作者: Nobumitsu Hanioka , Hiroyuki Iwabu , Hiroyuki Hanafusa , Shintaro Nakada , Shizuo Narimatsu
DOI: 10.1111/J.1742-7843.2011.00790.X
关键词:
摘要: Abstract: UDP-glucuronosyltransferases (UGTs) are conjugation enzymes, which regulated in a tissue-specific manner by endogenous and environmental factors. In this study, we focused on UGT1A isoforms broadly expressed hepatic extrahepatic tissues examined the expression inducibility of UGT1As (UGT1A1 UGT1A3–1A10) MCF-7 cells (human breast carcinoma cell line). Reverse transcription polymerase chain reaction (RT-PCR) analysis demonstrated that UGT1A1, UGT1A6 UGT1A9 mRNAs as well transcriptional regulators (AhR, aryl hydrocarbon receptor; Arnt, AhR nuclear translocator; ERα, oestrogen receptor α; ERβ, β; GR, glucocorticoid receptor) cells. mRNA level was significantly increased to 1.9 times β-naphthoflavone (BNF), whereas UGT1A1 levels were not affected BNF. There no significant changes treatment with phenobarbital (PB) dexamethasone (DEX) The kinetics 7-ethyl-10-hydroxycamptothecin (SN-38), 5-hydroxytryptamine (5-HT) 4-methylumbelliferone (4-MU) glucuronidation microsomes from control BNF-treated fitted Michaelis–Menten model, Vmax CLint values 7.5–8.5 5.9–10.4 BNF treatment, respectively. These findings suggest induces increase may be mediated but pregnane X (PXR)/constitutive androstane (CAR). information gained study should help predict assess toxicity chemicals.