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

BA Hart, JM Simons - Biotechnology therapeutics, 1992 - europepmc.org
BA Hart, JM Simons
Biotechnology therapeutics, 1992europepmc.org
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 …
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.
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