米非司酮对动物子宫、肝脏胞浆受体结合力的影响  

Effect of Mifepristone on Progesterone and Glucocorticoid Receptor Binding Affinities of Different Animals

作　　者：潘燕[1] 程英惠 熊忠明[1] 田红[1] 胡艳群[1] 肖慧珠[1] 吴昌杰[1] 朱长虹[1] 

机构地区：[1]华中科技大学同济医学院计划生育研究所,武汉430030 [2]湖北省孝感市孝南区妇幼保健院,孝感432100

出　　处：《华中科技大学学报（医学版）》2004年第6期683-686,共4页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

摘　　要：目的　从受体药理特性上分析米非司酮的抗生育作用及与糖皮质激素的作用。方法　应用放射配体结合检测技术 ,以3 H R5 0 2 0和3 H 地塞米松作为示踪物 ,采用饱和竞争性抑制分析方法 ,观察米非司酮与兔、猕猴子宫胞浆孕激素受体及大鼠肝脏糖皮质激素受体结合特性。结果　米非司酮可与兔、猕猴子宫胞浆孕激素受体牢固结合 ,很小剂量就可抑制3 H R5 0 2 0与孕激素受体结合。兔子宫孕激素受体结合实验所用米非司酮与孕酮的IC50 (5 0 %抑制浓度 )值分别为 6 6 1nmol/L、 2 6 2 0nmol/L ,差异有极显著性意义 (P <0 0 1) ,RBA (相对结合力 )为孕酮的 4 0倍 ;猕猴子宫胞浆孕激素受体结合实验中米非司酮与孕酮的IC50 值分别为 17 2 0、 30 2 0nmol/L ,差异有显著性意义 (P <0 0 5 ) ,其RBA为孕酮的 1 8倍。米非司酮可与大鼠肝脏胞浆糖皮质激素受体结合 ,较低浓度范围内就可抑制地塞米松与糖皮质激素受体结合 ,米非司酮、地塞米松的IC50 分别为 4 2 1、 14 5 0nmol/L ,RBA为地塞米松的 3 4倍。结论　对孕激素受体药理特性进行评估 ,米非司酮与孕激素受体有很强的亲和力 ,表现为较强的抗孕激素作用。以孕激素受体结合力为参照标准 ,显示米非司酮对孕激素受体结合力强度明显强于米非司酮对糖皮质激素受体结?Objective To determine the effect of mifepristone on progestero ne and glucocorticoid receptor binding affinities of different animals. Methods By using radioligand binding assay, the receptor bindin g affinities of mifepristone to rabbit, rhesus monkey uterus cytosol progesteron e receptor and rat liver cytosol glucocorticoid receptor were measured. Results 3H-R5020 and mifepristone could bind specifically to the progesterone receptor. In the experiment of rabbit uterus cytosol progester one receptor, the IC 50 values of mifepristone and progesterone were 6.61 nmol/L and 26.20 nmol/L respectively with the difference being significant. The relative binding affinities (RBA) of mifepristone were 4.0 times as high as RB A of progesterone. In the experiment of rhesus monkey uterus cytosol progesteron e receptor, the IC 50 values of mifepristone and progesterone were17.20 nm ol/L and 30.20 nmol/L respectively with the difference being significant too. T he RBA of mifepristone were 1.8 times as high as RBA of progesterone. 3H-Dex amethasone could bind specifically to the glucocorticoid receptor. The IC 50 values of mifepristone and dexamethasone were 4.21 and14.50 nmol/L respecti vely. RBA of mifepristone were 3.4 times as high as RBA of dexamethasone. Conclusion Mifepristone had high binding affinities to progeste rone receptor and it could strongly block the binding of progesterone to uterus progesterone receptor. In contrast to the data obtained with the the progestin R BA, the intensity of RBA of progestin receptor was higher than glucocorticoid re ceptor.

关 键 词：米非司酮 孕激素受体 胞浆 子宫 糖皮质激素受体 地塞米松 孕酮 猴子 猕猴 动物 

分 类 号：R737[医药卫生—肿瘤] R169.42[医药卫生—临床医学]