The açaí palm (Euterpe oleracea Mart.), a species belonging to the Arecaceae family, has been cultivated for thousands of years in tropical Central and South America as a multipurpose dietary plant. The recent introduction of açaí fruit and its nutritional and healing qualities to regions outside its origin has rapidly expanded global demand for açaí berry. The health-promoting and disease-preventing properties of this plant are attributed to numerous bioactive phenolic compounds present in the leaf, pulp, fruit, skin, and seeds. The purpose of this review is to present an up-to-date, comprehensive, and critical evaluation of the health benefits of açaí and its phytochemicals with a special focus on cellular and molecular mechanisms of action. In vitro and in vivo studies showed that açaí possesses antioxidant and anti-inflammatory properties and exerts cardioprotective, gastroprotective, hepatoprotective, neuroprotective, renoprotective, antilipidemic, antidiabetic, and antineoplastic activities. Moreover, clinical trials have suggested that açaí can protect against metabolic stress induced by oxidation, inflammation, vascular abnormalities, and physical exertion. Due to its medicinal properties and the absence of undesirable effects, açaí shows a promising future in health promotion and disease prevention, in addition to a vast economic potential in the food and cosmetic industries.