小檗碱体内药代动力学及药理活性研究进展

Research Progress on the Pharmacokinetics and Pharmacological Activities of Berberine

小檗碱是黄连、黄柏等中药材的主要活性成分之一,属于单苄异喹啉类季铵型生物碱,具有抗菌、消炎、抗心律失常、降血脂、降血糖以及抗肿瘤等多种药理活性。但小檗碱的口服生物利用度低,存在原形成分体内暴露水平与药效不相关的问题,提示小檗碱进入体内后可能产生了其他一些具有活性的代谢产物。因此,该文围绕小檗碱体内药物代谢、药物动力学及药理活性研究进展进行综述,有助于对小檗碱体内物质基础及药理活性有一概貌性的了解。

Berberine is one of the main active components of Coptis chinensis Franch,Phellodendron amurense Rupr and other traditional Chinese herbal medicines,which belongs to mono-benzylisoquinoline quaternary ammonium alkaloids. It possesses anti-bacterial,anti-inflammatory,anti-arrhythmic,hypolipidemic,hypoglycemic and anti-tumor activities. However,the fact,namely the low oral bioavailability of berberine and uncorrelation between its in vivo the exposure level and the efficacy,suggests that berberine may produce some other active metabolites after exposed to the body. Therefore,this paper aims to review the drug metabolism and pharmacokinetics in vivo and pharmacological activities of berberine. It is hoped that this review could contribute to a general understanding of the material basis and pharmacological activities of berberine in vivo.