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ber碱是一种从几种草药中分离出来的生物活性生物碱，具有多种药理作用，包括抗微生物，抗糖尿病和抗癌活性。同时，小ber碱口服后会发生广泛的新陈代谢，这导致其血浆暴露极低。因此，认为小碱的代谢物也对其药理作用起很大作用。沿着这些思路，本文综述了黄连素的代谢途径和基于鉴定出的代谢物的代谢器官的代谢研究，还涵盖了其活性代谢物的药理活性。简言之，黄连的主要代谢途径是去甲基化，demethylenation，还原，羟基化和随后的共轭体内。与小ber碱相比，活性代谢产物如哥伦巴胺，小ber红素和脱甲基小ber碱也表现出相似的药理作用，例如抗氧化剂，抗炎，抗肿瘤，抗微生物，保肝，神经保护，降血脂和降血糖作用。总的来说，小ber碱及其代谢产物构成了体内小ber碱的物质基础。