Background/Aims: The prevalence of cardiovascular diseases (CVD) is rising and it is the prime cause of death in all developed countries. Bioactive compounds (BACs) can play a role in CVD prevention and treatment. To examine the scientific evidence supporting BACs groups' efficacy in CVD prevention and treatment, we conducted a systematized review. Methods: All available information on Medline, LILACS and EMBASE; all randomized controlled trials (RCTs) with prospective, parallel or crossover designs in humans in which the BACs effect was compared with that of placebo/control. Vascular homeostasis, blood pressure, endothelial function, oxidative stress and inflammatory biomarkers were considered primary outcomes. Results: We selected 26 articles, verifying their quality based on the Scottish Intercollegiate Guidelines Network, establishing diverse quality levels of scientific evidence according to the design and bias risk of a study. Grades of recommendation were included, depending on the evidence strength of antecedents. Conclusions: Evidence shows that certain BACs' derivative from active lipids and nitrogen compounds, mainly from horse chestnut seed extract, sterol plants, allium derivatives, and certain doses of beta-glucans, can be helpful in decreasing the prevalence of CVD risk factors. However, further rigorous evidence is necessary to support and prove BACs' effect on CVD prevention and treatment.