Nowadays cancers pose a great threat to the health of human beings. Based on studies on the flavonoids and other bioactive compounds of Citrus fruits in current literature, it was widely suggested that the consumption of Citrus fruits is beneficial to the prevention and treatment of human chronic diseases including cancers. In the past decades, the study concerning Citrus flavonoids has covered various areas including the type, content and distribution of flavonoids in fruits; their variation between wild and cultivated genotypes; their antioxidant, antiinflammation, anti-aging, antimicrobial and anticarcinogenic activities. To enlighten future Citrus germplasm study, this review introduces briefly the functions of main types of Citrus flavonoids, including antioxidant, antiinflammation and anti-aging activities, and their relationships to human cancers. Most importantly, the mechanisms of action by which Citrus flavonoids play their roles in human cancer prevention and treatment were summarized.