【作者】 罗新根；

【导师】 陈海生； 张卫东；

【作者基本信息】 第二军医大学 ， 天然药物化学， 2001， 硕士

【摘要】 云南狗牙花（Ervatamia yunnanensis Tsiang）是夹竹桃科狗牙花属植物，分布于云南、广西。民间主要用于治疗高血压、腹痛等。云南狗牙花总碱具有非常强的镇痛及脑保护作用。为了进一步寻找具有活性的化学成分，我们对云南狗牙花生物碱及其它部分进行了成分分离，应用现代层析方法共分得16个化合物，根据理化数据和光谱分析(¹H-NMR，¹³C-NMR，DEPT，¹H-¹H COSY，¹³C-¹H COSY，NOESY，COLOC，HMQC，HMBC，EI-MS，FAB-MS)确定了它们的化学结构。并对总碱及部分单体化合物进行了抗成瘾和抗肿瘤活性实验。发现云南狗牙花总碱能够阻断Morphine依赖小鼠复吸模型的再点燃。并且本身不具有阿片样身体依赖性，但各单体化合物的活性还有待进一步观察。16个化合物的结构如下： SUB 1 β-谷甾醇（β-sitosterol） SUB 2 胡萝卜甙（dancosterol） SUB 3 丁香树脂醇（syringaresinol） SUB 4 pinoresinol SUB 5 羽扇豆醇乙酸酯（lupenyl acetate） SUB 6 苦参碱（matrine） SUB 7 冠狗牙花碱（coronaridine） SUB 8 19，20-dihydroisostitsirikine SUB 9 19-s-heyneanine SUB 10 ibogamine SUB 11 EYA-1 SUB 12 19-s-voacangarine and 11-methoxyl-19s-heyneanine SUB 13 EYA-2 SUB 14 conodurine SUB 15 19，20-E-vallesamine SUB 16 10-hydroxy-19，20-dihydroisositsirikine 以上化合物中，SUB2、SUB5、SUB8、SUB9、SUB12、SUB13、SUB14、SUB15均为首次从该植物中分得，其中SUB3、SUB4、SUB6为该属植物中首次发现的结构类型，SUB11、SUB16为新化合物。更多还原

【Abstract】 Dried stem of Ervatamia yunnanensis Tsiang is a folk medicine used for the treatment of hypertension and abdominal pain. The plant is a shrub or arbor distributed in the Yunnan and Guangxi provinces. Total Ervatamia yunnanensis Tsiang alkaloid showed significant antinociceptive effects and cerebral protecttive effects. In order to find the active constituents, fifteen compounds and a mixture with two alkaloids have been isolated from the total Ervatamia yunnanensis Tsiang alkaloid and the other part. The structure of the compounds were elucitated by the analysis of EI-MS, 1H-NMR, 13CNMR and 2D-NMR. In the pharmacological experiments, the total Ervatamia yunnanensis Tsiang alkaloid showed the effects on block of rein~tatement of place preference in relapse model morphine dependment mice. And it didn’t show the psychic dependence and physical dependence itself in mice. The compounds are showed as the following:SUB 1f3-sitosterolSUB 2dancosterolSUB 3syringaresinolSUB 4pinoresinolSUB 5lupenyl acetateSUB 6matrineSUB 7coronaridineSUB 819, 20-dihydroisostitsirikineSUB 91 9-s-heyneanineSUB 10ibogamineSUB 11EYA-lSUB 121 9-s~voacangarine and 11 -methoxyl- 1 9s-heyneanineSUB 13EYA-2SUB 14conodurineSUB 1519, 20-E-vallesamineSUB 1610-hydroxy-19, 20-dihydroisositsirikineSUB2~ SUBS. SUB8~ SUB9~. SUB12-. SUB13.. SUB14 and SUB 15 were isolated from Ervatamia yunnanensis for the first time. SUB3 .. SUB4 -. SUB6 were first isolated from Ervatamia genus. SUB 11 and SUB 16 are new compounds.更多还原