Disease relevance of Orpanoxin

• Orpanoxin, a nonsteroidal anti-inflammatory drug (NSAID) lacking gastric ulcerogenic effects in the therapeutic dose range in rats, was compared with six reference NSAIDs for oral activity in the rat paw carrageenin-induced edema assay [1].
• In the guinea-pig u.v.-induced erythema model, application (1 h after u.v.) of 1, 5, and 10% (w/v) orpanoxin creams (containing 10% urea) significantly inhibited erythema at 2, 3, and 4 h post-irradiation [1].

High impact information on Orpanoxin

• Effects of orpanoxin on arachidonic acid metabolism of human polymorphonuclear leucocytes and platelets in vitro [2].
• 4. These results indicate that the discrepancy between the low potency of orpanoxin in inhibiting bovine seminal vesicle cyclo-oxygenase in vitro and its high potency as an anti-inflammatory agent in vivo is not explained by its having an additional lipoxygenase inhibitory mechanism [2].
• It was concluded that orpanoxin has anti-inflammatory activity comparable to reference NSAIDs in the rat paw edema test, is active orally in rat, mouse, and guinea-pig models, and shows topical activity in the guinea-pig and the mouse [1].
• In comparison, exposure of hepatocytes to the highest dose of orpanoxin resulted only in increased vacuolation, a slight increase in cellular debris, and increased electron density of the cytoplasm of hepatocytes [3].

References