Daza F J, Parrilla R, Martín-Requero A
Department of Pathophysiology and Human Molecular Genetics, Centro de Investigaciones Biológicas (CSIC), Velázques 144, Madrid-28006, Spain.
Biochem J. 1998 Apr 1;331 ( Pt 1)(Pt 1):89-97. doi: 10.1042/bj3310089.
This work aimed to investigate the acute effect of the thyroid hormone 3,5,3'-tri-iodo-L-thyronine (T3) in regulating the hepatic metabolism either directly or by controlling the responsiveness to Ca2+-mobilizing agonists. We did not detect any acute metabolic effect of T3 either in perfused liver or in isolated liver cells. However, T3 exerted a powerful inhibitory effect on the alpha1-adrenoreceptor-mediated responses. The promptness of this T3 effect rules out that it was the result of rate changes in gene(s) transcription. T3 inhibited the alpha1-adrenoreceptor-mediated sustained stimulation of respiration and release of Ca2+ and H+, but not the glycogenolytic or gluconeogenic responses, in perfused liver. In isolated liver cells, T3 enhanced the alpha1-agonist-induced increase in cytosolic free Ca2+ and impeded the intracellular alkalinization. Since T3 also prevented the alpha1-adrenoreceptor-mediated activation of protein kinase C, its effects on pH seem to be the result of a lack of activation of the Na+/H+ exchanger. The failure of T3 to prevent the alpha1-adrenergic stimulation of gluconeogenesis despite the inhibition of protein kinase C activation indicates that the elevation of cytosolic free Ca2+ is a sufficient signal to elicit that response. T3 also impaired some of the angiotensin-II-mediated responses, but did not alter the effects of PMA on hepatic metabolism, indicating, therefore, that some postreceptor event is the target for T3 actions. The differential effect of T3 in enhancing the alpha1-adrenoreceptor-mediated increase in cytosolic free Ca2+ and preventing the activation of protein kinase C, provides a unique tool for further investigating the role of each branch of the signalling pathway in controlling the hepatic functions. Moreover, the low effective concentrations of T3 (<= 10 nM) in perturbing the alpha1-adrenoreceptor-mediated response suggests its physiological significance.
这项工作旨在研究甲状腺激素3,5,3'-三碘-L-甲状腺原氨酸(T3)直接或通过控制对Ca2+动员激动剂的反应性来调节肝脏代谢的急性效应。我们在灌注肝脏或分离的肝细胞中均未检测到T3的任何急性代谢效应。然而,T3对α1-肾上腺素能受体介导的反应具有强大的抑制作用。这种T3效应的迅速性排除了它是基因转录速率变化结果的可能性。在灌注肝脏中,T3抑制α1-肾上腺素能受体介导的呼吸持续刺激以及Ca2+和H+的释放,但不抑制糖原分解或糖异生反应。在分离的肝细胞中,T3增强了α1-激动剂诱导的胞质游离Ca2+增加,并阻碍了细胞内碱化。由于T3还阻止了α1-肾上腺素能受体介导的蛋白激酶C激活,其对pH的影响似乎是由于Na+/H+交换体缺乏激活所致。尽管抑制了蛋白激酶C激活,但T3未能阻止α1-肾上腺素能刺激的糖异生,这表明胞质游离Ca2+的升高是引发该反应的充分信号。T3还损害了一些血管紧张素-II介导的反应,但未改变佛波酯对肝脏代谢的影响,因此表明某些受体后事件是T3作用的靶点。T3在增强α1-肾上腺素能受体介导的胞质游离Ca2+增加和阻止蛋白激酶C激活方面的差异效应,为进一步研究信号通路各分支在控制肝脏功能中的作用提供了独特工具。此外,T3在干扰α1-肾上腺素能受体介导的反应中的低有效浓度(<=10 nM)表明了其生理意义。