For many decades, the use of synthetic chemicals as drugs has been effective in the treatment of most diseases. Moreover, from ancient to modern history, many traditional plant based medicines are playing an important role in health care. Phytochemicals are natural bioactive compounds found in vegetables, fruits, medicinal plants, aromatic plants, leaves, flowers and roots which act as a defense system to combat against diseases. The phytochemicals from natural products cover a diverse range of chemical entities such as polyphenols, flavonoids, steroidal saponins, organosulphur compounds and vitamins. A number of bioactive compounds generally obtained from terrestrial plants such as isoflavones, diosgenin, resveratrol, quercetin, catechin, sulforaphane, tocotrienols and carotenoids are proven to reduce the risk of cardiovascular diseases and aid in cardioprotection which is the leading cause of death globally. The cardioprotective effects of the various phytochemicals are perhaps due to their antioxidative, antihypercholesteroemic, antiangiogenic, anti-ischemic, inhibition of platelet aggregation and anti inflammatory activities that reduce the risk of cardiovascular disorders. The multi-faceted role of the phytochemicals is mediated by its structure-function relationship and can be considered as leads for cardiovascular drug design in future. This review summarizes the findings of recent studies on selected phytochemicals as prophylactic and therapeutic agents in cardioprotection.