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

Ken Ichiro Taura, Eri Naito, Yuji Ishii, Masa Aki Mori, Kazuta Oguri, Hideyuki Yamada

研究成果: ジャーナルへの寄稿学術誌査読

25 被引用数 (Scopus)

抄録

The effects of cytochrome P450 (P450, CYP) ligands and permeabilization of microsomes on 3-hydroxybenzo(a)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.

本文言語英語
ページ(範囲)56-60
ページ数5
ジャーナルBiological and Pharmaceutical Bulletin
27
1
DOI
出版ステータス出版済み - 1月 2004

!!!All Science Journal Classification (ASJC) codes

  • 薬理学
  • 薬科学

フィンガープリント

「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」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

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