Piper nigrum (family Piperaceae) is a valuable medicinal plant. Black pepper is one of the important spices, rich in aromatic and medicinal components along with an appreciable level of several other functional components having healthpromoting properties. It contains major pungent alkaloid. Many investigators have isolated different types of compounds, i.e. Phenolics, flavonoids, alkaloids, amides and steroids, lignans, neo-lignans, terpenes and many other compounds. Some of the compounds are Brachyamide B, Dihydropipericide(2E,4E)-N-Eicosadienol- pereridine, N-trans-Feruloyltyramine, N-Formyl piperidine, (2E,4E)-N-isobuty ldecadienamid, isobutyl-eicosadienamide, Tricholein, Trichostachine, isobutyleicosatrienamide, Isobutyl-octadienamide, Piperamide, Piperamine, Piperettine, Pipericide, Piperine, Piperolein B, Sarmentine, Sarmentosine, Retrofractamide A. Black pepper is used as a medicinal agent, a preservative, and in perfumery. Whole Peppercorn of Piper nigrum or its active components is being used in different types of foods and as medicine. Piperine (1-peperoyl piperidine) is known to possess many interesting pharmacological actions such as antihypertensive and antiplatelets, antioxidant, antitumor, antiasthmatics, antipyretic, analgesic, anti-inflammatory, antidiarrheal, antispasmodic, anxiolytic, antidepressants, hepato-protective, immunomodulatory, antibacterial, antifungal, anti-thyroids, antiapoptotic, anti-metastatic, antimutagenic, anti-spermatogenic, anti-Colon toxin, insecticidal and larvicidal activities, etc. Piperine has been found to enhance the therapeutic efficacy of many drugs, vaccines and nutrients by increasing oral bioavailability and by inhibiting various metabolizing enzymes. It is also known to enhance cognitive action and fertility. Piperine is also found to stimulate the pancreatic and intestinal enzymes which aid in digestion. Many therapeutic activities of this spice are attributed to the presence of piperine apart from other chemical constituents. Piper nigrum is also used as a flavoring agent. Recently, many studies have shown anticancer activities of piperine, a pungent alkaloid found in black pepper and some other Piper species. The collected preclinical data can be useful in the design of future researches especially clinical trials with piperine. It is, therefore, concluded that black pepper and its bioactive compound, piperine exhibit wide spectrum therapeutic potential and have also emerged as an excellent adjuvant to enhance the therapeutic efficacy of the concurrently administered drugs and nutrients.