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  

Luteolin activates the cystic fibrosis transmembrane conductance regulator chloride channel

作　　者：侯曙光[1] 林森[1] 于波[1] 金伶伶[1] 杨红[1] 

机构地区：[1]辽宁师范大学生物制药中心

出　　处：《中国临床药理学与治疗学》2008年第3期249-253,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金(30470405;30570864;30670477)

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。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.

关 键 词：囊性纤维化跨膜电导调节因子 高血压 Cl^-转运 木犀草素 激活剂 

分 类 号：R965.2[医药卫生—药理学]