SELECTIVE-INHIBITION OF PLATELET LIPOXYGENASE BY ESCULETIN

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  • 1 January 1982
    • journal article
    • research article
    • Vol. 713  (1) , 68-72
Abstract
The effects of coumarin and its derivatives on rat platelet lipoxygenase and cyclooxygenase activities were studied. Esculetin (6,7-dihydroxycoumarin) inhibited lipoxygenase more strongly than cyclooxygenase; its concentration for 50% inhibition (IC50) was 0.65 .mu.M for platelet lipoxygenase and 0.45 mM for platelet cyclooxygenase. Esculin (the 6-glucoside of esculetin) and umbelliferone (7-hydroxycoumarin) also selectively inhibited the lipoxygenase, though less strongly (IC50 = 290 and 500 .mu.M, respectively). 4-Hydroxycoumarin and coumarin had no inhibitory effect on either enzyme at concentrations up to 1 mM. The mechanism of the lipoxygenase inhibition by esculetin was non-competitive. Other antioxidants (hydroquinone, gallic acid and ascorbic acid) were less inhibitory to both enzymes and showed little selectivity.