积雪草酸衍生物的合成及其体外抗肿瘤活性研究

Synthesis and anti-tumor activity of novel asiatic acid derivatives in vitro

目的:设计并合成11个积雪草酸C2,3,23,28衍生物,并对其体外抗肿瘤活性进行测试。方法:以积雪草酸为先导化合物,对其C2,3,23及28位进行结构改造,合成11个积雪草酸衍生物。采用MTT法,选用高表达人癌细胞SGC-7901和A549,对目标化合物进行初步的体外抗肿瘤活性测试。结果:目标化合物对2种细胞株的抑制率均高于积雪草酸,其中化合物14和15的抗肿瘤活性与阳性对照紫杉醇相当。结论:经过结构改造后得到的积雪草酸衍生物具有一定的抗肿瘤活性,值得进一步研究。

Objective： To design and synthesize 11 asiatic acid derivatives,and to study their anti-tumor activities in vitro. Methods： Asiatic acid was used as starting material to synthesize eleven asiatic acid derivatives by structural modification at C-2,3,23 and C-28 carboxyl group. Their cytotoxicity in vitro against various cancer cell lines SGC-7901 and A549 was evaluated by MTT assay. Results： The target compounds were characterized by MS and1 H NMR. The results of experiments indicated that the inhibitory activities of asiatic acid derivatives were higher than those of asiatic acid in vitro. Compound 14 and 15 have similar anti-tumor activity to the positive control drug paclitaxel. Conclusion： The novel asiatic acid derivatives which were synthesized by structure modification have good anti-tumor activities,and are worthy further study.