茯砖茶中几种单体成分功效的高通量筛选研究

Investigation on the Function of Monomers in FuzhuanTea by High-Throughput Screening

选择与降脂减肥作用相关的FXR、LXR、PPARδ、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。

Six compounds separated from Fuzhuan Tea were tested by High-Throughput Screening of model FXR, LXR, PPAR δ, PPAR-γ and 3T3-L1 related to the lipid-depressing and anti-obesity. 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 50 μg/ml. The activating value of GA and ECG was 1.766 and 3.220 respectively. EGCG was very active on the concentration of 10 μg/ml and 50 μg/ml. The active value reached 6.0 when the concentration was 50 μg/ml. To PPAR δ, the three compounds were active when the concentration was 50 μg/ml. The activating value of GC to PPAR -γ model was 1.619. The activating value of 3- methoxy- 4,5-dihydroxy-benzoic acid in PPAR -γ model was 1.734. The restraining value of 3,4-dihydroxy-benzoic acid in FXR model was 3.641, while that of CDCA（CK） was 6.435. All the results showed that all the compounds were functional ones.