In this study， human hepatoma cells （HepG2） were treated with α-LA-OA， bovine-α-lactalbumin （α-LA） and the control solution. The effects of α-LA-OA on glycolysis and mitochondrial aerobic respiration were evaluated by the Seahorse Flux. These results indicated that α-LA-OA significantly reduced the glycolysis ability and mitochondrial aerobic respiration ability of HepG2， as well as the ATP levels （P<0.05），whereas α-LA and the control solution did not exhibit the above effects （P>0.05）. This study laid a theoretical basis for the development of tumor-targeted drugs.