糖皮质激素可能通过抑制环磷酸腺苷磷酸二酯酶参与环磷酸腺苷水平的升高。
Possible participation of glucocorticoid in elevation of 3',5'-cyclic AMP levels through inhibition of cyclic AMP phosphodiesterase.
作者信息
Tanigawa Y, Kitamura A, Kawamura M, Shimoyama M, Fujii K, Kohri Y, Ueda I
出版信息
Physiol Chem Phys. 1978;10(5):443-8.
Administration of prednisolone and cholate to rats elevated levels of cAMP (adenosine 3',5'-cyclic monophosphate) by 1.5- to 2.0-fold. Compounds such as prednisolone, hydrocortisone, cholate, and deoxycholate were found to be potent inhibitors of partially purified cAMP phosphodiesterase prepared from rat liver. Kinetic analysis showed that the prednisolone inhibition was noncompetitive with a Ki of 8.9 x 10(-4) M. These results suggest that in addition to increasing DNA-dependent RNA polymerase activity in vivo, a large application of glucocorticoid may incur elevation of intracellular cAMP levels.
给大鼠注射泼尼松龙和胆酸盐可使环磷酸腺苷（cAMP）水平升高1.5至2.0倍。已发现泼尼松龙、氢化可的松、胆酸盐和脱氧胆酸盐等化合物是从大鼠肝脏制备的部分纯化的cAMP磷酸二酯酶的有效抑制剂。动力学分析表明，泼尼松龙的抑制作用是非竞争性的，抑制常数（Ki）为8.9×10⁻⁴M。这些结果表明，除了在体内增加依赖DNA的RNA聚合酶活性外，大量应用糖皮质激素可能会导致细胞内cAMP水平升高。
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