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J Glob Antimicrob Resist ; 18: 187-194, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-30797085

RESUMO

OBJECTIVES: Green tea contains a predominant set of polyphenolic compounds with biological activities. The aim of this study was to investigate the antileishmanial activities of the main components of green tea, including catechin, (-)-epicatechin, epicatechin gallate (ECG) and (-)-epigallocatechin 3-O-gallate (EGCG), against Leishmania infantum promastigotes. METHODS: Green tea ligands and the control drug pentamidine were docked using AutoDock 4.3 software into the active sites of trypanothione synthetase and arginase, which were modelled using homology modelling programs. The colorimetric MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay was used to measure L. infantum promastigotes at different concentrations of green tea compounds in a concentration- and time-dependent manner. Results were expressed as 50% and 90% inhibitory concentrations (IC50 and IC90, respectively). RESULTS: In silico and in vitro assays showed that all of the green tea compounds have antileishmanial activity. EGCG and ECG were the most active compounds against L. infantum promastigotes, with IC50 values of 27.7µM and 75µM and IC90 values of 88.4µM and 188.7µM, respectively. Pentamidine displayed greater growth inhibition than all of the other tested compounds in a concentration- and time-dependent manner. CONCLUSION: In this study, in silico and docking results were in accordance with the in vitro activity of the compounds. Moreover, EGCG and ECG showed reasonable levels of selectivity for Leishmania.


Assuntos
Leishmania infantum/efeitos dos fármacos , Exsudatos de Plantas/farmacologia , Chá/química , Amida Sintases/química , Amida Sintases/efeitos dos fármacos , Antioxidantes/farmacologia , Arginase/química , Arginase/efeitos dos fármacos , Catequina/análogos & derivados , Proliferação de Células/efeitos dos fármacos , Simulação por Computador , Irã (Geográfico) , Leishmaniose Visceral/parasitologia , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Pentamidina/química , Pentamidina/farmacologia , Inibidores de Proteases/farmacologia
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