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基于重组HepG2-P4503A4与HepG2-P4503A46全细胞体外药物代谢比较研究
Comparison of the Drug Metabolic Characteristics of Recombinant Cell Lines HepG2-P4503A4 and HepG2-P4503A46 on Whole Cell Level
薛正楷1,罗祎2,魏泓3
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DOI:
作者单位:(1. 泸州职业技术学院酿酒与生物医学工程研究所,四川泸州646005; 2. 重庆医科大学附属第一医院妇产科,重庆 400016;3.第三军医大学实验动物中心,重庆 400038)
中文关键字:细胞色素P4503A4;细胞色素P4503A46;全细胞;药物代谢
英文关键字:cytochromeP4503A4; cytochromeP4503A46; whole cell; drug metabolism
中文摘要:本研究以探针药物硝苯地平(NF)、睾酮(TST)及其抑制剂酮康唑(KCZ)与重组HepG2-P4503A4HepG2-P4503A46细胞全细胞在优化的重组细胞浓度、药物浓度、孵育时间等条件下进行体外孵育,通过高效液相色谱仪检测其药物代谢(抑制)动力学参数,并将二者进行比较分析。重组HepG2-P4503A46HepG2-P4503A4细胞的硝苯地平、睾酮的代谢活性无显著差异(P0.05);在010 μM的浓度范围内,酮康唑对硝苯地平和睾酮的抑制活性均随酮康唑浓度的增加而增加,且其IC50值均低于1 μM,为nM级,表明酮康唑对二者的硝苯地平代谢具有较强的抑制活性,抑制剂酮康唑对重组HepG2-P4503A46HepG2-P4503A4细胞的抑制活性差异不显著(P0.05)。本研究表明无论是底物代谢或底物抑制活性,重组HepG2-P4503A46细胞均与重组HepG2-P4503A4细胞差异不显著,P4503A46可能为巴马小型猪体内人P4503A4的同源酶。
英文摘要:The probe drugs nifedipine(NF), testosterone(TST) and ketoconazole (KCZ) were incubated with whole cells from the recombinant cell lines of HepG2-P4503A4 and HepG2-P4503A46 in optimal conditions. High performance liquid chromatograph (HPLC) was employed to analyze the metabolites and metabolic characteristics after the incubation was ended. The results showed that there were no significant differences of the metabolic activities of nifedipine and testosterone (P0.05) between HepG2-P4503A4 and HepG2-P4503A46; the inhibitory activities of ketoconazole to recombinant cell HepG2-P4503A4 and HepG2-P4503A46 were elevated along with the increasing of the concentration (010 μM) of ketoconazole, and the IC50 values for nifedipine and testosterone were low to nM level, this suggested that ketoconazole had a strong inhibitory effect on both substrates and no significant difference was observed. HepG2-P4503A46 had no significant difference on the substrate metabolic activities and inhibitory activities to HepG2-P4503A4. 
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国内统一连续出版物号:51-1193/Q |国际标准出版物号:1000-7083
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