Kava or kava-kava (Piper methysticum) is a plant used for the production of a ritual drink with tranquilizing properties. The kavalactones are the main compounds of the kava drinks. There are many clinical trials on the use of kava product for anti-anxiety, and a systematic review supports the use of kava for the treatment of generalized anxiety (Sarris et al., 2009). Adverse effects on the liver have been reported, and kava is regulated in a number of countries (Teschke, 2010). Studies of kava extracts or kavalactones have been focused on elucidating the mechanism underlying its anti-anxiety and sleep-inducing ability, which has been attributed to its modulation of the γ-aminobutyric acid (GABA) receptor. Recent studies on the mechanisms of action for isolated kavalactones have revealed other neuroprotective activities not directly related to their GABAergic effects. These findings suggest that the use of kava might also be beneficial for the treatment of many degenerative diseases or nervous system conditions.