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Coprinellus miaceus, belongs to Coprinaceae of Agaricales, Basidiomycota, has been used for an edible purposes in asian countries. This experiment was initiated to evaluate the free radical scavenging, free radical scavenging, anti-acetylcholinesterase, anti-inflammatory and α-glucosidase inhibitory activities of C. micaceus fruiting bodies extracted with methanol and hot water. In 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, the scavenging activities of methanol and hot water extracts were lower than that of positive control, BHT. The chelating effects of methanol and hot water extracts were significantly higher than positive control, BHT at the concentrations of 0.125-2.0 mg/mL. In the reducing power assay, methanol and hot water extracts exhibited the lower activities than the positive control, BHT at the 0.125-0.2 mg/mL concentration. In the HPLC analysis of phenolic acids profile of the mushroom fruiting bodies, 4 phenolic compounds including procatechuic acid, chlorogenic acid, (-)-epicatechin, and naringin were detected. The tyrosinase inhibitory activities of methanol and hot water extracts were 91.33% and 91.99% at 2.0 mg/mL concentration, while the inhibitory activity of kojic acid, the positive control, was 99.61%. Nitric oxide (NO) production in lipopolysaccahride (LPS) activated RAW 264.7 cells were inhibited by the methanol extract in a concentration dependent manner. In the acetylcholinesterase (AChE) inhibitory activity assay, methanol and hot water extracts of the mushroom inhibited the AChE by 94.64% and 74.19%, respectively at the 1.0 mg/mL concentration, whereas galanthamine, the standard drug inhibited the AChE activity by 97.80% at the same concentration. The methanol and hot water extracts of the mushroom inhibited the α-glucosidase activity by 62.26% and 67.59%, respectively at the 2.0 mg/mL concentration, while acarbose, the positive control inhibited the α-glucosidase activity by 81.81% at the same concentration. Therefore, it is concluded that fruiting bodies of C. micaceus contained natural antioxidant, anti-inflammatory, anti-acetylcholinesterase and α -glucosidase inhibitory substances which might be used for promoting human health.