Involvement of the CYP1A Subfamily in Stereoselective Metabolism of Carvedilol in β-Naphthoflavone-Treated Caco-2 Cells(Biopharmacy)
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概要
- 論文の詳細を見る
We have previously reported that the metabolism of S-carvedilol in β-naphthoflavone (β-NF)-treated Caco-2 cells is faster than that of R-carvedilol. The aim of the present study was to identify the enzyme responsible for the stereoselective metabolism of carvedilol in the cells. The expression of cytochrome P450 (CYP) 1A1 and CYP1A2 mRNA, but not CYP2D6, CYP3A4, and CYP2C9 mRNA, was increased in β-NF-treated Caco-2 cells, as compared with non-treated cells. Furafylline, an inhibitor of the CYP1A subfamily, decreased the metabolism of S-carvedilol in Caco-2 cells cultured on plastic dishes. In addition, the glucuronidation of carvedilol was not significant in microsomes of β-NF-treated Caco-2 cells. On the other hand, the oxidation of S-carvedilol in microsomes of β-NF-treated Caco-2 cells was faster than that of R-carvedilol, and furafylline decreased the oxidative activity of S-carvedilol. These findings suggested that the CYP1A subfamily was responsible for the stereoselective metabolism of carvedilol in β-NF-treated Caco-2 cells.
- 2009-03-01
著者
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Akao Teruaki
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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TAGUCHI Masato
Graduate School of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
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HASHIMOTO Yukiya
Graduate School of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
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Hashimoto Y
Graduate School Of Pharmaceutical Sciences Kyushu University
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Hashimoto Yuichi
Institute Of Molecular & Cellular Biosciences University Of Tokyo
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Harada Yuichi
Center For Influenza Virus Research National Institute Of Infectious Diseases
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Ishida Kazuya
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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Taguchi Masato
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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Hashimoto Yukiya
Graduate School Of Medicine And Pharmaceutical Sciences Univ. Of Toyama
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Hashimoto Y
Institute Of Molecular & Cellular Biosciences The University Of Tokyo
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Hashimoto Yuichi
Institute of Molecular & Cellular Biosciences, The University of Tokyo
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Akao Teruaki
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama
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Akao Teruaki
Graduate School of Medicine and Pharmaceutical Sciences
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