应用超滤液相色谱技术筛选中药抑制磷酸二酯酶4活性成分

Screening of phosphodiesterase 4 inhibitors from traditional Chinese medicine by ultrafiltration HPLC

本文应用超滤液相色谱技术,结合体外活性实验筛选了中药红花、土茯苓和防风中抑制磷酸二酯酶4活性成分。红花、土茯苓和防风提取物的IC50值分别为0. 03μg·μL-1,0. 06μg·μL-1和0. 05μg·μL-1,实验结果表明红花对磷酸二酯酶4具有强抑制作用,其次为防风、土茯苓。红花黄色素、落新妇苷和5-氧甲基维斯阿米苷的IC50值分别为41. 83μM,8. 11μM和3. 62μM,与磷酸二酯酶4有较好的结合能力,分别为红花、土茯苓和防风中主要抑制磷酸二酯酶-4活性成分。

In vitro phosphodiesterase 4（PDE 4）inhibition assays and ultrafiltration HPLC were combined to screen the enzyme inhibitors from selected Chinese medicinal herbs Carthamus tinctorius L, Smilax glabra Roxb and Saposhnikovia divaricata for the first time.The potency of the PDE 4 inhibitors identified in ultrafiltration HPLC was compared to the IC 50’s obtained from in vitro enzyme inhibition assay.The IC 50 of C.tinctorius,S.glabra,S.divaricata extracts were 0.03 μg·μL -1 ,0.06 μg·μL^ -1 and 0.05 μg·μL ^-1 ,respectively,suggesting that C.tinctorius extract was the strongest 5-PDE 4 inhibitor,followed by S.divaricata and S.glabra extracts.As a result,anhydrosafflor yellow B,astilbin and 4＇-O-β-D-glucosyl-5-O-methylvisamminol had the highest binding ability to PDE 4,the IC 50 of anhydrosafflor yellow B,astilbin and 4＇-O-β-D-glucosyl-5-O-methylvisamminoland were 41.83 μM,8.11 μM and 3.62 μM,were the main contributors to the PDE 4 inhibitory activities of C.tinctorius , S.glabra and S.divaricata extracts,respectively.