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首页> 外文期刊>The Korean Journal of Physiology & Pharmacology >Bisphenol A and 4-tert-Octylphenol Inhibit Cx46 Hemichannel Currents
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Bisphenol A and 4-tert-Octylphenol Inhibit Cx46 Hemichannel Currents

机译：双酚A和4-叔辛基酚抑制Cx46半通道电流

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摘要

Connexins (Cx) are membrane proteins and monomers for forming gap junction (GJ) channels. Cx46 and Cx50 are also known to function as conductive hemichannels. As part of an ongoing effort to find GJ-specific blocker(s), endocrine disruptors were used to examine their effect on Cx46 hemichannels expressed in Xenopus oocytes. Voltage-dependent gating of Cx46 hemichannels was characterized by slowly activating outward currents and relatively fast inward tail currents. Bisphenol A (BPA, 10 nM) reduced outward currents of Cx46 hemichannels up to ~18% of control, and its effect was reversible (n=5). 4- tert -Octylphenol (OP, 1 μM) reversibly reduced outward hemichannel currents up to ~28% (n=4). However, overall shapes of Cx46 hemichannel current traces (outward and inward currents) were not changed by these drugs. These results suggest that BPA and OP are likely to occupy the pore of Cx46 hemichannels and thus obstruct the ionic fluxes. This finding provides that BPA and OP are potential candidates for GJ channel blockers.
机译：连接蛋白（Cx）是膜蛋白，是形成间隙连接（GJ）通道的单体。还已知Cx46和Cx50充当导电半通道。作为寻找GJ特异性阻滞剂的不断努力的一部分，使用内分泌干扰物来检查它们对非洲爪蟾卵母细胞中表达的Cx46半通道的影响。 Cx46半通道的电压依赖性门控的特征是缓慢激活外向电流和相对快的内向尾电流。双酚A（BPA，10 nM）降低了Cx46半通道的外向电流，最高可达到对照的18％，其作用是可逆的（n = 5）。 4-叔辛基苯酚（OP，1μM）可逆地减少了向外的半通道电流，最高可达〜28％（n = 4）。但是，这些药物并未改变Cx46半通道电流迹线的整体形状（外向和内向电流）。这些结果表明，BPA和OP可能占据Cx46半通道的孔，从而阻碍了离子通量。这一发现提供了BPA和OP是GJ通道阻滞剂的潜在候选者。

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