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  • Title: Selective inhibitors of platelet lipoxygenase: 4,7,10,13-eicosatetraynoic acid and 5,8,11,14-henicosatetraynoic acid.
    Author: Wilhelm TE, Sankarappa SK, VanRollins M, Sprecher H.
    Journal: Prostaglandins; 1981 Feb; 21(2):323-32. PubMed ID: 6784191.
    Abstract:
    Nine acetylenic acids were evaluated to determine what structural features are required for selective inhibition of platelet lipoxygenase. Both 4,7,10,13-icosatetraynoic acid and 5,8,11,14-henicosatetraynoic acid inhibited the synthesis of 12-L-hydroxy-5,8,10,14-icosatetraenoic acid (HETE) more than 95 percent without significantly altering the production of either thromboxane B2 or 12-L-hydroxy-5,8,10-heptadecatrienoic acid (HHT). The ID50 concentrations (microM) for inhibiting the synthesis of thromboxane B2 and HETE were respectively 51 and 0.46 with 4,7,10,13-icosatetraynoic acid while similar concentrations of 64 and 0.31 were found for 5,8,11,14-henicosatetraynoic acid.
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