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J Nat Prod ; 79(5): 1459-63, 2016 05 27.
Artigo em Inglês | MEDLINE | ID: mdl-27096224

RESUMO

Verbascoside (1) is a phenylethanoid glycoside that has antileishmanial activity against Leishmania infantum and Leishmania donovani. In this study, we verified the activity of 1 on Leishmania amazonensis and arginase inhibition. Compound 1 showed an EC50 of 19 µM against L. amazonensis promastigotes and is a competitive arginase inhibitor (Ki = 0.7 µM). Docking studies were performed to assess the interaction of 1 with arginase at the molecular level. Arginase is an enzyme of the polyamine biosynthesis pathway that is important to parasite infectivity, and the results of our study suggest that 1 could be useful to develop new approaches for treating leishmaniasis.


Assuntos
Arginase/antagonistas & inibidores , Glucosídeos/farmacologia , Leishmania/efeitos dos fármacos , Leishmania/enzimologia , Leishmaniose/tratamento farmacológico , Fenóis/farmacologia , Animais , Invertebrados/metabolismo , Estrutura Molecular
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