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 GABA
A at 1.0 μM.
1 Yangonin also binds the central cannabinoid (CB
1) receptor with a K
i value of 0.72 μM, 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 (IC
50s = 15-59 mg/mL).
4 
