Kavain

Kavain is a kavalactone and the major constituent of the pepper plant kava (P. methysticum) and has diverse biological activities. It is a positive allosteric modulator of α4β2δ subunit-containing GABAA 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. Kavain reduces growth of WPMY-1 prostate cancer cells (IC50 = 5.2 µg/ml). It reduces LPS-induced TNF-α production in primary murine macrophages in a concentration-dependent manner. In vivo, kavain (1 mg/animal) reduces hind paw swelling and TNF-α...