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

Abstract

Summary

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 synthe-tase, 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.

The authors thank Mr. Giovanni Ghinzone for assisting in the prostaglandin synthetase assays; Dr. Domenica Selva for assisting in the anti-inflammation studies; and Miss Maria Carla San Pietro for typing the manuscript.