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Abstract Background Black pepper [ Piper nigrum (L.), Family: Piperaceae] is used traditionally for the treatment of various diseases including; cough, cold, dyspnea throat diseases, intermittent fever, dysentery, stomachache, worms and piles. The pharmacological potential of black pepper is due to the presence of metabolites like phenolic compounds, alkaloids, flavonoids, carotenoids, terpenoids, etc. The multipurpose use of black pepper dried seeds has several other beneficial health effects that also received in the light of traditional as well as current medicine perspectives. The review aims to discuss the botany, phytochemical constituents, and pharmacological properties of piperine and black pepper essential oil (BPEO). Results Phytochemical analyses have described the main chemical constituents of black pepper, including carbohydrates, proteins, calcium, magnesium, potassium, iron, vitamin C, tannins, flavonoids and carotenoids. The volatile oil content ranges from 0.4 to 7 % in dried berries. The major constituents of BPEO are sabinene, 3-carene, D-limonene, α-pinene, caryophyllene, β-phellandrene, α-phellandrene, α-thujene, and β-bisabolene. Additionally, piperine is the naturally occurring and principal bioactive alkaloid constituent of black pepper owing to its potential therapeutic properties, including cerebral brain functioning and increased nutrient absorption. The BPEO has several biological roles, including antioxidant, anti-inflammatory, anticancer, anti-obesity, antidepressant, antidiabetic, antimicrobial, gastroprotective, and insecticidal activities. Conclusions This review examines and presents the appropriate evidence on black pepper and its traditional uses as well as biological activities of BPEO and piperine. Although several previous reports showed diverse biological effects for piperine and bioactive constitutes of BPEO. Thus, minimal investigations were conducted using animal models, and many of these studies also lacked appropriate experimental setting like doses, control details. Hence, future studies are necessary to understand the mechanism of piperine, BPEO, bioactive constituents and their effects upon their use by animal models and humans with the proper experimental procedure which we can facilitate the protection of human health from several diseases.