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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。
This article reports the anti-implantation, anti-early pregnancy and hormone activity of six steroidal ketoximes. The anti-implantation activity of SO-33 and SO-65 rats was slightly stronger than that of SO-33, SO-57 and SO-65 rats. None of the six compounds could maintain the ovarian and ovariectomized ovariectomized mice, and all the compounds except the SO-48 could maintain the pregnancy effect against progesterone. The effects of SO-33 and SO-36 on progesterone The inhibitory effect of decidual tumor reaction slightly stronger. All of the six compounds could increase the uterus weight of immature mice, and the activity of SO-57 and SO-48 were more obvious. SO-33, SO-35 and SO-57 could make the part of ovariectomized mice . SO-33, SO-35, SO-36 and SO-65 inhibited estrone uterine weight gain activity, and only SO-57 partially inhibited estrone vaginal cell keratinization. The ratio of anti-implantation activity and vaginal keratinization activity of SO-33 is 14 times stronger than that of ethinylestradiol. The results show that SO-33 has the characteristics of low estrogen activity, anti-progesterone and anti-implantation activity, it may develop into a new anti-implantation contraceptives.