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Cancer is one of the leading causes of deaths worldwide.Compounds derived from traditional Chinese medicines have been an important source of anticancer drugs and adjuvant agents to potentiate the efficacy of chemotherapeutic drugs and improve the side effects of chemotherapy.Herba epimediiis one of most popular herbs used in China traditionally for the treatment of multiple diseases, including osteoporosis, sexual dysfunction, hypertensionand common inflammatory diseases.Studies show Herba epimediialso possesses anticancer activity.Flavonol glycosides icariin and icariside Ⅱ are the main bioactive components of Herba epimedii.They have been found to possess anticancer activities against various human cancer cell linesin vitro and mouse tumor modelsin vivo via their effects on multiple biological pathways, including cell cycle regulation, apoptosis, angiogenesis, and metastasis, and a variety of signaling pathways including JAK2-STAT3, MAPK-ERK, and PI3k-Akt-mTOR.The review is aimed to provide an overview of the current research results supporting their therapeutic effects and to highlight the molecular targets and action mechanisms.