Involvement of P4503A in the metabolism of 7,8-benzoflavone by human liver microsomes

H. S. Lee Doping Control Center, Korea Institute of Science and Technology, PO Box 131, Chungrayang, Seoul, Korea

C. B. Jin Doping Control Center, Korea Institute of Science and Technology, PO Box 131, Chungrayang, Seoul, Korea

H. S. Chong Doping Control Center, Korea Institute of Science and Technology, PO Box 131, Chungrayang, Seoul, Korea

C. H. Yun Department of Biochemistry, Pai-Chai University, Taejon, Korea

J. S. Park Doping Control Center, Korea Institute of Science and Technology, PO Box 131, Chungrayang, Seoul, Korea

D. H. Kim Doping Control Center, Korea Institute of Science and Technology, PO Box 131, Chungrayang, Seoul, Korea

Abstract

1. The metabolism of 7,8-benzoflavone (ANF) was studied in human liver microsomal fractions. Five metabolites were generated and tentatively identified as ANF 5,6-oxide, 5,6-dihydrodiol, 7,8-dihydrodiol, 6-hydroxy ANF, and 7-hydroxy ANF based on UV and mass spectral analysis.

2. The involvement of P4503A in the metabolism of ANF was confirmed by the following observations: (1) correlation of ANF 5,6-oxide formation was noted with testosterone 6β-hydroxylation, an indicator of P4503A, in human liver microsomal fractions; (2) metabolism of ANF was inhibited by various selective P4503A enzyme inhibitors; (3) rabbit antibody raised against P4503A4 inhibited the ANF metabolism by > 80%; and (4) microsomal fractions that specifically expressed P4503A4 metabolized ANF to oxidized metabolites.

3. These results indicate that P4503A isoform(s) mainly metabolize ANF to oxidized derivatives in human liver microsomal fractions.

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Involvement of P4503A in the metabolism of 7,8-benzoflavone by human liver microsomes

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Involvement of P4503A in the metabolism of 7,8-benzoflavone by human liver microsomes

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