16-EPIESTRIOL - AN ANTIINFLAMMATORY STEROID WITHOUT GLYCOGENIC ACTIVITY

All of the steroidal anti-inflammatory drugs currently available are g lucocorticoids. They exhibit both glycogenic and anti-inflammatory act ivities. These two activities are usually considered inseparable. this glycogenic activity is responsible for most of the adverse side effec ts that severely limit clinical use of currently available steroidal a nti-inflammatory drugs. The purpose of this study was to determine if a steroid, 16-epiestriol, could exhibit significant anti-inflammatory activity without glycogenic activity. The anti-inflammatory activity o f 16-epiestriol was determined using a modified Winter's carrageenin r at paw edema model. The glycogenic activity of 16-epiestriol was deter mined by a modification of Venning's methods on liver and plasma gluco se concentrations. In each study, 16-epiestriol-treated animals were c ompared to untreated control and hydrocortisone-treated animals. In th e anti-inflammatory study, 18-epiestriol was more than twice as effect ive as hydrocortisone, on an equimolar basis, in preventing edema. 16- Epiestriol exhibited no effect on the liver or plasma glucose concentr ation in the glycogenic study. 16-Epiestriol exhibited potent anti-inf lammatory activity without glycogenic activity. 16-Epiestriol does not conform to classical steroidal structure-activity relationship theory .