Abstract:
: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 17alpha-chydroxylase activity of CYP17 was investigated. CYP2C18 catalyzed BPA metabolism most efficiently, followed by CYP2C19 and CYP2C9. CYP2C9 and CYP2C18 exhibited the highest affinity (Km=3.9 microM) for BPA metabolism. The Vmax of CYP2C18 (8.10 nmol x min(-1) x nmol CYP(-1)) was 5 times higher than that of CYP2C9. Although the Vmax 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 (Vmax/Km) 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 17alpha-hydroxylase activity of CYP17 with a Ki value of 71 microM, 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.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Niwa T,Fujimoto M,Kishimoto K,Yabusaki Y,Ishibashi F,Katagiri Mdoi
10.1248/bpb.24.1064subject
Has Abstractpub_date
2001-09-01 00:00:00pages
1064-7issue
9eissn
0918-6158issn
1347-5215journal_volume
24pub_type
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2017-01-01 00:00:00
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