细胞色素P450的立体选择S-oxidation负责flosequinan在大鼠肝微粒体和人类。
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横井Kashiyama E T, Odomi M, Funae Y,井上K, Kamataki T
细胞色素P450的立体选择S-oxidation负责flosequinan在大鼠肝微粒体和人类。
药物金属底座Dispos。1997年6月25日(6):716 - 24。
- PubMed ID
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9193873 (在PubMed]
- 文摘
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细胞色素P450的形式参与的立体选择S-oxidation flosequinan [(+ / -) 7-fluoro-1-methyl-3-methylsulfinyl-4-quinolone]研究了体外利用大鼠的肝微粒体和人类。大鼠肝微粒体补充NADPH催化四种不同S-oxidations,来自硫化flosequinan (FS;7-fluoro-1-methyl-3-methylthio-4-quinolone) R(+) -和S (-) -flosequinan(分别R-FSO和S-FSO)和从R-FSO和S-FSO flosequinan砜(FSO2;7-fluoro-1-methyl-3-methylsulfonyl-4-quinolone)。的活动从雄性大鼠肝微粒体中的所有S-oxidases高于雌性老鼠。S-oxidases测量的活动在一个较高的底物浓度(1毫米)与苯巴比妥治疗诱导的大鼠和地塞米松。治疗的老鼠3-methylcholanthrene也诱导活动,但只有低底物浓度(50 microM),除了S-oxidase催化的反应R-FSO FS。氯贝酸和乙醇引起的酶没有参与氧化反应底物浓度低。S-oxidases的活动的内容与细胞色素P450 (CYP) 3酶。Anti-CYP3A2抗血清抑制S-oxidases催化反应的活动从FS R-FSO(40%)和S-FSO(60%)的高底物浓度和抑制S-oxidases的活动,因此催化反应R-FSO和S-FSO FSO2(70%)在高、低底物浓度。 These results suggest that CYP3A is the major enzyme involved in all S-oxidation pathways in flosequinan metabolism in rats. On the other hand, except for the S-oxidation of FS to R-FSO, the rates of the other three S-oxidations by liver microsomes from 30 individual humans correlated highly with each other, suggesting that the same enzyme would be involved in the three S-oxidations. Anti-CYP3A2 antisera inhibited the activities of all the S-oxidases in human liver microsomes ranging from 40 to 80%, suggesting that CYP3A is also involved in all of the S-oxidations of flosequinan in humans.
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