Tocotrienols, a group of Vitamin E stereoisomers, offer many health benefits including their ability to lower cholesterol levels, and provide anticancer and tumor-suppressive activities. Several recent studies determined the cardioprotective abilities of tocotrienols, although the number is only 1% compared to the study with tocopherols. Both in acute perfusion experiments and in chronic models, tocotrienols attenuate myocardial ischemia-reperfusion injury, artherosclerosis, and reduced ventricular arrythmias. Apart from the antioxidative role of tocotrienols, it appears that tocotrienols mediated cardioprotection is also achieved through the preconditioning-like effect, the best yet devised method of cardioprotection. Hence, tocotrienols likely fulfills the definition of a pharmacological preconditioning agent and give a tremendous opportunity to place tocotrienols as an important therapeutic option in cardiovascular system.