Piperine is a simple alkaloid isolated from the seeds of Piper nigrum. Piperine and its derivatives
exhibited a wide range of biological properties such as antitumor activity, antioxidant activity, antiinflammatory
activity, antimycobacterial activity, insecticidal activity, etc. Although five excellent reviews
have recently been described by Srinivasan in 2007, Mao in 2011, Butt in 2013, and Meghwal in 2013,
respectively, their topics were mainly focused on the biological effects. Therefore, in the present review, the progress in
the structural modifications on the aliphatic chain and the amide moiety of piperine was reported. Meanwhile, the
biological activities and structure-activity relationship of piperine and its derivatives were also described.