Correlation of Anti-Inflammatory Activity with Inhibition of Prostaglandin Synthesis Activity of Nonsteroidal Anti-Estrogens and Estrogens

Abstract

Diethylstilbestrol, clomiphene, ethamoxytriphetol and triparanol were 0.18, 1.0, 0.02 and 0.01 times as potent in the in vitro inhibition of prostaglandin synthetase, respectively as was indomethacin. In the in vivo carrageenan-induced rat paw edema studies, diethylstilbestrol was more potent as an anti-inflammatory agent than was clomiphene, and ethamoxytriphetol and triparanol were only marginally effective. The most potent of the compounds tested was indomethacin. The results reported demonstrate that the nonsteroidal anti-inflammatory agents and the nonsteroidal estrogens and anti-estrogens share the property of inhibition of prostaglandin synthetase.