刺囊酸在不同种属肝微粒体中代谢消除和酶动力学的比较研究  

Comparative Study on Metabolic Elimination and Enzyme Kinetics of Echinocystic Acid in Liver Microsomes of Different Species

作　　者：陈瑞 朱高峰 姜云芳 CHEN Rui;ZHU Gao-feng;JIANG Yun-fang(Guizhou Provincial Engineering Research Center for R&D and Utilization of Chemical Synthetic Drugs,Guizhou Guiyang 550004;School of Basic Medical Sciences,Guizhou Medical University,Guizhou Guiyang 550004;School of Medicine and Health Management,Guizhou Medical University,Guizhou Guiyang 550004,China)

机构地区：[1]贵州省化学合成药物研发利用工程技术研究中心,贵州贵阳550004 [2]贵州医科大学基础医学院,贵州贵阳550004 [3]贵州医科大学医药卫生管理学院,贵州贵阳550004

出　　处：《广州化工》2022年第18期79-82,共4页GuangZhou Chemical Industry

基　　金：贵州省科技计划项目(黔科合支撑[2020]4Y234);贵州省卫生计生委科学技术基金项目(gzwjkj2023-511)。

摘　　要：建立测定肝微粒体孵育体系中刺囊酸的方法,并比较其在不同种属肝微粒体(大鼠、比格犬、人)中的代谢消除速率。使用NADPH将不同种属肝微粒体在孵育体系中进行激活。孵育60 min后,刺囊酸在大鼠、比格犬、人肝微粒体中的平均剩余浓度百分比的比率为44.65%、99.25%、99.73%。大鼠肝微粒体中的刺囊酸的代谢稳定性比在人和比格犬肝微粒体中的代谢稳定性差。本研究建立的HPLC测定方法简便,快速,灵敏度高,可应用于体外生物代谢稳定性的相关研究。A method for the determination of echinocystic acid in the incubation system of liver microsomes was established,and its metabolic elimination rate in different species of liver microsomes(rat,beagle,human)was compared.Different species of liver microsomes were activated in an incubation system using NADPH.After 60 min incubation,the ratios of the mean residual concentration percentages of echinocystic acid in rat,beagle and human liver microsomes were 44.65%,99.25%and 99.73%.The metabolic stability of echinocystic acid in rat liver microsomes was poorer than that in human and beagle dog liver microsomes.HPLC assay method was simple,rapid and highly sensitive,which can be applied to the related research of biological metabolism stability in vitro.

关 键 词：刺囊酸 肝微粒体 不同种属 酶动力学 

分 类 号：R979.1[医药卫生—药品]