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

• Luize Patrícia Shima

  Mestranda do Programa de Pós-graduação em Ciências Farmacêuticas

• Ueda-Nakamura Tânia

  Laboratório de Microbiologia Aplicada aos Produtos Naturais e Sintéticos, Departamento de Análises Clínicas

• Filho Benedito Prado Dias

  Laboratório de Microbiologia Aplicada aos Produtos Naturais e Sintéticos, Departamento de Análises Clínicas

• Cortez Diógenes Aparício Garcia

  Laboratório de Farmacognosia, Departamento de Farmácia e Farmacologia, Universidade Estadual de Maringá

• Nakamura Celso Vataru

  Laboratório de Microbiologia Aplicada aos Produtos Naturais e Sintéticos, Departamento de Análises Clínicas

抄録

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-, ¹³C-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 (IC₅₀) of 7.0, 7.5, and 8.0 μg/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.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 29 (10), 2126-2130, 2006

  公益社団法人 日本薬学会

キーワード

• anti-trypanosoma
• neolignan
• <i>Piper regnellii</i>
• <i>Trypanosoma cruzi</i>

詳細情報

• CRID: 1390001204625494912
• NII論文ID: 110004810305
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.29.2126
• ISSN: 13475215
• ISSN: 09186158
• NDL書誌ID: 8064351
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I8064351
• Web Site: http://www.jstage.jst.go.jp/article/bpb/29/10/29_10_2126/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2007074338
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可