There is no doubt that diet could effectively improve health and halt cancers. Dietary phytochemical compounds and their derivatives represent a cornucopia of effectively anticancer compounds. This review discusses existing data on the anticancer activities of curcumin, and then offers possible explanations for and mechanisms of its cancer-preventive action. This review also offers insights into the molecular mechanism and targets through which curcumin modulates cell cycle, apoptotic signals, anti-apoptotic proteins, miRNAs, Wnt/beta-catenin signaling, protein kinases, nuclear factor-κB, proteasome activation, epigenetic regulation including DNA methylation and histone modification. Finally, this review provides explanations for how curcumin reverses the multi-drug resistance (MDR) of cancer cells.