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Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase
Author(s) -
Silva Edson Roberto,
Brogi Simone,
Grillo Alessandro,
Campiani Giuseppe,
Gemma Sandra,
Vieira Paulo Cezar,
Maquiaveli Claudia do Carmo
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13391
Subject(s) - arginase , biochemistry , leishmania , chemistry , caffeic acid , biology , pharmacology , arginine , amino acid , parasite hosting , world wide web , computer science , antioxidant
Abstract This study describes the activity of five natural hydroxycinnamic acids and derived compound: caffeic ( 1 ), rosmarinic ( 2 ), chlorogenic ( 3 ), and cryptochlorogenic ( 4 ), acids and isoverbascoside ( 5 ). All compounds inhibited Leishmania amazonensis arginase with IC 50 —in range of 1.5—11 μM. Compounds 2 and 5 also showed activity against promastigotes of L. amazonensis with IC 50 = 61 (28–133) μM and IC 50 = 14 (9–24) μM, respectively. Further computational studies applying molecular docking simulations were performed on the competitive inhibitors to gain insight into the molecular basis for arginase inhibition and could be exploited to the development of new antileishmanials drug targeting parasite arginase.