云南狗牙花活性成分的研究
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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,~(13)C-NMR,DEPT,~1H-~1H COSY,~(13)C-~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。
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 1 f3-sitosterol
     SUB 2 dancosterol
     SUB 3 syringaresinol
     SUB 4 pinoresinol
     SUB 5 lupenyl acetate
     SUB 6 matrine
     SUB 7 coronaridine
     SUB 8 19, 20-dihydroisostitsirikine
     SUB 9 1 9-s-heyneanine
     SUB 10 ibogamine
     SUB 11 EYA-l
     SUB 12 1 9-s~voacangarine and 11 -methoxyl- 1 9s-heyneanine
     SUB 13 EYA-2
     SUB 14 conodurine
     SUB 15 19, 20-E-vallesamine
     SUB 16 10-hydroxy-19, 20-dihydroisositsirikine
     SUB2~ 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.
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