He Lan, Liu Yumei, Shi Jiangong, Pei Qiang
Department of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Steroids. 2006 Jun;71(6):476-83. doi: 10.1016/j.steroids.2006.01.006. Epub 2006 Feb 28.
Cholest-4 alpha-methyl-7-en-3beta-ol (1) has potent inhibitory activity against pc 12 tumor with 0.5043 ratio (10 microg/mL). This paper describes a series of structural modification of this compound, which focus on 3beta-hydroxyl group and 7(8)-double bond. The synthesized derivatives of 1 were tested for human cancer cell lines including colon cancer (HCT-8), liver cancer (BEL-7402) and nasopharyngeal cancer (KB) cells. The results showed that cholest-4 alpha-methyl-8-en-3beta,7 alpha-diol 6a inhibits KB cell significantly with IC(50) 1.32 x 10(-9)microg/mL. In addition, the cytotoxic properties of this compound against HCT-8 and BEL-7402 are excellent with IC(50) 1.2 microg/mL.
胆甾-4α-甲基-7-烯-3β-醇（1）对PC12肿瘤具有强大的抑制活性，抑制率为0.5043（10微克/毫升）。本文描述了该化合物的一系列结构修饰，重点是3β-羟基和7（8）-双键。对1的合成衍生物进行了针对包括结肠癌细胞（HCT-8）、肝癌细胞（BEL-7402）和鼻咽癌细胞（KB）在内的人类癌细胞系的测试。结果表明，胆甾-4α-甲基-8-烯-3β，7α-二醇6a对KB细胞有显著抑制作用，IC50为1.32×10-9微克/毫升。此外，该化合物对HCT-8和BEL-7402的细胞毒性特性优异，IC50为1.2微克/毫升。
