α-葡萄糖苷酶抑制活性跟踪分离芙蓉菊中的活性成分

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。

Bioactivity guided isolation of alpha-glucosidase inhibitor from wholeherbs of Crossostephium chinense

Object: To provide more proofs for expounding the genetic relationships among the (varietal) species in genus Fritillaria from Sichuan Province. Method: The ISSR marker technique was used to study relationships and genetic polymorphism of nineteen populations in ten species and one varietal species of genus Fritillaria. Genetic similarities were calculated by using NTSYS software and the dendrogram was constructed by using UPGMA method. Result: Eleven primers were selected from 35 ISSR primers, and 179 DNA fragments were amplified from 19 populations. Of which, 179 fragments were polymorphic (percentage of polymorphic bands was 86.8%). The genetic similarity among all accessions ranged from 0.569 to 0.855. Clustering analysis showed that the 19 populations of Fritillaria could be distinctively classified into 4 groups. F. cirrhosa, F. przewalskii, F. unibracteata var. longinectarea and F. dajinensis were in the first group; The second group was the cluster of F. unibracteata and F. mellea (wild and cultivated species); The third group was F. sulcisquamosa, F. thunbergii, wabunesis and F. delavayi; F. hupehensis alone formed the fourth group. Conclusion: ISSR marker technique is suitable for the genetic diversity of Fritillaria from Sichuan Province. Interspecific identifications among the four original species of Bulbus Fritillariae Cirrhosae recorded by pharmacopoeia of China, and between them and the other species of genus Fritillaria from Sichuan Province could not be gained by using ISSR markers technique. In addition, the cluster result of genus Fritillaria had some relationships with the geographical distribution.