生物活性

• 靶点

  COX1 IC50:13μM

  COX2 IC50:370μM

• 描述Cyclooxygenase (COX) is an enzyme that mainly contains a house-keeping enzyme COX-1 and an inducible cyclooxygenase COX-2. COX-1 is expressed throughout the body and important for gastrointestinal protection while the expression of COX-2 is related to cytokines, growth factors and other inflammatory ulcerogenic stimuli^[1]. Ibuprofen, which is one of the most widely used analgesic-antipyretic-anti-inflammatory drugs today, is a COX inhibitor with IC₅₀ value of 2.7 μM for COX-1 and 1.8 μM for COX-2^[2]. In the COX-2 inhibitory assay based on the inhibition potential of conversion of arachidonic acid to prostaglandin H₂ by human recombinant COX-2, Ibuprofen was prepared at a concentration of 50 μg/ml and the COX-2 inhibitory activity was 57.3% ^[3] .
  In carrageenan-induced rat paw dedma model of wistar albino rat, 20 mg/kg by weight of ibuprofen was administered orally. The paw volume of the rat was measured at hourly interval for 3 h (0, 1, 2 and 3 h) and the percent inhibition of edema was 65.9% ^[4] . For the analgesic activity experiment, acetic acid induced writhing method on swiss CD1 mice was used. 10 mg/kg, 20 mg/kg and 70 mg/kg of Ibuprofen was given to the mice orally and the inhibition of analgesic activity after 30 mins was 48%, 53% and 67%, respectively^[5].
• 作用机制COX enzymes oxygenate polyunsaturated fatty acids to prostaglandin endoperoxides and then generate prostaglandins and thromboxanes. Ibuprofen is weak, competitive inhibitors of COX-2 oxygenation of arachidonic acid and potent, noncompetitive inhibitor of 2-arachidonoylglycerol oxygenation^[6].

• 动物研究
  剂量	Rat: 1 mg/kg - 30 mg/kg[7] (i.p.)
  给药途径	i.p.