积雪草酸的结构修饰与生物活性研究进展  

Advances in the study of structural modification and biological activities of asiatic acid

作　　者：刘斌[1,2] 唐文强 仝红娟 朱周静 唐初 LIU Bin;TANG Wen-qiang;TONG Hong-juan;ZHU Zhou-jing;TANG Chu(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;School of Life Science and Technology,Xidian University,Xi'an 710126,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 [3]西安电子科技大学生命科学技术学院,陕西西安710126

出　　处：《药学学报》2022年第7期1962-1976,共15页Acta Pharmaceutica Sinica

基　　金：陕西省自然科学基础研究计划项目(2021JM-540,2021JQ-885);陕西省中药绿色制造技术协同创新中心重点培育项目(2019XT-1-05);咸阳市分子影像与药物合成重点实验室项目(2021QXNL-PT-0008)。

摘　　要：积雪草酸是来自天然植物的乌苏烷型五环三萜,具有多种药理活性,例如抗肿瘤、降糖、抗炎、抗菌等。由于溶解性差、生物利用度低等限制了积雪草酸在临床上的广泛应用。为了克服这些缺点,学者们对其进行了大量的结构修饰与改造,发现了大量结构新颖、活性优良的积雪草酸衍生物。本文综述了积雪草酸近20年来的结构修饰、生物活性、构效关系及作用机制的相关研究进展,以期为积雪草酸类药物开发提供参考。Asiatic acid(AA)is a ursane pentacyclic triterpenoids,which possesses a wide range of pharmacological activities,such as anti-tumor,hypoglycemic,anti-inflammatory,anti-bacterial.Due to poor solubility and low bioavailability,clinical application of asiatic acid is limited.To address these defects,the structural modifications of AA have been carried out,and large numbers of AA-based derivatives with novel structure and eximious biological activity have been developed.In this paper,the research progress of structural modifications,biological activity,structure-activity relationship and mechanism studies in recent twenty years are reviewed,which provides reference for development of AA-related drugs.

关 键 词：积雪草酸 衍生物 结构修饰 生物活性 构效关系 

分 类 号：R914[医药卫生—药物化学]