米非司酮受体结合力及抗糖皮质激素活性的研究

目的:探讨米非司酮与孕激素受体及糖皮质激素受体相互作用的关系。方法:以放射配体结合实验测定米非司酮与家兔子宫胞浆孕激素受体及大鼠肝细胞浆糖皮质激素受体的相对结合亲和力。结果:与孕酮相比较,米非司酮的相对结合亲和力(RBA)为396.67±25.32,50%抑制浓度(IC50)为(6.61±1.20)nmol/L,P<0.01;与地塞米松相比较,米非司酮的RBA为344.41±57.41,50%IC50为(4.21±1.02)nmol/L,P<0.05。结论:米非司酮与孕激素受体的结合力强于孕酮,具有强的抗孕激素作用和一定的抗糖皮质激素作用。     

Glucocorticoids in T cell apoptosis and function

Glucocorticoids (GCs) are a class of steroid hormones which regulate a variety of essential biological functions. The profound anti-inflammatory and immunosuppressive activity of synthetic GCs, combined with their power to induce lymphocyte apoptosis place them among the most commonly prescribed drugs worldwide. Endogenous GCs also exert a wide range of immunomodulatory activities, including the control of T cell homeostasis. Most, if not all of these effects are mediated through the glucocorticoid receptor, a member of the nuclear receptor superfamily. However, the signaling pathways and their cell type specificity remain poorly defined. In this review, we summarize our present knowledge on GC action, the mechanisms employed to induce apoptosis and the currently discussed models of how they may participate in thymocyte development. Although our knowledge in this field has substantially increased during recent years, we are still far from a comprehensive picture of the role that GCs play in T lymphocytes. Received 20 August 2005; received after revision 27 September 2005; accepted 10 October 2005     

Tissue-specific modulation of rat glucocorticoid receptor binding activity by melatonin

The effect of melatonin and 2-Iodomelatonin on nuclear and cytosolic glucocorticoid receptors in the brain, pituitary, thymus and liver has been examined. The results indicate that both melatonin and 2-Iodomelatonin administration is associated with marked changes in the density and the affinity of cytosolic and nuclear forms of glucocorticoid receptors. These observations are discussed in the context of a possible involvement of pineal melatonin in the mechanisms regulating the behaviour and metabolism of steroid receptors.     

肾上腺糖皮质激素水平与肾病综合征相关性的临床研究

目的探讨肾上腺糖皮质激素水平与肾病综合征患者发病、预后的关系.方法采用放射免疫分析方法分组检测健康志愿者30例,肾病综合征患者组31例.结果两组血清皮质醇水平差异无统计学意义（P〉0.05）,但患有肾病综合征的血浆白蛋白降低程度极低的（〈20 g/L）患者其血清皮质醇水平偏低.经过激素治疗后,起效较慢,4～6周后24 ...     

大鼠股骨生物力学实验研究

通过三点弯曲实验研究肾上腺次全切除术对大鼠股骨弯曲力学特性的影响及不同剂量糖皮质激素替代治疗后对大鼠生物力学特性的影响．研究结果表明，肾上腺次全切除可导致大鼠股骨生物力学特性降低，其原因与糖皮质激素不足造成的骨丢失有关；其生物力学特性的降低表现为骨刚度较韧度变化更明显，在激素治疗中骨刚度的恢复较韧度迟缓；补充糖皮质激素对骨代谢有剂量依赖性调节作用．术后补充糖皮质激素对骨的生物力学性能恢复随药物剂量的加大而显著增加．     

Corticosterone activates Erk1/2 mitogen-activated protein kinase in primary hippocampal cells through rapid nongenomic mechanism

Nongenomic effects of glucocorticoids (GC) in various cell types have been well documented, but it still remains unknown whether the mechanism also works in hippocampus which is a crucial target of glucocorticoids in neural system during physiological and/or pathophysiological processes. We present here that corticosterone (B) could rapidly activate Erk1/2 mitogen-activated protein kinase (MAPK) in primarily cultured hippocampal cells within minutes, with a bell-shaped time dependent curve which peaked at 15min and then went down to normal level in 30 min. This activation was blocked by protein kinase C (PKC) inhibitor (Go6976), G protein inhibitor (GDPβs), and MEK(MAPK/extracellular signal-regulated kinase kinase) inhibitor(PD98059), but not by protein kinase A (PKA) inbibitor (H89), tyrosine kinase inhibitor (genistein), and glucocorticoid receptor ( GR ) antagonist (RU38486). Thus, the rapid activation of Erk1/2 MAPK in primary hippocampal cells induced by B was likely mediated by a G protein coupled receptor (GPCR) pathway with involvement of PKC, which belonged to the nongenomic rather than genomic mechanism of GC' s effects.