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W. Xie, M. F. Yeuh, A. Radominska-Pandya, S. P. Saini, Y. Negishi, B. S.Bottroff, G. Y. Cabrera, R. H. Tukey and R. M. Evans, “Control of Steroid, Heme, and Carcinogen Metabolism by Nuclear Pregnane X Receptor and Constitutive Androstane Receptor,” Proceedings of the National Academy of Sciences of the United States of America, Vol. 100, No. 7, 2003, pp. 4150-4155. doi:10.1073/pnas.0438010100

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• TITLE: Induction of Cytochrome P450 2A6 by Bilirubin in Human Hepatocytes

  AUTHORS: Hiromi Tanii, Yoshihisa Shitara, Mikako Torii, Shuichi Sekine, Hiroshi Iwata, Toshiharu Horie

  KEYWORDS: CYP2A6; Hepatocytes; Hyperbilirubinemia; RT-PCR

  JOURNAL NAME: Pharmacology & Pharmacy, Vol.4 No.2, April 15, 2013

  ABSTRACT: The influence of bilirubin on mRNA expression of cytochrome P450 (CYP), UDP-glucuronosyltransferase (UGT) and nuclear receptors in human hepatocytes was investigated. The treatment of the hepatocytes with 40 μg/mL bilirubin, which corresponds to hyperbilirubinemia, resulted in 1.7-fold increase of CYP2A6 mRNA compared to the vehicle control while CYP2A6 mRNA did not change after treatment with 1 μg/mL bilirubin, corresponding to physiologically normal level. No significant change of mRNA expression by 40 μg/mL bilirubin treatment was observed for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and CYP3A5, UGT1A1, UGT1A3, UGT1A6, UGT2B4, UGT2B7, UGT2B10 and UGT2B15, constitutive androstane receptor (CAR), pregnane X receptor (PXR), retinoid X receptor α (RXRα) and hepatocyte nuclear factor-4α (HNF-4α). The induction profile of bilirubin was different from that of rifampicin, a typical PXR activator. This study demonstrated that CYP2A6 can be induced by bilirubin in a concentration dependent manner.