积雪草酸衍生物的合成与表征及其抗肿瘤活性研究

Synthesis and Characterization of Asiatic Acid Derivatives and Its Anti-tumor Activities

以积雪草酸为原料,对其C-2,C-3,C-23和C-28位基团进行结构修饰,设计并合成3类共10个化合物,并经IR、M S、1H NM R确证其结构.采用M TT法研究部分积雪草酸衍生物对人胃腺癌细胞株SGC-7901,人非小细胞肺癌细胞株A549和人成纤维肉瘤细胞株HT-1080的体外细胞毒活性.结果显示:化合物AA-Ⅲ2的IC50值较小,对上述3种细胞有较好的抑制作用,值得进一步研究.

Natural active product is an important source of anti-cancer drugs. Through C-2,C-3,C-23 and C-28 for structural modification,three types of ten newcompounds of asiatic acid derivatives were designed and synthesized. The target compounds were not reported,and confirmed its structure by IR,MS,1H NMR. Anti-tumor activities of asiatic acid and these derivatives against SGC-7901,A549 and HT-1080 cells in vitro were investigated by MTT assay. The results indicated that compound AA-III2 had stronger cell growth inhibitor than other products. It is worth to be intensively further studies.