The purpose of this review was to discuss the physiological and biochemical mechanisms mediating the exercise-induced cardiovascular effects. The effects of regular exercise in heart structure/function are reviewed. It is documented that regular exercise improves the plasticity of left ventricular mass and function. Moreover, exercise training has the potential to prevent myocardial damage related to ischemia/reperfusion injury by inducing key antioxidative enzymes. In systolic heart failure, endurance exercise can induce reverse remodelling with improvement of diastolic and systolic left ventricular function. The authors also review the vascular effects of exercise. The majority of exercise effects on the vascular endothelium are mediated by intermittent increases of laminar shear stress associated with increased cardiac output. Many molecular pathways are induced such as the activation of endothelial nitric oxide synthase, resulting in an increase of nitric oxide, responsible for vasodilatation of the arteries. Thus, these findings suggest that physical activity has strong beneficial effects on the cardiovascular system and that further studies are necessary to optimize the clinical efficacy of exercise training interventions.