Kava Fact of the Day Yangonin (Y) #3

[The Kap'n]

Kava, the plant we’ve come to know and love, is turning out to be a deeper mystery than we had first imagined. The actions of this plant are complex, and continue to be researched. Of the 6 kavalactones commonly found in kava in the most abundance, yangonin will be of interest for today.

What is yangonin? Yangonin (4-Methoxy-6-[(E)-2-(4-methoxyphenyl)ethenyl]pyran-2-one) is one of the six major kavalactones found in the kava plant [1]. Yangonin has been found to have several functions among many likely unknown functions. One is that yangonin has been shown to exert a protective effect on cholestasis, or when the flow of bile from the liver is reduced or blocked. Yangonin has a regulative effect on hepatic genes which contribute to the increased transport and metabolism of toxic bile acids, as well as the decreased synthesis of bile acids [3]. Yangonin has been shown to decrease dopamine levels in the brain [4]. Another reported effect is that yangonin has a measurable affinity for the cannabinoid receptor CB1. This is the same receptor that is activated heavily by Δ9-THC, the primary active chemical in cannabis. Yangonin has about 170 times less affinity for the CB1 receptor when compared to THC [2]. The effect, if present, will be slight and this could lend evidence toward the thought that yangonin may possibly contribute to kavas anxiolytic effect in this manner.

[1]Yangonin. (2020, December 02). Retrieved December 23, 2020, from https://en.wikipedia.org/wiki/Yangonin

[2]Ligresti A, Villano R, Allarà M, Ujváry I, Di Marzo V. Kavalactones and the endocannabinoid system: the plant-derived yangonin is a novel CB₁ receptor ligand. Pharmacol Res. 2012 Aug;66(2):163-9. doi: 10.1016/j.phrs.2012.04.003. Epub 2012 Apr 14. PMID: 22525682.

[3]Kong, Y., Gao, X., Wang, C., Ning, C., Liu, K., Liu, Z., . . . Meng, Q. (2018). Protective effects of yangonin from an edible botanical Kava against lithocholic acid-induced cholestasis and hepatotoxicity. European Journal of Pharmacology, 824, 64-71. doi:10.1016/j.ejphar.2018.02.002

[4]Baum SS, Hill R, Rommelspacher H. Effect of kava extract and individual kavapyrones on neurotransmitter levels in the nucleus accumbens of rats. Prog Neuropsychopharmacol Biol Psychiatry. 1998 Oct;22(7):1105-20. doi: 10.1016/s0278-5846(98)00062-1. PMID: 9829291.

 

[kavakarma]

If one does drink 40 grams or 43.1 grams, respectively, of a kava with a lab chemotype analysis for 2.32% Yangonin, this is a consumed quantity of 928, and 1000 milligrams Yangonin. Here is my math.

2.32% @ 40g = ( 1g = 2.32% of 1,000mg is 23.2mg/gram) * 40 is ((20*40=800)+(3*40=120)+(.2*40=8)) =928mg per 40 grams kava.
43.1g kava = 1 gram of Yangonin. Dividing this figure by four to see a 10 and three quarters gram serving, which is about two tablespoons. If your kava is not as strong and your extraction is not similar divide this final result of 250 in half for skepticism. for


Hypothesis: An average serving of Yangonin is between 250 and 928 mg, with 125-1000mg yangonin a probable range to fall in at servings of kava between 2tbsp and 40g, which test at 2.32% kavalactones. On the higher end, a 40gram serving of this kava should have equal or greater affinity for the CB1 receptor than a 5mg serving of delta 9-THC. This sample test is from Art of Kava's new batch of Koro island, which I brought up because their first batch was potent in lactones, and I wanted larger numbers for my math example to be more accurate .

edit: rephrase, "Yangonin has 170x less affinity for CB1 than delta 9 THC--average servings of yangonin may meet or exceed 170x the average serving which is consumed for delta 9 THC"

The math continues. If the cannaboid THC is averagely consumed in amounts of 1 to 50mg by those who do, and some outliers on the higher end like upwards of 500mg. I'm going to estimate based on experience that 2.5mg, 5mg, and 10mg are going to be the most reliable serving sizes by average.

So we are seeing 170x less activity for Yangonin than delta 9 thc at the CB1 receptor. Yet we also may observe the lower end servings of yangonin typically fall in the 125-250mg range, while the lesser amounts of thc consumed is usually 2.5mg, which is 50 to 100 times less than 125-250mg quantity by quantity. 25-50x less at the mid level 5mg thc and 12.5-25x less when considering the ten mg thc.

For a yangonin serving in the high end, at 928mg, we find the amount ingested in milligrams is 185.6 times greater in proportion to a 5mg portion of thc. 185.6 is larger than 170, granting a 40 gram serving of aforementioned kava 1.09 times greater affinity for the CB1 receptor than a 5mg portion of THC will offer.


What do you think, @Kapmcrunk ? Am I able to clean this up in any way? Do you believe I'm poised to mathematically imply that based on the numbers given and the results of this one experiment, Yangonin is consumed in servings which are large enough in relation to the average serving of THC in order that the affinity ends up being quite close and similar? Thank you.

 

[kavakarma]

I just realized this is irrelevant because the study was performed on rats. My questions.
When reading the content of a kava root, I see fiber, starch, minerals, water, kavalactones, and occasionally protein. Usually it adds up to 100.0, with kavalactones being anywhere from 5% to 14%. On chemotypes, the percent of each major is listed, such that you have a figure or a percent for how much of the plant is that lactone. In my example I used 2.32%, meaning it is 2.32% of the plant. What is the unit of measurement here? Is milligrams appropriate to measure 2.32%? How do I know if it is 2.32 % by mass?

What is the range of difference between lactone test results of water extraction and the lab methanol sonification process? Is it quite close or does it vary significantly?

I believe pooling averages would allow for lists and excel sheets in which many conclusions can be made and drzwn about the kavalactones, their individual actions and entourage effect.

 

[The Kap'n]

I just realized this is irrelevant because the study was performed on rats. My questions.
When reading the content of a kava root, I see fiber, starch, minerals, water, kavalactones, and occasionally protein. Usually it adds up to 100.0, with kavalactones being anywhere from 5% to 14%. On chemotypes, the percent of each major is listed, such that you have a figure or a percent for how much of the plant is that lactone. In my example I used 2.32%, meaning it is 2.32% of the plant. What is the unit of measurement here? Is milligrams appropriate to measure 2.32%? How do I know if it is 2.32 % by mass?

What is the range of difference between lactone test results of water extraction and the lab methanol sonification process? Is it quite close or does it vary significantly?

I believe pooling averages would allow for lists and excel sheets in which many conclusions can be made and drzwn about the kavalactones, their individual actions and entourage effect.

Remember that out of the 5%-14% total kavalactone percentage you're only getting maybe 5% of that when you use traditional prep. Not only that, yangonin is quite difficult to extract with water, so you may be seeing even less than 5% of total percentage of yangonin in the root. Your total extraction amounts will be in the singles of milligrams most likely.