As olive oil is the main source of calories in the Mediterranean diet, a large number of studies have been carried out to characterize its role in various diseases and exploitation for the prevention and treatment of hypertension, carcinogenesis, diabetes, atherosclerosis, and other diseases. As one of the major polyphenols present in virgin olive oil, hydroxytyrosol shows a variety of pharmacological activities such as antioxidant properties, anticancer, anti-inflammatory, and neuroprotective activities, and beneficial effects on the cardiovascular system, which show its potentiality for the development of dietary supplements. In the future, more attention should be paid to its action mechanism in vivo and synergistic effect. Further research will be performed to provide the theoretical basis for hydroxytyrosol and its derivatives use as health supplements.