Liu Songcan, Zhang Xinfeng, Qiu Furong, Miao Ping, Shen Shujiao, Zhu Leilei, Zeng Jin, Jiang Jian
Department of Clinical Pharmacology, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Evid Based Complement Alternat Med. 2015;2015:802903. doi: 10.1155/2015/802903. Epub 2015 Jan 6.
Coptis chinensis is commonly used in traditional Chinese medicine. The study investigated metabolic interaction of the active constituents (berberine, coptisine, palmatine, and jatrorrhizine) of Coptis chinensis in human liver microsomes. After incubation of the four constituents of Coptis chinensis in HLMs, the metabolism of the four constituents was observed by HPLC. The in vitro inhibition experiment between the active constituents was conducted, and IC50 value was estimated. Coptisine exhibited inhibitions against the formation of the two metabolites of berberine with IC50 values of 6.5 and 8.3 μM, respectively. Palmatine and jatrorrhizine showed the weaker inhibitory effect on the formation of the metabolites of berberine. Berberine showed a weak inhibitory effect on the production of coptisine metabolite with an IC50 value of 115 μM, and palmatine and jatrorrhizine had little inhibitory effect on the formation of coptisine metabolite. Berberine, coptisine, and jatrorrhizine showed no inhibitory effect on the generation of palmatine metabolite (IC50 > 200 μM). The findings suggested that there are different degrees of metabolic interaction between the four components. Coptisine showed the strongest inhibition toward berberine metabolism.
黄连常用于传统中药。该研究调查了黄连活性成分（小檗碱、黄连碱、巴马汀和药根碱）在人肝微粒体中的代谢相互作用。在人肝微粒体中孵育黄连的四种成分后，通过高效液相色谱法观察这四种成分的代谢情况。进行了活性成分之间的体外抑制实验，并估算了半数抑制浓度（IC50）值。黄连碱对小檗碱的两种代谢产物的形成表现出抑制作用，IC50值分别为6.5和8.3 μM。巴马汀和药根碱对小檗碱代谢产物的形成表现出较弱的抑制作用。小檗碱对黄连碱代谢产物的产生表现出较弱的抑制作用，IC50值为115 μM，而巴马汀和药根碱对黄连碱代谢产物的形成几乎没有抑制作用。小檗碱、黄连碱和药根碱对巴马汀代谢产物的生成没有抑制作用（IC50>200 μM）。研究结果表明，这四种成分之间存在不同程度的代谢相互作用。黄连碱对小檗碱代谢的抑制作用最强。
