Yangonin (Yan)

Yangonin is one of the six major kavalactones found in the kava plant. It has been shown to possess significant binding affinity for the cannabinoid receptor CB1, where it behaves as an agonist. As a result, yangonin may be responsible for some of kava's intoxicating effects. The CB1 activity of yangonin likely contributes to its psychoactive effects. This, along with the GABAergic effects of other kavalactones has given kava a use in the ethnobotanical treatment of anxiety, insomnia, pain, and other disorders. However, anxiety relief is unlikely to be contributed to yangonin's CB1 agonistic properties as CB1 agonism can be anxiogenic rather than anxiolytic. Yangonin displays marked in vitro toxicity on human hepatocytes with approximately 40% reduction in viability based on an ethidium bromide assay. The predominant mode of cell death turned out to be apoptosis rather than necrosis. No significant changes were observed in glutathione levels.