Black pepper (Piper nigrum L.) is an important healthy food owing to its antioxidant, antimicrobial potential and gastro-protective modules. Black pepper, with piperine as an active ingredient, holds rich phytochemistry that also includes volatile oil, oleoresins, and alkaloids. It has also been extensively explored for its biological properties and its bioactive phyto-compounds. In addition to its culinary uses, pepper has important medicinal and preservative properties, and, more recently, piperine has been shown to have fundamental effects on p-glycoprotein and many enzyme systems, leading to biotransformative effects including chemoprevention, detoxification, and enhancement of the absorption and bioavailability of herbal and conventional drugs The alkaloid piperine improves the therapeutic value of several drugs, vaccines and nutrients by enhancing bioavailability through inhibiting numerous digestive enzymes. Piperine also aids in digestion through stimulating pancreatic and intestinal enzymes, and enriches cognitive skills and fertility. Furthermore, piperine is recognized as delivering several therapeutic activities distinct from other chemical components. This study endeavors to systematically review précised data on the traditional uses and pharmacological properties of black pepper. Besides, this review presents a summary of the data on the chemical composition of black pepper, including minerals, vitamins, carotenoids and flavonoids, and various therapeutic benefits. Up to date existing information, various metabolites have been isolated from P. nigrum. Among them, biologically active alkaloid piperine and the main essential oils constituents including β-caryophyllene, limonene, sabinene, α-pinene, β-bisabolene and α-copaene can serve as a new natural source for use in food, aroma, cosmetics and pharmaceutical industries.