Inhibition of Human Hepatic Cytochrome P450s and Steroidogenic CYP17 by Nonylphenol
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概要
- 論文の詳細を見る
Effect of nonylphenol on aminopyrine N-demethylase activity, a typical drug-metabolizing enzyme activity, by ten kinds of human hepatic cytochrome P450s(CYP)and on progesterone 17α-hydroxylase activity by steroidogenic CYP17 was investigated. When determined at 2 mM substrate concentration, nonylphenol(1mM)most efficiently inhibited aminopyrine N-demethylation by CYP2C9 and CYP2C19, by 61% and 59%, respectively, followed by CYP2D6, CYP1A2, CYP2C18 and CYP2C8(46-51%), whereas inhibition of the activities by other CYPs was less than 27%. Additionally, nonylphcnol competitively inhibited diclofenac 4'-hydroxylation by CYP2C9 and S-mephenytoin 4'-hydroxylation by CYP2C19 with K_i values of 5.3 and 37μM, respectively. Furthermore, nonylphenol exhibited a competitive inhibition of progesterone 17α-hydroxylase activity by CYP17 with K_i value of 62 μM. These results suggest that nonylphenol inhibits human hepatie CYPs, especially CYP2C9 and CYP2C19, and steroidogenic CYP17 activities.
- 公益社団法人日本薬学会の論文
- 2002-02-01
著者
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Niwa T
近畿大学 薬学部
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Yoshida Yuzo
School Of Pharmaceutical Sciences Mukogawa Women's University
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Yoshida Y
Biotechnology Laboratory Sumitomo Chemical Co. Ltd.
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Yoshida Y
Tokyo Metropolitan Inst. Of Medical Sci. Tokyo
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Yabusaki Y
Sumitomo Chemical Co. Ltd. Hyogo Jpn
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Yabusaki Yoshiyasu
Biotechnology Laboratory Sumitomo Chemical Co. Ltd.
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Fuji Masahiro
Shionogi Research Laboratories Shionogi & Co. Ltd.
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KISHIMOTO Kae
Biotechnology Laboratory, Sumitomo Chemical Co., Ltd.
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Niwa T
Post-marketing Development Research Center Fujisawa Pharmaceutical Co. Ltd.
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Kishimoto Kae
Biotechnology Laboratory Sumitomo Chemical Co. Ltd.
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KATAGIRI Masanao
Division of Natural Science, Osaka Kyoiku University
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NIWA Toshiro
Division of Natural Science, Osaka Kyoiku University
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MAEKAWA Yyumi
Division of Natural Science, Osaka Kyoiku University
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FUJIMOTO Megumi
Division of Natural Science, Osaka Kyouiku University
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ISHIBASHI Fumihide
Division of Natural Science, Osaka Kyouiku University
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Fujimoto M
Division Of Natural Science Osaka Kyouiku University
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Maekawa Yyumi
Division Of Natural Science Osaka Kyoiku University
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Niwa Toshiro
Post Marketing Product Development Astellas Pharma Inc.
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Ishibashi Fumihide
Division Of Natural Science Osaka Kyouiku University
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Katagiri M
Osaka Kyoiku Univ. Osaka Jpn
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Katagiri Masanao
Division Of Natural Science Osaka Kyoiku University
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Maekawa Yumi
Division of Natural Science, Osaka Kyoiku University
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