六种甾体酮肟的抗生育作用及激素活性

本文报道六种甾体酮肟的抗着床、抗早孕作用及激素活性的分析比较。SO-33和SO-65大鼠抗着床活性稍强,SO-33、SO-57和SO-65大鼠抗早孕活性稍强。六种化合物都不能维持去卵巢大鼠妊娠和诱发去卵巢小鼠蜕膜瘤反应;除SO-48外,其余化合物均能对抗孕酮的维持妊娠作用;SO-33和SO-36对孕酮蜕膜瘤反应的抑制作用稍强。六种化合物都可使未成熟小鼠子宫增重,以SO-57和SO-48活性更为显著;SO-33、SO-35和SO-57可使部分去卵巢小鼠阴道上皮细胞角化。SO-33、SO-35、SO-36和SO-65可抑制雌酮的子宫增重活性,只有SO-57能部分抑制雌酮的阴道细胞角化反应。SO-33的抗着床活性与阴道细胞角化活性的比率比炔雌醇强14倍。结果表明SO-33具有雌激素活性低,抗孕激素及抗着床活性强等特点,有可能发展成为新型抗着床避孕药。

ANTIFERTILITY EFFECTS AND HORMONE ACTIVITYIFS OF SIX STEROID OXIMES

Antifertility effects and hormonal activitics of norethisterone oxime (SO-33), norethis-terone oxime acetate (SO-36), Siloxy-northisterone oxime (SO-35), R-2010 oxime (SO-57), R-2323 oxime (SO-65) and durabolin oxime (SO-48) had been studied. The anti-implantation and interceptive effects, as well as the antiprogesterone activity in deciduomaformation and pregnancy maintenance in ovariectomized animals of the 6 steroid oximeswere compared. The induction of uterine hypertrophia and vagina epidermal cornificationby the steroid oximes in mice were also investigated. As a result, SO-33 would beprosumably developed as a new antiimplantative agent because of its weaker estrogenicityand its much stronger anti-implantation and antiprogestational activity as well.