Yangonin is a natural kavalactone from the kava plant, P. methysticum. It enhances the binding of bicuculline at the γ-amino butyric acid (GABA) receptor GABAA at 1.0 ?M.1 Yangonin also binds the central cannabinoid (CB1) receptor with a Ki value of 0.72 ?M, but whether it serves as an agonist or antagonist at this receptor remains to be determined.2 Yangonin blocks the activation of NF-κB by TNF-α.3 It also inhibits anchorage-dependent and independent growth of bladder cancer cell lines through induction of autophagic cell death (IC50s = 15-59 mg/mL).4
1.Boonen, G., and H?berlein, H.Influence of genuine kavapyrone enantiomers on the GABAA binding sitePlanta Med.64(6)504-506(1998) 2.Ligresti, A., Villano, R., Allará, M., et al.Kavalactones and the endocannabinoid system: The plant-derived yangonin is a novel CB1 receptor ligandPharmacol. Res.66(2)163-169(2012) 3.Ma, J., Liang, H., Jin, H.R., et al.Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunitJ. Pharmacol. Sci.118(4)447-454(2012) 4.Zhongbo, L., U-Syn, H., Ke, Y., et al.Kavalactone yangonin induces autophagy and sensitizes bladder cancer cells to flavokawain A and docetaxel via inhibition of the mTOR pathwayJ. Biomed. Res.(2017)