四氢小檗碱衍生物的合成及活性研究现状  

Review of synthesis and activity of tetrahydroberberine derivatives

作　　者：王可心 王越 张华林 韩维娜[1] WANG Ke-xin;WANG Yue;ZHANG Hua-lin;HAN Wei-na(College of Pharmacy,Harbin Medical University,Harbin 150081,Heilongjiang Province,China)

机构地区：[1]哈尔滨医科大学药学院,黑龙江哈尔滨150081

出　　处：《中国临床药理学杂志》2021年第18期2520-2522,共3页The Chinese Journal of Clinical Pharmacology

基　　金：哈尔滨医科大学2019年双一流青苗破土经费基金资助项目(31021190046)。

摘　　要：四氢小檗碱为季铵型异喹啉类生物碱小檗碱的还原产物,具有抗菌、降糖、降血脂、抗心律失常等多种活性。同时四氢小檗碱不稳定,存在口服生物利用率低,靶向性不强等缺点,因此,针对四氢小檗碱进行结构改造的研究也越来越多。近年来四氢小檗碱的改造主要集中在9位、12位以及7位氮原子上,本文对四氢小檗碱及其衍生物的合成和活性研究进行综述。Tetrahydroberberine is the reduction product of quaternary ammonium isoquinoline alkaloid berberine,which has antibacterial,hypolipidemic,hypoglycemic,arrhythmia and other activities.Meanwhile,tetrahydroberberine is unstable,with low oral bioavailability and poor target.Therefore,there are more and more researches on the structural modification of tetrahydroberberine.In recent years,the modification of tetrahydroberberine is mainly focused on the 9,12,and 7-position nitrogen atom.In this paper,the synthesis and activity of tetrahydroberberine and its derivatives are reviewed.

关 键 词：四氢小檗碱衍生物 活性 合成路线 

分 类 号：R28[医药卫生—中药学]