Pleurotus citrinopileatus was successfully cultivated and commercially available in Korea. The antioxidant, xanthine oxidase, tyrosinase inhibitory activities and polyphenol contents of fruiting bodies of Pleurotus citrinopileatus extracted with acetone, hot water and methanol (hereinafter referred to Fr. Ace, Fr. HW and Fr. MeOH). The antioxidant activities on β-carotene-linoleic acid in the Fr. Ace, Fr. HW and Fr. MeOH were 96.12%, 94.21% and 96.52%, respectively at the concentration of 20 mg/ml. Xanthine oxidase inhibition activity in the Fr. Ace, Fr. HW and Fr. MeOH were 30.12%, 35.42% and 29.02%, respectively at the concentration of 5 mg/ml. Tyrosinase inhibition activity in the Fr. Ace, Fr. HW and Fr. MeOH were 58.78%, 49.25% and 63.29%, respectively at the concentration of 1.0 mg/ml. Total polyphenol contents in the Fr. Ace, Fr. HW and Fr. MeOH were 18.99 mgGAEs/g, 16.73 mgGAEs/g and 18.66 mgGAEs/g. These experimental results suggested that fruiting bodies of P. citrinopileatus contained good physio-chemical substances for promoting human health.