In order to explore the comprehensive utilization value of L. macranthoides, investigated the particle structure, effective compositions contents, dissolution rate and antioxidant activity of L. macranthoides processed ultrafine and common grinding. It was found that the ultrastructure of L. macranthoides was changed by ultrafine grinding, and its cell wall and crude fiber structure were destroyed. The dissolution contents of chlorogenic acid, Macranthoidin B, Dipsacoside B, Luteolin 7-glucoside and caffeic acid were increased after ultrafine grinding. The dissolution rate of chlorogenic acid from ultra-fine griding powder was significantly higher than that of common griding power of L. macranthoides. Furthermore, scavenging ability of DPPH· were investigated. The DPPH· scavenging ability of L. macranthoides power were increased to 1.36 times by ultrafine grinding. Ultrafine grinding improved the physical-chemical properties of L. macranthoides, destroyed its intact structure of tissues and cells at the original state, improved its antioxidant capacities, and had a certain potential in the application of food and medicine industries.