Poletto Chaves Luiz Artur, Varanda Wamberto Antonio
Department of Physiology, University of São Paulo, Av. Bandeirantes 3900, 14049-900, Ribeirão Preto/SP, Brazil.
Pflugers Arch. 2008 Nov;457(2):493-504. doi: 10.1007/s00424-008-0525-2. Epub 2008 Jun 24.
Production and secretion of testosterone in Leydig cells are mainly controlled by the luteinizing hormone (LH). Biochemical evidences suggest that the activity of Cl(-) ions can modulate the steroidogenic process, but the specific ion channels involved are not known. Here, we extend the characterization of Cl(-) channels in mice Leydig cells (50-60 days old) by describing volume-activated Cl(-) currents (I(Cl,swell)). The amplitude of I(Cl,swell) is dependent on the osmotic gradient across the cell membrane, with an apparent EC(50) of approximately 75 mOsm. These currents display the typical biophysical signature of volume-activated anion channels (VRAC): dependence on intracellular ATP, outward rectification, inactivation at positive potentials, and selectivity sequence (I(- )> Cl(- )> F(-)). Staurosporine (200 nM) did not block the activation of I(Cl,swell). The block induced by 5-nitro-2-(3-phenylpropylamino) benzoic acid (NPPB; 128 microM), SITS (200 microM), ATP (500 microM), pyridoxal-phosphate-6-azophenyl-2',4'-disulfonate (PPADS; 100 miccroM), and Suramin (10 microM) were described by the permeant blocker model with apparent dissociation constant at 0 mV K(do) and fractional distance of the binding site (delta) of 334 microM and 47 %, 880 microM and 35 %, 2,100 microM and 49%, 188 microM and 27%, and 66.5 microM and 49%, respectively. These numbers were derived from the peak value of the currents. We conclude that I(Cl,swell) in Leydig cells are activated independently of purinergic stimulation, that Suramin and PPADS block these currents by a direct interaction with VRAC and that ATP is able to permeate this channel.
睾丸间质细胞中睾酮的产生和分泌主要受促黄体生成素(LH)调控。生化证据表明,Cl(-)离子的活性可调节类固醇生成过程,但具体涉及的离子通道尚不清楚。在此,我们通过描述容积激活的Cl(-)电流(I(Cl,swell)),扩展了对小鼠睾丸间质细胞(50 - 60日龄)中Cl(-)通道的特性描述。I(Cl,swell)的幅度取决于跨细胞膜的渗透梯度,其表观半数有效浓度(EC(50))约为75 mOsm。这些电流表现出容积激活阴离子通道(VRAC)的典型生物物理特征:依赖细胞内ATP、外向整流、在正电位下失活以及选择性序列(I(-)>Cl(-)>F(-))。星形孢菌素(200 nM)不阻断I(Cl,swell)的激活。5-硝基-2-(3-苯丙基氨基)苯甲酸(NPPB;128 microM)、4,4'-二异硫氰酸芪-2,2'-二磺酸(SITS;200 microM)、ATP(500 microM)、磷酸吡哆醛-6-偶氮苯基-2',4'-二磺酸盐(PPADS;100 microM)和苏拉明(10 microM)所诱导的阻断作用,根据通透阻滞剂模型进行描述,其在0 mV时的表观解离常数(K(do))以及结合位点的分数距离(δ)分别为334 microM和47%、880 microM和35%、2,100 microM和49%、188 microM和27%以及66.5 microM和49%。这些数值源自电流的峰值。我们得出结论,睾丸间质细胞中的I(Cl,swell)独立于嘌呤能刺激而被激活,苏拉明和PPADS通过与VRAC直接相互作用来阻断这些电流,并且ATP能够通透此通道。