Yangonin is one of the six major
kavalactones found in the
kava plant.[1] It has been shown to possess binding affinity for the
cannabinoid receptorCB1 (Ki = 0.72 μM), and selectivity vs. the
CB2 receptor (Ki >10 μM) where it behaves as an
agonist. The CB1 receptor affinity of yangonin suggests that the
endocannabinoid system might contribute to the complex human
psychopharmacology of the traditional kava drink and the
anxiolytic preparations obtained from the kava plant.[2]
Like other kavalactones, yangonin has been found to potentiate
GABAA receptors.[3] This may contribute to the anxiolytic properties of yangonin and kava as a whole.
Further in vitro studies have also demonstrated yangonin to be an inhibitor of
monoamine oxidase,[citation needed] with a moderate preference for
isozyme B, which could open the door to a wide range of interactions.
Toxicity
Yangonin displays marked in vitro toxicity on human
hepatocytes with approximately 40% reduction in viability based on an
ethidium bromide assay.[4] The predominant mode of cell death turned out to be
apoptosis rather than
necrosis. No significant changes were observed in
glutathione levels.[4]
^Ligresti, A.; Villano, R.; Allarà, M.; Ujváry, I. N.; Di Marzo, V. (2012). "Kavalactones and the endocannabinoid system: The plant-derived yangonin is a novel CB1 receptor ligand". Pharmacological Research. 66 (2): 163–169.
doi:
10.1016/j.phrs.2012.04.003.
PMID22525682.