中药治疗疾病的物质基础、药效和机制研究已较充分，然而靶点的研究进展相对缓慢，这和靶点研究本身的被动性和难度有一定关系。本文基于国内外文献报道，并结合笔者的研究实践，对此进行了较为系统的探讨。本文主要介绍三种技术路径：“线索”驱动、噬菌体展示以及亲和垂钓。并提及两种方案：酶解法和光交联法。基于这些技术方案，加强中药有效成分靶点研究的实践，将会有助于阐明中药治疗疾病的现代科学基础，有助于发展现代中药和创新中药。

Nowadays,there has been many researches on the material basis,effectiveness and action mechanisms of Chinese herbs.However,the action target research of active ingredients from herbs is relatively less,which may be associated with its own passivity and difficulty of current target research.For improving the target discovery efficiency of active components,it is critical to approach some initiatives by technical routes to find targets.In this review,based on the domestic and foreign literatures and our previous researches,three different technical routes for the target discovery of active ingredients were introduced in detail,including“clue”drive,phage display and pull-down,and other two options--drug affinity responsive target stability(DARTS)and light cross-linking.Using these technical approaches,it is benefitial to clarifing the modern science basis of Chinese herbs by strengthening the target research practice of active components,and developing modern and innovative Chinese herbs.

国家自然科学基金委青年基金项目（81303246）：脑局部糖原代谢在人参总皂苷抗应激致海马结构可塑性损伤中的作用研究，负责人：赵玉男；国家自然科学基金委重大研究计划（90713043）：基于小檗碱神经元保护作用探讨其PI3-K/AKT作用的始动位点及其信号转导，负责人：杜力军。