| Autor: |
Beer, María Florencia, Frank, Fernanda Maria, Germán Elso, Orlando, Ernesto Bivona, Augusto, Cerny, Natacha, Giberti, Gustavo, Luis Malchiodi, Emilio, Susana Martino, Virginia, Alonso, María Rosario, Patricia Sülsen, Valeria, Cazorla, Silvia Ines |
| Předmět: |
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| Zdroj: |
Pharmaceutical Biology; Oct2016, Vol. 54 Issue 10, p2188-2195, 8p |
| Abstrakt: |
ContextChagas’ disease and leishmaniasis produce significant disability and mortality with great social and economic impact. The genusStevia(Asteraceae) is a potential source of antiprotozoal compounds. ObjectiveAerial parts of fourSteviaspecies were screened onTrypanosoma 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 were assessed. Materials and methodsThe dichloromethane extract was fractionated by column chromatography. The isolated compounds were evaluated using concentrations of 0–100 μg/mL onT. cruziepimastigotes and onLeishmania braziliensispromastigotes for 72 h, on trypomastigotes and amastigotes ofT. cruzifor 24 h and 120 h, respectively. The compounds’ cytotoxicity (12.5–500 μg/mL) was assessed on Vero cells by the MTT assay. The structure elucidation of each compound was performed by spectroscopic methods and HPLC analysis. ResultsThe dichloromethane extracts ofSteviaspecies showed significant activity onT. cruziepimastigotes. The flavonoids eupatorin (1.3%), cirsimaritin (1.9%) and 5-desmethylsinensetin (1.5%) were isolated fromS. satureiifoliavar.satureiifoliaextract. Eupatorin and 5-desmethylsinensetin showed IC50values of 0.2 and 0.4 μg/mL onT. cruziepimastigotes and 61.8 and 75.1 μg/mL on trypomastigotes, respectively. The flavonoid 5-desmethylsinensetin showed moderate activity againstT. cruziamastigotes (IC50 value = 78.7 μg/mL) and was the most active compound onL. braziliensispromastigotes (IC50 value = 37.0 μg/mL). Neither of the flavonoids showed cytotoxicity on Vero cells, up to a concentration of 500 μg/mL. [ABSTRACT FROM PUBLISHER] |
| Databáze: |
Complementary Index |
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