Kavalactones are a class of
lactone compounds found in
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), ...
roots and
Alpinia zerumbet (Shell ginger). Kavalactones are under research for potential to have various
psychotropic effects, including
anxiolytic and
sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but t ...
/
hypnotic
Hypnotic (from Greek ''Hypnos'', sleep), or soporific drugs, commonly known as sleeping pills, are a class of (and umbrella term for) psychoactive drugs whose primary function is to induce sleep (or surgical anesthesiaWhen used in anesthesia ...
activities.
Enzyme inhibition
Kava extract has been shown in vitro to potentially inhibit a wide range of hepatic enzymes, suggesting a possible potential for interactions with many pharmaceuticals and herbal medications. In human volunteers in vivo inhibition is currently limited to CYP1A2, and CYP2E1 through use of probe drugs to measure inhibition.
Research
Several preliminary studies are assessing potential effects of kava, including its
anxiolytic actions
and
hepatotoxicity, but the role specifically of kavalactones among many other kava compounds for these effects remains under study.
Kavalactone type compounds may help protect against high glucose induced cell damage.
Toxicity
Several kavalactones (e.g.
methysticin and
yangonin
Yangonin is one of the six major kavalactones found in the kava plant. It has been shown to possess binding affinity for the cannabinoid receptor CB1 (Ki = 0.72 μM), and selectivity vs. the CB2 receptor (Ki >10 μM) where it behaves as an ago ...
) affect a group of
enzymes involved in
metabolism, called
CYP1A1.
Hepatotoxicity occurred in a small portion of previously healthy kava users,
Compounds
At least 18 different kavalactones have been identified to date, with methysticin being the first identified.
Multiple analogues, such as ethysticin, have also been isolated.
Some consist of a substituted α-pyrone as the lactone while others are partially saturated.
The average elimination half-life of kavalactones typically present in kava root is 9 hr.
Biosynthesis
The kavalactone biosynthetic pathway in Piper methysticum was described in 2019.
See also
* Pipermethystine
Pipermethystine is a toxic alkaloid present in the aerial (aboveground) portions of the kava plant. It is not a kavalactone, containing no lactone structure. Correctly prepared kava root products will contain almost no pipermethystine.
Toxicity
...
References
External links
*
The great kava boom: how Fiji's beloved psychoactive brew is going global
The Guardian, 2020
{{GABAAR PAMs
Monoamine oxidase inhibitors
GABAA receptor positive allosteric modulators
Anxiolytics
Analgesics
Sedatives
Anticonvulsants
Nootropics