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Kava Fact of the Day Kava, Caffeine, and CYP1A2

Orz[EST]

Kava Enthusiast
Anti-cancer activity was mentioned in relation to inhibition of Cytochrome CYP1A2.

That by itself is probably not cytotoxic or significantly pro-apoptotic for cancer cells. Kava helps cancer cells to give up their ambitious plan to take over and pack themselves up (apoptosis). Hence, there is more than one mechanism against cancer, a preventive and a [putative] curative one.
 

The Kap'n

The Groggy Kaptain (40g)
KavaForums Founder
Just a heads up about my fact of the day here. I'm starting to lean more towards a dynamic interaction instead of a kinetic one at CYP isozyme CYP1A2 after conversations with Dr. Schmidt. This is under review for now.
 

PapaCthulu

Kava Lover
I go to work at 1:20 in the morning. I have found that I only need around half a low calorie energy drink to get through the shift where I used to need 2.
 

Crowe

Kava Curious
Just a heads up about my fact of the day here. I'm starting to lean more towards a dynamic interaction instead of a kinetic one at CYP isozyme CYP1A2 after conversations with Dr. Schmidt. This is under review for now.
Really interesting. You know I have found that morning coffee really doesn't pack the bang that it did before kava. I do keep them spaced out though. Funny how we all react differently to things.
 

Jack3

Kava Enthusiast
Thats neat i must be different in though i can still drink a cup or shot of espresso and fall asleep haha.
With the exception of people with ADHD who respond differently to stimulants, caffeine—or any of the methylxanthines—will interfere with the quality of sleep even for those who can go straight to sleep immediately after drinking a cup of coffee.

The only 3 sources I have found in the medical/wellness field who discuss caffeine without selling it on the side suggest that caffeine should be used in a way that differs considerably from our cultural habit.

These are Dr Ari Whitten of www.theenergyblueprint.com who features numerous cutting edge podcasts with a variety of doctors from a rigorously empirical, well researched, and well documented point of view.

Dr Amen who has rehabilitated NFL athletes who have suffered major traumatic brain injuries.

And Wade Lightheart of Bio Optimizers.

A basic summary is that drinking coffee daily causes problems that cancel out the health benefits. Dr Amen says it’s hard on the kidneys and restricts blood flow to the brain. They make differing suggestions about how to optimize the benefits of the methylxanthines, but I will just share the basics here.

Take three days of total abstinence per week and stop taking any of these substances 8 hours before going to bed. Those two suggestions are the most important. For even better results, delay the first dose until three hours after awakening at which time the body has a drop in cortisol heading to the mid day slump. Also, use a variety of plants with this family of compounds such as coffee, tea, cacao, Yerba maté, guarana, and kola nut, to name a few. Variety is highly advisable.

On a personal note, please select fair trade, shade grown, organic varieties to show gratitude to the people who work hard to provide for us and for the sake of the soil and the water as well as the community of living things that coexist with the plants and help to make it all possible.
 

Jack3

Kava Enthusiast
@Jack3 Shade grown? That’s a new one for - do explain.
It has something to do with bird migration and I think also other animals. Perhaps it’s better for the coffee plants, too. I’ll have to look it up again.

Another fun fact is that the coffee bean is the seed that grows ina fruit that resembles a cherry. I’ve read about people enjoying the flavor although I don’t know if anyone knows about its nutrition.
 

Jack3

Kava Enthusiast
I was somewhat remiss in failing to mention how misleading and untrustworthy labeling often turns out to be. For a heartbreaking yet eye opening example, watch a Morgan Spurlock film called Holy Chicken wherein he exposes the fraud behind the “free range” label. To become thoroughly disillusioned, follow that with Planet of the Humans.

Please don’t stop there, because empowerment is available. Visit https://foodispower.org

This is a website of investigative journalists who work in the field to verify if and to what extent companies actually deliver on the claims of their labels.

I think it is important to mention that many of my concerns for justice and nature are probably going on with kava like everything else. It does appear that some vendors are taking initiative to be just in their dealings, but how would I really know.

Unless I go there and see for myself, it’s hard to be certain. I have supported local farms that either can’t afford certification or don’t have time for the paperwork, but when I volunteered on their farms I saw for myself that all is well with their work. The same is likely true for kava. Those that get certified may be frauds. Those uncertified may be the real deal.
 

The Kap'n

The Groggy Kaptain (40g)
KavaForums Founder
Certainly.

Above we can see a more detailed representation of the metabolism of caffeine. To the right we see Caffeine demethylated through the pathways CYP1A2 and lesser CYP2E1 pathway to theobromine. Theobromine is then broken down by xanthine oxidase into 3,7 DMU. We currently don't know kava's effect at xanthine oxidase (XO). There are studies showing that inhibition of XO being common by a variety of dietary flavonoids and chalcones [2]. Kavalactones and flavokavains fall into these categories, so the chance at inhibition at this spot is certainly not zero.

What I believe this to mean is that you'll likely see an effect at beverages high in caffeine, and likely mate as well due to it's caffeine level. Theobromine in mate may end up sticking around longer if kavalactones and FKs do indeed inhibit XO, but more research is needed in this area, as there are no studies that directly address XO inhibition with kava or constituents of kava.

What this means to you?

You may find a bit more stimulatory properties out of your mate depending on your personal physiology. The word is still out on whether kava inhibits that process of further breakdown of theobromine.



[1] Nehlig, Astrid. 2018. “Interindividual Differences in Caffeine Metabolism and Factors Driving Caffeine Consumption.” Pharmacological Reviews 70 (2): 384–411. https://doi.org/10.1124/pr.117.014407.

[2] Nagao, A., M. Seki, and H. Kobayashi. 1999. “Inhibition of Xanthine Oxidase by Flavonoids.” Bioscience, Biotechnology, and Biochemistry 63 (10): 1787–90. https://doi.org/10.1271/bbb.63.1787.
I know this will be be a blast from the past, but I just found research that looks to answer the following question:

"Do kavalactones inhibit Xanthine Oxidase (XO) activity?"

In this paper researchers compared the antioxidant properties, and the ability to inhibit xanthine oxidase on a number of different kavalactones and flavonoids found in kava.

In regards to Xanthine Oxidase, they found the crude (full spectrum) extract had an inhibitory property 21 times LESS than that of the known XO inhibitor, Allopurinol.

Another fun fact, they found that water extracted kava had the least XO inhibitory properties, with the 2nd highest antioxidant properties. Even more reason to go traditional in preparation, if you ask me.

This study also confirmed that while individual kavalactones themselves may be antibiotic, aqueous (traditional) preparations of kava are not. The aqueously prepared samples had the same antibiotic activity as what was seen in the control.

Minh, Truong Ngoc, Truong Mai Van, Tran Dang Khanh, and Tran Dang Xuan. 2022. “Isolation and Identification of Constituents Exhibiting Antioxidant, Antibacterial, and Antihyperuricemia Activities in Piper Methysticum Root.” Foods (Basel, Switzerland) 11 (23). https://doi.org/10.3390/foods11233889.
 

Alia

'Awa Grower/Collector
I know this will be be a blast from the past, but I just found research that looks to answer the following question:

"Do kavalactones inhibit Xanthine Oxidase (XO) activity?"

In this paper researchers compared the antioxidant properties, and the ability to inhibit xanthine oxidase on a number of different kavalactones and flavonoids found in kava.

In regards to Xanthine Oxidase, they found the crude (full spectrum) extract had an inhibitory property 21 times LESS than that of the known XO inhibitor, Allopurinol.

Another fun fact, they found that water extracted kava had the least inhibitory properties, with the 2nd highest antioxidant properties. Even more reason to go traditional in preparation, if you ask me.

This study also confirmed that while individual kavalactones themselves may be antibiotic, water extraction is not. The water extraction portion had the same antibiotic activity as what was seen in the control.

Minh, Truong Ngoc, Truong Mai Van, Tran Dang Khanh, and Tran Dang Xuan. 2022. “Isolation and Identification of Constituents Exhibiting Antioxidant, Antibacterial, and Antihyperuricemia Activities in Piper Methysticum Root.” Foods (Basel, Switzerland) 11 (23). https://doi.org/10.3390/foods11233889.
To be clear(er),water extracted kava had "second highest antioxidant properties."
However,
" individual kavalactones themselves may be antibiotic, water extraction is not."
That seems to read aqueous kava beverage has antibiotic ability but water extraction does not...
can this be made clearer, for folks?
As a side-- the study is saying kava drinking will not inhibit gout.
 

fueledbykava

Kava enthusiast
So anecdotally of course, nights where I've had caffeine during the day and kava I tend to have trouble sleeping and staying asleep. I haven't controlled for the kava yet by eliminating caffeine entirely, but it's an interesting data point as far as the pharmacokinetics of caffeine metabolism go IMO.
 

Edward

Aluballin' in the UK
Kava Vendor
So anecdotally of course, nights where I've had caffeine during the day and kava I tend to have trouble sleeping and staying asleep. I haven't controlled for the kava yet by eliminating caffeine entirely, but it's an interesting data point as far as the pharmacokinetics of caffeine metabolism go IMO.
Sorry if this has been mentioned before but maybe try a heavier kava? I have been drinking kava and coffee on the same days recently, usually with a good 8 or more hours between finishing one and starting the other, and I only notice a slight interaction between the two. Coffee the mornings after can be somewhat heightened, a higher buzz with longer lasting effects. I don't really notice the kava feeling much different when I drink that. I still sleep fine. Mind you if I only drink coffee for a few weeks my sleep isn't affected anyway.
 

fueledbykava

Kava enthusiast
Interesting, I would love to see more research showing the amount of time that kava consumption degrades CYP1A2 and increases concentrations xenobiotics like caffeine in a dose dependant manner of course for both kava and the xenobiotic. And by kava, of course I'd love to see it on a per-kavalactone basis. If heavier kavas have more or less effect on other drug metabolism, it'd be interesting to know since the kavalactone profile is obviously different than a much headier kava.
 

Zaphod

Kava Lover
With the exception of people with ADHD who respond differently to stimulants, caffeine—or any of the methylxanthines—will interfere with the quality of sleep even for those who can go straight to sleep immediately after drinking a cup of coffee.

The only 3 sources I have found in the medical/wellness field who discuss caffeine without selling it on the side suggest that caffeine should be used in a way that differs considerably from our cultural habit.

These are Dr Ari Whitten of www.theenergyblueprint.com who features numerous cutting edge podcasts with a variety of doctors from a rigorously empirical, well researched, and well documented point of view.

Dr Amen who has rehabilitated NFL athletes who have suffered major traumatic brain injuries.

And Wade Lightheart of Bio Optimizers.

A basic summary is that drinking coffee daily causes problems that cancel out the health benefits. Dr Amen says it’s hard on the kidneys and restricts blood flow to the brain. They make differing suggestions about how to optimize the benefits of the methylxanthines, but I will just share the basics here.

Take three days of total abstinence per week and stop taking any of these substances 8 hours before going to bed. Those two suggestions are the most important. For even better results, delay the first dose until three hours after awakening at which time the body has a drop in cortisol heading to the mid day slump. Also, use a variety of plants with this family of compounds such as coffee, tea, cacao, Yerba maté, guarana, and kola nut, to name a few. Variety is highly advisable.

On a personal note, please select fair trade, shade grown, organic varieties to show gratitude to the people who work hard to provide for us and for the sake of the soil and the water as well as the community of living things that coexist with the plants and help to make it all possible.
I think we should be careful to distinguish between coffee and caffeine (and its derivatives). Study after study, show drinking up to 2-3 cups of coffee per day has a positive effect on all-cause mortality. So the net benefit is positive. There is some speculation that this is due to the anti-oxidant effect of particular compounds since it is the same effect if you drink decaffeinated or caffeinated. (example: https://pubmed.ncbi.nlm.nih.gov/31055709/).
 

KavaTasteGood

Kava Curious
You have to take into acount the genetic background of people, it's not so black and white. Not sure there is net positive of 3 cup of coffea for slow metabolizers like me (CYP1A2 polymorphism). Fuck up my sleep and not sure if kava could not increase this even more. Feeling great on my morning matcha + my dear kava nights thought :)
 
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