Medicinal plants have been used as a source of medicine and they are in great demand worldwide. They have been used for many years to treat health disorders and prevent diseases. Plumbago zeylanica is one of the medicinal plants which are widely used for its therapeutic value. It contains several bioactive compounds like napthoquinones, flavonoids, alkaloids, glycosides, steroids, tri-terpenoids, tannins, fixed oils, fats, proteins, etc among all plumbagin is most important bioactive compounds. It possesses wide range of pharmaceutical activities such as anti-cancer, antidiabetic, anti-malarial, anti-microbial, etc. Several studies have been done in evaluation of its pharmaceutical activities. The aim of the present review is to provide a comprising knowledge related to the chemical composition and pharmaceutical activity of P. zeylanica.