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薯蓣皂苷元对A375、K562等细胞株具有抑制生长并诱导其凋亡的作用。其作用靶点之一是线粒体中的Bcl-2亚家族蛋白。本文以Bcl-2为靶点,运用Autodock设计并合成了一系列全新的薯蓣皂苷元衍生物,希望完善相关化合物的构效关系及提高其抗肿瘤活性。MTT法体外抗肿瘤活性研究结果表明,所设计的化合物大多对K562、A375、A549等3种肿瘤细胞株有较好的抑制作用,而对H293、L02等2种正常细胞株无明显作用。其中,化合物1、6～8对K562表现出了较好的活性(IC50值为1.96～4.35μmol.L-1)。
Diosgenin on A375, K562 and other cell lines have inhibited the growth and induce apoptosis. One of its targets is the Bcl-2 subfamily protein in mitochondria. In this paper, Bcl-2 as a target, the use of Autodock design and synthesis of a new series of diosgenin derivatives hope to improve the structure-activity relationship of related compounds and improve their anti-tumor activity. The results of in vitro antitumor activity assay by MTT assay showed that most of the designed compounds had good inhibitory effect on the three tumor cell lines such as K562, A375 and A549, but had no effect on the two normal cell lines such as H293 and L02. Among them, compounds 1,6-8 showed good activity on K562 (IC50 value 1.96 ~ 4.35μmol.L-1).