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目的初步研究异黄改构化合物F11的雌激素效应。方法构建去双卵巢大鼠动物模型,经腹腔注射F11[15、50、150 mg/(kg.d)3个剂量组(F11-15组、F11-50组、F11-150组)]共10周,同时设置阴性对照组,阳性对照组(E2)和假手术组,统计分析各组大鼠子宫湿质量/体质量情况,HE染色观察用药前后阴道涂片和子宫内膜变化情况;Westernblot检测子宫内膜组织ERα和ERβ的表达情况。结果 F11-50及F11-150组大鼠子宫湿质量/体质量显著高于阴性对照组(P<0.05),且F11-150组与E2和假手术组无显著差别(P>0.05)。阴性对照组大鼠阴道涂片以炎细胞为主,F11各组以角化上皮细胞为主,与E2和假手术组相似;F11各组较阴性对照组子宫内膜腺体数目增多,腺腔增大,F11-150组与E2和假手术组相似。F11各组ERα及ERβ蛋白表达均强于阴性对照组(P<0.05),其中ERα表达弱于E2和假手术组(P<0.01),而F11-150组ERβ的表达强于E2和假手术组(P<0.05)。结论 F11在增加去双卵巢大鼠子宫湿质量、阴道上皮成熟及子宫内膜ER的表达等方面均表现出雌激素效应,该效应主要通过ERβ介导。
Objective To study the estrogen effect of isoflavone modified compound F11. Methods The ovariectomized rats were divided into three groups (F11-15, F11-50, F11-150) by intraperitoneal injection of F11 [15, 50, 150 mg / (kg · d) Weeks, at the same time set the negative control group, positive control group (E2) and sham operation group, statistical analysis of each group of uterine wet weight / body weight, HE staining before and after treatment of vaginal smear and endometrial changes; Westernblot detection Endometrial tissue ERα and ERβ expression. Results The wet weight and body weight of rats in F11-50 and F11-150 groups were significantly higher than those in the negative control group (P <0.05). There was no significant difference between F11-150 group and E2 and sham operation group (P> 0.05). Negative control group of vaginal smears to inflammatory cells, F11 keratinocyte epithelial cells, and E2 and sham-operated group similar; F11 than the negative control group increased the number of endometrial glands, glandular cavity Increased, F11-150 group and E2 and sham group similar. The expression of ERα and ERβ in F11 groups were stronger than that in the negative control group (P <0.05), and the expression of ERα in the F11-150 group was weaker than that in the E2 and sham operation groups (P <0.01) Group (P <0.05). Conclusion F11 shows estrogen effect in increasing uterine wet weight, vaginal epithelial maturation and endometrial ER expression in ovariectomized rats, which is mainly mediated by ERβ.