PMID: 9180348Jan 1, 1997Paper

Expression and inducibility of UDP-glucuronosyltransferases 1-naphthol in human cultured hepatocytes and hepatocarcinoma cell lines

Life Sciences
A AbidJ Magdalou

Abstract

The UDP-glucuronosyltransferase (UGTs) isoforms involved in the conjugation of 1-naphthol were characterized in human cultured hepatocytes and in two human hepatocarcinoma cell lines, KYN-2 and Mz-Hep-1 in terms of expression, kinetics and induction by drugs. Their properties were compared to those of UGT1*6 stably expressed in the V79 cell line (V79UGT1*6), which glucuronidates 1-naphthol preferentially. The determination of kinetic constants for glucuronidation of 1-naphthol revealed a two-site model in human hepatocytes, but a one-site model in the two hepatocarcinoma cell lines. Southern blot analysis of RT-PCR products, showed that the UGT1*6 mRNA was expressed in KYN-2, but not in Mz-Hep-1 cells. However, a mRNA encoding a UGT different from UGT1*6 was expressed in Mz-Hep-1 cells. The two inducers, beta-naphthoflavone and rifampicin exerted a differential effect, depending on the cell lines considered. Altogether, the results suggest that, in hepatocytes, two UGT isoforms, which glucuronidate 1-naphthol are expressed and are differentialy regulated by inducers. Both KYN-2 and Mz-Hep-1 cells express one of the two different UGT isoforms found in hepatocytes. The UGT isoform present in KYN-2 cells corresponds to UGT1*6, whe...Continue Reading

References

Dec 18, 1978·European Journal of Clinical Pharmacology·K W BockD Josting
Nov 1, 1985·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·W G DippoldK H Meyer zum Büschenfelde
Nov 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·D HardingB Burchell
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Sep 7, 2004·Proceedings of the National Academy of Sciences of the United States of America·Young LeeRoger H Unger

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Citations

Mar 21, 2006·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Nobumitsu HaniokaShizuo Narimatsu
Jan 15, 2004·The Journal of Pharmacology and Experimental Therapeutics·Jessica B MillsSonia M F de Morais
Jul 3, 2007·Drug Metabolism and Pharmacokinetics·Xin LiAnna Radominska-Pandya
Jul 1, 1999·Alternatives to Laboratory Animals : ATLA·S CoeckeC Westmoreland

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