In this study, two species of mulberry leaves were used as materials and four different size powders (about 20-115 µm, 15-20 µm, 10-15 µm and <10 µm) were prepared. The effects of superfine grinding (SG) on the extraction of active components from mulberry leaves (MLs) and their antioxidant activities were investigated. The results indicated that the contents of the active component such as polyphenol, polysaccharides, alkaloids were increased markedly with the decreasing in the particle size, but there was a bit difference in flavonoids. Additionally, the antioxidants properties of MLs treated on 1,1-diphel-2-picrylhydraxyl (DPPH) radical scavenging activity and ferric reducing antioxidant power (FRAP) were also increased, but the scavenging activity in hydroxyl radical scavenging assay (HAS) decreased in the size of D10. These results indicated that SG could improve the extraction efficiency of active components from MLs and make its antioxidant activity enhance, implying that SG can be an effective way to improve the quality and functionality of MLs in foodstuff and pharmacological field.