小檗碱的结构修饰及其构效关系研究进展  

Advances in structural modification and structure-activity relationship of berberine

作　　者：吴龙龙 方方 WU Long-long;FANG Fang(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China;Department of Medicinal Chemistry,Anhui Academy of Chinese Medicine,Hefei 230012,China)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]安徽省中医药科学院药物化学研究所,合肥230012

出　　处：《中国新药杂志》2020年第11期1257-1264,共8页Chinese Journal of New Drugs

基　　金：安徽省高等学校自然科学研究重点项目(KJ2019A1004);安徽省高校优秀青年人才支持计划重点项目(gxyqZD2016129)。

摘　　要：小檗碱是从我国传统中药黄连和黄柏中提取出的一种季铵型异喹啉生物碱,具有抗菌、消炎、抗肿瘤、降血糖、降血脂等多种药理活性。对其结构进行修饰改造可以改变其理化性质并提高生物学活性,显著提高临床疗效,扩大应用范围。本文综述了近年有关小檗碱的结构修饰研究,重在介绍其分子结构中N7,C8,C9,C12和C13位点的结构修饰方法以及相关药效活性的变化,旨在为进一步深入探索小檗碱的构效关系和创新药物研究提供参考。Berberine is one of the quaternary ammonium isoquinoline alkaloids extracted from the traditional Chinese medicine such as Coptis and Phellodendron.It has many pharmacological activities such as anti-bacterial,anti-inflammatory,anti-tumor,hypoglycemic and hypolipidemic.Modification of its structure changes its physical and chemical properties,improves the biological activity,thus significantly improves clinical efficacy and expands the scope of application.This review summarizes the recent studies on the structural modifications of berberine,focusing on the structural modification methods on N7,C8,C9,C12 and C13 sites of its molecular structure and the changes in related pharmacodynamic activities.The aim is to provide a reference for further exploration of the structureactivity relationship of berberine and the research of innovative drugs.

关 键 词：小檗碱 结构修饰 药理活性 构效关系 

分 类 号：R914[医药卫生—药物化学] R975[医药卫生—药学]