Lee J W, Lee H J
J Steroid Biochem. 1985 Dec;23(6A):943-8. doi: 10.1016/0022-4731(85)90051-2.
The competitive binding of two new classes of anti-inflammatory steroids, the esters and amides derived from the epimers of 20 zeta-dihydroprednisolonic acid, to cytosol receptors from rat liver and thymus was studied. The relative inhibition of [3H]dexamethasone binding by the steroid derivatives was the same, irrespective of the receptor source, with the following order: dexamethasone greater than prednisolone greater than methyl 17,20 alpha-acetonidodihydroprednisolonate greater than methyl 17,20 beta-acetonidodihydroprednisolonate greater than N-propyl 20 alpha-dihydroprednisolonamide greater than methyl 20 alpha-dihydroprednisolonate greater than methyl 20 beta-dihydroprednisolonate greater than N-propyl 20 beta-dihydroprednisolonamide. The alpha-epimer of the steroids always showed a higher binding affinity than the corresponding beta-epimer. In an acute pharmacological study, prednisolone induced the suppression of plasma corticosterone and an increase in tyrosine aminotransferase activity and glycogen content of rat liver. The esters and amides had no effect on these parameters except in the case of the acetonide derivatives of the steroid acid esters which slightly increased liver glycogen content.
研究了两类新型抗炎甾体（即20ζ-二氢泼尼松龙酸差向异构体衍生的酯类和酰胺类）与大鼠肝脏和胸腺胞浆受体的竞争性结合。无论受体来源如何，甾体衍生物对[3H]地塞米松结合的相对抑制作用相同，顺序如下：地塞米松＞泼尼松龙＞17,20α-亚甲基二氢泼尼松龙酸甲酯＞17,20β-亚甲基二氢泼尼松龙酸甲酯＞N-丙基20α-二氢泼尼松龙酰胺＞20α-二氢泼尼松龙酸甲酯＞20β-二氢泼尼松龙酸甲酯＞N-丙基20β-二氢泼尼松龙酰胺。甾体的α-差向异构体总是比相应的β-差向异构体表现出更高的结合亲和力。在一项急性药理学研究中，泼尼松龙可导致大鼠血浆皮质酮水平降低，肝脏酪氨酸转氨酶活性及糖原含量升高。除甾体酸酯的亚甲基衍生物可使肝脏糖原含量略有增加外，酯类和酰胺类对这些参数均无影响。
