Mutagenic activation of 2-amino-3-methylimidazo[4,5-f]quinoline by complementary DNA-expressed human liver P-450

Cancer Res. 1990 Apr 1;50(7):2060-3.

Abstract

Eight forms of human liver microsomal P-450 were individually expressed in human hepatoma Hep G2 cells with a vaccinia virus cDNA expression system. Using the Ames test, each expressed P-450 was examined for its ability to activate to mutagenic products the compounds, 2-amino-3-methylimidazo[4,5-f]quinoline, 2-amino-3,4-dimethylimidazo[4,5-f]quinoline, 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline, and 2-amino-3,4,8-trimethylimidazo[4,5-f]quinoxaline, respectively. Three forms of human P-450 significantly activated 2-amino-3-methylimidazo[4,5-f]quinoline when the latter was at high substrate concentrations, but only a single form, P-450IA2, showed very high activation of all promutagens at lower substrate concentrations. Human IA2 had extraordinarily high affinity towards four promutagens tested and is likely the predominant P-450 enzyme responsible for their mutagenic activation in human liver.

MeSH terms

  • Biotransformation
  • Cytochrome P-450 Enzyme System / genetics
  • Cytochrome P-450 Enzyme System / metabolism*
  • DNA / genetics
  • Humans
  • Immunologic Techniques
  • In Vitro Techniques
  • Liver / enzymology
  • Mutagens / metabolism*
  • Quinolines / metabolism*
  • Recombinant Proteins / metabolism
  • Vaccinia virus

Substances

  • Mutagens
  • Quinolines
  • Recombinant Proteins
  • 2-amino-3-methylimidazo(4,5-f)quinoline
  • DNA
  • Cytochrome P-450 Enzyme System