Carpobrotus edulis is an important South African medicinal plants used as a food and therapeutic agent in traditional medicine. The aim of this study was to determine the phytochemical content, antioxidant, antiglycation and cytotoxic effect against Human Colon Cancer Cell Line (HCT-116) of aqueous and ethanol-water (1:1v/v) extracts of Carpobrotus edulis.The content of total phenolics and flavonoids in aqueous and ethanol-water extract were 151.99μg and 66.35μg gallic acid equivalents/mg of dry extract, and 38.84μg and 21.96μg quercetin/mg of dry extract, respectively. Furthermore, phenolic compositions analysis indicated the presence of seven majority compounds including sinapic acid, ferulic acid, luteolin7-o-glucoside, hyperoside, isoquercitrin, ellagic acid and isorhamnetin 3-O-rutinoside. The ethanol-water extract (100-1000μg/mL) showed better antioxidant activity than aqueous extract. Furthermore, Carpobrotus edulis extracts, especially ethanol-water extract significantly inhibited the formation of fluorescent advanced glycation end products, prevented oxidation-induced protein damage and exhibited a cytotoxic effect against HCT116 cells, with a significant decrease in cell viability after 24h of incubation. The results obtained suggest that the Carpobrotus edulis extracts could be used as an easily accessible source of natural antioxidants and as potential phytochemicals against protein glycation and colon cancer.