Metabolic syndrome (MetS) is a set of cardiovascular risk factors which severely increases the risk of type II diabetes, renal disease and cardiovascular disease. Over the last decades, the role of dietary bioactive substances in features of MetS has been extensively investigated. Due to their multiple properties, these plant-derived natural compounds have demonstrated to provide positive effects in obesity, diabetes, renal and in cardiovascular disease. Catechins of green tea and caffeine reduce body mass index and waist circumference. Catechins, anthocyanins and proanthocyanidins of cocoa reduce blood pressure and blood glucose. Curcumin and silymarin exert hepatoprotective effects. Monacolins of red yeast rice are effective cholesterol-lowering agents. However, inconsistent or conflicting results have been found in clinical trials when other promising compounds in vitro or in animal studies, such as policosanol, curcumin or silymarin, were used. Low oral bioavailability of substances, ineffective dosages, inadequate treatment duration and insufficient statistical approach may explain the lack of effectiveness observed in some human studies. Further clinical studies are needed to better understand the role of bioactive compounds in the prevention and management of MetS.