Natural products and health foods have recently received a lot of attention both by health professionals and the common population for improving overall well-being, as well as in the prevention of diseases including cancer. In this line, all types of fruits and vegetables have been re-evaluated and recognized as valuable sources of nutraceuticals. The great number of potentially active nutrients and their multifunctional properties make cactus pear (Opuntia spp.) fruits and cladodes perfect candidates for the production of health-promoting food and food supplements. Although traditionally appreciated for its pharmacological properties by the Native Americans, cactus pear is still hardly recognized because of insufficient scientific information. However, recent studies on Opuntia spp. have demonstrated cactus pear fruit and vegetative cladodes to be excellent candidates for the development of healthy food. Therefore, this review summarizes current knowledge on the chemical composition of Opuntia cacti with particular emphasis in its use as food and medicine.