Yangonin is one of the six major

kavalactone Kavalactones are a class of lactone compounds found in kava roots and Alpinia zerumbet (Shell ginger). Kavalactones are under research for potential to have various psychotropic effects, including anxiolytic and sedative/ hypnotic activities. En ...

s found in the kava plant. It has been shown to possess binding affinity for the

cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recep ...

CB₁ (K_i = 0.72 μM), and selectivity vs. the CB₂ receptor (K_i >10 μM) where it behaves as an agonist. The CB₁ receptor affinity of yangonin suggests that the

endocannabinoid system The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are endogenous lipid-based retrograde neurotransmitters that bind to cannabinoid receptors (CBRs), and cannabinoid receptor proteins that are expressed ...

might contribute to the complex human

psychopharmacology Psychopharmacology (from Greek grc, ψῡχή, psȳkhē, breath, life, soul, label=none; grc, φάρμακον, pharmakon, drug, label=none; and grc, -λογία, -logia, label=none) is the scientific study of the effects drugs have on mo ...

of the traditional kava drink and the

anxiolytic An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...

preparations obtained from the kava plant. Like other kavalactones, yangonin has been found to potentiate GABA_A receptors. This may contribute to the anxiolytic properties of yangonin and kava as a whole. Further ''

in vitro ''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called " test-tube experiments", these studies in biology ...

'' studies have also demonstrated yangonin to be an inhibitor of monoamine oxidase, 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

hepatocyte A hepatocyte is a cell of the main parenchymal tissue of the liver. Hepatocytes make up 80% of the liver's mass. These cells are involved in: * Protein synthesis * Protein storage * Transformation of carbohydrates * Synthesis of cholesterol, ...

s with approximately 40% reduction in viability based on an

ethidium bromide Ethidium bromide (or homidium bromide, chloride salt homidium chloride) is an intercalating agent commonly used as a fluorescent tag ( nucleic acid stain) in molecular biology laboratories for techniques such as agarose gel electrophoresis. It ...

assay. The predominant mode of cell death turned out to be apoptosis rather than necrosis. No significant changes were observed in

glutathione Glutathione (GSH, ) is an antioxidant in plants, animals, fungi, and some bacteria and archaea. Glutathione is capable of preventing damage to important cellular components caused by sources such as reactive oxygen species, free radicals, pe ...

levels.

Biosynthesis

Yangonin is

biosynthesized Biosynthesis is a multi-step, enzyme- catalyzed process where substrates are converted into more complex products in living organisms. In biosynthesis, simple compounds are modified, converted into other compounds, or joined to form macromolecules ...

from

coumaroyl-CoA Coumaroyl-coenzyme A is the thioester of coenzyme-A and coumaric acid. Coumaroyl-coenzyme A is a central intermediate in the biosynthesis of myriad natural products found in plants. These products include lignols (precursors to lignin and ligno ...

and malonyl-CoA. : Biosynthesis of yangonin

References

{{Dopaminergics Kavalactones Phenol ethers Analgesics CB1 receptor agonists GABAA receptor positive allosteric modulators Monoamine oxidase inhibitors