异补骨脂查尔酮抑制IL-4产生及其机制研究  

Inhibition of isobavachalcone on IL-4 production and its mechanism

作　　者：梁正[1,2] 杨春[3] 李峥[1] 李强[4] 吴震州[1] 

机构地区：[1]南开大学生命科学学院,天津300071 [2]成都中医药大学,四川成都611137 [3]四川中医药高等专科学校,四川绵阳621000 [4]集宁师范学院,内蒙古集宁012000

出　　处：《中草药》2013年第10期1299-1304,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金杰出青年项目(30890143)

摘　　要：目的从补骨脂单体化学成分中筛选抗哮喘的小分子化合物,并阐释其抗哮喘作用机制。方法基于IL-4在哮喘病理中的作用,采用IL-4-GFP转基因报告小鼠(4get鼠)和流式细胞术,设计一种抑制白细胞介素-4(IL-4)产生的抗哮喘药物筛选新方法。结果与DMSO组相比,异补骨脂查尔酮能显著抑制Th2细胞中IL-4的产生(P<0.001),减少转录因子GATA-3的表达(P<0.01),降低信号转导与转录激活因子STAT6磷酸化水平(P<0.01)。结论异补骨脂查尔酮通过抑制STAT6磷酸化而减少GATA-3的表达,从而抑制IL-4的产生,其具有开发成为治疗哮喘药物的潜力。Objective To screen the small molecular compounds with anti-asthma activity from Psoralea corylifolia monomor and explain its regulation mechanism.Methods Based on the effect of IL-4 in pathological features of masthma,a high throughput screening system was designed by using 4get mice and flow cytometry to inhibit IL-4 production so as to anti-asthma.Results Compared with DMSO group,isobavachalcone showed high ability of inhibiting IL-4 production in Th2 cells（P ＆lt; 0.001）,down-regulating GATA-3 expression（P ＆lt; 0.01）,and decreasing the level of STAT6 phosphorylation（P ＆lt; 0.01）.Conclusion Isobavachalcone could inhibit the IL-4 production through down-regulating the GATA-3 expression by controling the level of STAT6 phosphorylation.Isobavachalcone is a potential drug for the treatment of asthma.

关 键 词：抗哮喘药 异补骨脂查尔酮 白细胞介素-4 STAT6 GATA-3 流式细胞术 

分 类 号：R974.3[医药卫生—药品]