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Metabolic syndrome is defined by the presentation of a wide array of interconnected physiological, biochemical, clinical, and metabolic abnormalities that mainly increase the risk of type 2 diabetes mellitus and cardiovascular disease, which is commonly recognized as the primary clinical outcome. Pharmacological treatment for those whose risk factors are not adequately reduced with lifestyle changes remains challenging due to the polypharmacy, the risk of side effects and interactions especially in long-term treatments. The aim of this study was a systematic review of the literature published in previous years about the effects of coumarins against metabolic syndrome using in-vivo animal models. All studies included where pharmacological treatment was given to animals with obesity or diabetes mellitus. Studies included at least 75% of guidelines of the Gold Standard Publication Checklist (GSPC) for improved design, reporting and scientific quality of animal studies. Twenty studies reporting on the effects of different pharmacological treatments were included. Evidence supports that coumarins derivatives present lipid lowering and antidiabetic effects. However, only animal studies were found, so it is necessary the development of clinical studies with improved trial designs. Especially with the most promising compounds.