草乌的化学成分及镇痛活性研究

doi:10.5246/jcps.2018.12.087

中国药学(英文版) ›› 2018, Vol. 27 ›› Issue (12): 855-863.DOI: 10.5246/jcps.2018.12.087

草乌的化学成分及镇痛活性研究

李倩^1,2, 孙淑仃¹, 王梅英², 李彩凤², 袁丹^1*, 付宏征^2*

1. 沈阳药科大学中药学院, 辽宁沈阳 110016
2. 北京大学医学部药学院天然药物及仿生药物国家重点实验室, 北京 100191

收稿日期:2018-06-01 修回日期:2018-06-26 出版日期:2018-12-30 发布日期:2018-10-08
通讯作者: Tel.: +86-010-82805212, E-mail: drhzfu@sina.com
基金资助:
National Natural Science Foundation of China (Grant No. 30973628) and the National Science and Technology Major Project of China (Grant No. SQ2018ZX090301).

Chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb.

Qian Li^1,2, Shuding Sun¹, Meiying Wang², Caifeng Li², Dan Yuan^1*, Hongzheng Fu^2*

1. College of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, China
2. State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China

Received:2018-06-01 Revised:2018-06-26 Online:2018-12-30 Published:2018-10-08
Contact: Tel.: +86-010-82805212, E-mail: drhzfu@sina.com
Supported by:
National Natural Science Foundation of China (Grant No. 30973628) and the National Science and Technology Major Project of China (Grant No. SQ2018ZX090301).

摘要/Abstract

摘要：

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。

关键词: 草乌, 化学成分, 结构鉴定, 镇痛活性, 分子对接

Abstract:

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.

Key words: Aconitum kusnezoffii Reichb., Chemical constituents, Structural identification, Analgesic activity, Molecular docking

中图分类号:

R284

Supporting:

李倩, 孙淑仃, 王梅英, 李彩凤, 袁丹, 付宏征. 草乌的化学成分及镇痛活性研究[J]. 中国药学(英文版), 2018, 27(12): 855-863.

Qian Li, Shuding Sun, Meiying Wang, Caifeng Li, Dan Yuan, Hongzheng Fu. Chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb.[J]. Journal of Chinese Pharmaceutical Sciences, 2018, 27(12): 855-863.

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草乌的化学成分及镇痛活性研究

Chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb.

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