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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
Further Information

Publication History

received July 14, 2008 revised Dec. 19, 2008

accepted Dec. 25, 2008

Publication Date:
24 February 2009 (online)

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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

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Prof. Dr. Maysa Furlan

Institute of Chemistry
São Paulo State University

P.O Box. 355

14800–900 Araraquara SP

Brazil

Phone: + 55 16 33 01 66 78

Fax: + 55 16 33 22 79 32

Email: maysaf@iq.unesp.br