Activity of Neolignans Isolated from Piper regnellii (MIQ.) C. DC. var. pallescens (C. DC.) YUNCK against Trypanosoma cruzi(Pharmacognosy)

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概要

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• The in vitro antiproliferative effects of 4 neolignans purified from the ethyl-acetate extract from leaves of Piper regnellii (MIQ.) C. DC. var. pallescens (C. DC.) YUNCK against Trypanosoma cruzi were investigated. These isolated compounds were identified through spectral analyses of UV, EI-MS, ^1H-, ^<13>C-NMR, H-H COSY, gNOE, HETCOR, and HMBC. The compounds eupomatenoid-5, eupomatenoid-6, and conocarpan showed considerable activity against epimastigote forms of T. cruzi, with 50% inhibition concentrations (IC_<50>) of 7.0, 7.5, and 8.0μg/ml respectively. After methylation, these compounds showed a lessened inhibitory activity to the growth of the protozoan, suggesting that loss of the hydroxyl group from their molecules reduces the activity. The compound eupomatenoid-3 showed lower activity than the hexane fraction. Eupomatenoid-5 was significantly more active than benznidazole, the antiparasitic drug of choice for treatment of Chagas' disease. The crude extract, hexane fraction, and eupomatenoid-5 caused no lysis in sheep blood at concentrations which inhibit the growth of epimastigote forms. The compound eupomatenoid-5 showed low cytotoxic effects against Vero cells. These results provide new perspectives on the development of novel drugs obtained from natural products with trypanocidal activity. However, the extracts and active compound isolated from P. regnellii var. pallescens should be further studied in animal models for in vivo efficacy.

• 2006-10-01

著者

• Filho Benedito

  Programa De Pos-graduacao Em Ciencias Farmaceuticas Universidade Estadual De Maringa

• LUIZE Patricia

  Mestranda do Programa de Pos-graduacao em Ciencias Farmaceuticas

• UEDA-NAKAMURA Tania

  Laboratorio de Microbiologia Aplicada aos Produtos Naturals e Sinteticos, Departamento de Analises C

• FILHO Benedito

  Laboratorio de Microbiologia Aplicada aos Produtos Naturals e Sinteticos, Departamento de Analises C

• CORTEZ Diogenes

  Laboratorio de Farmacognosia, Departamento de Farmacia e Farmacologia, Universidade Estadual de Mari

• NAKAMURA Celso

  Laboratorio de Microbiologia Aplicada aos Produtos Naturals e Sinteticos, Departamento de Analises C

• CORTEZ Diogenes

  Programa de Pos-graduacao em Ciencias Farmaceuticas, Universidade Estadual de Maringa

• NAKAMURA Celso

  Programa de Pos-graduacao em Ciencias Farmaceuticas, Universidade Estadual de Maringa

• Cortez Diogenes

  Programa De Pos-graduacao Em Ciencias Farmaceuticas Universidade Estadual De Maringa

• Ueda-nakamura Tania

  ブラジル

• Nakamura Celso

  Programa De Pos-graduacao Em Ciencias Farmaceuticas Universidade Estadual De Maringa

• Filho Benedito

  Laboratorio De Fisiologia E Bioquimica De Microrganismos-centro De Biociencias E Biotecnologia-unive

関連論文

• Activity of Neolignans Isolated from Piper regnellii (MIQ.) C. DC. var. pallescens (C. DC.) YUNCK against Trypanosoma cruzi(Pharmacognosy)
• Antileishmanial activity of Eugenol-rich essential oil from Ocimum gratissimum
• Structural Changes at the Site of Tritrichomonas foetus-Erythrocyte Interaction
• Antileishmanial activity of a guaianolide from Tanacetum parthenium (L.) Schultz Bip
• Evaluation of antileishmanial activity of eupomatenoid-5, a compound isolated from leaves of Piper regnellii var. pallescens

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