Wang Kun, Feng Xinchi, Chai Liwei, Cao Shijie, Qiu Feng
a School of Chinese Materia Medica , Tianjin University of Traditional Chinese Medicine , Tianjin , P.R. China.
b Tianjin State Key Laboratory of Modern Chinese Medicine , Tianjin University of Traditional Chinese Medicine , Tianjin , P.R. China.
Drug Metab Rev. 2017 May;49(2):139-157. doi: 10.1080/03602532.2017.1306544. Epub 2017 Apr 3.
Berberine, a bioactive alkaloid isolated from several herbal substances, possesses multiple pharmacological effects, including antimicrobial, antidiabetic, anticancer activities. Meanwhile, berberine undergoes extensive metabolism after oral administration which results in its extremely low plasma exposure. Therefore, it is believed that the metabolites of berberine also contribute a lot to its pharmacological effects. Along these lines, this review covers the metabolism studies of berberine in terms of its metabolic pathways and metabolic organs based on the identified metabolites, and it also covers the pharmacological activities of its active metabolites. In brief, the predominant metabolic pathways of berberine are demethylation, demethylenation, reduction, hydroxylation and subsequent conjugation in vivo. Active metabolites such as columbamine, berberrubine and demethyleneberberine also exhibit similar pharmacological effects by comparison with berberine, such as antioxidant, anti-inflammatory, antitumor, antimicrobial, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic effects. Overall, berberine together with its metabolites formed the material basis of berberine in vivo.
小檗碱是一种从多种草药中分离出的生物活性生物碱，具有多种药理作用，包括抗菌、抗糖尿病、抗癌活性。同时，小檗碱口服后会经历广泛的代谢，导致其血浆暴露量极低。因此，人们认为小檗碱的代谢产物对其药理作用也有很大贡献。基于这些，本综述根据已鉴定的代谢产物，从小檗碱的代谢途径和代谢器官方面涵盖了小檗碱的代谢研究，还涵盖了其活性代谢产物的药理活性。简而言之，小檗碱在体内的主要代谢途径是去甲基化、去亚甲基化、还原、羟基化以及随后的结合反应。与小檗碱相比，如黄连碱、小檗红碱和去亚甲基小檗碱等活性代谢产物也表现出类似的药理作用，如抗氧化、抗炎、抗肿瘤、抗菌、肝脏保护、神经保护、降血脂和降血糖作用。总体而言，小檗碱及其代谢产物共同构成了小檗碱在体内的物质基础。
