Kavain is a kavalactone and the major constituent of the pepper plant kava (P. methysticum) and has diverse biological activities.1,2,3,4 It is a positive allosteric modulator of α4β2δ subunit-containing GABAA receptors with EC50 values of 25 and 59 ?M in the presence and absence of 300 ?M kavain, respectively, in Xenopus oocytes expressing human receptors.1 Kavain reduces growth of WPMY-1 prostate cancer cells (IC50 = 5.2 ?g/ml).2 It reduces LPS-induced TNF-α production in primary murine macrophages in a concentration-dependent manner.3 In vivo, kavain (1 mg/animal) reduces hind paw swelling and TNF-α production in wild-type, but not Erk-/-, mice in a mouse model of collagen-induced arthritis. Kavain also reduces acetic acid-induced abdominal constrictions in mice (ED50= 15.71 mg/kg).4
1.Chua, H.C., Christensen, E.T., Hoestgaard-Jensen, K., et al.Kavain, the major constituent of the anxiolytic kava extract, potentiates GABAA receptors: Functional characteristics and molecular mechanismPLoS One11(6)e0157700(2016) 2.Li, X., Liu, Z., Xu, X., et al.Kava components down-regulate expression of AR and AR splice variants and reduce growth in patient-derived prostate cancer xenografts in micePLoS One7(2)e31213(2012) 3.Tang, X., and Amar, S.Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAFToxicol. Res. (Camb).5(1)188-196(2016) 4.Kormann, E.C., de Aguiar Amaral, P., David, M., et al.Kavain analogues as potential analgesic agentsPharmacol. Rep.64(6)1419-1426(2012)