Literature DB >> 8395842

The effects of inducing agents on cytochrome P450 and UDP-glucuronyltransferase activities in human HEPG2 hepatoma cells.

H Doostdar1, M H Grant, W T Melvin, C R Wolf, M D Burke.   

Abstract

Selective induction in vitro of cytochrome P450-dependent mixed-function oxidase (MFO) and UDP-glucuronyltransferase (GT) activities was observed in the human HepG2 hepatoma cell line. 1,2-Benzanthracene (BA) induced MFO O-dealkylation activities for ethoxyresorufin, methoxyresorufin and benzyloxyresorufin, whereas phenobarbitone (PB) selectively induced pentoxyresorufin O-dealkylation and rifampicin (RIF) selectively induced benzyloxyresorufin O-dealkylation. Antibody inhibition experiments indicated that ethoxyresorufin and methoxyresorufin O-dealkylations were catalysed mainly by the P450 1A subfamily in untreated and BA-induced HepG2 cells, that additional unidentified P450 forms were considerably involved in methoxyresorufin and benzyloxyresorufin O-dealkylations and that the P450 2B subfamily was partially responsible for pentoxyresorufin O-dealkylation in PB-induced cells. Bilirubin GT activity was induced by PB, BA, RIF and dexamethasone, but 1-naphthol, morphine and testosterone GT activities were not induced by any of these treatments.

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Year:  1993        PMID: 8395842     DOI: 10.1016/0006-2952(93)90548-b

Source DB:  PubMed          Journal:  Biochem Pharmacol        ISSN: 0006-2952            Impact factor:   5.858


  9 in total

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Journal:  Cell Stress Chaperones       Date:  2012-02-26       Impact factor: 3.667

2.  A Physiologically Based Pharmacokinetic Model for Optimally Profiling Lamotrigine Disposition and Drug-Drug Interactions.

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3.  Induction of zidovudine glucuronidation and amination pathways by rifampicin in HIV-infected patients.

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Journal:  Br J Clin Pharmacol       Date:  1999-08       Impact factor: 4.335

Review 4.  Pharmacokinetic interactions with rifampicin : clinical relevance.

Authors:  Mikko Niemi; Janne T Backman; Martin F Fromm; Pertti J Neuvonen; Kari T Kivistö
Journal:  Clin Pharmacokinet       Date:  2003       Impact factor: 6.447

Review 5.  Human cell lines in pharmacotoxicology. An introduction to a panel discussion.

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6.  Effect of rifampicin on pravastatin pharmacokinetics in healthy subjects.

Authors:  Carl Kyrklund; Janne T Backman; Mikko Neuvonen; Pertti J Neuvonen
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7.  Discrimination between Crigler-Najjar type I and II by expression of mutant bilirubin uridine diphosphate-glucuronosyltransferase.

Authors:  J Seppen; P J Bosma; B G Goldhoorn; C T Bakker; J R Chowdhury; N R Chowdhury; P L Jansen; R P Oude Elferink
Journal:  J Clin Invest       Date:  1994-12       Impact factor: 14.808

8.  Profound reduction in tamoxifen active metabolite endoxifen in a breast cancer patient treated with rifampin prior to initiation of an anti-TNFα biologic for ulcerative colitis: a case report.

Authors:  Sara L Henderson; Wendy A Teft; Richard B Kim
Journal:  BMC Cancer       Date:  2016-05-11       Impact factor: 4.430

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Authors:  Carlijn H C Litjens; Laurens F M Verscheijden; Celine Bolwerk; Rick Greupink; Jan B Koenderink; Petra H H van den Broek; Jeroen J M W van den Heuvel; Elin M Svensson; Martin J Boeree; Cecile Magis-Escurra; Wouter Hoefsloot; Reinout van Crevel; Arjan van Laarhoven; Jakko van Ingen; Saskia Kuipers; Rovina Ruslami; David M Burger; Frans G M Russel; Rob E Aarnoutse; Lindsey H M Te Brake
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  9 in total

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