Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis.
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.
Department of Chemistry, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
Claudia C
CC
Maquiaveli
Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.
João F
JF
Lucon-Júnior
European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
Simone
S
Brogi
European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
Giuseppe
G
Campiani
European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.
Sandra
S
Gemma
Department of Chemistry, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
Paulo C
PC
Vieira
Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.
Edson R
ER
Silva
D000818:Animals; D001119:Arginase / Q000037:antagonists & inhibitors*; D005960:Glucosides / Q000494:pharmacology*; D007448:Invertebrates / Q000378:metabolism; D007891:Leishmania / Q000187:drug effects* / Q000201:enzymology*; D007896:Leishmaniasis / Q000188:drug therapy*; D015394:Molecular Structure; D010636:Phenols / Q000494:pharmacology*; D059808:Polyphenols
D001119:Arginase; D005960:Glucosides; D010636:Phenols; C058956:acteoside; D059808:Polyphenols