Kawain
Kavain has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kawain is advanced glycation endproduct inhibitors, can increase the mean life span of Caenorhabditis elegans exposed to high glucose.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Compounds.2023, 3(1), 169-179.
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Prog Neuropsychopharmacol Biol Psychiatry. 1997 May;21(4):697-706.
Effects of kawain and dihydromethysticin on field potential changes in the hippocampus.[Pubmed:
9194150]
1. The kava-pyrones Kawain and dihydromethysticin are constituents of Piper methysticum which exert anticonvulsant, analgesic and anxiolytic properties.
METHODS AND RESULTS:
3. Kawain and dihydromethysticin reduced reversibly the frequency of occurrence of fp in a concentration range from 5 to 40 mumol/l and 10 to 40 mumol/l, respectively. 4. Reduction of the fp frequency after addition of subthreshold concentrations of 5 mumol/l Kawain and 10 mumol/l dihydromethysticin indicated additive actions of both drugs. 5. Since the serotonin-1A agonist ipsapirone also exerts anxiolytic effects, subthreshold concentrations of Kawain or dihydromethysticin were combined with a subthreshold concentration of ipsapirone in another set of experiments. Combining Kawain and ipsapirone or dihydromethysticin and ipsapirone caused a reduction of the rate of fp to 0.76 and 0.81 of the baseline value, respectively.
CONCLUSIONS:
6. The findings suggest that (i) single constituents of Piper methysticum may have additive actions, (ii) that the two components Kawain and dihydromethysticin may enhance the effects of the anxiolytic serotonin-1A agonist ipsapirone and (iii) that activation of NMDA receptors and/or voltage dependent calcium channels may be involved in the elementary mechanism of action of some kava-pyrones.
Drug Metab Dispos. 2005 Oct;33(10):1555-63.
Pharmacokinetics and disposition of the kavalactone kawain: interaction with kava extract and kavalactones in vivo and in vitro.[Pubmed:
16033948]
METHODS AND RESULTS:
The oral pharmacokinetics of the kavalactone, Kawain (100 mg/kg), were determined in rats with and without coadministration of kava extract (256 mg/kg) to study the effect of the extract on drug disposition. Kawain was well absorbed, with >90% of the dose eliminated within 72 h, chiefly in urine. Compared with Kawain alone, coadministration with kava extract caused a tripling of Kawain AUC(0-8 h) and a doubling of C(max). However, a 7-day pretreatment with kava extract (256 mg /kg/day) had no effect on the pharmacokinetics of Kawain administered on day 8.
CONCLUSIONS:
The 7-day pretreatment with kava extract only modestly induced hepatic P450 activities.
Planta Med. 2014 Aug;80(12):1001-8.
Kavalactones, a novel class of protein glycation and lipid peroxidation inhibitors.[Pubmed:
25098935]
Kawain, methysticin, and dihydromethysticin, all belonging to the group of kavalactones, were identified as advanced glycation endproduct inhibitors.
METHODS AND RESULTS:
With IC50 values of 43.5 ± 1.2 μM and 45.0 ± 1.3 μM for Kawain and methysticin, respectively, the compounds inhibited the in vitro protein glycation significantly better than aminoguanidine (IC50 = 231.0 ± 11.5 μM; p = 0.01), an established reference compound. Kawain and methysticin also inhibited the formation of dicarbonyl compounds, which are intermediates in the process of advanced glycation endproduct formation.
CONCLUSIONS:
Similarly, Kawain and aminoguanidine prevented the formation of thiobarbituric reactive substances in both low-density lipoprotein and linoleic acid oxidation. Moreover, Kawain and aminoguanidine prevented advanced glycation endproduct formation by chelating Fe(3+) and Cu(2+) two to three times better than aminoguanidine. Furthermore, Kawain increased the mean life span of Caenorhabditis elegans exposed to high glucose.
