Medicinal plants are major source of bioactive compounds and chemical structures that gives potential beneficial effects. Ocimum sanctum (Tulsi) belongs to the Lamiaceae family, cultivated around tropical and semitropical zone of India and other surrounding Asian countries. In the present review on O. sanctum, the traditional uses, chemical constituents and pharmacological activities are explored. Various medicinal and therapeutic characteristics of Tulsi are found in the aerial parts, roots, leaves and seeds which havea broad range of activity on human being. O. sanctumhas multiple medicinal and therapeutic properties such as antibacterial, anticholinesterase, antioxidant, antifungal, antimicrobial, antiaflatoxigenic, anti-inflammatory and antinoceceptive, anticandidal, toxicological, anti-stress and anticonvulsant, anticancer, wound healing activities.Recent research has proven the anticancer and anti-HIV activity of O. sanctum. The chemical compounds of O. sanctum like alkaloids, phenolics, phenyl, coumarins, flavonoids, fatty acids, essential oils, steroidal, and tannin contents play an important role in herbal medicine. This paper examines the various traditional uses, phytochemical constituents and therapeutic potentials of Tulsi plant will be helpful in the treatment of oral diseases and many medicinal disorders and also will be useful in the expansion of new active principles.