Apocynin is a most widely studied pan-NADPH-oxidase inhibitor and a scavenger of hydrogen peroxide, as well as inhibits rho kinases. Apocynin could eliminate hydrogen peroxid in a dose-dependent manner at concentration ranging in 3-100μM. Intraperitoneal injection with Apocynin at dose of 5mg/kg reduced lung injury and blocked NADPH oxidase activation in lung tissues by carrageenan in mice. The administration of Apocynin significantly reduced ICAM-1, P-selectin induced by carrageenan and attenuated neutrophil infiltration into the lung tissue. Also Apocynin attenuated carrageenan-induced TNF-α and IL-1β, iNOS expression, Fas ligand, apoptosis and Bax expression, as well as prevented carrageenan-induced inhibition of Bcl-2 expression and activation of NF-κB pathway and MAPK pathway at 4h post carrageenan injection. Some study showed that Apocynin may work as an antioxidant more than a NADPH oxidase inhibitor for apocynin failed to inhibit superoxide anion generation in HEK293 cells overexpressing NADPH oxidase isoforms (Nox1, Nox2, or Nox4).
作用机制
Apocynin is an oxidase assembly inhibitor which can inhibit association of p47phox with membrane-bound heterodimer.[5]
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