Yoshida A, Taniguchi S, Mitani Y, Ueda Y, Urabe K, Adachi T, Shigemasa C, Abe K, Mashiba H
1st Department of Internal Medicine, Tottori University School of Medicine, Yonago, Japan.
Horm Metab Res. 1988 Sep;20(9):566-9. doi: 10.1055/s-2007-1010886.
To clarify the in vivo events following administration of steroid hormones, the effect of molybdate on the cytoplasmic glucocorticoid receptor (GR) translocation in rat livers after administration of glucocorticoids was examined. After injection of hydrocortisone-succinate (Hydro) (200 micrograms/150 g rat) into the inferior vena cava of adrenalectomized rats, 3H-dexamethasone (3H-Dex) binding in liver cytosol rapidly decreased within 5 min, followed by a rapid replenishment. This decrease in binding was partially prevented by pre-treating the animals with 20 mg of sodium molybdate (Mo), which was considered to inhibit GR activation. Administration of 200 micrograms/150 g body weight of hydrocortisone caused a rapid replenishment of the binding sites following the depletion. Administration of molybdate 5 min after the hydrocortisone injection did not influence the replenishment. The GR content was increased significantly 20 min after the administration of molybdate in intact rats but not in adrenalectomized rat. It is concluded that activation of the hormone receptor complex observed in vitro also occurs in vivo after administration of glucocorticoid to animals.
为了阐明给予甾体激素后的体内事件，研究了钼酸盐对给予糖皮质激素后大鼠肝脏细胞质糖皮质激素受体（GR）转位的影响。将氢化可的松琥珀酸钠（Hydro）（200微克/150克大鼠）注入肾上腺切除大鼠的下腔静脉后，肝细胞质中3H-地塞米松（3H-Dex）的结合在5分钟内迅速下降，随后迅速补充。这种结合的下降部分被用20毫克钼酸钠（Mo）预处理动物所阻止，这被认为抑制了GR的激活。给予200微克/150克体重的氢化可的松导致耗尽后结合位点的迅速补充。氢化可的松注射5分钟后给予钼酸盐不影响补充。在完整大鼠中给予钼酸盐20分钟后GR含量显著增加，但在肾上腺切除大鼠中未增加。得出的结论是，体外观察到的激素受体复合物的激活在给予动物糖皮质激素后在体内也会发生。
