The anti-inflammatory effects of Acanthopanax senticosus leaves (ASL) and the effects of extrusion were evaluated. ASL exhibited in vitro and in vivo antiinflammatory activities in experimental systems. Extrusion increased the effect of ASL. ASL reduced C48/80-induced histamine release from HMC-1 cells as well as in vivo model, suggesting that ASL induces mast cell stabilization and has an anti-histamine activity. The effects of ASL and extruded ASL (ASLE) on pro-inflammatory cytokine production were evaluated. ASL treatment reduced MCP- 1, TNF-α, and IL-1β mRNA expressions and decreased their protein levels in HMC-1 cells. Decreases in serum NO, MDA, and TNF-α levels were observed in acute inflammatory rats, and extrusion increased the effects of ASL in a dose-dependent manner. These data support pharmacological basis of ASL and the effect of extrusion for future treatment of inflammation.