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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase

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Author(s):
da Silva, Edson Roberto [1] ; Brogi, Simone [2] ; Grillo, Alessandro [2] ; Campiani, Giuseppe [2] ; Gemma, Sandra [2] ; Vieira, Paulo Cezar [3] ; Maquiaveli, Claudia do Carmo [4]
Total Authors: 7
Affiliation:
[1] Univ Sao Paulo, Dept Vet Med, Pirassununga - Brazil
[2] Univ Siena, Dept Biotechnol Chem & Pharm, European Res Ctr Drug Discovery & Dev NatSynDrugs, Via Aldo Moro 2, Siena - Italy
[3] Univ Fed Sao Carlos, Dept Chem, Sao Carlos, SP - Brazil
[4] Univ Anhembi Morumbi, Sao Carlos - Brazil
Total Affiliations: 4
Document type: Journal article
Source: CHEMICAL BIOLOGY & DRUG DESIGN; v. 93, n. 2, p. 139-146, FEB 2019.
Web of Science Citations: 2
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 IC50 -in range of 1.5-11 mu M. Compounds 2 and 5 also showed activity against promastigotes of L. amazonensis with IC50 = 61 (28-133) mu M and IC50 = 14 (9-24) mu M, 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. (AU)

FAPESP's process: 17/06917-4 - Study of the polyamine synthesis pathway and trypanothione synthesis for the development of new drugs for the treatment of leishmaniasis
Grantee:Edson Roberto da Silva
Support Opportunities: Regular Research Grants