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H. H. Gerets, K. Tilmant, B. Gerin, H. Chanteux, B. O. Depelchin, S. Dhalluin and F. A. Atienzar, “Characterization of Primary Human Hepatocytes, HepG2 Cells, and HepaRG Cells at the mRNA Level and CYP Activity in Response to Inducers and Their Predictivity for the Detection of Human Hepatotoxins,” Cell Biology & Toxicology, Vol. 28, No. 2, 2012, pp. 69-87. doi:10.1007/s10565-011-9208-4

has been cited by the following article:

• 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.