Comparison of the levels of enzymes involved in drug metabolism between transgenic or gene-knockout and the parental mice

Toxicol Pathol. 2001:29 Suppl:161-72. doi: 10.1080/019262301753178573.

Abstract

Drug-metabolizing enzymes are involved in the metabolic activation or detoxification of carcinogens. To evaluate animals developed as models for alternative carcinogenicity testing, we investigated whether or not a gene manipulation including the transgene of ras and the knocking out of a tumor suppressor gene such as p53 or XPA could alter the expression of representative drug-metabolizing enzymes directly or indirectly. Expression of several isoforms of cytochrome P450 (CYP) in the liver of rasH2, p53 (+/-), Tg.AC, and XPA (-/-) mice with or without treatment of prototype inducer. phenobarbital or 3-methylcholanthrene, was analyzed by Western immunoblotting in comparison with their parental strains of mice. In addition, the activities of 3 major phase II enzymes, UDP-glucronosyltransferase, sulfotransferase, and glutathione S-transferase, were compared between the gene-manipulated and the corresponding parental strains of mice. Results demonstrate that XPA gene knockout appeared to increase constitutive expression of CYP2B and CYP3A isoforms. Overexpression of human c-Ha-ras gene or p53 gene knockout appeared to increase constitutive UGT activity toward 4-nitrophenol. The content or activities of almost all other enzymes examined in the present study do not appear to be affected by the gene manipulation.

Publication types

  • Comparative Study
  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animal Testing Alternatives
  • Animals
  • Carcinogenicity Tests / methods*
  • Carcinogens / toxicity
  • Cytochrome P-450 Enzyme System / biosynthesis*
  • Cytochrome P-450 Enzyme System / genetics
  • DNA-Binding Proteins / genetics
  • Disease Models, Animal*
  • Enzyme Induction / drug effects
  • Female
  • Genes, p53
  • Genes, ras
  • Isoenzymes
  • Liver / drug effects
  • Liver / enzymology*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mice, Transgenic
  • RNA-Binding Proteins / genetics
  • Rats
  • Xeroderma Pigmentosum Group A Protein

Substances

  • Carcinogens
  • DNA-Binding Proteins
  • Isoenzymes
  • RNA-Binding Proteins
  • Xeroderma Pigmentosum Group A Protein
  • Xpa protein, mouse
  • Cytochrome P-450 Enzyme System