新型齐墩果酸衍生物的合成及其抗肿瘤活性

Synthesis and Anticancer Activities of Novel Oleanolic Acid Derivative

以齐墩果酸(1)为原料,经3-羟基乙酰化,17-位羧基甲酯化,11-位碳羰基化及光照反应,首次实现了1的10-位角甲基的活化,合成了新型的齐墩果酸衍生物———3β-乙酰氧基-11α-羟基-11,25-环-齐墩果-12-烯-28-酸甲酯(4),其结构经1H NMR,13C NMR,IR和MS表征。采用SRB法测试了1～4及1的衍生物7～9对N-04,Bre-04和Lu-04细胞株的体外抑制活性,结果表明,4,8和9具有明显的抑制肿瘤细胞生长的能力。

A novel oleanolic acid（1） derivative,methyl 3β-acetoxy-11α-hydroxy-11,25-cyclo-olean-12-en-28-oate（4）,was synthesized by acetylation of 3-hydroxyl,methyl-esterification of 17-carboxyl,carbonylation of C-11 and rradiation from 1.The structure was characterized by 1H NMR,13C NMR,IR and MS.The growth-inhibitory activities of 1~4 and derivatives（7~9） of 1 against N-04,Bre-04,and Lu-04 in vitro were determined by SRB assay.The results showed that 4,8 and 9 exhibited potent anti-tumor activities.