Flavonoids: potent inhibitors of arachidonate 5-lipoxygenase

Biochem Biophys Res Commun. 1983 Oct 31;116(2):612-8. doi: 10.1016/0006-291x(83)90568-5.

Abstract

Various flavonoids were found to be relatively selective inhibitors of arachidonate 5-lipoxygenase which initiates the biosynthesis of leukotrienes with the activity of slow reacting substance of anaphylaxis. Cirsiliol (3',4',5-trihydroxy-6,7-dimethoxyflavone) was most potent, and the enzyme partially purified from rat basophilic leukemia cells was inhibited by 97% at a concentration of 10 microM (IC50, about 0.1 microM). 12-Lipoxygenases from bovine platelets and porcine leukocytes were also inhibited but at higher concentrations (IC50, about 1 microM), and fatty acid cyclooxygenase purified from bovine vesicular gland was scarcely affected. The compound at 10 microM suppressed by 99% the immunological release of slow reacting substance of anaphylaxis from passively sensitized guinea pig lung (IC50, about 0.4 microM).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arachidonate Lipoxygenases
  • Blood Platelets / enzymology
  • Cattle
  • Dose-Response Relationship, Drug
  • Flavones*
  • Flavonoids / pharmacology*
  • Guinea Pigs
  • Leukocytes / enzymology
  • Lipoxygenase Inhibitors*
  • Lung / drug effects
  • Male
  • Muscle Contraction / drug effects
  • SRS-A / metabolism
  • Swine

Substances

  • Flavones
  • Flavonoids
  • Lipoxygenase Inhibitors
  • SRS-A
  • cirsiliol
  • Arachidonate Lipoxygenases