INVESTIGADORES
MALCHIODI Emilio Luis
artículos
Título:
Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. satureiifolia
Autor/es:
FRANK, FERNANDA MARIA ; BIVONA, AUGUSTO ERNESTO ; CERNY, NATACHA; MALCHIODI, EMILIO LUIS; CAZORLA, SILVIA I.
Revista:
PHARMACEUTICAL BIOLOGY
Editorial:
TAYLOR & FRANCIS INC
Referencias:
Lugar: Londres; Año: 2016
ISSN:
1388-0209
Resumen:
Context Chagas? disease and leishmaniasis produce significant disability and mortality with greatsocial and economic impact. The genus Stevia (Asteraceae) is a potential source of antiprotozoalcompounds.Objective Aerial parts of four Stevia species were screened on Trypanosoma cruzi. Steviasatureiifolia (Lam.) Sch. Bip. var. satureiifolia (Asteraceae) dichloromethane extract was selected for abioassay-guided fractionation in order to isolate its active compounds. Additionally, theantileishmanial activity and the cytotoxicity of these compounds on mammalian cells wereassessed.Materials and methods The dichloromethane extract was fractionated by column chromatography.The isolated compounds were evaluated using concentrations of 0?100 mg/mL on T. cruziepimastigotes and on Leishmania braziliensis promastigotes for 72 h, on trypomastigotes andamastigotes of T. cruzi for 24 h and 120 h, respectively. The compounds? cytotoxicity (12.5?500 mg/mL) was assessed on Vero cells by the MTT assay. The structure elucidation of eachcompound was performed by spectroscopic methods and HPLC analysis.Results The dichloromethane extracts of Stevia species showed significant activity on T. cruziepimastigotes. The flavonoids eupatorin (1.3%), cirsimaritin (1.9%) and 5-desmethylsinensetin(1.5%) were isolated from S. satureiifolia var. satureiifolia extract. Eupatorin and 5-desmethylsinensetinshowed IC50 values of 0.2 and 0.4 mg/mL on T. cruzi epimastigotes and 61.8 and75.1 mg/mL on trypomastigotes, respectively. The flavonoid 5-desmethylsinensetin showedmoderate activity against T. cruzi amastigotes (IC50 value┬╝78.7 mg/mL) and was the most activecompound on L. braziliensis promastigotes (IC50 value┬╝37.0 mg/mL). Neither of the flavonoidsshowed cytotoxicity on Vero cells, up to a concentration of 500 mg/mL.