唐希灿, 金国章, 冯洁, 张振德, 韩怡凡. 毛叶轮环藤生物碱的肌松药理作用研究J. 药学学报, 1980, 15(9): 513-519.
引用本文: 唐希灿, 金国章, 冯洁, 张振德, 韩怡凡. 毛叶轮环藤生物碱的肌松药理作用研究J. 药学学报, 1980, 15(9): 513-519.
Tang Xican, Jin Guozhang, Feng Jie, Zhang Zhende , Han Yifan, . STUDIES ON THE NEUROMUSCULAR BLOCKING ACTIVITY OF ALKALOIDS OF CYCLEA BARBATA (WALL) MIERSJ. Acta Pharmaceutica Sinica, 1980, 15(9): 513-519.
Citation: Tang Xican, Jin Guozhang, Feng Jie, Zhang Zhende , Han Yifan, . STUDIES ON THE NEUROMUSCULAR BLOCKING ACTIVITY OF ALKALOIDS OF CYCLEA BARBATA (WALL) MIERSJ. Acta Pharmaceutica Sinica, 1980, 15(9): 513-519.

毛叶轮环藤生物碱的肌松药理作用研究

STUDIES ON THE NEUROMUSCULAR BLOCKING ACTIVITY OF ALKALOIDS OF CYCLEA BARBATA (WALL) MIERS

  • 摘要: 本文研究了从毛叶轮环藤分离到的汉防己甲素,高阿洛莫林碱,左旋箭毒碱和异谷树碱的肌松作用。家免垂头试验表明,他们的碘甲烷盐均有肌松作用,但以左旋箭毒碱和高阿洛莫林碱的作用较强。将左旋箭毒碱制备成二甲基左旋箭毒碱氯甲烷盐衍生物后,肌松作用增强1.5~3倍。对小鼠,家免,猫和狗的肌松作用比右旋筒箭毒碱约强0.5~4倍,对大鼠的肌松作用强度与右旋筒箭毒碱相当。左旋箭毒碱,二甲基左旋箭毒碱及高阿洛莫林碱的作用均类似于右旋筒箭毒碱,属于非去极化型肌松剂。给麻醉猫、狗快速静注2~3倍肌松剂量的左旋箭毒碱或二甲基左旋箭毒碱,有降压和组胺释放作用。对猫颈交感神经节无抑制作用。对离体家兔及豚鼠廻肠的阿托品样作用很弱。家兔连续静注达40~50倍垂头剂量,对心电图无明显影响,静注5~10倍垂头剂量,48-72小时后剖杀检查,未见对内脏器官有明显病理损害。小鼠及大鼠试验结果表明二甲基左旋箭毒碱的治疗指数高于右旋筒箭毒碱。

     

    Abstract: The neuromuscular blocking activity of l-curine, homoaromoline, d-tetrandrine and d-chondrodendrine isolated from the root of Cyclea barbata Miers in Hai-nan Island was studied. In rabbits the head-drop test showed that the quaternary salts of l-curarine and homoaromoline were more potent than the other two alkaloids. Dimethyl l-curine dimethiodide or dimethochloride derivatives were prepared and examined in conscious rabbits, mice, rats, cats and dogs. It was found that the dimethyl derivatives were about 1.5~3 times stronger than the parent compound and were 0.5~4 times more active than tubocurarine except in rats. In sciatic-tibialis preparations of anaesthetized rabbits, the neuromuscular block produced by l-curine and its derivatives or homoaromoline was readily reversed by neostigmine, antagonized by suxamethonium and augmented by tubocurarine. Tetanus was poorly sustained during its partial block, and the post-tetanus twiching were temporarily increased in amplitude. In conscious chicks it produced a flaccid paralysis. The results indicate that the quaternary salts of these three compounds are nondepolarizing blocking drugs like tubocurarine. In threefold neuromuscular blocking doses, l-curine and its dimethyl derivative all produced hypotension in anaesthetized cats and dogs and released histamine in anaesthetized dogs, but these effects were less potent than tubocurarine. In contrast to tubocurarine, its ganglion blocking effects were absent. In conscious and artificially ventilated rabbits, l-curine or dimethyl l-curine at 40~50 times the head-drop dose produced no marked changes in EGG. In rabbits sacrificed 48~72 hours after successive injection of 5~10 times head-drop dose of l-curine or dimethyl l-curine, no obvious pathological change in various tissues was found. In mice and rats, l-curine and dimethyl l-curine had a higher therapeutive index than tubocurarine.

     

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