【作者】 傅冬和； 刘仲华； 黄建安； 陈金华； 陈惠衡；

【Author】 Fu Dong-he~(1 2) Liu Zhonghua~(1 2*) Huang Jianan~(1 2) Cheng Jinhua~1 Cheng Huiheng~2 (1 Tea Key Lab of the Ministry of National Teaching,Hunan Agricultural University, 2 College of Horticulture and Landscape,Hunan Agricultural University,Hunan,ChangSha 410128)

【机构】 湖南农业大学教育部茶学重点实验室； 湖南农业大学园艺园林学院；

【摘要】 选择与降脂减肥作用相关的FXR、LXR、PPAR 6、PPARγ及3T3-L1模型对从茯砖茶中分离制备的6个单体化合物进行高通量药物筛选研究,结果表明,各单体对所选模型均有活性。对于FXR激活模型,没食子酸(GA)和表儿茶素没食子酸酯(ECG)在50μg/mL的初筛浓度时激活值分别达1.766和3.220:表没食子儿茶素没食子酸酯(EGCG)在10μg/mL和50μg/mL的初筛浓度时激活作用均较强,特别是50μg/ml的初筛浓度时,其激活倍数达6.000;对于PPARδ模型,此三种单体添加量均需达50μg/mL,作用才显著。在初筛浓度为30μg/mL时,没食子儿茶素(GC)对PPARγ模型的激活倍数达1.619;3-甲氧基-4,5-二羟基苯甲酸(MDBA)对PPARγ模型的激活倍数达1.734;3,4-二羟基苯甲酸(DBA)对FXR抑制值为3.641,明显小于对照初级胆汁酸鹅脱氧胆酸(CDCA)的抑制值6.435,因此其抑制模型的作用非常明显。以上试验结果说明此6个化合物均为活性化合物。更多还原

【Abstract】 6 compounds separated from Fuzhuan Tea were tested by High-Throughput Screening of model FXR,LXR,PPARd,PPARγand 3T3-L1.The results showed that all monomers were active to the models selected.To the active model FXR,gallic acid and ECG were active on the concentration of 50μg/mL.The activate value of GA and ECG was 1.766 and 3.220 separately.EGCG was very active on the cocentration of 10μg/mL and 50μg/mL.The active value reached 6.000 when the concentration was 50μg/mL.To PPARd,the three compounds were active when the concentration was 50μg/mL.The active value of GC to PPARγwas 1.619.The active value of 3-methoxy-4,5-dihydroxy-benzoic acid to PPARγwas 1.734.The restraining multiple to FXR of 3,4-dihyddroxy-benzoic acid was 3.641,while that of CK CDCA was 6.435.All the results showed that all the compounds were functional ones.更多还原