An in depth review on Nigella sativa and its derived constituents has been necessitated which has been sketched in this paper from the research reports obtained from PubMed and ScienceDirect databases. Findings of this meticulous review suggest that N. sativa possesses various important phytoconstituents and derived compounds with diverse biological effects including antioxidant, anti-inflammatory, anti-bacterial, anti-fungal, anti-parasitic, anti-protozoal, antiviral, cytotoxic, anticancer, and neuro-, gastro-, cardio-, hepato- and nephro-protective activities. In addition, N. sativa implies beneficiary effects on reproductive, pulmonary and immune systems along with diabetes mellitus (type 2 diabetes), fertility, breast cancer, dermatological complications, dehydration, dyspepsia, osmotic balance and others. Amongst several isolated chemical moieties of N. sativa, thymoquinone may be one of the best targets for treatment of microbial infections, inflammations, cancer, metabolic syndromes, and many other diseases. The N. sativa is evident to promote health in some non-clinical and clinical studies and it may serve to be one of the best sources for modern phyto medicine.