元宝草中一个新的间苯三酚及其乙酰胆碱酯酶抑制活性研究  

A new phloroglucinol from Hypericum sampsonii and it’s anti-acetylcholinesterase activity

作　　者：高圆媛 邓青 何清 李娜娜 何洁 GAO Yuan-yuan;DENG Qing;HE Qing;LI Na-na;HE Jie(Shanghai Municipal Hospital of Tradition Chinese Medicine,Shanghai 200071,China;Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Huangpu District Hospital of Integrated Traditional Chinese and Western Medicine,Shanghai 200010,China)

机构地区：[1]上海市中医医院,上海200071 [2]上海中医药大学,上海201203 [3]上海市黄浦区中西医结合医院,上海200010

出　　处：《中成药》2024年第6期1900-1905,共6页Chinese Traditional Patent Medicine

基　　金：上海市临床重点专科建设项目(shslczdzk04901);上海市“科技创新行动计划”扬帆计划项目(20YF1446100);上海市中医医院未来计划项目(WL-QNRC-2022002K)。

摘　　要：目的研究元宝草化学成分及其乙酰胆碱酯酶抑制活性。方法元宝草二氯甲烷部位采用硅胶柱色谱、Sephedex LH-20、MCI和半制备HPLC等进行化分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用Ellman法测定其乙酰胆碱酯酶抑制活性。结果从中分离得到8个化合物,分别鉴定为元宝草素A(1)、hyperbeanin A(2)、hyperpatulol I(3)、hyperhenone I(4)、hypercohone G(5)、hyperbeanol G(6)、hyperlagarin A(7)、hyperascyrone D(8)。化合物抑制乙酰胆碱酯酶IC 50值均在1.16~5.15μmol/L之间。结论化合物1为间苯三酚类新化合物。所有化合物均具有一定程度的乙酰胆碱酯酶抑制活性,是阿尔茨海默病治疗药物的潜在活性先导化合物。AIM To study the chemical constituents and their anti-acetylcholinesterase activtities from Hypericum sampsonii Hance.METHODS The dichloromethane extract of H.sampsonii was isolated and purified by silica gel column chromatography,Sephadex LH-20,MCI and semi-preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their anti-acetylcholinesterase activities were determined by Ellman method.RESULTS Eight compounds were isolated and and identified as hypsamsion A(1),hyperbeanin A(2),hyperpatulol I(3),hyperhenone I(4),hypercohone G(5),hyperbeanol G(6),hyperlagarin A(7)and hyperascyrone D(8).The IC 50 values of the compounds against acetylcholinesterase were 1.16-5.15μmol/L.CONCLUSION Compound 1 is a novel phloroglucinol.To a certain extent,all compounds have anti-acetylcholinesterase activities,and are potential active lead compounds for the treatment of of Alzheimer’s disease.

关 键 词：元宝草 二氯甲烷部位 间苯三酚 分离鉴定 乙酰胆碱酯酶抑制活性 阿尔茨海默病 

分 类 号：R284.1[医药卫生—中药学]