小檗碱类生物碱的生物转化及其酶学机制  

Biotransformation and enzymatic mechanism of protoberberine alkaloids

作　　者：郑守豪 廖国建[1] 胡昌华[1] ZHENG Shou-hao;LIAO Guo-jian;HU Chang-hua(College of Pharmaceutical Sciences,Southwest University,Chongqing 400715,China)

机构地区：[1]西南大学药学院,重庆400715

出　　处：《中国中药杂志》2020年第24期5884-5889,共6页China Journal of Chinese Materia Medica

基　　金：国家重点研发计划项目(2017YFC170260103)。

摘　　要：小檗碱类生物碱是黄连等传统中草药中的主要活性成分,属于季铵型异喹啉类生物碱,被广泛应用于治疗胃肠炎、肠道感染和眼结膜炎等疾病。最近研究显示对小檗碱类生物碱进行结构改造可以产生具有新的药理作用和生物活性的衍生物,但转化机制尚未明确。该文总结了小檗碱类生物碱的生物转化及其酶学机制,为新结构新活性小檗碱类衍生物的开发提供研究基础和新的思路。Protoberberine alkaloids belong to the quaternary ammonium isoquinoline alkaloids,and are the main active ingredients in traditional Chinese herbal medicines,like Coptis chinensis.They have been widely used to treat such diseases as gastroenteritis,intestinal infections,and conjunctivitis.Studies have shown that structural modification of the protoberberine alkaloids could produce derivative compounds with new pharmacological effects and biological activities,but the transformation mechanism is not clear yet.This article mainly summarizes the researches on the biotransformation and structure modification of protoberberine alkaloids mainly based on berberine,so as to provide background basis and new ideas for studies relating to the mechanism of protoberberine alkaloids and the pharmacological activity and application of new compounds.

关 键 词：小檗碱 生物转化 肠道微生物 酶催化 GcvT 

分 类 号：R284[医药卫生—中药学]