木犀草素促进囊性纤维化跨膜电导调节因子氯离子通道开放

目的：研究木犀草素对依赖于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：利用稳定共表达人CFTR与一种对卤族元素敏感的荧光绿蛋白突变体（EYFP-H148Q）的Fischer大鼠甲状腺（FRT）细胞模型，测定木犀草素对CFTR介导的I^-内流速度。结果：木犀草素能够以剂量依赖的方式激活CFTR的I^-转运，其对CFTR Cl^-通道的激活效应具有作用迅速、可逆的特点。木犀草素在发挥激活作用时依赖于腺苷环化酶激动剂Forskolin的存在，其单独与细胞孵育不提高细胞内cAMP的水平。结论：发现了木犀草素能够以剂量依赖方式激活CFTR，并且初步确定了木犀草素通过直接与CFTR结合发挥作用。

Luteolin activates the cystic fibrosis transmembrane conductance regulator chloride channel

AIM： To investigate the activation effect of luteolin on cAMP-dependent cystic fibrosis transmembrane conductance regulator （CFTR） chloride channel. METHODS： A stable transfected epithelial cell line coexpression human CFTR and a green fluorescent protein mutant with ultra-high halide sensitivity （YFP-H148Q） were used to determine CFTR-mediated iodide influx rate. RESULTS： Luteolin increased dose-dependently CFTR-mediated iodide influx. The activity was rapid, reversible and Forskolin-dependent. Luteolin had additive effect with Forskolin mixture and did not elevate intracellular cAMP concentration wirhout Forskolin. CONCLUSION： The study identified luteolin could dose-dependently activate CFTR and provided that luteolin acted by combining with CFTR directly.