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Tribulus terrestris (puncture vine) belongs to family Zygophyllaceae and it is a herbaceous, mat forming plant in nature. It extensively grows in warm dry tropics all over the world and ecologically adaptated as a typical C-4 xeromorphic plant. T. terrestris is a noxious weed along with its use in many countries as a folk medicine for different purposes from time immemorial. Ancient records describe various medicinal properties of T. terrestris as a popular source to cure variety of different disease conditions in China, India, and Greece. The plant is used directly as a herb or as a main component for production of a number of medicines and food supplements such as for physical rejuvenation, therapy for the conditions affecting liver, kidney, cardiovascular system and immune systems. Also it is used as a folk medicine for increased muscle strength, sexual potency and in treatments of urinary infections, heart diseases and cough. It is considered invigorating stimulant, aphrodisiac, and nutritive. This review discusses the most commonly recognized medicinal properties of this herb. The chemistry of T. terrestris extracts to establish the relationship between medicinal properties of this important plant will also be reviewed.