Activity and inducibility of drug-metabolizing enzymes in immortalized hepatocyte-like cells (mhPKT) derived from a L-PK/Tag1 transgenic mouse

Exp Cell Res. 1997 Aug 1;234(2):362-72. doi: 10.1006/excr.1997.3626.

Abstract

This report describes the establishment and characterization of the mhPKT cell line derived from the liver of a transgenic mouse harboring the simian virus (SV40) large T and small t antigens placed under the control of the 5' regulatory sequence of the rat L-type pyruvate kinase (L-PK) gene. mhPKT cells had a prolonged life span, expressed the SV40-encoded nuclear large T antigen when grown in glucose-enriched medium, and induced tumors when injected subcutaneously into athymic (nu-nu) mice. Growth on petri dishes or filters yielded multiple layers of cuboid cells, with numerous spaces between adjacent cells that were closed by junctional complexes. These bile canaliculi-like structures exhibited numerous microvilli in which villin, an actin-binding brush-border protein, colocalized with actin. These bile canaliculi-like structures appeared to be functional as they accumulated fluorescein. mhPKT cells conserved the expression of the liver-specific transcription factors HNF1, HNF3, HNF4, and DBP together with substantial levels of L-PK and albumin but not alpha-fetoprotein mRNA transcripts. mhPKT cells mainly metabolized testosterone into androstenedione and 6beta-hydroxytestosterone, as in vivo. 3-Methylcholanthrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) markedly increased ethoxyresorufin-O-deethylase activity and the related cytochrome P450 (CYP) 1A1/2 protein, whereas alpha-naphtoflavone antagonized the TCDD-elicited induction. Phenobarbital slightly increased the CYP2B-mediated activities of pentoxyresorufin-O-depentylase, 2beta- and 16beta-testosterone hydroxylase. mhPKT cells also had substantial sulfotransferase, UDP-glucuronyltransferase, and glutathione S-transferase activities. This model may serve as a tool for long-term in vitro studies of xenobiotic metabolism, potent CYP inducers, and hepatocyte damage due to drugs and other factors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antigens, Polyomavirus Transforming
  • Bile Canaliculi
  • Carbohydrates
  • Cell Line, Transformed / metabolism*
  • Cytochrome P-450 Enzyme System / metabolism
  • Diet
  • Gene Expression
  • Glutathione / metabolism
  • Liver / cytology*
  • Liver / enzymology*
  • Liver Neoplasms, Experimental / chemically induced
  • Methylcholanthrene / pharmacology
  • Mice
  • Mice, Transgenic
  • Pharmaceutical Preparations / metabolism*
  • Polychlorinated Dibenzodioxins / pharmacology
  • Pyruvate Kinase / genetics
  • RNA, Messenger / analysis
  • Simian virus 40
  • Testosterone / metabolism
  • Transcription Factors / genetics

Substances

  • Antigens, Polyomavirus Transforming
  • Carbohydrates
  • Pharmaceutical Preparations
  • Polychlorinated Dibenzodioxins
  • RNA, Messenger
  • Transcription Factors
  • Testosterone
  • Methylcholanthrene
  • Cytochrome P-450 Enzyme System
  • Pyruvate Kinase
  • Glutathione