H. Qi
2000
Citations
0
Influential Citations
4
Citations
Quality indicators
Journal
Acta pharmaceutica Sinica
Abstract
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.