Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase

Autor(es)

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]

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: CHEMICAL BIOLOGY & DRUG DESIGN; v. 93, n. 2, p. 139-146, FEB 2019.
• Citações Web of Science: 2

Resumo

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)

• Processo FAPESP: 17/06917-4 - Estudo da via de síntese de poliaminas e síntese de tripanotiona para desenvolvimento de novos fármacos para tratamento da leishmaniose
• Beneficiário: Edson Roberto da Silva
• Modalidade de apoio: Auxílio à Pesquisa - Regular