Currently, there is considerable interest in the anticancer effects of red beetroot (Beta vulgaris L.) pigment extract, which is used worldwide as red food color E162 and as a natural colorant in cosmetics and drugs. Of particular significance is its broad spectrum of multi-organ antitumor activity demonstrable in laboratory animal models. Further, this nontoxic plant extract, when used in combination with potent anticancer drugs such as doxorubicin (Adriamycin), has the potential to act synergistically and mitigate treatment-related drug toxicity. Betanin, the betacyanin constituent primarily responsible for red beet color, is an antioxidant with an exceptionally high free radical-scavenging activity and is a modulator of oxidative stress. Research focused on anticancer activities of beetroot extract, in animal models, has unraveled their potential benefits as chemopreventive and chemotherapeutic agents, although further progress is needed on the identification and elucidation of anticancer mechanism(s) of individual active constituent(s) in additional well-designed experimental models and clinical trials, as discussed in this chapter.