齐墩果酸和甘草次酸衍生物的合成与表征及抗癌活性研究

Synthesis of oleanolic acid and glycyrrhetinic acid derivatives and the study of anti-cancer activities

齐墩果酸和甘草次酸属于五环三萜类化合物,在自然界中分布广泛并显示出多种生物活性,如保肝、抗炎、抗菌、抗病毒等多种药理作用,并具有良好的抗癌活性.首先以齐墩果酸和甘草次酸为先导化合物,对其结构进行了修饰,共合成了15种中间体和最终产物,利用IR和1H NMR波谱技术对其结构进行了表征.然后对部分化合物进行了人宫颈癌细胞(Hela)和人乳腺癌细胞(MCF—7)体外抗肿瘤活性测试.结果显示,2个化合物抑制癌细胞的活性优于先导化合物.

Oleanolic acid and glycyrrhetinic acid belong to pentacyclic triterpenoid of natural products.They widely distributed in nature and show many bioactivities such as protect liver,anti-inflammatory,antibacterial,antiviral pharmacological.They also have good anti-cancer activity.So oleanolic acid and glycyrrhetinic acid were took as the lead compounds for modifying their structures in this paper.Fifteen kinds of intermediates and final products were synthesized through modification of oleanolic acid and glycyrrhetinic acid.These compounds were characterized by IR and 1H NMR techniques.The anti-cancer activity of some compounds were investigated against human cervical cancer cells（Hela） and human breast cancer cells（MCF—7）.The results showed that the inhibit activities of two compounds are more significantl than lead compounds.