高乌头中二萜生物碱成分及其生物活性研究  

Diterpenoid Alkaloids from the Aconitum sinomontanum and Their Bioactivities

作　　者：石新卫[1,2] 路强强 周亚福 王宇超[1] 薛文娇[2] 陈尘 万一 SHI Xin-wei;LU Qiang-qiang;ZHOU Ya-fu;WANG Yu-chao;XUE Wen-jiao;CHEN Chen;WAN Yi(Shaanxi Engineering Research Centre for Conservation and Utilization of Botanical Resources,Xi'an Botanical Garden of Shaanxi Province(Institute of Botany of Shaanxi Province),Xi'an 710061,China;Engineering Center of QinLing Mountains Natural Products,Shaanxi Academy of Sciences,Microbiology Institute of Shaanxi,Xi'an 710043,China)

机构地区：[1]陕西省植物资源保护与利用工程技术研究中心,陕西省西安植物园(陕西省植物研究所),西安710061 [2]陕西省科学院秦岭天然产物工程中心,陕西省微生物研究所,西安710061

出　　处：《时珍国医国药》2020年第9期2078-2081,共4页Lishizhen Medicine and Materia Medica Research

基　　金：陕西省科学院科技计划顶目(2018nk-01);陕西省自然科学基础研究计划资助项目(2020JM-708);国家自然科学基金(31200257);2018年中医药公共卫生服务补助资金第四次全国中药资源普查项目(财社[2018]43号)。

摘　　要：目的研究高乌头根部二萜生物碱的化学成分及其生物活性。方法采用正、反相柱层析等色谱手段进行分离纯化,利用理化性质及现代波谱技术鉴定其结构;再采用96孔板稀释法评价单体化合物1~6的海虾致死活性。结果从高乌头根部提取高乌甲素后的浸膏中分离出6个二萜生物碱,分别鉴定为:10-羟基刺乌宁(1)、sepaconitine(2)、高乌甲素(3)、冉乌碱(4)、N-去乙酰高乌甲素(5)和N-去乙酰冉乌碱(6)。结论二萜生物碱是高乌头药材的主要及有效化学成分,其中化合物1和2为首次从该种植物中分离得到,化合物1的单晶为首次培养和报道。化合物1~6具有中等的海虾致死活性,其LC50值均小于85.72 mg/L。Objective To investigate the diterpenoid alkaloids from the roots of Aconitum sinomontanum Nakai and their bioactiv-ities.Methods The chemical constituents were isolated and purified by various chromatographic techniques,and their structures were elucidated on the basis of nuclear magnetic resonance and mass spectroscopic analysis.The brine shrimp lethality activities of compounds 1~6 were tested by dilution method of 96-well plate.Results From the Aconitum sinomontanum,Seven diterpenoid alkaloids were established on the basis of spectral and chemical evidences as 10-lappaconidine(1),sepaconitine(2),lappaconitine(3),ranaconitine(4),N-deacetyllappaconitine(5),and N-deacetylranaconitine(6).Conclusion Diterpe-noid alkaloids were the main and effective chemical components from the roots of Aconitum sinomontanum.Compounds 1and 2 were obtained from this plant for the first time.Specifically,the single crystal of compound 1 was cultivated and reported for the first time.Compounds 1-6 showed significant brine shrimp lethality,with the lethal concentration 50(IC50)of less than 85.72 mg/L.

关 键 词：高乌头 二萜生物碱 化学成分 细胞毒活性 

分 类 号：R284.1[医药卫生—中药学]