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Epimedium koreanum Nakai is a commonly used herbal medicine owing to its health beneficial effects. This study examined the anti-cancer effect of E. koreanum extracts and icariin, which is the main prenylated compound. on a human breast cancer cell line (MDA-MB-231). In the Annexin V-FITC/PI staining experiment, the apoptotic ratio in the plants cultivated in South Korea, North Korea and China was 6.44%, 24.73% and 14.11%,respectively. RT=PCR was used to examine the effects of E. koreanum cultivated in North Korea on the expression of the apoptosis-related gene. The effects of Icariin on the apoptotic pathway were investigated. As a result, the p53level increased significantly in a time-dependent manner. The Bcl-2 level decreased, and the Bax and p53 levels increased in a dose-dependent manner. These results suggest that Icarii canact as a potent anti-tumor agent, and is a promising candidate for health food materials against human breast cancer cells.