Valeryl salicylate is a selective inhibitor of Cox-1.
ChEBI: A valerate ester that is salicylic acid in which the phenolic hydrogen is replaced by a valeryl (pentanoyl) group.
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].
Valeryl salicylate (3, 10, 30 mg/kg; i.p.) shows anti-inflammatory effect in arachidonic acid (HY-109590)-induced ear oedema and Carrageenan (HY-125474)-induced paw oedema[1].
| Animal Model: | 25-30g, Swiss male mice (arachidonic acid induces Ear oedema)[1] |
| Dosage: | 1.5, 4.5, 15, 45 μg per ear |
| Administration: | |
| Result: | Showed the anti-inflammatory effect of topical administration and resulted in significant inhibition of the ear oedema of28, 36, 40, and 58% at 1.5, 4.5, 15, 45 μg per ear. |
| Animal Model: | 25-30g, Swiss male mice (Carrageenan-induced paw oedema)[1] |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | I.p. |
| Result: | Promoted a significant inhibition of 43.3, 53.3 and 66.6% at 3, 10, 30 mg/kg, respectively. |
[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.
