小檗碱是从中草药黄连等植物中提取分离得到的一类异喹啉类生物碱。近十年来,已经有2 000多篇国 内外文献报道了小檗碱及其衍生物在治疗肿瘤、糖尿病、心血管疾病、高血脂、炎症、细菌和病毒感染、脑缺血性损 伤、精神疾病、阿尔茨海默病(Alzheimer disease) 、骨质疏松等多方面的临床应用、药效机制以及该类化合物的构效关 系等研究结果。这些结果表明小檗碱生理功能广泛,潜在的结构改造和开发应用价值很大,但还未见系统的回顾和 综述。本文对这些文献进行了系统地分析整理,主要从临床应用与药效机制、分子药理、体内吸收代谢、构效关系四 个方面来介绍小檗碱及其衍生物的研究进展,旨在为进一步深入开展以药效机制为基础的小檗碱结构改造和创新 药物研究提供比较系统的信息。
Berberine is a isoquinoline alkaloid extracted from Chinese herbs such as Coptidis rh izom e. In the past decade, there are more than 2 000 published papers studying the clinical app lication, pharmacodynamic mechanism and structure2activity relationship ( SAR) of berberine and its derivatives, for treating tumor, diabetes, cardiavascellum disease, hyperlipemia, inflammation, bacterium and virus infection, cerebral ischemia trauma, mental disease, Alzheimer disease, osteoporosis, and so on. These results demonstrate that berberine has wide physiologic function and has great potential for structural modification as new drug lead. However, there is no systematic review about the study of berberine and its derivatives up to now. This paper is a systematic review of the research advances of berberine and its derevatives in clinical app lication, pharmacodynamic mechanisms, molecular pharmacology, absorp tion and metabolism, and SAR studies. The current review would p rovide some useful information for further study on structuralmodification of berberine for discovering new drug leads based on its pharmacodynamic mechanisms.