论文部分内容阅读
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]-E_2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,AF-53小于1。经平行比较,在大鼠以EE 抗生育效应和雌激素活性的相对效价的比值为1,则在抗着床时,AF-45和AF-53的比值为22.64和15.7;在终止早孕时,各为5.7和4.5。同样,当EE 的抗生育效应和RBA 比值为1时,则AF-45在抗着床作用时与RBA 的比值为19.1,终止早孕时为3.84;AF-53则远远大于1。可见,AF-45和AF-53的抗生育效价与雌激素活性不相平行;雌激素活性不是AF-45和AF-53引起抗生育作用的唯一因素,两者存在一定程度的分化。至于AF-45和AF-53在体外与子宫胞浆ERc 的RBA 的显著差异,看来与AF-53的2β、17β-位上的双丙酸酯基团有关。
In this paper, we observed the relative uterine weight gain of ethinyl estradiol (EE), anodithin (AF-45) and anordrin (AF-53) ERc) interactions and anti-fertility effects, thereby analyzing the three estrogen activity and anti-fertility effects. The results indicated that the ability of [~ 3H] -E_2 to bind ERc in uterine cytoplasm was parallel to that of uterine weight gain. If the relative binding affinity (RBA) of ERc in uterine cyst and the relative uterine The weight gain ratio is 1, the ratio of AF-45 is close to 1, and AF-53 is less than 1. In parallel, the ratio of the relative titers of EE antifertility effect to estrogenic activity in rats was 1, then the ratio of AF-45 to AF-53 at anti-implantation was 22.64 and 15.7; at termination of first trimester , Each of 5.7 and 4.5. Similarly, when the ratio of anti-fertility effects to RBA of EE was 1, the ratio of AF-45 to RBA in anti-implantation was 19.1, ending at 3.84 in early pregnancy and AF-53 being much greater than 1. It can be seen that the titers of antifertility of AF-45 and AF-53 are not parallel to the activity of estrogen. The activity of estrogen is not the only factor that causes AF-45 and AF-53 to resist reproductive function. Significant differences in the RBA of AF-45 and AF-53 in vitro with uterine cytoplasmic ERc appear to be related to the dipropionate group at the 2 [beta], 17 [beta] -position of AF-53.