Adipose tissue secretes many adipokines that regulate important physiological functions. Growing studies have highlighted that these bioactive molecules may contribute to the development of metabolic and cardiovascular diseases. Adipokines exert systemic metabolic effects and independent activity on numerous cells of the cardiovascular system, including cardiomyocytes and vascular cell walls. Adiponectin shows anti-inflammatory and anti-atherosclerotic activity on blood vessels. Conversely, resistin is endowed with pro-inflammatory effects and stimulates the proliferation of smooth muscle cells, thus promoting the development of atherosclerotic plaque. Leptin plays an important role in cardiac remodeling and blood pressure regulation through the activation of the sympathetic system. Obesity is a pathological condition associated with hypertrophy of white adipose tissue, which stimulates the production of pro-inflammatory adipokines while, it reduces the production of anti-inflammatory adipokines. The delicate balance among the production of pro-and anti-inflammatory molecules generated by adipose tissue affects, not only the development of metabolic complications associated with obesity, but also the onset and progression of atherosclerosis. Therefore, adipokines may be regarded as potential agents of clinical interest in the treatment of a wide range of metabolic disorders and as potential biomarkers useful for early detection of metabolic, cardiovascular and inflammatory diseases.