The Anti-inflammatory Effect of Coumarin and its Derivatives

D.   J.   Hadjipavlou-Litina; K.   E.   Litinas; C.      Kontogiorgis

doi:10.2174/187152307783219989

Abstract

Inflammation is the primary host defense mechanism against all forms of injury. Excessive or inadequate activation of the system can have serious effects, as can the failure of inactivation mechanisms. Coumarins can reduce tissue edema and inflammation and inhibit prostaglandin biosynthesis, which involves fatty acid hydroperoxy intermediates. It is to be expected that coumarins might affect the formation and scavenging of reactive substances derived from oxygen species (ROS) and influence processes involving free radical-mediated injury, as can flavonoids. During these years a small number of (Q)SAR studies concerning coumarins as NSAIDs has been presented and reviewed. In this research we tried to examine the structure-function relationship for coumarins, presenting antiinflammatory activity. Coumarin (1), the prototypical compound presents anti-inflammatory activity. The hydroxylaromatic substituted derivatives (5- or 6- or 7-hydroxy or the vicinal dihydroxy) seems to be potent inhibitors of lipoxygenase. Several synthetic derivatives simple or more complicated were found to be potent antiinflammatories/antioxidant agents.

Keywords: Coumarins, antiinflammatories/antioxidant agents, structure-activity relationships

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