周美华, 李全, 包亚敏, 林加宝, 褚云鸿. 17β-羟-7α-甲-5-雄 烯-3-酮的抗生育作用及其激素活性J. 药学学报, 1981, 16(1): 8-8.
引用本文: 周美华, 李全, 包亚敏, 林加宝, 褚云鸿. 17β-羟-7α-甲-5-雄 烯-3-酮的抗生育作用及其激素活性J. 药学学报, 1981, 16(1): 8-8.
Zhou Meihua, Li Quan, Bao Yamin, Lin Jiabao , Chu Yunhong, . ANTIFERTILITY EFFECT OF 17β-HYDROXY-7α-METHYLANDROST-5-EN-3-ONE AND ITS HORMONAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1981, 16(1): 8-8.
Citation: Zhou Meihua, Li Quan, Bao Yamin, Lin Jiabao , Chu Yunhong, . ANTIFERTILITY EFFECT OF 17β-HYDROXY-7α-METHYLANDROST-5-EN-3-ONE AND ITS HORMONAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1981, 16(1): 8-8.

17β-羟-7α-甲-5-雄 烯-3-酮的抗生育作用及其激素活性

ANTIFERTILITY EFFECT OF 17β-HYDROXY-7α-METHYLANDROST-5-EN-3-ONE AND ITS HORMONAL ACTIVITY

  • 摘要: 本工作表明17β-羟-7α-甲-5-雄烯-3-酮在妊娠小鼠、大鼠均有抗早孕和抗着床作用。在小鼠,17β-羟-7α-甲-5-雄烯-3-酮抗早孕作用的ED50=0.159±0.055mg/kg。17β-羟-7α-甲-5-雄烯-3-酮在抗早孕剂量时能明显抑制假孕小鼠的蜕膜反应。甲地孕酮能完全对抗其抗早孕作用,也能完全对抗其抑制蜕膜反应的作用。早孕大鼠皮下注射17β-羟-7α-甲-5-雄烯-3-酮24小时后血浆孕酮浓度已明显下降。以上结果提示17β-羟-7α-甲-5-雄烯-3-酮抗早孕作用可能与其抑制孕酮合成有关。此外,本文对17β-羟-7α-甲-5-雄烯-3-酮的雌素活性和孕激素活性也进行了观察。

     

    Abstract: In the present study, 17β-hydroxy-7α-methylandrost-5-en-3-one was shown to terminate pregnancy following subcutaneous administration of doses of 10 mg/kg on the 1st and 2nd days or the 7th and 8th days of pregnancy in rats and on the 1st and 2nd days or 4th and 5th days in mice. The ED50 of 17β-hydroxy-7α-methylandrost-5-en-3-one to terminate early pregnancy in mice was 0.159±0.055 mg/kg.Concomitant administration of megestrol acetate completely abolished the anti-pregnancy effect of 17β-hydroxy-7α-methylandrost-5-en3—one in mice, but HCG showed no such antagonism when administered in a similar way.17β-hydroxy-7α-methylandrost-5-en-3-one administered at comparable doses terminating the early pregnancy could significantly inhibit the decidual reaction in pseudopregnant mice, and this inhibition was abolished by concomitant administration of megestrol acetate.After subcutaneous injection of 17β-hydroxy-7α-methylandrost-5-en-3-one on the 7th and 8th days of pregnancy in rats, the peripheral plasma level of progesterone decreased markedly at 24hr after the administration of this drug. Results obtained from the endometrial carbonic anhydrase test of immature rabbits showed that 17β-hydroxy-7α-methylandrost-5-en-3-one was devoid of antiprogestational activity. Also, data in the viginal conification test of ovariectomized mice demonstrated 17β-hydroxy-7α-methylandrost-5-en-3-one to have an antiestrogen activity but not an estrogen activity.From the above mentioned results, it may be concluded, that: (1) 17β-hydroxy-7α-methylandrost-5-en-3-one possesses antifertility effect, (2) the effect of 17β-hydroxy-7α-methylandrost-5-en-3-one to terminate early pregnancy is related to its inhibition on deciduoma, and (3) these effects of 17β-hydroxy-7α-methylandrost-5-en-3-one are not resulted from its antiprogestational activity, but rather, may bear some relationships to reduction of the plasma level of progesterone.

     

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