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新型三唑类化合物Ⅱ3的镇痛作用及对环氧酶活性的影响

Analgesic effects of new triazole compounds Ⅱ3 and their effects on the activity of cycloxygenase

  • 摘要: 目的 : 研究化合物Ⅱ3的镇痛作用及其对环氧酶-1(COX-1)和环氧酶-2(COX-2)活性的影响。 方法 : 采用小鼠热板实验和扭体实验研究化合物Ⅱ3的镇痛作用;利用放免法测定巨噬细胞中PGE2的含量,考察化合物Ⅱ3对COX-2活性的影响;测定内皮细胞中6-酮-前列腺素F(6-keto-PGF)含量,考察化合物Ⅱ3对COX-1活性的影响。 结果 : 化合物Ⅱ3高、中、低3个剂量组均可以延长小鼠的热痛阈值,延长造模后小鼠第一次出现扭体反应的时间并减少15 min内扭体反应出现的次数(P<0.05,P<0.01);在1×10-5,1×10-6,1×10-7 mol/L浓度时均能抑制小鼠腹腔巨噬细胞PGE2的生成, 1×10-6 mol/L浓度显著地抑制生成后的COX-2活性,在相同浓度下对新生小牛胸主动脉内皮细胞6-keto-PGF生成的抑制作用相对较弱。 结论 : 化合物Ⅱ3具有一定的镇痛作用,而且对COX-2具有选择性抑制作用。

     

    Abstract: Aim :To investigate the analgesic effect of the new triazole compounds II3 and effects on cycloxygenase-1(COX-1) as well as cycloxygenase-2(COX-2). Methods :The hot plate and the stretching settings in mice were utilized to study the effects of compounds II3 on acute pain.Radioimmunologic kits were used to assay the contents of PGE2 in macrophage and 6-keto-PGF in endodermis,which represents the activities of COX-2 and COX-1,respectively. Results :Compounds II3 (15,30,60 mg/kg) prolonged the pain liminal value and the writhing response time in the initial appearance,and reduced the frequency of the writhing response in 15 min after exposure of the mice to glacial acetic acid(P<0.05,P<0.01).Compounds II3,at the concentrations of 1×10-5,1×10-6,and 1×10-7 mol/L,markedly inhibited the production of PGE2 in macrophage,and also impeded the activity of COX-2 at 1×10-6 mol/L.But the inhibition of 6-keto-PGF in endodermis using the same settings of compounds Ⅱ3 was found to be limited. Conclusion :Compounds Ⅱ3 has analgesic effects on the acute pain and selective inhibition on COX-2.

     

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