首页|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

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

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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IC50值均在1.16-5.15 μmol/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.
A new phloroglucinol from Hypericum sampsonii and it's anti-acetylcholinesterase activity
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 IC50 values of the compounds against acetylcholinesterase were 1.16-5.15 μmol/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.

Hypericum sampsonii Hance.dichloromethane fractionphloroglucinolisolation and identificationanti-acetylcholinesterase activityAlzheimer's disease

高圆媛、邓青、何清、李娜娜、何洁

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上海市中医医院,上海 200071

上海中医药大学,上海 201203

上海市黄浦区中西医结合医院,上海 200010

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

上海市临床重点专科建设项目上海市"科技创新行动计划"扬帆计划项目上海市中医医院未来计划项目

shslczdzk0490120YF1446100WL-QNRC-2022002K

2024

10.3969/j.issn.1001-1528.2024.06.021

中成药
国家食品药品监督管理局,信息中心中成药信息站,上海中药行业协会

中成药

CSTPCD北大核心
影响因子：1.217
ISSN：1001-1528
年,卷(期)：2024.46(6)