Methysticin Explained

Methysticin is one of the six major kavalactones found in the kava plant.[1] Research suggests that methysticin and the related compound dihydromethysticin have CYP1A1 inducing effects which may be responsible for their toxicity.[2] Additionally, methysticin has been shown to potentiate GABAA receptor activity, contributing to the overall anxiolytic profile of the kava plant.[3]

Toxicity

Methysticin induces the function of the hepatic enzyme CYP1A1. This enzyme is involved in the toxification of benzo[''a'']pyrene into (+)-benzo[''a'']pyrene-7,8-dihydrodiol-9,10-epoxide, a highly carcinogenic substance. Another related compound is dihydromethysticin, which also induces the function of CYP1A1.[4] [5] No report so far has described enhancement of CYP1A1 expression in animals or humans in vivo from any constituent of kava.[6]

Notes and References

  1. Evaluation of the effects of Kava on the Liver. Fiji School of Medicine. 2002-12-03. Joji. Malani. 2009-09-04. dead. https://web.archive.org/web/20090320001735/http://www.spc.int/cis/documents/Kava%20article%20DrMalani.pdf. 2009-03-20.
  2. Methysticin and 7,8-dihydromethysticin are two major kavalactones in kava extract to induce CYP1A1.. Li Y, Mei H, Wu Q, Zhang S, Fang JL, Shi L, Guo L . Toxicological Sciences. 21908763. 10.1093/toxsci/kfr235. 124. 2. Dec 2011. 388–99. 5736320.
  3. Influence of genuine kavapyrone enantiomers on the GABA-A binding site . 9776662 . 1998 . Boonen . G. . Häberlein . H. . Planta Medica . 64 . 6 . 504–506 . 10.1055/s-2006-957502 . 45511040 .
  4. Beresford . AP . CYP1A1: friend or foe? . Drug Metab Rev . 25 . 4 . 503–17 . 1993 . 10.3109/03602539308993984 . 8313840.
  5. Uno . S . Dalton TP . Durkenne S . Curran CP . Oral exposure to benzo[a]pyrene in the mouse: detoxication by inducible cytochrome P450 is more important than metabolic activation. . Molecular Pharmacology . 65 . 5 . 1225–37 . 2004 . 10.1124/mol.65.5.1225 . 15102951. 24627183 .
  6. Yamazaki . Yuko . Hashida . Hiroko . Arita . Anna . Hamaguchi . Keiko . Shimura . Fumio . 2008 . High dose of commercial products of kava (Piper methysticum) markedly enhanced hepatic cytochrome P450 1A1 mRNA expression with liver enlargement in rats . Food and Chemical Toxicology. 46 . 12 . 3732–3738 . 10.1016/j.fct.2008.09.052 . 0278-6915 . 18930106.

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