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来自印度楝树的新型抗锥虫四环三萜类化合物。

New antitrypanosomal tetranotriterpenoids from Azadirachta indica.

作者信息

Githua Mercy, Hassanali Ahmed, Keriko Joseph, Murilla Grace, Ndungu Mary, Nyagah Gathu

机构信息

Department of Chemistry, Jomo Kenyatta University of Agriculture and Technology, Nairobi, Kenya.

出版信息

Afr J Tradit Complement Altern Med. 2010 Apr 3;7(3):207-13. doi: 10.4314/ajtcam.v7i3.54776.

Abstract

Organic extracts of the leaves of Azadirachta indica A. Juss. yielded ten antitrypanosomal terpenoids. Three of these (1-3), are novel and are derivatives of nimbolide and nimbin. They were extracted from chloroform fraction of methanol extract. These compounds were found to exhibit strong antitrypanosomal activities against Trypanosoma brucei rhodesiense with MIC values ranging of 6.9, 15.6 and 7.8 µg/ml respectively and were more active than Cymerlarsan (a standard drug), which had an MIC value of 187.5 µg/ml when tested against T. b. rhodesiense. The structures were elucidated by spectroscopic methods including; NMR, MS, UV and IR.

摘要

印楝(Azadirachta indica A. Juss.)叶的有机提取物产生了十种抗锥虫萜类化合物。其中三种(1-3)是新的,是印楝二酮和印楝素的衍生物。它们是从甲醇提取物的氯仿馏分中提取的。发现这些化合物对布氏罗得西亚锥虫表现出很强的抗锥虫活性,MIC值分别为6.9、15.6和7.8μg/ml,并且比赛美拉胂(一种标准药物)更具活性,赛美拉胂在针对布氏罗得西亚锥虫进行测试时的MIC值为187.5μg/ml。通过包括核磁共振(NMR)、质谱(MS)、紫外光谱(UV)和红外光谱(IR)在内的光谱方法阐明了其结构。

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