β-甘草次酸选择性调节法呢醇X受体活性  

Modulating effect of β-glycyrrhetic acid on the activity of farnesoid X receptor

作　　者：刘文明[1] 王海彬[2] 刘丽 周曦[1] 王军舰[1] 

机构地区：[1]中国科学院广州生物医药与健康研究院,广州510530 [2]广州中医药大学第一附属医院,广州510405 [3]铜陵市第二人民医院,铜陵244000

出　　处：《中国新药杂志》2010年第19期1798-1802,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30672463;30973761);广东省自然科学基金(8151040701000016)

摘　　要：目的:探讨β-甘草次酸对法呢醇X受体(FXR)活性的影响。方法:利用瞬时转染的方法,在肝癌细胞HepG2中,检测β-甘草次酸对FXR活性的影响;Celltiter-Glo检测β-甘草次酸对HepG2细胞活力的影响;实时定量PCR检测β-甘草次酸对FXR靶基因的影响。结果:β-甘草次酸特异性和剂量依赖性的降低鹅脱氧胆酸所诱导的FXR的活性,并且能选择性地降低FXR靶基因的表达。结论:β-甘草次酸能选择性地调节FXR活性。Objective： To investigate the modulating effect of β-glycyrrhetic acid（β-GA） on the activity of farnesoid X receptor（FXR）.Methods： FXR was transiently transfected into HepG2 cells,and the effect of β-GA on FXR activity was determined.The effect of β-GA on HepG2 cell viability was detected by Celltiter-Glo.The effect of β-GA on FXR target genes was determined by real-time q-PCR.Results： β-GA specifically and does-dependently decreased the activity of FXR induced by CDCA,and selectively down-regulated the expressions of FXR target genes.Conclusion： β-GA can selectively modulate the activity of FXR.

关 键 词：β-甘草次酸 法呢醇X受体 肝癌细胞HEPG2 

分 类 号：R962.2[医药卫生—药理学] R971[医药卫生—药学]