酪氨酸酶抑制剂对生育期雌性大鼠的抗生育效应研究

目的:动物实验观察酪氨酸酶抑制剂对生育期雌性大鼠的抗生育效应。方法:将90只检查阴栓为阳性的小鼠随机分为3组,每组30只。低剂量组每日灌胃大豆异黄酮40mg·kg-1·d-1;高剂量组每日灌胃大豆异黄酮80mg·kg-1·d-1,正常对照组每日灌胃等量生理盐水。于D4观察囊胚和胚胎个数,D6观察着床胚胎数,D20剖腹检查活胎数。结果:D4正常对照组、低剂量组和高剂量组的囊胚发育率分别为84.8%(106/125),65.63%(84/128),62.4%(78/125)。D6正常对照组、低剂量组和高剂量组的平均着床胚胎数分别为5.25个,1.71个和1.33个。D20剖宫取胎,正常对照组、低剂量组和高剂量组的平均活胎数分别为4.6个,0.9个和0.7个。3组相比较,正常对照组的囊胚发育率、平均着床胚胎数和平均活胎数显著高于低剂量组和高剂量组(P<0.05)。结论:大豆异黄酮作为一种酪氨酸酶抑制剂,可抑制生育期的雌性小鼠胚泡的发育和胚胎着床,但具体剂量和机制需进一步深入研究。     

Evaluation of khat (Catha edulis Forssk) for antifertility activity in rats

The effect of the methanolic extract of khat (Catha edulis Forssk) was studied on female fertility in rats. The parameters included the effect on oestrus cycle, implantation, foetal loss, abortion, inhibition of uterotrophic activity and teratogenicity. The extract, in the doses of 250 and 500 mg/kg, produced dose dependent and significant anti-implantation activity. However, it failed to produce complete infertility in this dose range. Treatment of animals during day 8 to day 12 of pregnancy produced significant abortifacient activity. There was significant decrease in the weight and length of foetuses delivered by rats treated with the extract but there were no gross abnormalities in the organs of the offsprings. It also produced significant anti-oestrogenic activity as assessed by the mean weight of the uteri of rats treated with oestradiol and its combination with the khat extract.     

米非司酮对大鼠的抗着床作用研究

研究了米非司酮对大鼠的抗着床作用。大鼠在妊娠d1、d2或d3口服米非司酮10mg/kg,每天1次,连续3d,有显著的抗着床作用、大鼠妊娠d1单次给米非司酮40mg/ks无抗着床作用,妊娠d2给40mg/ks,d3给10mg/kg有显著的抗着床作用。给药组大鼠子宫内膜发育延迟,蜕膜不能形成,影响孕卵着床。     

炔诺酮肟对家兔卵巢作用的形态学研究

家兔从妊娠第1天始,每天经口给予炔诺酮肟4mg/kg,连续3天,第9天处死。取卵巢作HE、ACP、ALP、SDH及3β-HSD染色,部分卵巢作超微结构观察。结果表明:炔诺酮肟呈明显的抗着床作用,卵巢黄体平坦,缩小。光镜观察,黄体细胞呈较明显的颗粒变性及空泡变性。组化染色,ACP活性增强(P<0.01)。3β-HSD活性减弱(P<0.01),ALP及SDH活性无明变化(P>0.05)。超微结构可见,黄体细胞胞质中滑面内质网明显减少,脂滴聚集,溶酶体数量增多,形状多样,脂质空泡化及类似髓鞘样结构等。提示由于药物抑制了卵巢3β-HSD活性,使卵巢激素生物合成受阻;此外,ACP活性增加,提示溶酶体通透性增加。     

Postcoital administration of asoprisnil inhibited embryo implantation and disturbed ultrastructure of endometrium in implantation window in mice

Asoprisnil, a member of the selective progesterone receptor modulators, exerts high progesterone receptor selectivity, endometrial targeted advantages and significant anti-implantation effect in rats. The purpose of this study was to confirm the anti-implantation effect of asoprisil, investigate the ultrastructural changes of the peri-implantation endometrium in mice and explore the effect of asoprisnil on endometrial receptivity and its targeted contraceptive proficiency. Post-coitus mice were administered with different dosages (0.2, 0.1, 0.05 mg·g -1 ·day -1 ) of asoprisnil from day 1 of pregnancy to day 3. Then 3 animals in each group were killed on day 5 of pregnancy, and uteri were collected to examine the ultrastructural changes of endometria under a transmission electron microscope (TEM). A total of 80 animals were sacrificed on day 8 of pregnancy, and the uterine horns were examined for the presence or absence of nidation sites and the number of implantation embryos. The results showed that the implantation rate and the average number of implantation embryos in asoprisnil groups were statistically significantly decreased as compared with the vehicle control group (P<0.05). The TEM results revealed that, in vehicle control group, the tight junction between the luminal epithelia cells was short and straight, the gap was wide; the luminal epithelia cells were covered with plenty of short, clavate and neatly arranged microvilli; the endometril stromal cells were large with plenty of cytoplasm, and showed significant decidual change; there was more than one nucleus in stromal cells, and the karyotheca was integrity. In low dosage and high dosage asoprisnil groups, the tight junction was longer and more curve than in the vehicle control group; microvilli were uneven and asymmetrically distributed in luminal epithelia; the stromal cells were small and the decidual change was not significant; there were karyopyknosis and karyolysis in stromal cells; there were abnormal thick-wall vessels in the endometrium. It was suggested that asoprisnil changed the ultrastructure of the endometrium in implantation window, disturbed the endometrial receptivity and finally resulted in embryo implantation failure.     

炔诺酮肟与炔诺酮抗着床作用的比较及其对卵巢孕酮分泌的影响

本文比较了炔诺酮肟与炔诺酮对大鼠,金地鼠及家兔3种动物的抗着床作用,用放射免疫法测定了两药引起大鼠卵巢静脉血中孕酮含量的变化。结果显示:随动物种属不同,炔诺酮肟的抗着床作用比母体炔诺酮强2～10倍。最小100％抗着床剂量的炔诺酮肟能抑制大鼠卵巢分泌孕酮,其作用比同等剂量的炔诺酮明显增强。提示炔诺酮A环三位酮基肟化能提高炔诺酮的抗着床作用,并增强其对卵巢孕酮生物合成的抑制。     

怀牛藤总皂甙抗生育作用及其机理

给小鼠灌服怀牛藤总皂甙（ABS）75，150，300mg／kg，表明ABS具有明显的抗着床、抗早孕作用，且呈剂量依赖性关系，其ED50分别为96±27和145±51mg／kg。ABS的抗早孕作用，可被外源性黄体酮、人绒毛膜促性腺激素和泰必利部分拮抗。ABS300mg／kg可显著抑制假孕小鼠和去卵巢小鼠的子宫蜕膜细胞反应，但无雌激素样作用和抗雌激素样作用。     

环硫雄醇对鼠生殖功能的影响

环硫雄醇为抗乳腺癌药物,具有明显抗雌激素作用。为探讨该药对生殖功能的影响,本研究系用雌性小鼠进行环硫雄醇的抗着床及抗早孕实验;同时,将该药用于雌性大白鼠,测定其对子宫孕激素活性与血清孕激素水平的影响。结果表明:该药对雌性小鼠有明显的抗着床作用,但无明显抗早孕作用;对大白鼠子宫孕激素活性可能有增进作用,而对血清孕激素水平有下降的影响。     

家兔抗着床实验中炔诺酮肟对子宫内膜影响的形态学研究

家兔从妊娠第1天开始,每天灌服炔诺酮肟4mg/kg,连续3天,第9天处死。取子宫作HE、PAS、ACP、AKP及SDH染色。结果表明,炔诺酮肟呈明显的抗着床作用。光镜观察,子宫内膜呈退行性改变,蜕膜化减弱。组织化学染色,AKP活性减弱(P<0.05),糖原含量下降(P<0.01),ACP及SDH活性无明显变化。提示:给药后子宫内膜生长发育受抑制、代谢降低,致使胚泡与子宫内膜不能同步,可能与抗着床机理有关。     

Post-Coital Antifertility Activity of Hibiscus rosa-sinensis Linn. roots

Ancient literature mentions the use of a number of plants/preparationsfor fertility regulation. Some local contraceptive agents havealso been described in Ayurvedic and Unani texts. Documentedexperiments or clinical data are, however, lacking. Therefore,the present study was undertaken to explore the antifertilityand estrogenic activity of ethanolic extract of the roots ofHibiscus rosa-sinensis Linn. A strong anti-implantation (inhibition100%) and uterotropic activity was observed at the dose levelof 400 mg/kg body weight. Histological studies were carriedout to confirm this effect.