Santos Augusto L, Yamamoto Eduardo S, Passero Luiz Felipe D, Laurenti Márcia D, Martins Ligia F, Lima Marta L, Uemi Miriam, Soares Marisi G, Lago João Henrique G, Tempone Andre G, Sartorelli Patricia
Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of São Paulo, Rua Prof. Artur Riedel, n° 275 - Jd. Eldorado, CEP 09972-270, Diadema, São Paulo, Brazil.
Laboratory of Pathology of Infectious Diseases, Medical School, University of São Paulo, Av. Dr. Arnaldo, 455 - Cerqueira César, CEP 01246-903, São Paulo, SP, Brazil.
Chem Biodivers. 2017 May;14(5). doi: 10.1002/cbdv.201600458.
Bioactivity-guided fractionation of antileishmanial active extract from leaves of Casearia arborea led to isolation of three metabolites: tricin (1), 1',6'-di-O-β-d-vanilloyl glucopyranoside (2) and vanillic acid (3). Compound 1 demonstrated the highest activity against the intracellular amastigotes of Leishmania infantum, with an IC value of 56 μm. Tricin (1) demonstrated selectivity in mammalian cells (SI > 7) and elicited immunomodulatory effect on host cells. The present work suggests that tricin modulated the respiratory burst of macrophages to a leishmanicidal state, contributing to the parasite elimination. Therefore, the natural compound tricin could be further explored in drug design studies for leishmaniasis treatment.