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蟾蜍灵激活低分化鼻咽癌细胞氯通道

ISSN号：1000-4718
期刊名称：中国病理生理杂志
时间：2011.4.4
页码：671-676
分类：R739.63[医药卫生—肿瘤;医药卫生—临床医学]
作者机构：[1]广东医学院生理学教研室,广东湛江524023, [2]暨南大学医学院,广东广州510632, [3]暨南大学药学院,广东广州510632
相关基金：国家自然科学基金资助项目（No.30771106;No.30870567;No.30871267;No.90913020;No.U0932004）; 广东省自然科学基金资助项目（No.07005974）; 广东医学院青年基金资助项目（No.XQ06013）
相关项目：基于GABA受体靶标的新型一叶萩型生物碱的发现及其构效关系和作用机制研究

关键词：蟾蜍灵, 鼻咽肿瘤, 氯通道, Bufalin, Nasopharyngeal neoplasms, Chloride channels

中文摘要：

目的：研究蟾蜍灵（bufalin）对低分化鼻咽癌（CNE-2Z）细胞氯通道的激活作用以及通道的特性。方法：采用全细胞膜片钳技术记录蟾蜍灵激活CNE-2Z细胞膜电流并分析其电流特征。结果：细胞外灌流1μmol/L的蟾蜍灵可诱发CNE-2Z细胞产生一个氯电流,该电流潜伏期较长,为（12.1±6.4）min,其翻转电位接近氯离子平衡电位。该电流具有较明显的外向优势,没有明显的时间依赖性失活和电压依赖性失活。氯通道阻断剂他莫昔芬（tamoxifen）可完全抑制该电流,细胞外灌流高渗液也可完全抑制该电流。结论：蟾蜍灵可以激活CNE-2Z细胞氯通道产生氯电流,与容积激活性氯电流相比,该电流的潜伏期较长,并且有更明显的外向优势。

英文摘要：

AIM：To investigate the activation of chloride channels induced by bufalin and the properties of the channels in poorly differentiated nasopharyngeal carcinoma（CNE-2Z）cells.METHODS：The technique of whole-cell patch clamp was used to record the chloride currents and to analyze the characteristics of the currents in CNE-2Z cells. RESULTS：A chloride current was slowly activated by extracellular application of bufalin（1μmol/L）.The activation of the current was slower than that of the volume-activated chloride current,with an activation latency of（12.1±6.4）min. The reversal potential of the current was close to the calculated Cl~-equilibrium potential（E_（Cl）=-0.9 mV）.The chloride current was outward-rectified and did not show significant time-dependent or voltage-dependent inactivation.The chloride channel blocker tamoxifen completely inhibited the outward and inward currents.The current was also completely inhibited by extra-cellular application of 47%hypertonic solution.CONCLUSION：Bufalin activates chloride channels and induces a chloride current in CNE-2Z cells.Compared with the volume-activated chloride current in CNE-2Z cells,the activation latency of the bufalin-induced current is longer and the outward rectification is more obvious.

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