水马桑化学成分及其乙酰胆碱酯酶抑制活性研究

Study on the Chemical Constituents of Weigela japonica var.sinica and its Acetylcholinesterase Inhibitory Activity

目的:研究水马桑乙酸乙酯部位的化学成分及其乙酰胆碱酯酶抑制活性。方法:采用硅胶柱层析、Sephadex LH-20凝胶柱色谱和制备高效液相技术等进行分离纯化,根据理化性质和波谱数据鉴定化合物结构。通过改良的Ellman法测试所有化合物对乙酰胆碱酯酶的抑制活性。结果:从水马桑乙醇提取物的乙酸乙酯部位分离得到6个香豆素类化合物,分别鉴定为:东莨菪内酯(1)、东莨菪苷(2)、秦皮素(3)、秦皮苷(4)、臭矢菜素A(5)、臭矢菜素B(6)。活性测试结果表明化合物6显示乙酰胆碱酯酶抑制活性,半数抑制浓度(IC50)为3.32±0.01 mmol/L。结论:其中,化合物2~6为首次从该属植物中分离得到,且以上所有化合物均为首次从该植物中分离得到,水马桑中香豆素成分有一定的乙酰胆碱酯酶抑制活性。

Objective:To study the chemical constituents of ethyl acetate extract of Weigela japonica var.sinica and its inhibitory activity of acetylcholinesterase.Methods:The compounds were isolated and purified by silica gel column chromatography,Sephadex LH-20 gel column chromatography and prepared high performance liquid chromatography(HPLC).The structures of the compounds were identified according to the physical and chemical properties and spectral data.The inhibitory activity of all compounds on acetylcholinesterase was tested by modified Ellman method.Results:Six coumarins were isolated from the ethyl acetate extract of the ethanol extract of Weigela japonica var.sinica and identified as scopoletin(1),scopolin(2),fraxein(3),fraxin(4),cleomiscosin A(5),cleomiscosin B(6).The result of activity test showed that compound 6 showed acetylcholinesterase inhibitory activity,the half inhibitory concentration(IC50)was 3.32±0.01 mmol/L.Conclusion:Among them,compounds 2 to 6 are isolated from this genus for the first time,and all compounds are isolated from this plant for the first time.Coumarin in Weigela japonica var.sinica had certain acetylcholinesterase inhibitory activity.