Plant kingdom represents a big reservoir of phytoconstituents with therapeutic potential, many of which could also serve as lead for the development of new chemical entities for various pathological states in future. Recently, USFDA has started up a new category of herbal drugs and products which are scientifically prepared and which will be leading the market exclusively like new pharmaceutical products. This has opened up a new window of opportunity for the Asian countries like India and China, which have rich heritage of traditional systems of medicines like Ayurveda and Traditional Chinese Medicine (TCM). Ocimum species have a high index in a variety of pharmacological activities like antimicrobial, immunomodulatory, antistress, anti-inflammatory, antiulcer, antidiabetic, hepatoprotective, chemoprotective, antihyperlipidemic, cardioprotective, antioxidant, antitussive, radioprotective, memory enhancing, antiarthritic, antifertility, antihypertensive, anticoagulant, anticataract, anthelmintic and antinociceptive activities. The current review is about collation of all the available data on identified chemical constituents as well as the reported pharmacological activities of Ocimum species, with special reference to Ocimum sanctum.