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目的:研究甲基hispolon的雌激素样作用,为寻找良好的雌激素替代药物提供依据。方法:通过细胞增殖实验检测甲基hispolon的雌激素作用和抗雌激素作用;采用酶联免疫法检测甲基hispolon对去氧乙烯基环己烯(VCD)处理的卵巢早衰SD大鼠血清中E_2的影响,并考察其对子宫和卵巢组织病理学的研究。结果:计算机分子对接模拟甲基hispolon与雌激素受体有较强的结合能力。体外细胞增殖实验表明,10~(-8)~10~(-6)mol/L甲基hispolon能刺激MCF-7细胞的增殖,具有雌激素样作用,而对MAD-MB-231无明显影响;在10~(-8)~10~(-4)mol/L能抑制E_2诱导的MCF-7细胞的增殖,具有抗雌激素作用;ICI182,780能阻断甲基hispolon在10~(-7)~10~(-5)mol/L时对MCF-7细胞的增殖作用。体内实验结果显示甲基hispolon在1.25~5 mg/kg能增加卵巢早衰SD大鼠血清中E_2的水平;病理检查结果表明,甲基hispolon能增加卵巢内正常卵泡的数量,改善卵巢早衰病理变化。结论:甲基hispolon有雌激素样作用,具有替代雌激素药用的前景。
OBJECTIVE: To study the estrogen-like effect of methylprednisolide and to provide a basis for finding a good estrogen replacement drug. Methods: The estrogen and antiestrogen of methylphepolon were detected by cell proliferation assay. The levels of E_2 in serum of premature ovarian failure rats treated with desoxyvinylcyclohexene (VCD) were detected by enzyme - linked immunosorbent assay And investigate its effects on histopathology of uterus and ovary. Results: Computer molecular docking simulated methyl hispolon with estrogen receptor has strong binding ability. The in vitro cell proliferation assay showed that histidine at 10 -8 -8 mol / L stimulated the proliferation of MCF-7 cells with estrogen-like activity but had no effect on MAD-MB-231 ; 10 ~ (-8) ~ 10 ~ (-4) mol / L could inhibit E_2-induced proliferation of MCF-7 cells with anti-estrogen effect; ICI182,780 can block methyl hispolon in 10 ~ (- 7) ~ 10 ~ (-5) mol / L on the proliferation of MCF-7 cells. In vivo experiments showed that histidine at 1.25-5 mg / kg increased the level of E_2 in serum of SD rats with premature ovarian failure. Methyl hispolon increased the number of normal follicles in ovary and the pathological changes of premature ovarian failure. Conclusion: Methylphepolon has estrogen - like effect and has the prospect of replacing estrogen.