【摘要】 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CFTRCl-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For-skolin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。更多还原

【Abstract】 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.更多还原