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重组CYP3A46细胞微粒体体外药物代谢动力学分析

In vitro analysis on pharmacokinetics by microsomes from recombinant CYP3A46 cell lines
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摘要 通过对巴马小型猪CYP3A46重组细胞微粒体体外药物代谢动力学特征比较分析,为巴马小型猪应用于临床前药理试验提供科学依据。分析重组CYP3A4、CYP3A46细胞微粒体药物代谢动力学参数Vmax、Km(S50)、Clint及IC50均表明:CYP3A46的硝苯地平、睾酮的代谢活性及酮康唑的抑制活性均比较接近CYP3A4(P>0.05),CYP3A46是否是CYP3A4的同源酶需要进一步研究确定。 The objective was to provide a scientific basis for the use of Bama miniature pig as a clinlical experimental animal by comparatively analyzing pharmacokinetic parameters of microsomes from stably expressing recombinant cell lines human CYP3A4 and Sus scrofa CYP3A46-Bama. The results demonstrated that the metabolic activities of microsomes from recombiant cell lines CYP3A46 to nifedipine and testosterone were very close to that of CYP3A4 based on the analysis of pharmacokinefic parameters Vmax, Km（S50） and Clint, so were the inhibitory activities of ketoconazole to CYP3A46 and CYP3A46 based on IC50S. Further researches should do to determine whether human CYPSA4 and Sus scrofa CYPSA46 were homologous enzymes.
作者 薛正楷 魏弘
机构地区 泸州职业技术学院生物医学工程研究所 第三军医大学基础医学院实验动物中心
出处 《广东农业科学》 CAS CSCD 北大核心 2014年第7期124-129,共6页 Guangdong Agricultural Sciences
基金 国家"十五"科技攻关计划重点项目(2004BA717B 23)
关键词 重组细胞 微粒体 人CYP3A4 小型猪CYP3A46 药物代谢 recombinant cell line microsomes human CYP3A4 Sus scrofa CYP3A46 drug metabolism
分类号 S571.1 [农业科学—茶叶生产加工] Q946-33 [生物学—植物学]
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参考文献19

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广东农业科学
2014年 第7期

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