| 采用重组人源CYP酶研究艾瑞昔布的体外羟基化代谢 |
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| 引用本文： | 李强,黄海华,董宇,钟大放. 采用重组人源CYP酶研究艾瑞昔布的体外羟基化代谢[J]. 药学学报, 2005, 0(5) |
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| 作者姓名： | 李强 黄海华 董宇 钟大放 |
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| 作者单位： | 吉林大学生命科学学院 吉林长春130023(李强)，沈阳药科大学微生物学教研室 辽宁沈阳110016(黄海华)，沈阳药科大学药物代谢与药物动力学实验室 辽宁沈阳110016(董宇)，沈阳药科大学药物代谢与药物动力学实验室 辽宁沈阳110016(钟大放) |
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| 基金项目： | 国家高技术研究发展计划 ( 863 计划 )课题(2003AA2Z347C). |
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| 摘 要： | 目的 探讨新型抗炎镇痛药艾瑞昔布在人体内的羟基化代谢酶。方法 用体外重组的人源细胞色素P450(CYP)进行孵育代谢实验,液相色谱多级质谱法分析代谢产物和残留的母体药物,利用整体归一化法对4种CYP酶的代谢作用大小进行评估。结果 艾瑞昔布羟基化代谢可由CYP2C9,CYP2D6和CYP3A4催化,其各自作用大小分别为62.5%, 21.1%和16.4%。结论 CYP2C9为艾瑞昔布羟基化的主要代谢酶。
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| 关 键 词： | 细胞色素P450 羟基化代谢 艾瑞昔布 液相色谱多级质谱法 整体归一化 |
Investigation on the hydroxylation metabolism of imrecoxib in vitro by using recombinant human CYPs |
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| LI Qiang. Investigation on the hydroxylation metabolism of imrecoxib in vitro by using recombinant human CYPs[J]. Acta pharmaceutica Sinica, 2005, 0(5) |
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| Authors: | LI Qiang |
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| Abstract: | Aim To identify the drug-metabolizing enzymes involved in the hydroxylation of the new anti-inflammatory and anodyne imrecoxib. Methods Imrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vitro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method. Results Imrecoxib is metabolized by CYP2C9, CYP2D6 and CYP3A4, with the rate of 62.5%, 21.1% and 16.4%, respectively. Conclusion CYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism. |
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| Keywords: | cytochrome P450 hydroxylation metabolism imrecoxib liquid chromatography-multistage mass spectrometry total normalized rate |
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