目的 设计并合成积雪草酸C₂、C₃、C₂₃、C₂₈衍生物,并对其体外抗肿瘤活性进行研究.方法 以天然产物积雪草酸为先导化合物,对C₂、C₃、C₂₃位羟基及C₂₈位羧基进行结构改造,并采用SRB法对目标化合物进行初步的体外抗肿瘤活性研究.结果 设计并合成了目标化合物,利用MS及¹H-NMR确证了结构;体外实验中,积雪草酸衍生物的抗肿瘤活性明显高于积雪草酸,并优于对照药吉非替尼.结论 积雪草酸衍生物具有良好的抗肿瘤活性,值得进一步研究.

Objective To design and synthesize asiatic acid C₂, C₃, C₂₃, and C₂₈ derivatives, and to study their antitumor activities in vitro. Methods Asiatic acid was used as starting material to synthesize the target compounds by structural modification at C₂, C₃, and C₂₃ hydroxyl groups, and C₂₈ carboxyl group. The antitumor activities of the compounds were tested by SRB assay. Results The target compounds were synthesized and characterized by MS and ¹H- NMR. The in vitro antitumor activity experiments showed that the antitumor activity of asiatic acid derivatives were higher than those of asiatic acid in vitro, and were better than control drug gefitinib. Conclusion Asiatic acid derivatives have good antitumor activities which could be a valuable candidate for further development.

国家自然科学基金资助项目(21372156);辽宁省教育厅高等学校优秀人才支持计划资助项目(LR2013017);沈阳市科技计划资助项目(F13-316-1-47)