Oszter A, Vértes Z, Töröcsik B, Környei J L, Kovács K A, Vértes M
Medical Faculty, Institute of Physiology, University of Pécs, Szigeti str.12, H-7643, Pécs, Hungary.
J Steroid Biochem Mol Biol. 2000 Sep;74(1-2):25-32. doi: 10.1016/s0960-0760(00)00085-6.
The effects of a single injection or continuous infusion of opioid peptide, [D-Met(2),pro(5)]enkephalinamide (ENK) on the hormone binding and transcriptional properties of estrogen receptors were investigated in estradiol (E(2)) treated rat uterus. The level of estrogen- (ER) and progesterone receptor (PR) proteins, the hormone binding of E(2) receptors and the effects of single injection of ENK with or without naltrexone (NAL) on the E(2)-induced changes in the level of Fos and Jun proteins and the binding of AP-1 proteins to DNA were studied. The receptor proteins levels were determined by Western blots and the binding of AP-1 to DNA by electrophoretic mobility shift assay. Both the ER and PR protein concentrations and the [3H]Estradiol binding to the high affinity nuclear receptors decreased after ENK treatment during the first two days. At 72 h the PR concentration decreased further, while no significant changes were found in the level of ER, however, at this time the former competitive E(2) binding turned into positive cooperativity. The E(2)-induced increase in the level of Fos proteins and the binding of AP-1 proteins to DNA was inhibited by a single injection of ENK. We conclude that the endogenous opioid peptides may interact with E(2) in the gene regulation of rat uterus.
研究了在经雌二醇（E₂）处理的大鼠子宫中，单次注射或持续输注阿片肽[D-蛋氨酸（2），脯氨酸（5）]脑啡肽酰胺（ENK）对雌激素受体的激素结合和转录特性的影响。研究了雌激素受体（ER）和孕激素受体（PR）蛋白水平、E₂受体的激素结合情况，以及单次注射ENK（有无纳曲酮（NAL））对E₂诱导的Fos和Jun蛋白水平变化以及AP-1蛋白与DNA结合的影响。通过蛋白质免疫印迹法测定受体蛋白水平，通过电泳迁移率变动分析测定AP-1与DNA的结合情况。在ENK处理后的前两天，ER和PR蛋白浓度以及[³H]雌二醇与高亲和力核受体的结合均降低。在72小时时，PR浓度进一步降低，而ER水平未发现显著变化，然而此时前者的竞争性E₂结合转变为正协同作用。单次注射ENK可抑制E₂诱导的Fos蛋白水平升高以及AP-1蛋白与DNA的结合。我们得出结论，内源性阿片肽可能在大鼠子宫的基因调控中与E₂相互作用。
