小檗碱及药根碱在大鼠肝微粒体中的代谢转化研究  

Metabolic Transformation of Berberine and Jatrorrhizine in Rat Liver Microsomes

作　　者：杨岩涛[1,2,3,4] 杨岩 江欢英 李森[1,4] 刘金玲[1,4] 周晋 周逸群[1,3,4] 贺福元 YANG Yantao;YANG Yan;JIANG Huanying;LI Sen;LIU Jinling;ZHOU Jin;ZHOU Yiqun;HE Fuyuan(College of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China;State Key Laboratory of Bioactive Substance and Function of Natural Medicines & Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;Hunan Provincial Key Laboratory of Druggability and Preparation Modification of Traditional Chinese Medicine, Changsha, Hunan 410208, China;Laboratory for Supramolecular Mechanism and Mathematic-Physics Characterization for Chinese Materia Medica, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China)

机构地区：[1]湖南中医药大学药学院,湖南长沙410208 [2]天然药物活性物质与功能国家重点实验室中国医学科学院北京协和医学院药物研究所,北京100050 [3]中药成药性与制剂制备湖南省重点实验室,湖南长沙410208 [4]湖南中医药大学中医药超分子机理与数理特征化实验室,湖南长沙410208

出　　处：《湖南中医药大学学报》2019年第3期326-330,共5页Journal of Hunan University of Chinese Medicine

基　　金：天然药物活性物质与功能国家重点实验室开放课题(GTZK201607);湖南省教育厅优秀青年基金(2015B172);湖南省中医药科研基金(201494);湖南省"十二五"省级药学重点学科(1007)开放基金

摘　　要：目的进行小檗碱和药根碱在大鼠肝微粒体中的代谢转化研究,尝试给中药有效成分的体外和体内关联研究提供一定的参考。方法制备大鼠肝微粒体,用Brad ford法测定酶活性,以此配制大鼠肝微粒体体外温孵体系,加入药物温孵,用质谱进行检测测定并比较小檗碱、药根碱代谢产物图谱。结果检测到小檗碱经大鼠肝微粒体代谢后产物中有药根碱,药根碱经大鼠肝微粒体代谢后产物中有巴马汀,但小檗碱代谢产物中未见巴马汀。结论小檗碱和药根碱是同母核生物碱,在肝微粒体中孵化可相互影响,但体外代谢无法简单关联体内代谢过程。Objective To investigate the metabolic transformation of berberine and jatrorrhizine in rat liver microsomes, and to provide a reference for the in vitro and in vivo association studies of active constituents in traditional Chinese medicine (TCM).Methods The rat liver microsome was prepared, and the enzymatic activity was determined by Brad ford method to prepare the in vitro incubation system of rat liver microsomes.After the incubation in the presence of berberine and jatrorrhizine, mass spectrometry was used to detect and compare the metabolites of berberine and jatrorrhizine.Results After the metabolic transformation in rat liver microsomes, jatrorrhizine was one of the metabolites of berberine;palmatine was one of the metabolites of jatrorrhizine, but not of berberine.Conclusion Berberine and jatrorrhizine are from the same parent alkaloid and they can affect each other during the incubation in liver microsomes.However, the in vitro metabolism cannot be associated with the in vivo metabolism.

关 键 词：小檗碱 药根碱 肝微粒体 代谢转化 代谢物 

分 类 号：R393[医药卫生—基础医学] R285.5