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No correlation between binding of glucocorticosteroids to specific cytoplasmic proteins in vivo and enzyme induction in the rat liver

机译:糖皮质激素与体内特定细胞质蛋白的结合与大鼠肝脏中的酶诱导之间没有相关性

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pTime- and dose-dependence of the formation of the different cytoplasmic hormone-protein complexes were studied in the rat liver after administration in vivo of [3H]cortisol or [3H]dexamethasone and compared with the stimulation of RNA polymerase B and induction of tyrosine aminotransferase and tryptophan oxygenase. No correlation could be found between formation in vivo of any of the five cytoplasmic hormone-protein complexes found and stimulation of RNA polymerase B activity or enzyme induction. After administration of [3H]cortisol, different metabolites of cortisol could be demonstrated in the isolated hormone-protein complexes. No time- or dose-dependence of the metabolite patterns could be observed after application of hormone doses that were in the range of the biologically active doses. After administration of [3H]dexamethasone, the same hormone-protein complexes were observed, which contained, however, the injected steroid instead of metabolites. These results seem to indicate that the cytoplasmic binding components present in the rat liver are enzymes involved in the metabolism of the glucocorticosteroids and that dexamethasone binds to these enzymes as a substrate analogue./p
机译:在体内施用[3H]皮质醇或[3H]地塞米松后,在大鼠肝脏中研究了不同细胞质激素-蛋白质复合物形成的时间和剂量依赖性,并与刺激RNA聚合酶B和诱导酪氨酸转氨酶和色氨酸加氧酶。在体内发现的五种细胞质激素-蛋白质复合物中的任何一种的体内形成与RNA聚合酶B活性或酶诱导的刺激之间均未发现相关性。服用[3H]皮质醇后,可以在分离的激素-蛋白质复合物中显示皮质醇的不同代谢产物。在应用处于生物活性剂量范围内的激素剂量后,未观察到代谢产物模式的时间或剂量依赖性。施用[3H]地塞米松后,观察到相同的激素-蛋白质复合物,但其中包含注射的类固醇而不是代谢产物。这些结果似乎表明,大鼠肝脏中存在的胞质结合成分是糖皮质激素代谢中涉及的酶,地塞米松作为底物类似物与这些酶结合。

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