非普拉宗对环氧酶活性的影响

EFFECTS OF FEPRAZONE ON CYCLOOXYGENASE IN VITRO

目的 研究非普拉宗 (feprazone,Fep)对环氧酶 1和环氧酶 2活性的影响。方法 用放免法测定PGE2 含量反映环氧酶 2活性 ,测定 6 酮 前列腺素F1α含量反映环氧酶 1活性。结果 Fep在 0 1,1 0 ,10 0 μmol·L-1能剂量依赖性抑制小鼠腹腔巨噬细胞PGE2 生成 ,在相同浓度下对小牛主动脉内皮细胞 6 keto PGF1α生成抑制作用较弱。结论 Fep显著抑制PGE2 生成 ,对PGI2 生成影响较小 ,提示其对环氧酶

AIM To study the effects of feprazone (Fep) on cyclooxygenase (COX) activities in vitro . METHODS Prostaglandin E 2(PGE 2) in cultured mouse peritoneal macrophage supernatants induced by lipopolysaccharide (LPS) 1 mg·L -1 was measured with radioimmunoassay (RIA) method using 3H labelled PGE 2. The 6 keto PGF 1α in cultured bovine arterial endothelial cell (BAEC) supernatants was measured with RIA method using 125 I labelled 6 keto PGF 1α . RESULTS Fep markedly inhibited PGE 2 production in a good concentration dependent manner at the concentrations of 0 1, 1 0 and 10 0 μmol·L -1 . The IC 50 of Fep is 1 0 μmol·L -1 . Fep significantly decreased 6 keto PGF 1α production at the concentration of 10 0 μmol·L -1 . CONCLUSION The results showed that the inhibitory effect of Fep on COX2 is 10 fold more than that on COX1. Thus, it is suggested that Fep have more potential inhibitory effect on COX2 and lower gastrointestinal toxicity than normal nonsteroidal antiinflammatory drugs such as aspirin, indomethacin and meloxicam.