A selective, irreversible inhibitor of COX-1
Valeroyl Salicylate is an irreversible and selective inhibitor of cyclooxygenase-1 (COX-1) with IC50 values of 0.8 and 15 mM for ovine COX-1 and -2, respectively [1].
Cyclooxygenase (COX), also known as prostaglandin-endoperoxide synthase (PTGS, PGHS), is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1][2].
Valeroyl Salicylate is an irreversible and selective inhibitor of cyclooxygenase-1 (COX-1) with IC50 values of 0.8 and 15 mM for ovine COX-1 and -2, respectively. In cos-1 cells expressing either COX-1 or -2, 500 μM of valeroyl salicylate inhibited human COX-1 and -2 by 85% and 15%, respectively. The half-lives for inactivation of human recombinant COX-1 in the presence of 500 μM valeroyl salicylate was 12 minutes [2].
参考文献:
[1].? Johnson JL, Wimsatt J, Buckel SD, et al. Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledons. Arch Biochem Biophys. 1995 Dec 1;324(1):26-34.
[2].? Bhattacharyya DK, Lecomte M, Dunn J, et al. Selective inhibition of prostaglandin endoperoxide synthase-1 (cyclooxygenase-1) by valerylsalicylic acid. Arch Biochem Biophys. 1995 Feb 20;317(1):19-24.
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