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环氧化酶Ⅱ抑制剂体外筛选模型的研究
Study on screening the cyclooxygenase-2 inhibitor by in vitro method
【摘要】 目的 建立环氧化酶Ⅱ活性的检测模型 ,提供环氧化酶Ⅱ抑制剂的筛选模型及非甾体类抗炎药 (nonsteoroidalanti in flammatorydrug ,NSAID)筛选的方法。 方法 利用NIH 3T3细胞在血清存在情况下能诱导生成环氧化酶Ⅱ的特性 ,通过加入底物花生四烯酸 ,检测终产物前列腺素E2 (PGE2 )含量的变化 ,判断化合物对环氧化酶Ⅱ的作用。以rofecoxib(罗非昔布 )为阳性药来判断该模型能否用于环氧化酶Ⅱ活性的检测。结果 Rofecoxib能明显的抑制环氧化酶Ⅱ的活性。结论 该方法可以用于环氧化酶Ⅱ抑制剂的筛选
【Abstract】 OBJECTIVE To establish the assay model of cyclooxygenase-2 activity and provide the screening method of NSAIDs.METHODS Observations were made that cyclooxygenase-2 was induced in the exist of FCS.The inhibitory potency of the compounds was evaluated by determining the concentration of PGE 2.Rofecoxib employed as the reference drug was used to evaluate whether this method was available to determine the inhibitory potency of cyclooxygenase-2.RESULTS The results proved that rofecoxib can inhibit the activity of cyclooxygenase-2.CONCLUSION The in vitro method can be used to screen the cyclooxygenase-2 inhibitor.
- 【文献出处】 中国药学杂志 ,Chinese Pharmaceutical Journal , 编辑部邮箱 ,2003年04期
- 【分类号】R965.1
- 【被引频次】5
- 【下载频次】294