摘要
In the present study,we aimed to investigate the chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb. The isolation and purification of components were achieved by a series of chromatography, including silica gel, Sephadex LH-20 and HPLC. By using spectroscopic analysis, their structures were identified. Using PDE-4A as analgesic target, moleculardocking was conducted between isolated compounds by using Schrodinger software. Neoline is a typical non-ester diterpene alkaloid. It was studied by using the mouse torsion body method and hot plate method. A total of 12 diterpene alkaloids were obtainedand identified as Mesaconitine(1), Bewutine (2), Bewudine (3), Songoramine (4), Songorine (5), Neoline (6), Talasamine (7), isotalatizidine (8), Hokbusine A (9), Mesaconine (10), 8-OEt-14-benzoylmesaconine (11), 8-Methoxy-14-benzoyl-beiwutinine (12).Compounds 9 and 12 were isolated from Aconitum kusnezoffii Reichb. for the first time. Twelve diterpenealkaloids could act on the analgesic target. Neoline is a typical non-ester diterpene alkaloid. It had significant analgesic effect. Diterpene alkaloids were the main components of Aconitum kusnezoffiiReichb., and they had good analgesic activity.
本文对草乌的化学成分及镇痛活性进行研究,采用硅胶、Sephadex LH-20、HPLC等系列色谱法对其进行分离纯化,采用波谱等手段对其结构进行了鉴定。以PDE-4A为镇痛靶点,使用薛定谔软件对分离出来的化合物进行分子对接。尼奥林是一种典型的非酯型二萜生物碱,使用热板镇痛法和醋酸扭转体法研究它的镇痛活性。结果发现,12种二萜生物碱被分离得到,他们的结构分别为新乌头碱(1),北乌碱(2),北乌定(3),去氢宋果灵(4),宋果灵(5),尼奥林(6),塔拉萨敏(7),异塔拉乌头定(8),荷克布星A (9),新乌头原碱(10), 8-乙酰基-14-苯甲酰基中乌头原碱(11), 8-甲氧基-14-苯甲酰-beiwutinine(12)。其中化合物9,12首次从草乌中分离得到,12种二萜生物碱都可以作用于镇痛靶点PDE-4A。尼奥林是典型的非酯型二萜生物碱,它具有很好的镇痛活性。
基金
National Natural Science Foundation of China(Grant No.30973628)
the National Science and Technology Major Project of China(Grant No.SQ2018ZX090301)
