双炔失碳醇和双炔失碳酯的雌激素活性与抗生育作用关系的探讨

Relationship Between the Estrogenic Activities of Ethynyl Estradiol,AF-45 and AF-53 and Their Antifertillty Effects

本文观察了乙炔雌二醇（ＥＥ）、双炔失碳醇（ＡＦ－４５）和双炔失碳酯（ＡＦ－５３）的相对子宫增重效价、与子宫胞浆雌二醇受体（ＥＲｃ）的相互作用特性和抗生育效应由此分析三者的雌激素活性和抗生育效应的关系。结果指示，三者在竞争［＾３Ｈ］－Ｅ２结合大鼠子宫胞浆ＥＲｃ的能力和相对子宫增重效价相平行，若以ＥＥ的子宫胞浆ＥＲｃ的相对结合亲和力（ＲＢＡ）和相对子宫增重效价的比值为１，则ＡＦ－４５的比值接近于１。

This report is on relative Estrongenicity potency,relative binding affinity(RBA)for uterinecytosol Estradiol receport and relative antiftertility potency by an Ethynyl estradiol(EE).Anorstoroide(AF-45),Anordin(AF-53)in rats and to detrnonstrate the relationship between their hormornalactivities and antifertillty effects.The RBA of the three compounds for uterine cytosol estradiol receporsparalleled the relative potenc of uterine weight.As the ratio of RBA and relative potency of uterineweight for EE was equal to 1,the ratio AF-45 was close to 1 and the ratio for AF-53<1.It hasbeen dechled through petalled comparison that if value of EE antifertillty effect and estrgenieityrelative potency was equal to 1,the ratio value of AF-45 or AF-53 is 22.64 or 15.7 when theywere used for the antionplantation;as the terminating early pregnancy,the value of AF-45 or AF-53is 5.7 or 4.5.Similary,if the rarions of antifertility effect and RBA was equal to 1,the value ofAF-45 was 19.1 or 3.84 when they were used for the antionplantation or the termining earlyprenaney.It was clear that the antifertitility effect of AF-45 or AF-53 was not parallels with relativeostogenicity potency.The estigenicity potency was not the only factor,which set off the antigertilityeffect of AF-45 and AF-53,there existed differentiation to a certain extent,it was suggested that theRBA of AF-45,and AF-53 for urerine cytosol estradiol recetors in was been markedly different,which might be associated with the substilution of diproprionte on 2 and 17 possitiom of AF-53.