In vitro Trypanocidal Activity of Phenolic Derivatives from Peperomia obtusifolia

Jonas da Silva Mota; Ana Cristina Leite; João Marcos Batista Junior; Silvia Noelí López; Daniela Luz Ambrósio; Gabriela Duó Passerini; Massuo Jorge Kato; Vanderlan da Silva Bolzani; Regina Maria Barretto Cicarelli; Maysa Furlan

doi:10.1055/s-0029-1185364

Planta Medica, Table of Contents

Planta Med 2009; 75(6): 620-623
DOI: 10.1055/s-0029-1185364

Pharmacology

Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

In vitro Trypanocidal Activity of Phenolic Derivatives from Peperomia obtusifolia

Jonas da Silva Mota¹ , Ana Cristina Leite² , João Marcos Batista Junior² , Silvia Noelí López² , Daniela Luz Ambrósio³ , Gabriela Duó Passerini³ , Massuo Jorge Kato⁴ , Vanderlan da Silva Bolzani² , Regina Maria Barretto Cicarelli³ , Maysa Furlan²

¹Institute of Chemistry, Mato Grossodo Sul State University, Dourados, MS, Brazil
²Institute of Chemistry, São Paulo State University, Araraquara, SP, Brazil
³School of Pharmaceutical Sciences, São Paulo State University, Araraquara, SP, Brazil
⁴Institute of Chemistry, University of São Paulo, São Paulo, SP, Brazil

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)-2H-1-benzopyran-6-carboxylic acid, with IC₅₀ values of 3.1 µM (almost three times more active than the positive control benznidazole, IC₅₀ 10.4 µM) and 27.0 µM, respectively. Cytotoxicity assays using peritoneal murine macrophages indicated that the chromanes were not toxic at the level of the IC₅₀ 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)-2H-1-benzopyran-6-carboxylic acid from P. obtusifolia.

Key words

chromanes - Peperomia obtusifolia - Piperaceae - Trypanosoma cruzi

Full Text

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Prof. Dr. Maysa Furlan

Institute of Chemistry
São Paulo State University

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