Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis

Autor(es)

Maquiaveli, Claudia C. ^[1] ; Lucon-Junior, Joao F. ^[2] ; Brogi, Simone ^{[3, 4]} ; Campiani, Giuseppe ^{[3, 4]} ; Gemma, Sandra ^{[3, 4]} ; Vieira, Paulo C. ^[1] ; Silva, Edson R. ^[2]

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Carlos, Dept Chem, Rod Washington Luis, Km 235, BR-13565905 Sao Carlos, SP - Brazil

^[2] Univ Sao Paulo, Dept Vet Med, Ave Duque Caxias Norte 225, BR-13635900 Pirassununga, SP - Brazil

^[3] Univ Siena, European Res Ctr Drug Discovery & Dev NatSynDrugs, Via Aldo Moro 2, I-53100 Siena - Italy

^[4] Univ Siena, Dept Biotechnol Chem & Pharm, Via Aldo Moro 2, I-53100 Siena - Italy

• Tipo de documento: Artigo Científico
• Fonte: Journal of Natural Products; v. 79, n. 5, p. 1459-1463, MAY 2016.
• Citações Web of Science: 13

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 mu M against L. amazonensis promastigotes and is a competitive arginase inhibitor (K-i = 0.7 mu M). 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. (AU)

• Processo FAPESP: 14/18642-1 - Utilização da enzima arginase como alvo terapêutico para desenvolvimento de protótipos leishmanicidas
• Beneficiário: Edson Roberto da Silva
• Modalidade de apoio: Auxílio à Pesquisa - Regular