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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. Yangonin also binds the central cannabinoid (CB₁) 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. Yangonin blocks the activation of NF-κB by TNF-α. It also inhibits anchorage-dependent and independent growth of bladder cancer cell lines through induction of autophagic cell death (IC₅₀s = 15-59 mg/mL).

It is soluble in organic solvents such as methanol, ethanol, and DMSO. It is derived from the root of Piper methysticum Forst.

ChEBI: Yangonin is a member of 2-pyranones and an aromatic ether.

CB1: 1.79 μM (IC₅₀); CB1: 0.72 μM (Ki); RelA

[1] ALESSIA LIGRESTI . Kavalactones and the endocannabinoid system: The plant-derived yangonin is a novel CB1 receptor ligand[J]. Pharmacological research, 2012, 66 2: Pages 163-169. DOI: 10.1016/j.phrs.2012.04.003
[2] G BOONEN  H H. Influence of genuine kavapyrone enantiomers on the GABA-A binding site.[J]. Planta medica, 1998, 64 6: 504-506. DOI: 10.1055/s-2006-957502
[3] JUAN MA . Yangonin Blocks Tumor Necrosis Factor-α–Induced Nuclear Factor-κB–Dependent Transcription by Inhibiting the Transactivation Potential of the RelA/p65 Subunit[J]. Journal of pharmacological sciences, 2012, 118 4: Pages 447-454. DOI: 10.1254/jphs.11215fp
[4] ZHONGBO LIU. Kavalactone yangonin induces autophagy and sensitizes bladder cancer cells to flavokawain A and docetaxel via inhibition of the mTOR pathway.[J]. Journal of Biomedical Research, 2017, 31 5: 408-418. DOI: 10.7555/jbr.31.20160160