柳杉叶马尾杉生物碱成分及抑制乙酰胆碱酯酶活性研究  

Alkaloids of Phlegmariurus cryptomerinus and their inhibitory activity on acetylcholinesterase

作　　者：姜雨辰 崔佳 黄昕玥 陈小华 廖珅 李丽梅 JIANG Yuchen;CUI Jia;HUANG Xinyue;CHEN Xiaohua;LIAO Shen;LI Limei(School of Pharmacy and Food,Southwest Minzu University,Chengdu 610041,China)

机构地区：[1]西南民族大学药学与食品学院,四川成都610041

出　　处：《西南民族大学学报(自然科学版)》2025年第1期65-70,共6页Journal of Southwest Minzu University(Natural Science Edition)

基　　金：国家自然科学基金项目(31870341);国家民委中青年英才培养计划项目;西南民族大学中央高校基本科研业务费专项资金项目(2023NYXXS084)。

摘　　要：柳杉叶马尾杉(Phlegmariurus cryptomerinus(Maxim.)Satou)的生物碱成分及神经保护活性至今未见研究报道。为探索其生物碱成分及抑制乙酰胆碱酯酶活性,采用薄层层析、柱层析和高效液相色谱等方法对其全草中生物碱成分进行分离和纯化,通过ESI-MS、^(1)H-NMR、^(13)C-NMR和ECD等波谱技术鉴定生物碱化合物的结构,采用改进的Ellman法对分离得到的化合物进行抑制乙酰胆碱酯酶活性筛选,并通过分子对接技术研究化合物与乙酰胆碱酯酶蛋白的作用机制.结果表明,从柳杉叶马尾杉全草总生物碱中分离得到3个生物碱化合物,分别鉴定为:4R,15R-huperzine R(1)、phlegmariurine B(2)和nankakurine A(3),其中nankakurine A(3)对乙酰胆碱酯酶活性的IC_(50)值为(46.51±0.49)μM,同时,分子对接结果显示,nankakurine A(3)可以作用于乙酰胆碱酯酶的外周阴离子位点,与作用位点亲和力良好达到了一定抑制作用.化合物1~3均为首次从该植物中分离得到,其中4R,15R-huperzine R(1)为首次从马尾杉属中分离得到。The alkaloid constituents of Phlegmariurus cryptomerinus(Maxim.)Satou and their neuroprotective activity have not been reported.In order to explore its alkaloid constituents and inhibit acetylcholinesterase activity,the alkaloids were isolated using HPLC,column chromatography,and TLC.The structures of the alkaloid compounds were identified using spectroscopic techniques such as ESI-MS,^(1)H-NMR,^(13)C-NMR,and ECD.The inhibitory activity against acetylcholinesterase was carried out using the modified Ellman method.The interaction mechanism between active compound and acetylcholinesterase was studied by molecular docking.Three alkaloid compounds,namely 4R,15R-huperzine R(1),phlegmariurine B(2),and nankakurine A(3),were isolated and identified from the whole plant of Phlegmariurus cryptomerinus.Nankakurine A(3)showed inhibitory activity on acetylcholinesterase with an IC_(50)of(46.51±0.49)μM.The molecular docking results showed that compound 3 could bind to the peripheral anionic site of acetylcholinesterase and showed good affinity for the action site.All three compounds were obtained for the first time from this plant,and 4R,15R-huperzine R(1)was first found in Phlegmariurus genus.

关 键 词：柳杉叶马尾杉 石松生物碱 4R 15R-huperzine R 乙酰胆碱酯酶 

分 类 号：R284[医药卫生—中药学]