Synthesis of plumbagin derivatives and their inhibitory activities against Ehrlich ascites carcinoma in vivo and Leishmania donovani promastigotes in vitro
Synthesis of plumbagin derivatives and their inhibitory activities against Ehrlich ascites carcinoma in vivo and Leishmania donovani promastigotes in vitro
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DOI：
10.1002/ptr.867
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发表时间：
2002-03-01
影响因子：
7.2
通讯作者：
Dinda, B
中科院分区：
文献类型：
--
作者：
Hazra, B;Sarkar, R;Dinda, B
首次将植物来源的具有生物活性的萘醌类化合物转化为氢醌类化合物，并对其抗肿瘤和抗利什曼活性进行了研究。对类似的二聚体化合物Diospyrin进行了类似的化学转化，并将其生物测定结果与白花蛇舌草素衍生物的结果进行了比较。白花蛇舌草素衍生物的合成并未使其抑瘤活性显著增强，但与其氢醌类似物相比，皂苷的抑瘤活性明显增强。皂苷转化为对苯二酚类化合物也导致了抗利什曼活性的显著增加，而类似的白花蛇毒转化则未能做到这一点。版权所有(C)2002 John Wiley Sons，Ltd.
Plumbagin, a plant-derived bioactive naphthoquinonoid compound, was converted to a hydroquinonoid derivative, which was studied for its tumour-inhibitory and antileishmanial activities for the first time. A similar chemical transformation was undertaken on an analogous dimeric compound, diospyrin, and its bioassay results were compared with those of the plumbagin derivative. Synthesis of the derivative of plumbagin did not result in a marked enhancement of the tumour-inhibitory activity, whereas the improvement was obvious in the case of diospyrin vis a vis its hydroquinonoid analogue. The conversion of diospyrin to the hydroquinonoid compound also led to a substantial increase in the antileishmanial activity, while a similar conversion of plumbagin failed to do so. Copyright (C) 2002 John Wiley Sons, Ltd.