Throughout history, many different cultures have recognized the potential use of Tribulus terrestris for prevention and treatment of various diseases. Recent studies support the effects of Tribulus terrestris and its extracts in a wide range of applications. These studies raised the possibility of revitalization of therapeutic values in different diseases. It has diuretic, aphrodisiac, Antiurolithic, immunomodulatory, anti-diabetic, absorption enhancing, hypolipidemic, cardio tonic, nervous system tonic, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, anthelmintic, parricidal, and anti-cariogenic activities. However, the exact mechanism of Tribulus terrestris and their long-term effects are not fully understood. Further studies are needed to elucidate the pathophysiological mechanisms of action of Tribulus terrestris as well as its efficacy and safety in treatment of various diseases.