Giannopoulos G, Jackson K, Tulchinsky D
J Steroid Biochem. 1983 Sep;19(3):1375-8. doi: 10.1016/0022-4731(83)90166-8.
The binding of [3H]dexamethasone to cytosol fractions of human myometrium, endometrium, decidua, chorion, amnion and placenta has been studied. All tissues examined contained high affinity, low capacity binding sites with high specificity for glucocorticoids. Maximum specific binding of [3H]dexamethasone was reached after about 10 h at 0-4 degrees C and remained stable for at least the next 12 h. Sucrose density gradient analysis showed that the binding macromolecules sedimented at 7.9 S in hypotonic solutions and at 4.35 in solutions containing 0.4 M KCl. In the presence of sodium molybdate, the sedimentation coefficients shifted both in the absence and presence of 0.4 M KCl to 8.9 and 5.7 S, respectively. The apparent equilibrium dissociation constants (Kd) of the glucocorticoid binding sites were similar in most tissues, ranging between 1 and 6 nM, with the exception of the placenta in which the binding sites showed a higher Kd (13-22 nM). In all tissues studied, the binding affinities were similar in nonpregnant and pregnant patients and in patients at different stages of pregnancy or in labor. The concentration of the binding sites in the different tissues ranged from 11 to 268 fmol/mg protein, higher concentrations being found in myometrium, placenta and amnion and lower concentrations found in endometrium, chorion and decidua. The number of binding sites was higher in the myometrium of nonpregnant than pregnant women, but was similar in the myometrium of women at term pregnancy before or during labor. In the placenta, the number of binding sites increased significantly from early pregnancy to midpregnancy, while in chorion, amnion and decidua the number of binding sites did not change during pregnancy. It is concluded that human uterine tissues, placenta and fetal membranes contain specific binding sites with properties characteristic of glucocorticoid receptors suggesting that these tissues may respond directly to glucocorticoids.
对[3H]地塞米松与人子宫肌层、子宫内膜、蜕膜、绒毛膜、羊膜和胎盘的胞浆部分的结合进行了研究。所有检测的组织都含有对糖皮质激素具有高特异性的高亲和力、低容量结合位点。[3H]地塞米松在0 - 4℃下约10小时后达到最大特异性结合，并在接下来至少12小时内保持稳定。蔗糖密度梯度分析表明，结合大分子在低渗溶液中沉降系数为7.9 S，在含0.4 M KCl的溶液中为4.35 S。在钼酸钠存在下，无论有无0.4 M KCl，沉降系数分别变为8.9和5.7 S。糖皮质激素结合位点的表观平衡解离常数（Kd）在大多数组织中相似，范围在1至6 nM之间，但胎盘的结合位点Kd较高（13 - 22 nM）。在所有研究的组织中，非妊娠和妊娠患者以及处于妊娠不同阶段或分娩期患者的结合亲和力相似。不同组织中结合位点的浓度范围为11至268 fmol/mg蛋白质，子宫肌层、胎盘和羊膜中的浓度较高，而子宫内膜、绒毛膜和蜕膜中的浓度较低。非妊娠女性子宫肌层中的结合位点数量高于妊娠女性，但足月妊娠女性分娩前或分娩期间子宫肌层中的结合位点数量相似。在胎盘中，结合位点数量从妊娠早期到妊娠中期显著增加，而在绒毛膜、羊膜和蜕膜中，结合位点数量在妊娠期间没有变化。结论是，人子宫组织、胎盘和胎膜含有具有糖皮质激素受体特性的特异性结合位点，表明这些组织可能直接对糖皮质激素产生反应。
