Isolation of antileishmanial sterol from the fruits of Cassia fistula using bioguided fractionation
Isolation of antileishmanial sterol from the fruits of Cassia fistula using bioguided fractionation
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DOI：
10.1002/ptr.2131
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发表时间：
2007-07-01
影响因子：
7.2
通讯作者：
Tempone, Andre G.
中科院分区：
文献类型：
--
作者：
Sartorelli, Patricia;Andrade, Samanta P.;Tempone, Andre G.
天然产品是开发被忽视疾病药物的新化学实体的丰富来源。利什曼病仍然困扰着世界上最贫穷的人口，全世界有1 200万病例。这项工作分析了决明子果实的粗提取物和馏分对利什曼病最引人注目和致命的疾病形式，内脏形式（VL）。果实正己烷提取物对利什曼原虫前鞭毛体表现出显著的抗利什曼原虫活性。查加斯。该超临界分级分离导致分离出甾醇，即麦角甾醇，其在不同的模型中进一步分析。前鞭毛体的半数抑制浓度（IC 50）为10.03 μ g/mL，细胞内无鞭毛体表现出高敏感性，IC 50为18.10 μ g/mL。对哺乳动物细胞毒性进行了评价，结果表明，clerosterol的毒性比标准药物喷他脒低3.6倍。未发现该化合物的抗真菌活性，对该化合物的进一步研究可能为开发新的VL治疗药物提供有用的工具。版权所有（C）2007约翰威利父子有限公司
Natural products represent a rich source of new chemical entities for the development of drugs for neglected diseases. Leishmaniasis still afflicts the poorest populations in the world, with 12 million cases worldwide. This work analysed crude extracts and fractions from the fruits of Cassia fistula against the most dramatic and fatal disease form of leishmaniasis, the visceral form (VL). Hexane extract from the fruits showed significant antileishmanial activity against the promastigote form of Leishmania L. chagasi. The bioguided fractionation resulted in the isolation of a sterol, clerosterol, which was further analysed in different models. Promastigotes presented an inhibitory concentration 50% (IC50) of 10.03 mu g/mL and intracellular amastigotes demonstrated high susceptibility, with an IC50 of 18.10 mu g/mL. Mammalian cytotoxicity was evaluated and it was demonstrated that clerosterol was 3.6-fold less toxic than the standard drug pentamidine. No antifungal activity of the isolated clerosterol was found. Future studies of the extracted compounds of Cassia fistula could be a useful tool for the development of new therapeutic agents for VL. Copyright (C) 2007 John Wiley & Sons, Ltd.