云南狗牙花吲哚类生物碱成分及其生物活性研究  

Antiaddictive indole alkaloids in Ervatamia yunnanensis and their bioactivity

作　　者：宣伟东[1] 陈海生[1] 袁志仙[2] 张晓冬[3] 黄矛[3] 

机构地区：[1]第二军医大学药学院天然药物化学教研室,上海200433 [2]解放军第411医院药研中心,上海200081 [3]第二军医大学基础医学部新药评价中心,上海200433

出　　处：《第二军医大学学报》2006年第1期92-96,共5页Academic Journal of Second Military Medical University

基　　金：国家自然科学基金(20272081).~~

摘　　要：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。Objective： To investigate the constituents of indole alkaloids in Ervalamia 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 evalualed 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 Ervalamia yunnanensis for the first time and coronaridine type indole alkaloids are the main antiaddictive constituents of E. yunnanensis.

关 键 词：云南狗牙花 吲哚生物碱类 吗啡依赖口 生物活性 

分 类 号：R284.2[医药卫生—中药学]