%0 Journal Article
%T Induction of Cytochrome P450 2A6 by Bilirubin in Human Hepatocytes
%A Hiromi Tanii
%A Yoshihisa Shitara
%A Mikako Torii
%A Shuichi Sekine
%A Hiroshi Iwata
%A Toshiharu Horie
%J Pharmacology & Pharmacy
%P 182-190
%@ 2157-9431
%D 2013
%I Scientific Research Publishing
%R 10.4236/pp.2013.42026
%X <span><span style=\"font-family:Verdana;\">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 ¦Ìg/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 ¦Ìg/mL bilirubin, corresponding to physiologically normal level. No significant change of mRNA expression by 40 ¦Ìg/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 </span><i><span style=\"font-family:Verdana;\">¦Á</span></i><span style=\"font-family:Verdana;\"> (RXR</span><i><span style=\"font-family:Verdana;\">¦Á</span></i><span style=\"font-family:Verdana;\">) and hepatocyte nuclear factor-4</span><i><span style=\"font-family:Verdana;\">¦Á</span></i><span style=\"font-family:Verdana;\"> (HNF-4</span><i><span style=\"font-family:Verdana;\">¦Á</span></i><span style=\"font-family:Verdana;\">). 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.</span></span><span></span>
%K CYP2A6
%K Hepatocytes
%K Hyperbilirubinemia
%K RT-PCR
%U http://www.scirp.org/journal/PaperInformation.aspx?PaperID=29747