Selective killing of tumor cells while mitigating damage to normal tissues is a major challenge for current therapeutic oncology strategies. Studies have shown that solid tumor cells are often in a state of oxygen, glucose, or other nutrient deprivation due to the rapid proliferation of tumor cells. Therefore, targeting glucose-deficient tumor cells may become a new strategy for selective killing of tumor cells. Burdock sapogenins are the main active components of the clinically used traditional Chinese medicine burdock. Existing studies have shown that burdock sapogenins have anti-tumor activity and can effectively inhibit tumor growth in a variety of tumor models. Yu Qiang’s group at the Shanghai Institute of Pharmaceutical Sciences, Chinese Academy of Sciences, conducted an in-depth study on the anti-tumor mechanism of burdock sapogenins and found that under glucose deficiency, burdock sapogenins caused the decrease of ATP level and the increase of reactive oxygen species level in tumor cells by inhibiting mitochondrial respiration, which led to the death of tumor cells. It was also found that the combination of burdock sapogenins and the glycolysis inhibitor 2-deoxy-D-glucose could selectively kill tumor cells with low toxicity to normal cells.