| 丹皮酚对囊性纤维化跨膜电导调节因子氯离子通道的激活作用 |
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| 引用本文： | 侯婷婷,葛红,孙娟娟,于波,杨红.丹皮酚对囊性纤维化跨膜电导调节因子氯离子通道的激活作用[J].中国临床药理学与治疗学,2008,13(11). |
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| 作者姓名： | 侯婷婷 葛红 孙娟娟 于波 杨红 |
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| 作者单位： | 辽宁师范大学生物技术与分子药物研发重点实验室,大连116029,辽宁 |
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| 基金项目： | 国家自然科学基金，教育部新世纪优秀人才支持计划，辽宁省高等学校优秀人才支持计划项目 |
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| 摘 要： | 目的:研究丹皮酚对依赖于3’,5’-环腺苷酸(cAMP)的囊性纤维化跨膜电导调节因子(CFTR)Cl-通道的激活作用。方法:利用Cl-通道细胞荧光测定模型进行测定丹皮酚对CFTR介导的I-内流速度。结果:丹皮酚对野生型和ΔF508突变型CFTR Cl-通道均具有激活作用,而对G551D突变型CFTR Cl-通道无激活作用。丹皮酚在发挥激活作用时具有快速、可逆的特点并依赖于腺苷环化酶激动剂Forskolin的存在。初步确定了丹皮酚通过直接与CFTR结合发挥作用。结论:研究提示CFTR可能是某些中药降压作用药靶之一。此外,本实验为传统中药的降压作用的分子药理学机制作了初步探讨。
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| 关 键 词： | 丹皮酚 囊性纤维化跨膜电导调节因子 高血压 Cl~-转运 激活剂 |
Natural compound paeonol activates cystic fibrosis transmembrane conductance regulator chloride channel |
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| HOU Ting-ting,GE Hong,SUN Juan-juan,YU Bo,YANG Hong.Natural compound paeonol activates cystic fibrosis transmembrane conductance regulator chloride channel[J].Chinese Journal of Clinical Pharmacology and Therapeutics,2008,13(11). |
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| Authors: | HOU Ting-ting GE Hong SUN Juan-juan YU Bo YANG Hong |
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| Institution: | HOU Ting-ting; GE Hong; SUN Juan-juan; YU Bo; YANG Hong Biotechnology and Molecular Pharmacology Center Liaoning Normal University; Dalian 116029; Liaoning; China; |
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| Abstract: | AIM: To study the activation of paeonol on CFTR Cl-channel depending on 3 ,5 -cAMP.METHODS: A cell-based fluorescence assay was used to determine CFTR-mediated iodide influx rate.RESULTS: Paeonol increased CFTR-mediate iodide influx in a dose-dependent way.The activation was rapid,reversible and cAMP-dependent.Paeonol had additive effect with FSK/IBMX mixture and showed different sensitivity to ΔF508-CFTR and G551D-CFTR,implied it worked through a direct binding mechanism.CONCLUSION: The study suggests that... |
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| Keywords: | paeonol cystic fibrosis transmembrane conductance regulator hypertension chlorine transport activator |
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