Several studies have focused on chemical agents, tailored from natural edible products, used to prevent and treat various diseases. β-elemene is a well-known compound derived from Curcuma wenyujin that possesses a wide spectrum of anticancer properties under preclinical and clinical conditions. Several studies have demonstrated its inhibitory effect both in humans and animals with cancers. Numerous in vivo and in vitro experimental models have revealed that β-elemene can modulate multiple molecular pathways involved in carcinogenesis. In general, (1) β-elemene itself can inhibit and kill tumor cells through a variety of mechanisms, and (2) can synergistically enhance the effect of radiotherapy and/or chemotherapy, (3) also can regulate autoimmune in the treatment of tumors. In this article, we critically focused on the available scientific evidence discussing the use of β-elemene in cancer prevention, and its molecular targets and mechanisms of action in different types of cancer. In addition, we have discussed its sources, chemistry, bioavailability, and future research directions.