified, with 54 compounds as potential active agents and presented by plant families in alphabetical order. (mdpi.com)
  • It was determined that the mode of action of these purines was trypanostatic, with the compounds becoming trypanocidal only at much higher concentrations. (asm.org)
  • These results indicate that acridine and dinitroaniline herbicides with the plant extracts are promising lead compounds for development as novel antileishmanial agents. (thefreedictionary.com)
  • Here, we evaluated how different warheads for a set of structurally similar related compounds could inhibit the activity of cruzipain and, ultimately, their trypanocidal effect. (rsc.org)
  • Eight compounds had multi-trypanocidal activity against T. cruzi and Leishmania spp. (unam.mx)
  • All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC50 values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. (brad.ac.uk)
  • Two of these huprines were also found to be active against a chloroquine-resistant strain of P. falciparum, thus emerging as interesting trypanocidal-antiplasmodial dual acting compounds, but they exhibited little selectivity for P. falciparum over L6 cells. (brad.ac.uk)
  • Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio. (brad.ac.uk)
  • Trypanosomiasis vaccine Trypanocidal+Agents at the US National Library of Medicine Medical Subject Headings (MeSH) MeSH list of agents 82014344 GOBLE, F. C. (January 1950). (wikipedia.org)
  • The BENEFIT project - Benznidazole Evaluation for Interrupting Trypanosomiasis - is an international, multicenter, double-blind, placebo-controlled trial of trypanocidal treatment with benznidazole in patients with chronic Chagas heart disease. (fiocruz.br)
  • The low efficacy and the adverse effects of some of the conventional antidiabetic agents together with the increasing global incidence of diabetes necessitate the urgent search for more potent and safer alternatives from natural sources such as medicinal plants. (pubmedcentralcanada.ca)
  • Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. (brad.ac.uk)
  • The use of these, or other antioxidants (along with a trypanocidal agent) would, no doubt, improve the efficacy and efficiency of chemotherapy. (bioline.org.br)
  • Objective: The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy. (eurekaselect.com)
  • Exploiting the drug-activating properties of a novel trypanosomal nitroreductase, Antimicrobial Agents and Chemotherapy, Hall et al, 54 (2010), 1193-1199. (qmul.ac.uk)
  • One of the greatest concerns in clinical trials is to provide an early surrogate biomarker of response to trypanocidal chemotherapy. (cdc.gov)
  • The present work reviews in detail the formulation and in-vitro/in-vivo analysis of different nanoformulations of nifurtimox and benznidazole in order to enhance their solubility, dissolution, bioavailability and trypanocidal activity. (bioportfolio.com)
  • These effects might be related to the trypanocidal action of benznidazole, a chemotherapeutic agent against Chagas' disease. (eurekamag.com)
  • Benznidazole (LAFEPE, Recife, Brazil), a nitroimidazole derivative, has also been widely used as an effective agent for antiparasitic therapy in cases of acute or sub-acute Chagas disease, including transfusion and laboratory-acquired disease and reactivation of infection in transplanted and other immunosuppressed patients. (fiocruz.br)
  • Bay leaf contains constituents which exhibit trypanocidal activity. (greenmedinfo.com)
  • Megazol (2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole), CAS number 19622-55-0, synthesized in 1968 by Berkelhammer and Asato [ 6 ] and characterized by Filardi and Brener [ 7 ] is an important nitroheterocyclic nitroimidazole containing the 1,3,4-thiadiazole nucleus and has proved to be a promising alternative due to its trypanocidal activity. (hindawi.com)
  • From this perspective, the aim of this work is to present new nitro analogs of megazol with trypanocidal activity designed using rational drug design strategies [ 15 , 16 ] in order to obtain substances with a similar pharmacodynamic profile but fewer side effects than megazol by removing its genotoxic effect, in accordance with WHO [ 17 ] proposals for the control neglected diseases. (hindawi.com)
  • Trypanocidal activity is conferred by peptide hydrophobicity and charge distribution and results from increased rigidity of the plasma membrane. (sigmaaldrich.com)
  • In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. (bvsalud.org)
  • Taken together with the oral absorption -enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line . (bvsalud.org)
  • These agents are used to treat infections caused by the protozoan T cruzi . (medscape.com)
  • Although CD represents an important public health problem, resulting in high morbidity and considerable mortality rates, few investments have been allocated towards developing novel anti- T. cruzi agents. (hindawi.com)
  • The top hit inhibited T. cruzi with EC 50 of 17 nM and was trypanocidal at 40 nM. (plos.org)
  • As the host immune response plays a pivotal role in the adverse events triggered by antigen release during treatment with trypanocidal drugs, the ability of hypnophilin to kill the intracellular forms of T. cruzi while modulating human PBMC proliferation suggests that this terpenoid may be a promising prototype for the development of new chemotherapeutical agents for Chagas disease. (fiocruz.br)
  • Kamdem, J.P. Chemical Characterization and Trypanocidal, Leishmanicidal and Cytotoxicity Potential of Lantana camara L. (Verbenaceae) Essential Oil. (mdpi.com)
  • A trypanocidal agent is an antiprotozoal agent that acts upon trypanosome parasites. (wikipedia.org)
  • Synthesis and biological evaluation of β-lapachone and nor-β-lapachone complexes with 2-hydroxypropyl-β-cyclodextrin as trypanocidal agents. (bioportfolio.com)
  • Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set of quinazolinone and quinazoline derivatives were studied as trypanocidal agents. (eurekaselect.com)
  • These novel and potential inhibitors constitute new drug candidates that must be biologically tested to define their value as an alternative chemotherapeutic agent in the treatment of these protozoan infections. (scielo.org.co)
  • In conventional practice, management of type 1 diabetes is by exogenous insulin while type 2 is by oral agents including the sulfonylureas, biguanides, α-glucosidase inhibitors, glitazones, gliptins, and the SGLT 2 inhibitors, which are used as monotherapy or in combination to achieve better glycemic regulation since they have different modes of action. (pubmedcentralcanada.ca)
  • There is an urgent need for better drugs against Leishmania , the etiological agent of the disease. (scielo.org.co)
  • The current antiprotozoal agents often derive their selectivity from selective accumulation by the parasite rather than the host cell ( 9 , 22 ). (asm.org)
  • Amino acids as selective sulfonamide acylating agents. (up.pt)
  • Its derivatives include fluorescent yellow dyes and the antiseptic agents acriflavine hydrochloride, acriflavine base, and proflavine. (thefreedictionary.com)
  • Derivatives of acridine are successful as antibacterial agents, finding their principal use as local antiseptics. (thefreedictionary.com)
  • This review indicates that the Nigerian flora may be suitable as a starting point in searching for new and more efficient trypanocidal molecules. (mdpi.com)
  • Long after the initial phase, the only period when the etiologic agent is readily found, clinical complications of the chronic phase appear in at least 30-40% of infected people. (fiocruz.br)
  • One potentially rapid and cost-effective approach to identifying and developing new trypanocidal drugs would be high throughput-screening of existing drugs already approved for other uses, as well as clinical candidates in late development. (nih.gov)
  • Based on the toxicity of DHA for trypanosomes compared with mammals, we consider DHA a starting point for a rational design of new trypanocidal drugs. (biomedsearch.com)
  • Taken together, our results suggest that L. camara essential oil may be an important source of therapeutic agents for the development of alternative drugs against parasitic diseases. (mdpi.com)
  • However, due to low profit prospects, the development of new trypanocidal drugs is not attractive to the pharmaceutical industry (Nwaka & Ridley 2003). (fiocruz.br)
  • This element has been used for centuries as a therapeutic agent and as a poison and continues to have limited use in some trypanocidal drugs such as melarsoprol and tryparsamide. (thefreedictionary.com)
  • Herein, nitroimidazoles (11-19) bearing different substituent groups were investigated for their potential induction of genotoxicity (comet assay) and mutagenicity ( Salmonella /Microsome assay) and the correlations of these effects with their trypanocidal effect and with megazol were investigated. (scielo.br)
  • In these assays, the crude extract was more effective than the isolated clerodanes DCTN or CTN on trypomastigote while the trypanocidal effect of the triterpene AAA was against epimastigotes as well as on intracellular amastigotes (Campos et al. (thefreelibrary.com)
  • To evaluate and compare the safety, tolerability, and efficacy of biweekly administration of 1 of 3 doses of aerosol pentamidine when used as a prophylactic agent in patients who have recovered from their first episode of AIDS-associated Pneumocystis carinii pneumonia (PCP). (clinicaltrials.gov)
  • Trypanocidal drug that acts on circulating trypomastigotes, as well as intracellular amastigotes. (medscape.com)
  • The pilot study investigates whether etiologic treatment significantly reduces parasite burden, as assessed by polymerase chain reaction-based techniques and also determines the safety and tolerability profile of the trypanocidal drug in this type of chagasic population. (fiocruz.br)
  • Consequently, conventional VSG-specific intact immunoglobulins are non-trypanocidal in the absence of complement. (prolekare.cz)
  • BA may be an effective agent for the prevention and treatment of cadmium-induced diseases in humans. (greenmedinfo.com)
  • Aqueous extract of Acalypha hispida leaves suggest trypanocidal effect. (2beingfit.com)
  • Evaluating 5-nitrofurans as trypanocidal agents. (surrey.ac.uk)
  • In addition, both therapeutic agents are available only as tablets and a liquid pediatric formulation is still lacking. (bioportfolio.com)
  • A prospective clinical study using one of three randomised trypanocidal agents. (thedonkeysanctuary.org.uk)
  • These facts suggest that trypanocidal therapy may positively impact the clinical course of patients with chronic Chagas heart disease. (fiocruz.br)
  • Nitrofurazone is a topical antibacterial agent indicated as an adjunctive therapy for second and third degree burns when resistance to other agents is a real or potential problem. (pharmacycode.com)