Medicinal flora have proven their significance as a source of biologically active ingredients used in folk medicine. These active molecules have therapeutic potential and a vital pool for identifying novel medicine. Medicinal plants are widely used in developing societies like in India, Pakistan, and Southern America because they are thought to be cheaper than modern medicines, most effective and readily available. They have been used for thousands of years to treat and prevent health disorders along with epidemics. Also, they utilized for flavour and for conserving food items. They play a golden role in the development of human culture. Plants produced the diversity of secondary metabolites that are responsible for the biological functions of plants used around the world. Calotropis procera is drought-resistant medicinal perennial shrub mostly found in arid to semi-arid areas. It is a major source of secondary metabolites including phenols, flavonoids, terpenoids, sugars, alkaloids, tannins cardenolides, glycoside, saponins and steroids. It has medicinal properties as hepatoprotective, antioxidant, inflammatory, antimicrobial, and antimalarial. It is vigorous used for the ailment of common diseases, i.e. fever, leprosy, eczema, diarrhea, dysentery and jaundice. This short-review about the phytochemistry of Calotropis procera and its traditional uses.