中文摘要：

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。

英文摘要：

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...