Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. Satureiifolia

BEER F.; FERNANDA FRANK; ELSO ORLANDO; BIVONA A.; CERNY N.; GUSTAVO GIBERTI; MALCHIODI, E; MARTINO, VIRGINIA; ALONSO MARÍA ROSARIO; SULSEN, VALERIA

PHARMACEUTICAL BIOLOGY

TAYLOR & FRANCIS INC

Lugar: Londres; Año: 2016

1388-0209

ABSTRACTContext Chagas? disease and leishmaniasis produce significant disability and mortality with great social and economic impact. The genus Stevia (Asteraceae) is a potential source of antiprotozoal compounds.Objective Aerial parts of four Stevia species were screened on Trypanosoma cruzi. Stevia satureiifolia (Lam.) Sch. Bip. var. satureiifolia (Asteraceae) dichloromethane extract was selected for a bioassay-guided fractionation in order to isolate its active compounds. Additionally, the antileishmanial 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. cruzi epimastigotes and on Leishmania braziliensis promastigotes for 72 h, on trypomastigotes and amastigotes of T. cruzi for 24 h and 120 h, respectively. The compounds? (12.5?500 mg/mL) cytotoxicity was assessed on Vero cells by MTT assay. The structure elucidation of each compound was performed by spectroscopic methods and HPLC analysis.Results The dichloromethane extracts Stevia species showed significant activity on T. cruzi epimastigotes. The flavonoids eupatorin (1.3%), cirsimaritin (1.9%) and 5-desmethylsinensetin (1.5%) were isolated from S. satureiifolia var. satureiifolia extract. Eupatorin and 5-desmethylsinensetin showed IC50 values of 0.2 and 0.4 mg/mL on T. cruzi epimastigotes and 61.8 and 75.1 mg/mL on trypomastigotes, respectively. The flavonoid 5-desmethylsinensetin showedmoderate activity against T. cruzi amastigotes (IC50 value¼78.7 mg/mL) and was the most active compound on L. braziliensis promastigotes (IC50 value¼37.0 mg/mL). Neither of the flavonoids up to a concentration of 500 mg/mL.