ABSTRACT
CDRI compound 85/287 a potent estrogen antagonist and antiimplantation agent in rat was studied to elucidate its mechanism of action. In ovariectomized rats 85/287 treatment antagonized estrogen stimulated uterine volume density, eosinophil leucocyte infiltration, stromal mitotic cell number and peroxidase activity. In parallel experiments in pregnant rats, uterine peroxidase activity also decreased significantly as compared to controls on day 5 post-coitum. The results show that 85/287 exerts its antiimplantation activity by inhibition of responses to estradiol action.
Subject(s)
Animals , Benzopyrans/pharmacology , Embryo Implantation/drug effects , Endometrium/anatomy & histology , Estrogen Antagonists/pharmacology , Female , Peroxidases/metabolism , Piperidines/pharmacology , Pregnancy , Rats , Rats, Sprague-DawleyABSTRACT
The effect of androgen and estrogen antagonists on estrogen induced responses in the epididymis of rat was studied. Estradiol benzoate administered to male rates on day 5 of life increased the epididymal weight, absolute volume density of fibromuscular stroma and its eosinophilic leucocyte numbers. Testosterone administration (day 5 life) alone did not have any stimulatory effect on the epididymis as an organ or its peroxidase activity on days 15 or 20 of life. On the other hand, testosterone/85/287 negated estradiol induced increase in the absolute volume density, eosinophilic leucocyte accumulation and peroxidase activity. Tamoxifen (Tam) with inherent estrogenic activity acted both as an agonist and an antagonist. Results of present studies support the contention that nonsteroidal antiestrogens (CDRI-85/287 and Tam) can modulate estradiol induced epididymal responses during the postnatal period of male rat.
Subject(s)
Animals , Cell Size/drug effects , Epididymis/cytology , Estrogen Antagonists/pharmacology , Estrogens/pharmacology , Male , Mitotic Index/drug effects , Peroxidase/analysis , RatsABSTRACT
The ethanolic extract of A. aureum and its fractions were evaluated for postovulatory antifertility activity in female rats. The water soluble fraction of ethanolic (95%) extract prevented (100%) pregnancy when administered to female rats on days 1-7 postcoitum. This fraction was found devoid of both estrogenic and antiestrogenic activities.