Vicent G P, Burton G, Ghini A, Lantos C P, Galigniana M D
Departamento de Química Biológica and PRHOM-CONICET, Universidad de Buenos Aires, Argentina.
J Steroid Biochem Mol Biol. 1998 Aug;66(4):211-6. doi: 10.1016/s0960-0760(98)00040-5.
The following in vitro glucocorticoid (GC) parameters of progesterone (P), 1-ene progesterone (deltaP), 11beta-hydroxyprogesterone (HOP), 11beta-1-ene progesterone (deltaHOP) and dexamethasone (Dexa) were assayed in the presence or absence of bovine calf serum (BCS): binding to thymus cytosol, dissociation of the glucocorticoid receptor (GR)-heat shock protein 90 (hsp90) complex (diss.), tyrosine aminotransferase (TAT) induction in hepatocytes and the inhibition of 3H-uridine and 35S-methionine uptake by thymocytes. Without BCS, steroids were in most cases active in this general order: Dex > deltaHOP > HOP > deltaP > P. BCS abolished all activities in P and deltaP, but left them unaltered in all other steroids, except diss. in HOP, which diminished intermediately. Binding of P, deltaP, HOP and deltaHOP to GR and CBG paralleled their in vivo activating effects on glycogen deposition.
in this steroid series, BCS, but not CBG, inhibits GC responses of P and deltaP. 11-Beta hydroxylation frees those molecules from the inhibitory effects of BCS.
在存在或不存在牛血清（BCS）的情况下，检测了孕酮（P）、1-烯孕酮（δP）、11β-羟基孕酮（HOP）、11β-1-烯孕酮（δHOP）和地塞米松（Dexa）的以下体外糖皮质激素（GC）参数：与胸腺细胞质的结合、糖皮质激素受体（GR）-热休克蛋白90（hsp90）复合物的解离（解离）、肝细胞中酪氨酸转氨酶（TAT）的诱导以及胸腺细胞对3H-尿苷和35S-甲硫氨酸摄取的抑制。在没有BCS的情况下，大多数情况下类固醇的活性顺序如下：地塞米松>DδHOP>HOP>δP>P。BCS消除了P和δP的所有活性，但在所有其他类固醇中使其保持不变，除了HOP中的解离，其活性中度降低。P、δP、HOP和δHOP与GR和CBG的结合与其体内对糖原沉积的激活作用平行。
在该类固醇系列中，BCS而非CBG抑制P和δP的GC反应。11-β羟基化使这些分子免受BCS的抑制作用。
