Conversion of chenodeoxycholic acid to cholic acid by human CYP8B1

Author:

Fan Linbing1,Joseph Jan Felix23,Durairaj Pradeepraj1,Parr Maria Kristina2,Bureik Matthias1

Affiliation:

1. School of Pharmaceutical Science and Technology, Health Sciences Platform , Tianjin University , Tianjin 30072 , China

2. Freie Universitaet Berlin, Institute of Pharmacy , Pharmaceutical and Medicinal Chemistry (Pharmaceutical Analyses) , Berlin , Germany

3. Freie Universitaet Berlin , Department of Biology, Chemistry, Pharmacy, Core Facility BioSupraMol , Berlin , Germany

Abstract

Abstract The human cytochrome P450 enzyme CYP8B1 is a crucial regulator of the balance of cholic acid (CA) and chenodeoxycholic acid (CDCA) in the liver. It was previously shown to catalyze the conversion of 7α-hydroxycholest-4-en-3-one, a CDCA precursor, to 7α,12α-dihydroxycholest-4-en-3-one, which is an intermediate of CA biosynthesis. In this study we demonstrate that CYP8B1 can also convert CDCA itself to CA. We also show that five derivatives of luciferin are metabolized by CYP8B1 and established a rapid and convenient inhibitor test system. In this way we were able to identify four new CYP8B1 inhibitors, which are aminobenzotriazole, exemestane, ketoconazole and letrozole.

Publisher

Walter de Gruyter GmbH

Subject

Clinical Biochemistry,Molecular Biology,Biochemistry

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