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n vitro Antileishmanial Activity of Hydroalcoholic Extract, Fractions, and Compounds Isolated from Leaves of Piper ovatum Vahl against Leishmania amazonensis

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RODRIGUES-SILVA D., NAKAMURA C. V., DIAS FILHO B. P., UEDA-NAKAMURA T., CORTEZ D. A. G.

Acta Protozoologica

2009

vol. 48

issue 1

We assessed the biological activity of a crude extract, a mixture of several fractions, and a pure compound obtained from Piper ovatum Vahl against promastigote and amastigote forms of Leishmania amazonensis. The medicinal plant P. ovatum is used popularly as an anesthetic and anti-inflammatory. This study included the extraction process and bioassay-guided fractionation by the adsorption chromatography and Sephadex LH-20 method. A progressive increase in the antileishmanial effect was observed in the course of fractionation. The 50% inhibitory concentration (IC50) for dichloromethane-ethyl acetate (1:1 v/v) fraction was 2.1 μg/ml and 24 μg/ml; mixture of piperovatine: piperlongumune (2:3) 0.9 μg/ml and 24 μg/ml; piperovatine (1) 9.5 μg/ml and 10 μg/ml; and piperlonguminine (2) 2.5 μg/ml and 9.0 μg/ml, for promastigote and amastigote forms, respectively. Cytotoxicity analysis indicated that these toxic concentrations were much higher for J774G8 macrophages and Vero cells than for the protozoans. The mixture of piperovatine: piperlongumune (2:3) showed important antiprotozoal activity against the amastigote and promastigote forms of L. amazonensis, and it produced morphological changes in promastigotes and amastigotes at 0.9 μg/ml and 24 μg/ml (50% growth inhibition concentration), respectively, including intense cytoplasmic vacuolization, mitochondrial swelling, and mitochondrial damage, as revealed by transmission electron microscopy.

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1 Acta Protozoologica

1 2009

1 CORTEZ D. A. G.

1 DIAS FILHO B. P.

1 NAKAMURA C. V.

1 RODRIGUES-SILVA D.

1 UEDA-NAKAMURA T.

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n vitro Antileishmanial Activity of Hydroalcoholic Extract, Fractions, and Compounds Isolated from Leaves of Piper ovatum Vahl against Leishmania amazonensis