Cancer is a pathology that impacts in a profound manner all over the world. The election strategy against cancer often uses chemotherapy and radiotherapy, which, more often than not, can present many side effects and are not always considered reliable efficacy. By contrast, it is widely known that a diet rich in fruit and vegetables has a protective effect against cancer insurgence and development. Polyphenols are generally believed to be responsible for those beneficial actions, at least partially. In this review, we highlight the metabolic interaction between polyphenols and our metabolism and discuss their potential for anticancer prevention and therapy.