The entourage effect of kavalactones.
For this kava fact we’re going to be directly looking at the activity of single kavalactones vs the activity of full spectrum extracts. We’ll be looking at brain concentrations of these kavalactones and how the absorption rates differ when given alone and together in a full spectrum extract.
Keledjian et al in 1988 assessed the ability of kavalactones to be taken up into the mouse brain. This study is routinely cited in kava research, and even though it’s old, it’s still quite important. The information here will come directly from this study.
Individual lactone concentration in brain matter:
The researchers injected mice with 100mg/kg (2.5mg of each KL when calculated out for a 25g mouse) of each kavalactone and studied the physical brain material to ascertain a concentration level of kavalactones. Figure 1 shows the results of this in a graphical format.
They Found: (ng = nanogram / mg = milligram)
Kavain was seen at the concentration level of 29.3ng/mg in brain tissues.
DHK was seen at the concentration level of 64.7ng/mg in brain tissues
DMY was seen at the concentration level of 10.4ng/mg in brain tissues
Yangonin was seen at the concentration level of 1.2ng/mg in brain tissues.
Full spectrum lactone concentration in brain matter:
The researchers also tested full spectrum extracts on the mice, and in table 2 a breakdown is listed of each kavalactone in the 120mg/kg full spectrum kava extract. Results of this are seen in figure 2.
This study suggests that the synergism of pharmacological activity appears to be due to potentiation of penetration into the brain when the kavalactones are given together instead of separately. It was also said that Yangonin and DMY were relatively ineffective when taken orally, but if given in combination with full spectrum extracts, a marked increase in action was observed. This may also suggest that the absorption of lactones in the intestines sees an increase when all the kavalactones are together.
I’ve taken the figures from this study and added them to a spreadsheet in order to more easily understand the effect that consuming kavalactones together can have. We see that DHK remained about the same, however all the other kavalactones were increased in absorption by a rather large amount. Yangonin saw an increase of about 20 times that of it’s application alone. More studies are necessary but evidence is beginning to support the idea that an entourage effect is strongly at play when considering the physiological actions of kava.
Keledjian, J., P. H. Duffield, D. D. Jamieson, R. O. Lidgard, and A. M. Duffield. 1988. “Uptake into Mouse Brain of Four Compounds Present in the Psychoactive Beverage Kava.” Journal of Pharmaceutical Sciences 77 (12): 1003–6.
(https://sci-hub.st/10.1002/jps.2600771203)
For this kava fact we’re going to be directly looking at the activity of single kavalactones vs the activity of full spectrum extracts. We’ll be looking at brain concentrations of these kavalactones and how the absorption rates differ when given alone and together in a full spectrum extract.
Keledjian et al in 1988 assessed the ability of kavalactones to be taken up into the mouse brain. This study is routinely cited in kava research, and even though it’s old, it’s still quite important. The information here will come directly from this study.
Individual lactone concentration in brain matter:
They Found: (ng = nanogram / mg = milligram)
Kavain was seen at the concentration level of 29.3ng/mg in brain tissues.
DHK was seen at the concentration level of 64.7ng/mg in brain tissues
DMY was seen at the concentration level of 10.4ng/mg in brain tissues
Yangonin was seen at the concentration level of 1.2ng/mg in brain tissues.
Full spectrum lactone concentration in brain matter:
This study suggests that the synergism of pharmacological activity appears to be due to potentiation of penetration into the brain when the kavalactones are given together instead of separately. It was also said that Yangonin and DMY were relatively ineffective when taken orally, but if given in combination with full spectrum extracts, a marked increase in action was observed. This may also suggest that the absorption of lactones in the intestines sees an increase when all the kavalactones are together.
I’ve taken the figures from this study and added them to a spreadsheet in order to more easily understand the effect that consuming kavalactones together can have. We see that DHK remained about the same, however all the other kavalactones were increased in absorption by a rather large amount. Yangonin saw an increase of about 20 times that of it’s application alone. More studies are necessary but evidence is beginning to support the idea that an entourage effect is strongly at play when considering the physiological actions of kava.
Keledjian, J., P. H. Duffield, D. D. Jamieson, R. O. Lidgard, and A. M. Duffield. 1988. “Uptake into Mouse Brain of Four Compounds Present in the Psychoactive Beverage Kava.” Journal of Pharmaceutical Sciences 77 (12): 1003–6.
(https://sci-hub.st/10.1002/jps.2600771203)
