非普拉宗对环氧酶活性的影响

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F_1α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-PGF_1α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-2有较强的抑制作用。

EFFECTS OF FEPRAZONE ON CYCLOOXYGENASE IN VITRO

AIM　To study the effects of feprazone (Fep) on cyclooxygenase (COX) activities in vitro. METHODS　Prostaglandin E₂(PGE₂) in cultured mouse peritoneal macrophage supernatants induced by lipopolysaccharide (LPS) 1 mg*L^-1 was measured with radioimmunoassay (RIA) method using ³H-labelled PGE₂. The 6-keto-PGF_1α in cultured bovine arterial endothelial cell (BAEC) supernatants was measured with RIA method using ¹²⁵I-labelled 6-keto-PGF_1α. RESULTS　Fep markedly inhibited PGE₂ production in a good concentration-dependent manner at the concentrations of 0.1, 1.0 and 10.0 μmol.L^-1. The IC₅₀ of Fep is 1.0 μmol.L^-1. Fep significantly decreased 6-keto-PGF1α 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.