The chestnut inner shell (CIS) has long been used as a medicinal herb for strengthening the antioxidant in the cosmetic industry. However, little is known about the antioxidant and anticancer effects of the CIS.The antioxidant and anticancer effects of CIS extracts (CISEs) were investigated by the use of various methods and cancer cell lines, respectively. The total polyphenol content of CISEs using ethanol, methanol, butanol, ethyl acetate and water were 53.30, 43.98, 32.16, 26.79 and 11.53 mg gallic acid equivalents g(-1), respectively. The CISEs using ethanol and methanol exhibited high antioxidant activities in the 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, β-carotene bleaching and ferric reducing ability of plasma assays; the effects were equivalent to those of butylated hydroxytoluene. All CISEs at 2.5 mg mL(-1) were shown to have a cytotoxic effect over 50%, and the CISE using ethyl acetate at 0.6 mg mL(-1) was proved to have 90% cytotoxic effect against the tested cancer cells.The ethanol and methanol CISEs had potent antioxidant effects, and the ethyl acetate CISE had the highest cytotoxicity. These results suggest that CISEs could be used as functional ingredients for antioxidant and anticancer effects in foods as extraction solvents.