神经药理学报 ›› 2014, Vol. 4 ›› Issue (2): 1-7.

• 名家论坛 •    下一篇

从姜黄素向阿尔茨海默病药物的研发谈活性化合物向新药发现的推进  

殷明, 王泽剑, 赵文娟   

  1. 上海交通大学药学院,上海,200240,中国
  • 出版日期:2014-04-26 发布日期:2014-06-27
  • 通讯作者: 殷明,男,医学博士,教授;研究方向:神经药理学;联系电话:021-34206836,E-mail:myin@sjtu.edu.cn
  • 基金资助:

    国家自然科学基金(81471232,81270432);上海市科委基金(14431901400);上海交通大学科技创新专项资金(14X130040002)。

From Curcumin Toward Treatment of Alzheimer’s Disease: Some Thoughts on New Drug Discovery

YIN Ming, WANG Ze-jian, ZHAO Wen-juan   

  1. Shanghai Jiaotong University School of Pharmacy, Shanghai, 200240, China
  • Online:2014-04-26 Published:2014-06-27
  • Contact: 殷明,男,医学博士,教授;研究方向:神经药理学;联系电话:021-34206836,E-mail:myin@sjtu.edu.cn
  • Supported by:

    国家自然科学基金(81471232,81270432);上海市科委基金(14431901400);上海交通大学科技创新专项资金(14X130040002)。

摘要: 过去的二十年中,国际上围绕姜黄素从活性研究向新药成药(例如阿尔茨海默病药物等)的推进,到目前基本证明是失败的,代表了生物医学领域围绕化合物研究思路的混乱。药理学研究中涉及到化合物分子的探索目的大致分为:对化学合成或分离提取的分子进行生物活性作用谱的观察记录;在取得初步活性和药效学、药动学数据基础上向新药研发的推进;对具有明确成药性前景的化合物进行作用机制研究;将具有比较明确作用机制的化合物用作“工具”,参加到生物医学的基础探索中去。因此,在着手进行一个化合物的研究之前,需要明确研究目的,进行结构比较和详尽的文献研究,否则可能会造成研究资源和时间的浪费。

关键词: 姜黄素, 阿尔茨海默病, 活性, 药效学, 机制, 成药性

Abstract: During the last two decades, the story of vigorous curcumin R&D from activity assay to pre-clinical and clinical trials for Alzheimer’s disease and to final failure represents a chaotic thinking on pharmaceutical drug development. The research goals of pharmacologically involved compounds are usually as follows: to observe and record the activity spectrum of synthesized or isolated molecules; to advance drug candidate development based on activity,pharmacodynamic and pharmacokinetic data; to study the mechanism of action of druggable compound; and to participate in the basic biomedical research with the compound as a tool after the mechanism has been well known. Therefore, to avoid the waste of research resources and time,it is necessary for people to set up a clear goal,compare the chemical structures and exhaustively review the literature before a compound is going to be studied.

Key words: curcumin, Alzheimer&, rsquo, s disease, activity, pharmacodynamics, mechanism, druggability

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