Kavalactones, mainly found in Piper methysticum, are a class of lactone compounds usually with an arylethylene-pyrone skeleton. Till now, fifty-one kavalactones have been isolated from the genera Piper, Alpinia, Amomum, Polygala, Goniothalamus, and Dumortiera. The bioactivities of six kavalactones, kawain, 7,8-dihydro- kawain, methysticin, dihydromethysticin, yangonin, and desmethoxyyagonin, have been studied extensively. This review aims to give an overview of kavalactones in the plants and their various bioactivities.