Cytochrome P450 1A1 (CYP1A1) Inhibitor α-Naphthoflavone Interferes with UDP-Glucuronosyltransferase (UGT) Activity in Intact but Not in Permeabilized Hepatic Microsomes from 3-Methylcholanthrene-Treated Rats : Possible Involvement of UGT-P450 Interactions
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概要
- 論文の詳細を見る
The effects of cytochrome P450 (P450, CYP) ligands and permeabilization of microsomes on 3-hydroxybenzo(α)pyrene [3-OH-B(a)P] glucuronidation mediated by rat hepatic microsomes were studied. While the UDP-glucuronosyltransferase (UGT) activity with non-permeabilized microsomes from 3-methylcholanthrene (MC)-treated rats was markedly reduced by α-naphthoflavone (NF), this inhibitor had hardly any effect when permeabilized microsomes were used in which the inhibitor was expected to have easy access to UGT. Kinetic analysis indicated that the inhibitory effect of α-NF is competitive. These results suggest that a UGT isoform(s) involved in 3-OH-B(a)P glucuronidation is interfered by a CYP1A inhibitor via a mechanism dependent on the intact nature of microsomal membranes in MC-treated rats. It is likely that P450 functions as a substrate transporter for some isoforms of UGT via possible interactions between UGT and P450.
- 公益社団法人日本薬学会の論文
- 2004-01-01
著者
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Ishii Yuji
Graduate School of Pharmaceutical Sciences, Kyushu University
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Yamada Hideyuki
Graduate School of Pharmaceutical Sciences, Kyushu University
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Ishii Yuji
Graduate School Of Pharmaceutical Sciences Kyushu Univ.
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Ishii Yuji
九州大学 薬学研究院
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Ishii Y
Graduate School Of Pharmaceutical Sciences Kyushu University
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OGURI Kazuta
School of Pharmaceutical Sciences, Kyushu University of Health and Welfare
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Oguri K
School Of Pharmaceutical Sciences Kyushu University Of Health And Welfare
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Ishii Yukimoto
Department Of Surgery Nihon University School Of Medicine
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Naito Eri
Graduate School of Pharmaceutical Sciences, Kyushu University
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TAURA Ken-ichiro
Graduate School of Pharmaceutical Sciences, Kyushu University
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MORI Masa-aki
Department of Health Sciences, School of Medicine, Kyushu University
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Oguri Kazuta
School Of Pharmaceutical Sciences Kyushu University Of Health And Welfare
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Oguri K
Faculty Of Pharmaceutical Sciences Kyushu University
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Oguri K
Kyushu Univ. Fukuoka Jpn
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Naito Eri
Graduate School Of Pharmaceutical Sciences Kyushu University
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Ishii Yuri
Central Research Laboratory Fancl Corporation
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Mori Masa-aki
Department Of Health Sciences School Of Medicine Kyushu University
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Yamada Hideyuki
Graduate School Of Pharmaceutical Sciences Kyushu University
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Yamada H
Faculty Of Pharmaceutical Sciences Kyushu University
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Yamada H
Graduate School Of Pharmaceutical Sciences Kyushu University
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Yamada Hideyuki
Graduate School Of Engineering Osaka Prefecture University
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Taura Ken-ichiro
Graduate School Of Pharmaceutical Sciences Kyushu University
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Yoshimura Hidetoshi
Department Of Food And Nutrition Nakamura Gakuen
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Oguri Kazuta
Faculty Of Pharmaceutical Sciences Kyushu University:(present Address)laboratory Of Safety Assessment Panapharm Laboratories Co. Ltd.:(present Address)department Of Food And Nutrition Nakamura Gakuen College
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