Methysticin 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 Kava or kava kava (''Piper methysticum'': Latin 'pepper' and Latinized Greek 'intoxicating') is a crop of the Pacific Islands. The name ''kava'' is from Tongan and Marquesan, meaning 'bitter'; other names for kava include ''ʻawa'' (Hawaiʻi), ...

plant. Research suggests that methysticin and the related compound dihydromethysticin have

CYP1A1 Cytochrome P450, family 1, subfamily A, polypeptide 1 is a protein that in humans is encoded by the ''CYP1A1'' gene. The protein is a member of the cytochrome P450 superfamily of enzymes. Function Metabolism of xenobiotics and drugs CYP1A1 ...

inducing effects which may be responsible for their toxicity. Additionally, methysticin has been shown to potentiate GABA_A receptor activity, contributing to the overall

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 anxi ...

profile of the kava plant.

Toxicity

Methysticin induces the function of the hepatic enzyme CYP1A1. This enzyme is involved in the

toxification Toxication, toxification or toxicity exaltation is the conversion of a chemical compound into a more toxic form in living organisms or in substrates such as soil or water. The conversion can be caused by enzymatic metabolism in the organisms, as we ...

of benzo 'a''yrene into (+)-benzo 'a''yrene-7,8-dihydrodiol-9,10-epoxide, a highly carcinogenic substance. Another related compound is dihydromethysticin, which also induces the function of CYP1A1. No report so far has described enhancement of CYP1A1 expression in animals or humans in vivo from any constituent of kava.

References

{{GABAAR PAMs Ethers Kavalactones Benzodioxoles Alkene derivatives GABAA receptor positive allosteric modulators Norepinephrine reuptake inhibitors Calcium channel blockers Sodium channel blockers Monoamine oxidase inhibitors