天然产物是小分子抑制剂的重要来源之一。然而由于天然产物种类繁多,结构多样,运用传统方法筛选效率低,工作量大。因此,寻找操作简单、效率高、成本低的抑制剂筛选方法一直是相关研究人员探索的课题。本文综述了近十年报道的从天然产物中筛选小分子抑制剂的方法,其中重点阐述了色谱质谱检测系统,并对筛选方法的运用前景进行讨论和展望,以供同行参考。 Natural products are one of the important sources of small molecule inhibitors. However, due to the wide range of natural products and the diversified structures, the traditional screening methods are inefficient and labor-intensive. Therefore, looking for an easy, efficient and low-cost inhibitor screening method has been a subject explored by relevant researchers. This review summarizes the methods reported in the last decade for screening small molecule inhibitors from natural products, focusing on the chromatographic mass spectrometry detection system and discussing and prospecting the application of screening methods for peer reference.