1. In vitro trypanocidal activity of phenolic derivatives from Peperomia obtusifolia.
- Author
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da Silva Mota J, Leite AC, Batista Junior JM, Noelí López S, Luz Ambrósio D, Duó Passerini G, Kato MJ, da Silva Bolzani V, Barretto Cicarelli RM, and Furlan M
- Subjects
- Animals, Chromans isolation & purification, Life Cycle Stages, Macrophages drug effects, Mice, Molecular Structure, Nitroimidazoles pharmacology, Phenols isolation & purification, Plant Extracts chemistry, Plant Leaves, Plant Stems, Trypanocidal Agents isolation & purification, Chromans pharmacology, Peperomia chemistry, Phenols pharmacology, Plant Extracts pharmacology, Trypanocidal Agents pharmacology, Trypanosoma cruzi drug effects
- Abstract
The trypanocidal activity of crude extracts and fractions from the leaves and stems of Peperomia obtusifolia (Piperaceae) was evaluated in vitro against the epimastigote forms of Trypanosoma cruzi. Bioactivity-guided fractionation of the most active extracts afforded seven known compounds, including three chromanes, two furofuran lignans and two flavone C-diglycosides. The most active compounds were the chromanes peperobtusin A and 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid, with IC (50) values of 3.1 microM (almost three times more active than the positive control benznidazole, IC (50) 10.4 microM) and 27.0 microM, respectively. Cytotoxicity assays using peritoneal murine macrophages indicated that the chromanes were not toxic at the level of the IC (50) for trypanocidal activity. This is the first report on the trypanocidal activity besides unspecific cytotoxicity of chromanes from Peperomia species. Additionally it represents the first time isolation of 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid from P. obtusifolia., (Copyright Georg Thieme Verlag KG Stuttgart. New York.)
- Published
- 2009
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