The biological activities of diethylstilbestrol and its derivatives.

Publisher Website
Google Scholar
Abstract
Diethylstilbestol (I), a nonsteroidal estrogen, showed strong coronary vasodilator action on isolated guinea-pig heart, as well as ichthyoctoxicity and antimicrobial activity. First, the coronary vasodilator action of I (ED50: 0.26 .mu.g/heart) on isolated guinea-pig heart was much stronger than that of papaverine (ED50: 7.0 .mu.g/heart) used as a standard. On the other hand, the activities of derivatives of I, i.e., I-diphosphate (II), I-dimethyl ether (III), I-diacetate (IV), I-dipropionate (V) and hexestrol (VI) were weaker than that of I. Second, I showed strong ichthyotoxicity (median tolerance limit at 48 h: 3.30 ppm in Oryzias latipes and 4.50 ppm in Carassius auratus). On the other hand, the ichthyotoxic activities of II-V were weaker than that of I. However, VI showed the same toxicity, as I on both fishes. Third, the antimicrobial acitivies of II-V were weaker than that of I, whereas that of VI was stronger. In particular, I and VI showed strong antifungal activity agasinst Trichophyton spp. It was concluded that both the hydroxyl groups attached to the benzene rings and the transolefin structure are necessary for coronary vasodilator action, while only the hydroxyl groups attached to the benzene rings are necessary for the ichthyotoxic and antimicrobial activities.

This publication has 0 references indexed in Scilit: