Russula compacta, a wild mushroom, belongs to Russulaceae, Russulales of Basidiomycota. This study was conducted to evaluate the free radical scavenging, anti-inflammatory, anticholinesterase and anti-α-glucosidase effects from fruiting bodies of R. compacta extracted with methanol and hot water. In 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging effects, the methanol and hot water extracts showed good scavenging effects comparable with positive control, BHT. The chelating effect of methanol and hot water extracts of the mushroom were significantly higher than the positive control, BHT. The reducing power of the methanol and hot water extracts of the mushroom were lower than the positive control at the concentrations tested. In the HPLC anaysis of phenolic acids profile of the mushroom extract, 7 phenolic acids such as gallic acid, vanillin, rutin hydrate, resveratol, quercetin formononetin, and biochanin-A were detected. Nitric oxide (NO) production in lipopolysaccahride (LPS) activated RAW 264.7 cells was inhibited by 1.5-fold with the treatment of methanol extract when compared with the control. In the anti-cholinesterase activity assay, the methanol extract inhibited the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) effects by 73.9% and 81.05% at the 1.0 mg/mL concentration, whereas galanthamine, the standard drug, inhibited the AChE and BChE activities by 97.80% and 81.12%, respectively at the same concentration. The methanol and hot water extracts of the mushroom inhibited the α-glucosidase activity by 55.44% and 62.00%, respectively at the 2.0 mg/mL concentration, while acarbose, the positive control inhibited the α-glucosidase activity by 81.81% at the 2.0 mg/mL concentration. From the experimental results, the fruiting bodies of R. compacta contained natural antioxidant, anti-inflammatory, anti-cholinesterase, and anti-diabetic substances, which might be used for health foods.