齐墩果酸衍生物合成及抗肿瘤活性的研究

Synthesis and Anti-tumor Activity of Oleanolic Acid Derivatives

通过齐墩果酸氧化成3-氧代齐墩果酸,再与2,4-二硝基-苯肼反应合成了3-(2’,4’-二硝基)-苯腙齐墩果酸,采用MTT法测定了三个化合物体外抗肿瘤活性。方差分析的多重比较结果表明齐墩果酸及其衍生物对肺癌LTEP-α-2细胞均有抑制作用,3-氧代齐墩果酸的活性最高,其抑制率为90.0%,IC50为24.2μg·mL-1。

3-（2,4-dinitrophenyl）-hydrazone oleanolic acid was prepared by the hydrazonation of 2,4-dinitrophenylhydrazine and 3-oxo-olean-12-en-28-oic acid which was synthesized by the oxidation of oleanolic acid. The in vitro antitumor activity of the three compounds obtained was investigated by MTT assay. The results showed that all compounds had significant anti-tumor activity on lung adenoma cell line LTEP-α-2 by analyses of variances,in which 3-oxo-oleanolic acid had the highest activity,inhibition ratio （IR）and IC50 were 90.0%,24.2 μg·mL-1,respectively.