刘智慧, 马浩, 王伟平, 徐少锋, 王玲, 石建功, 王晓良. 天麻素及派立辛改善东莨菪碱致学习记忆障碍的构效关系J. 药学学报, 2016,51(5): 743-748. doi: 10.16438/j.0513-4870.2016-0196
引用本文: 刘智慧, 马浩, 王伟平, 徐少锋, 王玲, 石建功, 王晓良. 天麻素及派立辛改善东莨菪碱致学习记忆障碍的构效关系J. 药学学报, 2016,51(5): 743-748. doi: 10.16438/j.0513-4870.2016-0196
LIU Zhi-hui, MA Hao, WANG Wei-ping, XU Shao-feng, WANG Ling, SHI Jian-gong, WANG Xiao-liang. Structure-activity relationship of gastrodin and parishins on learning and memory deficits induced by scopolamineJ. Acta Pharmaceutica Sinica, 2016,51(5): 743-748. doi: 10.16438/j.0513-4870.2016-0196
Citation: LIU Zhi-hui, MA Hao, WANG Wei-ping, XU Shao-feng, WANG Ling, SHI Jian-gong, WANG Xiao-liang. Structure-activity relationship of gastrodin and parishins on learning and memory deficits induced by scopolamineJ. Acta Pharmaceutica Sinica, 2016,51(5): 743-748. doi: 10.16438/j.0513-4870.2016-0196

天麻素及派立辛改善东莨菪碱致学习记忆障碍的构效关系

Structure-activity relationship of gastrodin and parishins on learning and memory deficits induced by scopolamine

  • 摘要: 天麻素是天麻的主要有效成分之一, 派立辛(parishin) 和parishin C 也是从传统中药天麻中提取到的水溶性单体化合物, 它们与天麻素在结构上关系紧密。Parishin 类化合物为天麻素与柠檬酸在不同羧基位点酯合后的化合物。为了比较它们改善学习记忆的能力, 本课题组采用东莨菪碱造成的学习记忆障碍模型和在体长时程增强(long-term potentiation, LTP) 记录, 研究了天麻素、parishin 和parishin C 的作用并分析其构效关系。Morris水迷宫实验中, 15 和50 mg·kg-1 parishin C, 以及150 mg·kg-1 parishin 可显著改善东莨菪碱损伤的空间学习记忆能力, 缩短寻找平台的潜伏期(P < 0.05), 而天麻素在150 mg·kg-1时的作用不显著。大鼠在体LTP 研究结果显示, parishin C(5、10 和20 mg·kg-1) 及parishin(10、30 和100 mg·kg-1) 均可剂量依赖地改善东莨菪碱抑制的LTP(P < 0.05); 天麻素(100 mg·kg-1) 仅有改善趋势(P > 0.05)。因而, 在东莨菪碱模型中parishin C 的作用强于parishin, 天麻素的作用最弱。

     

    Abstract: Gastrodin, parishin and parishin C were purified from a water extract of GE (rhizome of Gastrodia elata, an herb medicine for treatment of neuronal disorders). In order to compare the pharmacological effects of gastrodin, parishin and parishin C on improving cognition deficits, we tested them in an animal model of cognition disorders induced by scopolamine and in a study of in vivo long-term potentiation (LTP) recordings. In the Morris water maze task, parishin C (15 and 50 mg·kg-1, P < 0.05) and parishin (150 mg·kg-1, P < 0.05), improved spatial learning and memory significantly. However, gastrodin showed no significant effects at the dose of 150 mg·kg-1. In vivo LTP recordings showed that parishin C at 5, 10 and 20 mg·kg-1, parishin at 10, 30 and 100 mg·kg-1 reversed the suppression of LTP by scopolamine in rats in a dose-dependent manner. However, gastrodin at 100 mg·kg-1 showed only a modest effect. In summary, the action of parishin C in the improvement of dementia induced by scopolamine was more potent than parishin and gastrodin.

     

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