Tanii, Hiromi and Shitara, Yoshihisa and Torii, Mikako and Sekine, Shuichi and Iwata, Hiroshi and Horie, Toshiharu (2013) Induction of Cytochrome P450 2A6 by Bilirubin in Human Hepatocytes. Pharmacology & Pharmacy, 04 (02). pp. 182-190. ISSN 2157-9423
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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.
Item Type: | Article |
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Subjects: | East India Archive > Chemical Science |
Depositing User: | Unnamed user with email support@eastindiaarchive.com |
Date Deposited: | 01 Mar 2023 07:30 |
Last Modified: | 29 Jul 2024 11:20 |
URI: | http://ebooks.keeplibrary.com/id/eprint/401 |