Cardiovascular diseases (CVD) such as myocardial infarction and stroke are a major cause of morbidity and mortality worldwide. Impairment of the normal vasorelaxant functions of the vascular endothelium, termed endothelial dysfunction; appear to underlie the pathogenesis of CVD. Endothelial dysfunction is often secondary to abnormal increases in oxidative stress, inflammation and overactivity of the renin–angiotensin system (RAS), which makes these pathways attractive targets for therapeutic interventions. Given the side-effects associated with synthetic pharmaceutical agents, there is growing interest in using natural products such as bioactive peptides for treating chronic diseases like CVD. In this review, we discuss the potential for bioactive peptides with antioxidant, anti-inflammatory and RAS modulating properties for treating endothelial dysfunction and preventing CVD.