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50 µg/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10 µg/ml和50 µg/ml的初筛浓度时激活作用均较强,特别是50 µg/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50 µg/ml,作用才显著。在初筛浓度为30 µg/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, PPARδ, PPARγ 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 PPARδ, the three compounds were active when the concentration was 50 µg/ml. The activating value of GC to PPARγ model was 1.619. The activating value of 3- methoxy- 4,5-dihydroxy-benzoic acid in PPARγ 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.
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