α-葡萄糖苷酶抑制活性跟踪分离芙蓉菊中的活性成分  

Bioactivity guided isolation of alpha-glucosidase inhibitor from whole herbs of Crossostephium chinense

作　　者：吴琦[1] 杨秀伟[1] 邹磊[2,3] 傅德贤[3] 

机构地区：[1]北京大学天然药物及仿生药物国家重点实验室药学院天然药物学系,北京100191 [2]中国医药研究开发中心有限公司,北京102206 [3]中国科学院过程工程研究所生化工程国家重点实验室,北京100080

出　　处：《中国中药杂志》2009年第17期2206-2211,共6页China Journal of Chinese Materia Medica

基　　金：国家基础研究发展计划(973)项目(2001CB51008)

摘　　要：目的：研究芙蓉菊全草中具有抑制α-葡萄糖苷酶活性的化学成分。方法：采用体外α-葡萄糖苷酶抑制活性跟踪方法和各种柱色谱技术进行化学成分的分离和纯化；应用各种谱学方法鉴定化合物的结构；对单体化合物进行α-葡萄糖苷酶抑制活性试验，确定活性成分。结果：芙蓉菊70%乙醇提取物的醋酸乙酯萃取部分和水溶性部分对α-葡萄糖苷酶活性具有较强的抑制作用，从两部分分离鉴定了5，7-二羟基-3′，4′，5′-三甲氧基黄酮 （1），东莨菪素（2），艾菊素，粗毛豚草素（3），5，5′，7-三羟基-3′，4′-二甲氧基黄酮（4），柯伊利素（5），万寿菊黄素-3，6，7-三甲基醚（6），石杉黄素（7），东莨菪苷（8）和槲皮万寿菊素-3，6-二甲醚（9）。其中，化合物2，3，5～7，9对α-葡萄糖苷酶活性具有较强的抑制作用，IC50（μmol·L-1）值分别为（34.36±2.06），（146.28±12.44），（246.26±8.73），（74.06±3.83），（42.19±5.25），（136.20±25.73），强于同条件下的阳性对照药阿卡波糖[IC50 =（489.25±38.55）μmol·L-1]。化合物1，4，8和艾菊素的IC50值皆大于1 000 μmol·L-1。结论：化合物5和9为首次从该属植物中分离得到；化合物2，3，5～7，9对α-葡萄糖苷酶活性具有较强的抑制作用，其抑制作用类型属于竞争性抑制作用，它们可能是芙蓉菊防治糖尿病的物质基础。Objective： To investigate the chemical constituents of 70% aqueous ethanol extract from the whole plant of Crossostephium chinense for inhibitory activity against alpha-glucosidase. Method： A bioactivity-guided isolation and purification process was used to identify the alpha-glucosidase activity inhibiting components of the whole plant of C. chinense. The dried whole plants were extracted with 70% aqueous ethanol. The extract was suspended in water and then further fractionated successively with cyclohexane, ethyl acetate, and normal butanol,and tested for their inhibitory activity against alpha-glucosidase in vitro. The chemical structures of isolated compounds were determined by spectroscopic methods including NMR and MS, and comparison with data of authentic samples. All of compounds were assayed for their inhibitory activity against alpha-glucosidase in vitro. Result： The ethyl acetate and water layer fractions showed the strong inhibitory activity, and were subjected to column chromatography over the various stationary phases. Tricetin 3′,4′,5′- trimethylether （1）, scopoletin （2）, tanacetin, hispidulin （3）, apometzgerin （4）, chrysoeriol （5）, quercetagetin 3,6,7-trimethylether （6）, selagin （7）, scopolin （8）, and quercetagetin-3,6-dimethylether （9） were isolated and characterized by different spectroscopic techniques. Among them, compounds 2, 3, 5-7 and 9 for inhibitory activity against alpha-glucosidase with IC50 （μmol·L-1） values of （34.36±2.06）, （146.28±12.44）, （246.26±8.73）, （74.06±3.83）, （42.19±5.25） and （136.20±25.73）, respectively, were assayed as the active components. A positive drug, acarbose, showed the inhibitory activity against alpha-glucosidase with IC50 value of （489.25±38.55） μmol·L-1 in the same assay conditions with the above test compounds. The IC50 values of compounds 1, 4, 8 and tanacetin were all more than 1 000 μmol·L-1. Conclution： The compounds 5 and 9 were isolated from the genus Crossoste

关 键 词：芙蓉菊 黄酮 Α-葡萄糖苷酶 

分 类 号：R284.1[医药卫生—中药学]