(+)-Kavain

(+)-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 GABA_A receptors with EC₅₀ values of 25 and 59 µM in the presence and absence of 300 µM (+)-kavain, respectively, in Xenopus oocytes expressing human receptors.¹ (+)-Kavain reduces growth of WPMY-1 prostate cancer cells (IC₅₀ = 5.2 µg/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

WARNING This product is not for human or veterinary use.

1. Chua, H.C., Christensen, E.T., Hoestgaard-Jensen, K., et al. Kavain, the major constituent of the anxiolytic kava extract, potentiates GABA_A receptors: Functional characteristics and molecular mechanism. PLoS One 11(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 mice. PLoS One 7(2), e31213 (2012).

3. Tang, X., and Amar, S. Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAF. Toxicol. Res. (Camb). 5(1), 188-196 (2016).

4. Kormann, E.C., de Aguiar Amaral, P., David, M., et al. Kavain analogues as potential analgesic agents. Pharmacol. Rep. 64(6), 1419-1426 (2012).