Cordyceps sinensis (CS) is a well-known entamophagus fungus, naturally distributed in the Tibetan Plateau of Asia and Himalayas. Recently this synonym is transferred to Ophiocordyceps by both scientific and non-scientific communities. It is widely used as a tonic and medicinal food in traditional Chinese medicine (TCM), as it possess wonderful health benefits. To support its functional attributes, various investigations have been carried out to find out its adaptogenic, aphrodisiac, anti-oxidant, anti-aging, neuroprotective, nootropic, immunomodulatory, anti-cancer and hepatoprotective role. Its fruiting portion as well as the larvae possesses potent bio-active fractions and their composition almost found to be similar in both. The bioactive principles are nucleosides, exo-polysaccharides, sterols and, proteins, among others. Among nucleosides, adenosine and cordycepin are the major
biochemical markers. Further, different types of solvent extracts and their mixtures exhibit wide range of pharmacological activities, while the water and methanol extracts with the richest sources of nucleosides and polysaccharides also show wide range of pharmacological activities. This review gives a panoramic view of potential health benefits of various classes of bio-active fractions along with the need for sustainable management of CS for human wellness.