Piper nigrum L. is considered the king of spices throughout the world due to its pungent principle piperine. Peppercorn of Piper nigrum as a whole or its active components are used in most of the food items. Different parts of Piper nigrum including secondary metabolites are also used as drug, preservative, insecticidal and larvicidal control agents. Biologically Piper nigrum is very important specie. The biological role of this specie is explained in different experiments that peppercorn and secondary metabolites of Piper nigrum can be used as Antiapoptotic, Antibacterial, Anti-Colon toxin, Antidepressant, Antifungal, Antidiarrhoeal, Anti-inflammatory, Antimutagenic, Anti-metastatic activity, Antioxidative, Antiriyretic, Antispasmodic, Antispermatogenic, Antitumor, Antithyroid, Ciprofloxacin potentiator, Cold extremities, Gastric ailments, Hepatoprotective, Insecticidal activity, Intermittent fever and Larvisidal activity. Other roles of this specie includes protection against diabetes induced oxidative stress; Piperine protect oxidation of various chemicals, decreased mitochondrial lipid peroxidation, inhibition of aryl hydroxylation, increased bioavailability of vaccine and sparteine, increase the bioavailability of active compounds, delayed elimination of antiepileptic drug, increased orocecal transit time, piperine influenced and activate the biomembrane to absorb variety of active agents, increased serum concentration, reducing mutational events, tumour inhibitory activity, Piperine inhibite mitochondrial oxidative phosphorylation, growth stimulatory activity and chemopreventive effect. This review based on the biological role of Piper nigrum can provide that the peppercorn or other parts can be used as crude drug for various diseases while the secondary metabolites such as piperine can be used for specific diseases.