Metabolic activation of phenols by stimulated neutrophils: a concept for a selective type of anti-inflammatory drug

Biotechnol Ther. 1992;3(3-4):119-35.

Abstract

Apocynin (4-hydroxy-3-methoxy-acetophenone) is a potent and selective inhibitor of neutrophil oxyradical production. The mechanism of action involves metabolic activation in a (myelo)-peroxidase-dependent reaction. The reaction product(s) prevent(s) the assembly of the superoxide anion-generating NADPH:O2 oxidoreductase by conjugation to essential thiol groups. Different neutrophil functions that are essential to their bactericidal activity, however, remain intact. When administered orally a potent anti-inflammatory activity was found in rats with experimentally induced local or systemic inflammation.

Publication types

  • Review

MeSH terms

  • Acetophenones / pharmacology
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Biotransformation / drug effects
  • In Vitro Techniques
  • Male
  • Neutrophils / drug effects
  • Neutrophils / metabolism*
  • Phenols / pharmacokinetics*
  • Quinones / pharmacology
  • Rats
  • Respiratory Burst / drug effects

Substances

  • Acetophenones
  • Anti-Inflammatory Agents, Non-Steroidal
  • Phenols
  • Quinones
  • acetovanillone