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三萜酸的抗锥虫活性和急性毒性评价。

Trypanocidal activity and acute toxicity assessment of triterpene acids.

机构信息

Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil.

出版信息

Parasitol Res. 2010 Mar;106(4):985-9. doi: 10.1007/s00436-010-1740-2. Epub 2010 Feb 6.

Abstract

The present study evaluates the in vitro and in vivo trypanocidal activity of ursolic acid and oleanolic acid against the Bolivia strain of Trypanosoma cruzi. Their acute toxicity is also assessed on the basis of median lethal dose (DL50) determination and quantification of biochemical parameters. Ursolic acid is the most active compound in vitro, furnishing IC50 of 25.5 microM and displaying 77% of trypomastigote lysis at a concentration of 128 microM. In agreement with in vitro assays, the results obtained for the in vivo assay reveals that ursolic acid (at a dose of 20 mg/Kg/day) provides the most significant reduction in the number of parasites at the parasitemic peak. Results concerning the LD50 assay and the biochemical parameters evaluated in the present study demonstrate that these substances can be safely used on an experimental basis.

摘要

本研究评估了熊果酸和齐墩果酸对玻利维亚株克氏锥虫的体外和体内杀锥虫活性。还根据半数致死剂量 (DL50) 测定和生化参数定量评估了它们的急性毒性。熊果酸是体外最活跃的化合物,提供了 25.5 μM 的 IC50,在 128 μM 的浓度下显示出 77%的锥虫体溶解。与体外测定结果一致,体内测定结果表明,熊果酸(剂量为 20mg/Kg/天)在寄生虫高峰期可显著减少寄生虫数量。关于 LD50 测定和本研究中评估的生化参数的结果表明,这些物质可以在实验基础上安全使用。

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