Enzymes are important drug targets,and the development of enzyme inhibitors is significant for treatment of diseases.Natural products characterized by various kinds,diverse structures and extensive biological activities are an abundant source of enzyme inhibitors.However,natural products have complex structures and low content of active ingredients,so it is crucial to screen enzyme inhibitors efficiently and accurately.In recent years,with the deepening of research on the conformation of biological macromolecules and the vigorous development of computer science and the innovation of modern separation and analysis techniques and instruments,a series of novel screening techniques and methods of enzyme inhibitors have been developed.In this paper,rapid screening techniques and methods for natural enzyme inhibitors,including computer virtual screening,affinity screening based on the specific interaction between enzyme molecules and ligands,and biological activity assay combined with chromatographic separation,were systematically introduced,then their advantages and disadvantages of these methods were also compared,in order to provide references for the exploration of enzyme inhibitors in natural products from traditional Chinese medicine.