云南狗牙花吲哚类生物碱成分及其生物活性研究

目的:研究云南狗牙花吲哚类生物碱成分,阐明其戒毒活性的物质基础.方法:云南狗牙花茎枝粉末的95%乙醇提取浸膏经酸提碱沉后得到总生物碱(TEYA),TEYA经反复硅胶柱层析、Sephadex LH20 凝胶柱层析分离纯化化学成分,波谱学分析鉴定化学结构,采用条件性位置偏爱模型对单体化合物进行活性评价.结果:分离鉴定了9个吲哚类生物成分:冠狗牙花定碱(1),伏康京碱(2),3-R-乙氧基冠狗牙花定碱(3),3-S-乙氧基冠狗牙花定碱(4), 19-表-海尼山辣椒碱(5),海尼山辣椒碱(6),19-表-非洲伏康树碱(7),7-羟基冠狗牙花定碱(8),12-methoxyl-voaphylline(9).化合物2、7对吗啡的身体依赖性和精神依赖性都有一定的防治作用.结论:化合物3、4、8、9为首次从该植物中分离得到,冠狗牙花定碱类吲哚生物碱为云南狗牙花总碱的主要活性成分.

Antiaddictive indole alkaloids in Ervatamia yunnanensis and their bioactivity

Objective:To investigate the constituents of indole alkaloids in Ervatamia yunnanensis and their antiaddictive bioactivities. Methods: The preliminary alkaloids(TEYA) were extracted by 95% EtOH from the stems of Ervatamia yunnanensis.TEYA was then purified by silica gel and Sephadex LH20 column chromatography repeatedly and its structure was identified with spectral analysis.The antiaddictive effects of these indole alkaloids were evaluated by Conditioned Place Preference(CPP) experiments.Results: Nine indole alkaloids were obtained and identified as: coronaridine(1),voacangine(2),3-R-ethoxycoronaridine(3),3-S-ethoxycoronaridine(4), 19-epi-heyneanine(5),heyneanine(6),19-epi-voacristine(7),coronaridine hydroxyindolenine(8) and 12-methoxyl-voaphylline(9).Among them voacangine (2) and 19-epi-voacristine(7) were effective in prevention and treatment of addiction induced by morphine in rats(n=8).Conclusion: Compounds 3,4,8,and 9 have been isolated from Ervatamia yunnanensis for the first time and coronaridine-type indole alkaloids are the main antiaddictive constituents of E.yunnanensis.