选择性环氧合酶-2抑制剂体外筛选模型的建立  

A screening model of selective COX-2 inhibitors

作　　者：潘献柱[1] 王林[2] 程洁[1] 汪思应[1] 温晓雪[2] 彭涛[2] 

机构地区：[1]安徽医科大学病理生理学教研室 [2]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《中国新药杂志》2006年第23期2024-2027,共4页Chinese Journal of New Drugs

摘　　要：目的:建立选择性环氧合酶-2(COX-2)抑制剂筛选模型。方法:以脂多糖(LPS)为刺激剂刺激大鼠腹腔巨噬细胞产生前列腺素E2(PGE2),采用放免法确定最佳刺激浓度和时间,以选择性COX-2抑制剂戊地昔布和达布非隆(darbufelone)为阳性对照药验证实验模型。结果:达布非隆和戊地昔布对COX-2和COX-1的半数抑制浓度(IC50)的比值分别为3．175×10-4和3．576×10-3。结论:本实验建立的COX-2抑制剂筛选模型比较灵敏,可靠,可用于选择性COX-2抑制剂的筛选。Objective： To develop a screening model that may be used to screen selective COX- 2 inhibitors. Methods： Rats were abdominally injected with lipopolysaccharide （LPS） to stimulate the generation of PGE2 in macrophages. The optimal time and concentration of LPS administration were determined by radioimmunoassay. Darbufelone and Voldecoxib were used as the positive control. Results： The ratios of IC50 （COX-2）/IC50 （COX-1） of Darbufelone and Voldecoxib were 3. 175 × 10^-4 and 3. 576 × 10^-3, respectively. Conclusion： The sensitive screening model may be used for screening selective COX-2 inhibitors.

关 键 词：环氧合酶(COX) 选择性环氧合酶-2抑制剂 筛选模型 巨噬细胞 

分 类 号：R965.1[医药卫生—药理学] R971.1[医药卫生—药学]