Inhibition of Prostaglandin H2 Synthases by Salicylate is Dependent on the Oxidative State of the Enzymes
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Salicylic acid (SA) is an effective antipyretic and analgesic agent, yet at therapeutic concentrations exerting these effects SA lacks antiinflammatory action, distinguishing it from non-steroidal antiinflammatory drugs (NSAIDs) and selective inhibitors of prostaglandin H synthase-2 (PGHS-2). Only at concentrations much greater than are required for antipyresis does SA demonstrate antiinflammatory effects. In contrast to acetylsalicylic acid (aspirin), which irreversibly inhibits platelet PGHS-1 by acetylating a serine in the cyclooxygenase active site, SA is a weak inhibitor of platelet PGHS. The distinctive pharmacologic behavior of SA suggests that the molecular basis for its action differs from that of NSAIDs and PGHS-2 inhibitors.
KeywordsSalicylic Acid Lipid Hydroperoxide Inhibitory Potency Sodium Salicylate Salicylic Acid Level
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