羟泰米酚的抗着床作用及其对小鼠子宫雌二醇和孕酮受体含量的影响  

ANTI-IMPLANTATION EFFECT OF HYDROXYTAMOXIFEN AND ITS INFLUENCES ON THE CONTENT OF UTERINE ESTRADIOL AND PROGESTERONE RECEPTOR IN MICE

作　　者：秦武轩[1] 赵炳顺[1] 范植明 邹继超 

机构地区：[1]中国科学院动物研究所计划生育生殖生物学国家重点实验室,北京100080

出　　处：《动物学报》1995年第1期73-81,共9页ACTA ZOOLOGICA SINICA

基　　金："七五"中国科学院生物科学重大项目基金;美国洛克菲勒基金资助

摘　　要：经雌激素拮抗剂－羟泰米酚处理后的怀孕小鼠，胚泡着床受到明显抑制；同时，着床前子宫细 胞质雌二醇受体和孕酮受体明显减少，细胞核受体明显增加；拮抗剂还使血清雌激素和孕酮含量显 著降低。结果表明：羟泰米酚的抗着床作用效应与子宫雌二醇受体和孕酮受体的正常功能受到干扰 可能是有密切关系的。The effect of hydroxytamoxifen on fertility and its influences on the content of uterine estradiol and progesterone receptors in mice were studied. Hydroxytamoxifen was adminis- tered at different days of pregnancy. When the dose 10 ug-100ug was given before im- plantation-from D1 to D3, the pregnant rate of mice were 0%. If the drug administration af- ter implantation (D6-D7), the pregnant rate were no significant difference as compared with the control. These results indicated that the hydroxytamoxifen has a specific ability to preventing the implantation but only a small influence on early pregnancy. Twenty four hours after treatment with 50ug hydroxytamoxifen on D3, the cytosol estradiol receptors (ERc) decreased from 178.89 ± 60.58 fmol/mg protein to 73.96±9.16. The nuclear estradiol recep- tor (ERn) increased from 181.68 ±69.34fmol/mgDNA to 440.80±107. 37. The cytosol and the muclear progesterone receptors (PRc and PRn ) increased from 147.00± 72. 82fmol/mg protein and 24.75 ± 3.78fmol/mg DNA to 276.33 ± 90.53 and 65.74 ± 16.27fmol/mg protein respectively. The serum estrogen (E) and progesterone (P) level declined apparently as compared with the control (E: from 108.81 ±30.28 to 69.20 ± 26. 42pg/ml; P: from 8.86±t 0.87 to 4.65±. 25ng/ml). The time course of the dynamic alteration of ERc and ERn after hydroxytamoxifen administration showed a similar pattern as compared with the result of the experiment in rat after treatment with hydroxyta- moxifen. The results of competition binding assay in vitro indicated that hydroxytamoxifen possessed the binding affinity for uterine ERc. These results suggest that the antiimplantaion effect of hydroxytamoxifen and the influences on the level of ER and PR may be mediated by the interaction between ER and hydroxytamoxifen antagonizing the action of estradiol- ER. They play an important role for the implantation.

关 键 词：着床 雌激素拮抗剂 羟泰米酚 雌二醇 受体 孕酮 

分 类 号：R979.21[医药卫生—药品]