Synthesis of protopanaxadiol derivatives and evaluation of their anticancer activities.
Synthesis of protopanaxadiol derivatives and evaluation of their anticancer activities.
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DOI：
10.1097/cad.0b013e32833fde29
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发表时间：
2011-01
影响因子：
2.3
通讯作者：
Yuan CS
中科院分区：
文献类型：
--
作者：
Du GJ;Dai Q;Williams S;Wang CZ;Yuan CS
原人参二醇（PPD）是人参皂苷的一种苷元，在以前的研究中显示出抗癌活性。本文报道了9个含乙酰基取代的PPD衍生物的半合成。随后，研究了这9种类似物对不同人癌细胞系的抗增殖作用。化合物1和3与PPD和其他衍生物相比显示出更显著和更有效的抗增殖活性。流式细胞术分析表明，化合物1和3将细胞周期进程阻滞在G1期，并显著诱导癌细胞凋亡。
Protopanaxadiol (PPD), an aglycon of ginseng saponins, has shown anticancer activity in previous studies. Here we report the semi-synthesis of 9 PPD derivatives with acetyl substitutions. Subsequently, the antiproliferative effects of these 9 analogs on different human cancer cell lines were investigated. Compounds 1 and 3 showed more significant and more potent antiproliferative activity compared to PPD and other derivatives. A flow cytometric assay indicated that Compounds 1 and 3 arrested cell cycle progression in the G1 phase and significantly induced apoptosis of cancer cells.