Metabolism and Interaction of Bisphenol A in Human Hepatic Cytochrome P450 and Steroidogenic CYP17
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概要
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The metabolism of bisphenol A(BPA)was determined for 11 forms of human hepatic cytochromes P450(CYPs)expressed in the yeast Saccharomyces cerevisiae and for human steroidogenic CYP17 expressed in Escherichia coli. Additionally, the effect of BPA on the progesterone 17α-hydroxylase activity of CYP17 was investigated. CYP2C18 catalyzed BPA metabolism most efficiently, followed by CYP2C19 and CYP2C9. CYP2C9 and CYP2C18 exhibited the highest affinity(K_m=3.9μM)for BPA metabolism. The V_<max> of CYP2C18(8.10nmol・min^<-1>・nmol CYP^<-1>)was 5 times higher than that of CYP2C9. Although the V_<max> of CYP2C19 was 1.5 times higher than that of CYP2C18, the affinity of CYP2C19 was 12 times lower than that of CYP2C9 and CYP2C18. Therefore the intrinsic clearance(V_<max>/K_m)of CYP2C18 was more than 5 times higher than that of CYP2C9 and CYP2C19. On the other hand, BPA exhibited a competitive-type inhibition of the progesterone 17α-hydroxylase activity of CYP17 with a K_1 value of 71μM, whereas no metabolism of BPA by CYP17 was detected. These results suggest that BPA is mainly metabolized by the CYP2C subfamily in human liver, and that BPA inhibits human steroidogenic CYP17 activities.
- 公益社団法人日本薬学会の論文
- 2001-09-01
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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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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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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