Piperine was discovered in 1819 by Hans Christian Ørsted, who isolated it from the fruits of Piper Nigrum, the source plant of both the black and white pepper grains.

Piperine is the alkaloid responsible for the pungency of black pepper and long pepper, along with chavicine (an isomer of piperine). It has also been used in some forms of traditional medicine and as an insecticide. Piperine, along with its isomer chavicine, is the alkaloid responsible for the pungency of black pepper and long pepper. It has also been used in some forms of traditional medicine and as an insecticide.

Piperine forms monoclinic needles, is slightly soluble in water (40 mg/L, or 1g/25L (18°C)) and more so in alcohol, ether or chloroform. The solution in alcohol has a pepper-like taste. It yields salts only with strong acids.

Black pepper Extract contains 95% Piperine. Black Pepper Extract is involved in increasing the absorption of other nutrients in the body. The extract is also suggested to have anti-cancer properties and could enhance cognitive functions and provide anti-depressant effects.

Black pepper is sometimes applied directly to the skin for treating nerve pain (neuralgia) and a skin disease called scabies. Black and white pepper might help fight germs (microbes) and cause the stomach to increase the flow of digestive juices. Piperine also possesses anti-angiogenic activities.