Nigella sativa L. (NS) has a number of important biological activities, such as antioxidant, anti-inflammatory, antibacterial, antifungal, anti-viral, anti-parasitic and anti-protozoal, cytotoxic, anticancer, neuro-, gastro-, cardio-, hetapto-and nephroprotective activities. In addition, the NS exerts beneficiary effects on reproductive, pulmonary and immune systems as well as in diabetes mellitus (DM), fertility (male and female), breast cancer, dermatological complications, dehydration, dyspepsia, and osmotic balance and so on. Among the isolated constituents, thymoquinone (TQ) is a vastly studied phytochemical in NS. A number of reports suggest that, the NS may be one of the potential herbs in health promotion. This review paper will discuss the detailed and mechanistic aspects of the biological activity of N. sativa along with the reported phytoconstituents.