Cardiovascular diseases (CVDs) cause massive morbidity and mortality. In recent years, natural small-molecule therapeutics have attracted much attention for their significant efficacy. Articles have been published to study the intervention of natural drugs (including monomers, compounds, compound and neo-combinations) on one type of cardiovascular disease, but the number and variety of natural drugs included are small and insufficient, and there are no articles detailing the protective effects of different types of natural small molecule drugs on multiple cardiovascular diseases. Natural small molecule drugs have high biological activity and structural diversity, and are more likely to enter the body to exert their effects. In this article, we describe the efficacy of such drugs for anti-atherosclerosis, cardiomyocyte repair, and antagonism of ventricular remodeling, heart failure, and arrhythmias to provide an experimental basis for clinical research and identification of new therapeutic approaches.