Tribulus terrestris Linn. (Zygophyllaceae) has been used since ancient times to treat various health ailments. Different parts of the plant have been used by traditional physicians, however the dried entire fruit is more commonly used as ‘Gokshura’ and ‘Ikshugandha’ in Ayurveda and as ‘Khar-e-Khasak Khurd’ in Unani System of Medicine for its diuretic, aphrodisiac, emmenagogue, laxative, lactagogue, lithotriptic, demulcent, stomachic and astringent properties. It is therapeutically employed for its efficacy in vesicular calculi, urinary discharge, strangury, sexual debility, dysuria, burning micturation, ammenorrhoea, cough and asthma. Fruits contain traces of alkaloids, flavonoids, fixed oil, small quantity of essential oil, resins and nitrates. This review aims to provide an electronic database regarding phytopharmacological properties of T. terrestris, in particular with its description in Unani classical literature along with the recent research work done by many authors; so that future research work can be made at ease and it will help in revalidating scientifically the claimed activities of the drug mentioned in classical literatures and further exploration of any new therapeutic activity based on phyto-chemistry.