Mayer M, Shafrir E, Kaiser N, Milholland R J, Rosen F
Metabolism. 1976 Feb;25(2):157-67. doi: 10.1016/0026-0495(76)90046-9.
The mechanism of action of glucocorticoid hormones on rat skeletal muscle was studied by following their effect on muscle weight, free amino acid content, activity of amino acid-metabolizing enzymes, and binding to cytoplasmic receptor proteins. A significant reduction of gastrocnemius muscle and body weight occurred following administration of cortisol, triamcinolone diacetate, and triamcinolone acetonide to adrenalectomized rats. Treatment with triamcinolone diacetate also reduced the level of several free amino acids and enhanced the activity of a myofibrillar protease in skeletal muscle. The hormone had, however, no effect on the activity of various enzymes involved in amino acid catabolism in muscle. In nephrosis, another condition of muscle wasting, the level of several muscle amino acids were also reduced to a lesser extent. Cortisol and triamcinolone acetonide, both of which induce muscle wasting, were found to bind to two distinct cytoplasmic proteins in muscle. Binding of the labeled hormones was followed at 0 C and could be observed in presence of a 1000-fold excess of the catabolically inactive steroid epicortisol. Binding of 3H-triamcinolone acetonide. In vitro competition experiments further suggest a correlation between steroid binding to the 3H-dexamethasone or 3H-triamcinolone acetonide site and their potency to induce muscle catabolism. It is concluded that skeletal muscle is a direct target organ for glucocorticoids, and that muscle responsiveness involves binding of the active hormones to cytoplasmic receptor sites.
通过观察糖皮质激素对大鼠骨骼肌重量、游离氨基酸含量、氨基酸代谢酶活性以及与细胞质受体蛋白结合的影响,研究了糖皮质激素对大鼠骨骼肌的作用机制。给肾上腺切除的大鼠注射皮质醇、二醋酸曲安西龙和曲安奈德后,腓肠肌和体重显著降低。二醋酸曲安西龙治疗还降低了几种游离氨基酸的水平,并增强了骨骼肌中肌原纤维蛋白酶的活性。然而,该激素对肌肉中参与氨基酸分解代谢的各种酶的活性没有影响。在另一种肌肉萎缩疾病——肾病中,几种肌肉氨基酸的水平也有不同程度的降低。发现能诱导肌肉萎缩的皮质醇和曲安奈德可与肌肉中的两种不同细胞质蛋白结合。在0℃下追踪标记激素的结合情况,并且在存在1000倍过量的分解代谢无活性的类固醇表皮质醇的情况下也能观察到结合。3H-曲安奈德的结合。体外竞争实验进一步表明,类固醇与3H-地塞米松或3H-曲安奈德位点的结合与其诱导肌肉分解代谢的能力之间存在相关性。得出的结论是,骨骼肌是糖皮质激素的直接靶器官,并且肌肉反应性涉及活性激素与细胞质受体位点的结合。