Inhibition of Drug-Metabolizing Enzyme Activity in Human Hepatic Cytochrome P450s by Bisphenol A
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概要
- 論文の詳細を見る
Effect of bisphenol A on drug-metabolizing enzyme activities by human hepatic cytochrome P450s (CYP) was investigated. We measured aminopyrine N-demethylation by eleven kinds of cDNA-expressed CYPs. CYP2C19 and CYP2B6 catalyzed most efficiently the aminopyring N-demethylation, followed by CYP2C8 and CYP2D6. Bisphenol A (1 mM) most efficiently inhibited aminopyrine N-demethylation by CYP2C8 and CYP2C19 by 82% and 85%, respectively, whereas inhibition of the activities by CYP 2B6 and 2D6 was less than 40%. Bisphenol A exhibited a noncompetitive-type inhibition of aminopyrine N-demethylase activity by CYP2C8 with K_i value of 97 μM. Additionally, we investigated the inhibitory effect of bisphenol A on CYP2C19-mediated S-mephenytoin 4-hydroxylation. Bisphenol A exhibited a mixed-type inhibition with K_i value of 113 μM. These results suggest that bisphenol A inhibits human hepatic CYP activities, especially CYP2C8 and CYP2C19.
- 公益社団法人日本薬学会の論文
- 2000-04-01
著者
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Niwa T
近畿大学 薬学部
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Tsutsui Miki
Division Of Natural Science Osaka Kyoiku University
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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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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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ISHIBASHI Fumihide
Division of Natural Science, Osaka Kyouiku University
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Niwa Toshiro
Post Marketing Product Development Astellas Pharma Inc.
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Tsutsui Miki
Division Of Applied Chemistry In Bioscience Department Of Agrobioscience Graduate School Of Agricult
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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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