天然产物具有结构多样、生物活性广泛等特点，已经成为新药开发及先导化合物发现的主要来源。靶点不明确严重阻碍了许多天然产物的研究和开发进程，靶点解析也因此成为天然产物研究领域亟待突破的瓶颈问题和当前的热点问题。近年来，围绕天然产物靶点发现开展了大量研究，并逐步建立起较为系统的方法体系。天然产物靶点发现策略通常可根据是否需要对研究对象进行化学修饰，分为标记策略和非标记策略2大类。系统梳理上述2类策略框架下的主要靶点发现技术，重点总结各类方法的作用原理、技术优势、局限性、适用场景及其代表性应用案例，为天然产物作用机制研究以及靶点发现提供参考与思路。

Natural products, characterized by structural diversity and broad biological activities, have become a major source for drug discovery and lead compound identification. However, unclear targets have seriously hindered the research and development of many natural products, making target identification a critical bottleneck and a major focus in this field. In recent years, extensive efforts have been devoted to the discovery of natural product targets, and a relatively systematic methodological framework has gradually been established. According to whether chemical modification is required, current target identification strategies for natural products can be broadly classified into two categories:labeled and label-free approaches. This review systematically summarizes the major target identification techniques within these two strategic frameworks, with particular emphasis on their underlying principles, technical advantages, limitations, applicable scenarios, and representative applications, in order to provide references and insights for mechanistic studies and target discovery of natural products.

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国家自然科学基金资助项目（82474495）；国家重点研发计划项目（2020YFE0201800）；河南省高校科技创新人才支持计划（24HASTIT072）；河南省省级科技研发计划联合基金（学科类）项目（252301420113）