Chen X Z, Coady M J, Lapointe J Y
Département de Physique, Université de Montréal, Québec, Canada.
Biophys J. 1996 Nov;71(5):2544-52. doi: 10.1016/S0006-3495(96)79447-X.
The human Na(+)-glucose cotransporter (hSGLT1) has been shown to generate, in the absence of sugar, presteady-state currents in response to a change in potential, which could be fitted with single exponentials once the voltage had reached a new constant value. By the cut-open oocyte technique (voltage rising-speed approximately 1 mV/microsecond), phlorizin-sensitive transient currents could be detected with a higher time resolution during continuous intracellular perfusion. In the absence of sugar and internal Na+, and with 90 mM external Na+ concentration ([Na+]o), phlorizin-sensitive currents exhibited two relaxation time-constants: tau 1 increased from 2 to 10 ms when Vm decreased from +60 mV to -80 mV and remained at 10 ms for more negative Vm; tau 2 ranged from 0.4 to 0.8 ms in a weakly voltage-dependent manner. According to a previously proposed model, these two time constants could be accounted for by 1) Na+ crossing a fraction of the membrane electrical field to reach its binding site on the carrier and 2) conformational change of the free carrier. To test this hypothesis, the time constants were measured as [Na+]o was progressively reduced to 0 mM. At 30 and 10 mM external Na+, tau 1 reached the same plateau value of 10 ms but at more negative potentials (-120 and -160 mV, respectively). Contrary to the prediction of the model, two time constants continued to be detected in the bilateral absence of Na+ (at pH 8.0). Under these conditions, tau 1 continuously increased through the whole voltage range and did not reach the 10 ms level even when Vm had attained -200 mV while tau 2 remained in the range of 0.4-0.8 ms. These results indicate that 1) conformational change of the free carrier across the membrane must occur in more than one step and 2) Na+ binding/debinding is not responsible for either of the two observed exponential components of transient currents. By use of the simplest kinetic model accounting for the portion of the hSGLT1 transport cycle involving extracellular Na+ binding/debinding and the dual-step conformational change of the free carrier, tau 1 and tau 2 were fitted throughout the voltage range, and a few sets of parameters were found to reproduce the data satisfactorily. This study shows that 1) tau 1 and tau 2 correspond to two steps in the conformational change of the free carrier, 2) Na+ binding/debinding modulates the slow time constant (tau 1) and 3) a voltage-independent slow conformational change of the free carrier accounts for the observed plateau value of 10 ms.
已证明,在无糖情况下,人类钠 - 葡萄糖共转运蛋白(hSGLT1)会因电位变化产生稳态前电流,一旦电压达到新的恒定值,该电流可用单指数函数拟合。通过切开卵母细胞技术(电压上升速度约为1 mV/微秒),在连续细胞内灌注过程中,可以更高的时间分辨率检测到根皮素敏感的瞬态电流。在无糖且细胞内无钠,细胞外钠浓度([Na⁺]o)为90 mM的情况下,根皮素敏感电流表现出两个弛豫时间常数:当膜电位(Vm)从 +60 mV降至 -80 mV时,τ1从2 ms增加到10 ms,对于更负的Vm保持在10 ms;τ2以弱电压依赖性方式在0.4至0.8 ms范围内变化。根据先前提出的模型,这两个时间常数可由以下原因解释:1)钠离子穿过部分膜电场以到达其在载体上的结合位点;2)游离载体的构象变化。为了验证这一假设,在将[Na⁺]o逐渐降低至0 mM的过程中测量时间常数。在细胞外钠浓度为30 mM和10 mM时,τ1分别在更负的电位(-120 mV和 -160 mV)达到相同的10 ms平台值。与模型预测相反,在细胞内外均无钠(pH 8.0)的情况下仍能检测到两个时间常数。在这些条件下,τ1在整个电压范围内持续增加,即使Vm达到 -200 mV时也未达到10 ms水平,而τ2保持在0.4 - 0.8 ms范围内。这些结果表明:1)游离载体跨膜的构象变化必定发生在不止一个步骤中;2)钠离子的结合/解离与瞬态电流中观察到的两个指数成分均无关。通过使用最简单的动力学模型来解释hSGLT1转运循环中涉及细胞外钠离子结合/解离以及游离载体双步构象变化的部分,在整个电压范围内对τ1和τ2进行拟合,发现几组参数能够令人满意地重现数据。这项研究表明:1)τ1和τ2对应于游离载体构象变化的两个步骤;2)钠离子的结合/解离调节慢时间常数(τ1);3)游离载体的电压非依赖性慢构象变化导致观察到的10 ms平台值。