中药提取物对钙调磷酸酶-活化T细胞核因子通路的抑制作用  

Inhibitory Effect of Herbal Extracts on Ca N-NFAT Pathway

作　　者：刘芳[1] 林国超 敢小双 邓文娟 翟春涛 胡振林[2] 

机构地区：[1]中国人民解放军第四五五医院药剂科,上海200052 [2]中国人民解放军第二军医大学药学院生化药学教研室,上海200433 [3]无限极(中国)有限公司,广州510623 [4]上海莱博生物技术有限公司,上海200233

出　　处：《天然产物研究与开发》2016年第6期922-927,共6页Natural Product Research and Development

摘　　要：通过研究多种具有清热解毒、除湿功效的中草药提取物对钙调磷酸酶-活化T细胞核因子（Ca N-NFAT）信号通路的抑制作用发现天然的Ca N-NFAT通路抑制剂。采用荧光素酶报告基因方法,检测多种中药提取物对Ca N-NFAT信号通路影响;采用CCK8法检测中药提取物的非特异性细胞毒性。实验发现：多种中药提取物在1 mg/m L浓度时对PMA/A23187刺激的K562细胞内Ca N-NFAT通路具有抑制作用,并且没有显著的细胞毒作用;其中部分中药提取物在0.25~1 mg/m L剂量范围内对Ca N-NFAT通路具有剂量依赖性的抑制作用,结果提示这些中药提取物中可能含有能够有效抑制Ca N-NFAT信号通路的活性成分。The present study was aimed to discover novel inhibitors of CaN-NFAT pathway from herbal extracts. The lu- ciferase reporter assay was applied to screen the effective inhibitors of CaN-NFAT pathway from herbal extracts using K562 cells stably transfeeted with NFAT-driven lucfferase reporter. CCK-8 assay was used to evaluate their eytotoxicity. The results of lueffemse reporter assay and CCK8 eytotoxicity assay on a variety of herbal extracts showed that the herbal extracts of propolis, Crataegus pinnatifida Bunge, Carthamus tinctorius L. , Forsythia suspensa （ Thunb. ） Vabl, Rad/x ranunculi ternati,Taraxacum mongolicum,Leonurus sibiricus L. ,Herba epimedii effectively inhibited the activation of CaN-NFAT pathway in PMA/A23187-stimulated K562 cells at the concentration of 1 mg/mL without significant eytotox- icity. Dose-dependency study indicated that extracts of Colla Apis, Crataegus pinnatifida Bunge, Carthamus tinctorius L. , Artemisia carvifolia and Forsythia suspensa （ Thunh. ） Vahl inhibited the activation of CaN-NAb＇q＇ signal pathway dose-dependently .within the concentrations of 0.25-1 mg/mL. These results suggested that CaN-NFAT pathway might be one of the targets by which these herbs exert anti-inflammatory and immune-modulating effects, and that there might be inhibitors of CaN-NFAT pathway in these extracts.

关 键 词：钙调磷酸酶 活化T细胞核因子 信号转导 细胞因子 炎症 中药提取物 湿疹 

分 类 号：R967[医药卫生—药理学]