齐墩果酸的结构修饰研究进展  

Research progress in structural modification of oleanolic acid

作　　者：杨晓凤[1] 赵梅梅 高艳蓉 杜漠 YANG Xiao-feng;ZHAO Mei-mei;GAO Yan-rong;DU Mo(School of Pharmacy,Shaanxi Institute of International Trade&Commerce,Xianyang 712046,China;Collaborative Innovation Center of Green Manufacturing Technology for Traditional Chinese Medicine in Shaanxi Province,Xianyang 712046,China)

机构地区：[1]陕西国际商贸学院医药学院,陕西咸阳712046 [2]陕西省中药绿色制造技术协同创新中心,陕西咸阳712046

出　　处：《精细与专用化学品》2024年第10期42-44,54,共4页Fine and Specialty Chemicals

基　　金：陕西省大学生创新创业训练计划资助项目(S202013123049);陕西国际商贸学院校级资助项目(SMXY202123);咸阳市分子影像与药物合成重点实验室项目(2021QXNL-PT-0008)。

摘　　要：齐墩果酸是一种重要的天然产物,具有降糖、抗菌及抗肿瘤等多方面药理活性,但存在水溶性低、药理活性较弱以及生物利用度低等问题。针对这些问题,通常采用化学结构修饰的方法对其进行改进,从而改变其理化性质,进而改变生物活性,达到优化其临床应用的目的。重点介绍了在抗肿瘤研究领域,齐墩果酸的结构修饰研究进展,主要包括针对齐墩果酸结构中C-3位羟基、C-28位羧基和A环的结构修饰方法,并对其应用前景进行了展望,期望为齐墩果酸类抗肿瘤药物分子的开发提供参考。Oleanolic acid is an important natural product with many pharmacological activities, such as hypoglycemic, antibacterial and anti-tumor, but there are some problems such as low water-solubility, weak pharmacological activity and low bioavailability.To solve these problems, chemical methods were used to modify the structure to improve the physical and chemical properties, enhance the pharmacological activity, so as to improve the clinical application value.The progress of structural modification of oleanolic acid in the field of anti-tumor research was introduced, including the modification methods of C-3 hydroxyl group, C-28 carboxyl group and A ring, the prospect of its application was put forward, and it was expected to provide reference for the development of anti-tumor drugs of oleanolic acid.

关 键 词：齐墩果酸 抗肿瘤活性 结构修饰 研究进展 

分 类 号：TQ463[化学工程—制药化工]