Aerobic glycolysis is the most prominent feature of energy metabolism in malignant tumors.About 50% of ATP in tumor cells was synthesized through aerobic glycolysis.At the same time,various intermediate metabolites produced in the process of glycolysis were also important raw materials for the synthesis of proteins and other biological macromolecules.In addition,the increase of lactic acid caused by glycolysis pathway could provide an acidic growth environment for tumor cells,which was conducive to their infiltration and metastasis.Therefore,it played an important role in maintaining the energy demand of tumor cells,the balance of anabolism and tumor invasion and metastasis.Studies have shown that the process of aerobic glycolysis was closely related to glucose transporter,hexokinase,pyruvate kinase and phosphofructokinase.At present,targeting aerobic glycolysis-related transporters and key rate-limiting enzymes have become an effective way for the development of antineoplastic drugs.This paper summarizes the latest progress and mechanism of action of small molecule inhibitors targeting aerobic glycolysis-related proteins in natural products,with a view to providing new ideas and references for drug researchers in related fields.