[Higher microsomal monooxygenase activity in chloroquine-resistant strains of malarial plasmodium as a possible cause of drug stability]

Vopr Med Khim. 1983 Sep-Oct;29(5):63-5.
[Article in Russian]

Abstract

Ability to hydroxylate benz(alpha)pyrene--a substrate of arylhydrocarbone hydroxylase (AHH) was distinctly increased in lysates of erythrocytes containing malarial plasmodium. Hydroxylation of benz(alpha)pyrene was inhibited by methyrapone--an inhibitor of microsomal monooxygenases. Activity of AHH was increased from 2- to 3-fold in chloroquine-resistant plasmodium strains as compared with the drug-sensitive strains. Resistance of Plasmodium berghei to chloroquine appears to involve an activation of the monooxygenases system in the parasite.

Publication types

  • English Abstract

MeSH terms

  • Animals
  • Aryl Hydrocarbon Hydroxylases / metabolism*
  • Benzo(a)pyrene
  • Benzopyrenes / metabolism
  • Chloroquine / toxicity*
  • Drug Resistance
  • Drug Stability
  • Enzyme Activation
  • Kinetics
  • Microsomes / drug effects
  • Microsomes / enzymology*
  • Mutagens / metabolism
  • Plasmodium berghei / drug effects
  • Plasmodium berghei / enzymology*

Substances

  • Benzopyrenes
  • Mutagens
  • Benzo(a)pyrene
  • Chloroquine
  • Aryl Hydrocarbon Hydroxylases