Champigny G, Voilley N, Lingueglia E, Friend V, Barbry P, Lazdunski M
Institut de Pharmacologie Moléculaire et Cellulaire, Valbonne, France.
EMBO J. 1994 May 1;13(9):2177-81. doi: 10.1002/j.1460-2075.1994.tb06494.x.
Molecular cloning of the amiloride-sensitive Na+ channel has permitted analysis of the mechanisms of its stimulation by steroids. In rat lung cells in primary culture, where its mRNA has been detected, the activity of an amiloride-sensitive channel, highly selective for Na+, is controlled by corticosteroids. Dexamethasone (0.1 microM) or aldosterone (1 microM) induced, after a minimum 10 h treatment, a large increase of the amiloride-induced hyperpolarization and of the amiloride-sensitive current. A parallel increase in the amount of the mRNA was observed. The corresponding gene is thus a target for steroid action. Using synthetic specific agonists and antagonists for mineralo- and glucocorticoid receptors, it has been shown that the steroid action on Na+ channel expression is mediated via glucocorticoid receptors. Triiodothyronine, known to modulate steroid action in several tissues, had no effect on both the amiloride-sensitive Na+ current and the level of the mRNA for the Na+ channel protein, but potentiates the stimulatory effect of dexamethasone. The increase in Na+ channel activity observed in the lung around birth can thus be explained by a direct increase in transcription of the Na+ channel gene.
氨氯地平敏感的钠离子通道的分子克隆使得对其受类固醇刺激机制的分析成为可能。在已检测到其信使核糖核酸(mRNA)的原代培养大鼠肺细胞中,一种对钠离子具有高度选择性的氨氯地平敏感通道的活性受皮质类固醇控制。在经过至少10小时的处理后,地塞米松(0.1微摩尔)或醛固酮(1微摩尔)可使氨氯地平诱导的超极化和氨氯地平敏感电流大幅增加。同时观察到mRNA量的平行增加。因此,相应的基因是类固醇作用的靶点。使用针对盐皮质激素和糖皮质激素受体的合成特异性激动剂和拮抗剂已表明,类固醇对钠离子通道表达的作用是通过糖皮质激素受体介导的。已知可调节多个组织中类固醇作用的三碘甲状腺原氨酸,对氨氯地平敏感的钠离子电流和钠离子通道蛋白的mRNA水平均无影响,但可增强地塞米松的刺激作用。因此,出生前后在肺中观察到的钠离子通道活性增加可以通过钠离子通道基因转录的直接增加来解释。