Maximise Your Free Testosterone Levels

[matisvijs]

I’ve been interested in maximizing testosterone levels naturally for a while now. In this post, I’ll cover how to increase one’s free testosterone in particular: free testosterone being bioactive is what really delivers the testosterones positive effects on muscle growth, fat loss and physical, mental energy levels.

There are 3 variables that we can manipulate to SAFELY increase free testosterone levels:

1)Increase it directly - use substances that increase it directly like DHT and magnesium (See below), also use substances that increase factors, that help keep free T high (such as natural 5-ar enhancers i.e. glycine)

2)Lower SHBG (sex hormone binding globulin) and minimize factors that increase it - SHBG is a glycoprotein that binds to the two sex hormones: androgen and estrogen (androgen meaning testosterone in this case), rendering it inactive. Only a very small fraction of about 1-2% is unbound, or "free" (what we’re trying to increase here) and thus biologically active and able to enter a cell and activate its receptor.

3)Increase total testosterone levels – the higher our total testosterone levels, the higher free testosterone levels as, even though the percentage of free T may not change, the total amount of it will if we can maximize this variable. Regarding this point, along with substances that increase testosterone, we would also want to use safe and beneficial aromatase inhibitors and anti-estrogenic substances (Nettle root, vitamin E) as conversion to estrogen would reduce our total T levels (and our free T level as a chain reaction).


So, let’s look at some substances that fit the bill – some of these accomplish all three of our goals (i.e. raise free T, lower SHBG and raise total T):

Boron – often cited as a substance that can lower SHBG levels:
Comparative effects of daily and weekly boron supplementation on plasma steroid hormones and proinflammatory cytokines. - PubMed - NCBI - increased free T by 28%, estradiol decreased here as well and DHT was elevated

The significance of dietary boron, with particular reference to athletes. - PubMed - NCBI - increased T but also increased estradiol (CAREFUL) which makes it unclear whether boron increases or decreases estrogen. (might want to use with an AI, just to be safe)

The effect of boron supplementation on the distribution of boron in selected tissues and on testosterone synthesis in rats


· Magnesium – increases free testosterone(as well as blocks SHBG), here are some studies:

Effects of magnesium supplementation on testosterone levels of athletes and sedentary subjects at rest and after exhaustion. - PubMed - NCBI - raised free T levels by 24%

Magnesium and anabolic hormones in older men. - PubMed - NCBI

The Interplay between Magnesium and Testosterone in Modulating Physical Function in Men. - PubMed - NCBI

Magnesium effect on testosterone–SHBG association studied by a novel molecular chromatography approach - decreases SHBG


· Taurine – Raises testosterone in a pretty significant way:

CSD mRNA expression in rat testis and the effect of taurine on testosterone secretion. - PubMed - NCBI - normalised lowered T levels, as well as increased them significantly, in different settings, doubling them in some

Taurine enhances the sexual response and mating ability in aged male rats. - PubMed - NCBI - stimulated testosterone production in aged rats




· DHT – reduces estrogen, increases free T:

STUDIES ON THE TREATMENT OF IDIOPATHIC GYNAECOMASTIA WITH PERCUTANEOUS DIHYDROTESTOSTERONE - shows anti-gynecomastia effects as well

‘T + DHT/E2 ratio increased significantly (P < 0.02) to a normal mean value’

It does reduce circulating testosterone levels in studies but I expect DHT’s anti-e effects would mean that the FREE testosterone levels shouldn’t suffer that much.

As a sidenote, will probably do a seperate post on the various other benefits/beneficial actions of DHT: lowers estrogen, lowers prolactin, lowers serotonin, decreases symptoms of gynecomastia, reduces depression, improves spatial working memory, increases GABA, etc.

· Zinc – pretty well known for its effects as a testosterone booster:

The effect of exhaustion exercise on thyroid hormones and testosterone levels of elite athletes receiving oral zinc. - PubMed - NCBI

Effect of fatiguing bicycle exercise on thyroid hormone and testosterone levels in sedentary males supplemented with oral zinc. - PubMed - NCBI

Effect of zinc administration on plasma testosterone, dihydrotestosterone, and sperm count. - PubMed - NCBI - increases DHT

Impact of oral zinc therapy on the level of sex hormones in male patients on hemodialysis. - PubMed - NCBI

As a bonus, zinc is a prolactin inhibitor:

Zinc: an inhibitor of prolactin (PRL) secretion in humans. - PubMed - NCBI

Zinc acutely, selectively and reversibly inhibits pituitary prolactin secretion. - PubMed - NCBI


· Vitamin E – Acts as both, an estrogen receptor antagonist and an aromatase inhibitor, reduces estrogen levels:

Novel interactions of vitamin E and estrogen in breast cancer. - PubMed - NCBI

Is also a strong prolactin inhibitor on top of it: Effect of vitamin E therapy on sexual functions of uremic patients in hemodialysis. - PubMed - NCBI - decreased prolactin by 69% in the study.

Here’s Ray Peat’s article on it, where he discusses it’s anti-estrogenic effects:: Vitamin E: Estrogen antagonist, energy promoter, and anti-inflammatory



· Vitamin D – lowers SHBG, increases both free and total T:

Association of vitamin D status with serum androgen levels in men. - PubMed - NCBI - increases T, lowers SHBG

https://www.ncbi.nlm.nih.gov/pubmed/21154195 - increased T

https://www.ncbi.nlm.nih.gov/pubmed/18351428 - correlation between optimal vitamin D levls and higher testosterone levels.

Acts as an anti-estrogen:

http://press.endocrine.org/doi/abs/10.1210/en.2009-0855

https://www.fredhutch.org/en/news/c...-reduced-estrogen-and-breast-cancer-risk.html


· Caffeine – raises testosterone:

https://www.ncbi.nlm.nih.gov/pubmed/22349085

https://www.ncbi.nlm.nih.gov/pubmed/20737165

https://www.ncbi.nlm.nih.gov/pubmed/18458357


As a bonus caffeine also has some nice (well documented) liver protective effects (will post a seperate thread sometime).


· Nettle root – Lowers SHBG, on top of being an aromatase inhibitor.

Here’s a study on it lowering SHBG: https://www.ncbi.nlm.nih.gov/pubmed/7702715

Acts as an AI:

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3074486/

https://www.ncbi.nlm.nih.gov/pubmed/16643058


· Tribulus terrestris – one of the most popular OTC testosterone and DHT boosters, studies:

https://www.ncbi.nlm.nih.gov/pubmed/18068966 - from the study:

‘In primates, the increases in T (52%), DHT (31%) and DHEAS (29%) at 7.5mg/kg were statistically significant. In rabbits, both T and DHT were increased compared to control, however, only the increases in DHT (by 30% and 32% at 5 and 10mg/kg) were statistically significant. In castrated rats, increases in T levels by 51% and 25% were observed with T and TT extract respectively that were statistically significant.’

https://www.ncbi.nlm.nih.gov/pubmed/23723641 - an increase in testosterone was noted (16.3%) but failed to reach statistical significance.


· Selenium – anti-estrogenic:

https://www.ncbi.nlm.nih.gov/pubmed/22128327

https://www.ncbi.nlm.nih.gov/pubmed/16093440

https://www.ncbi.nlm.nih.gov/pubmed/15833885

· Vitamin K2 – increases testosterone levels in several studies:

https://www.ncbi.nlm.nih.gov/pubmed/21894328

https://www.ncbi.nlm.nih.gov/pubmed/15763078 - effects on estrogen


· Glycine – Upregulates 5-alpha reductase activity, increasing DHT, so acting in the opposite direction as drugs like finasteride(which have anti-androgenic activity):

https://www.ncbi.nlm.nih.gov/pubmed/18367344


· DHEA – here are some articles on its testosterone increasing properties:

https://www.ncbi.nlm.nih.gov/pubmed/20863330 - increased T but also increased estrogen

http://www.ncbi.nlm.nih.gov/pubmed/21789881 - again, increases in both T and E

https://www.ncbi.nlm.nih.gov/pubmed/19321570 - same thing, T, E go up

https://www.ncbi.nlm.nih.gov/pubmed/18029465 -same, that’s the reason I recommend to only take it with an aromatase inhibitor

https://www.ncbi.nlm.nih.gov/pubmed/16804050 - DHEA + AI

https://www.ncbi.nlm.nih.gov/pubmed/16487434

https://www.ncbi.nlm.nih.gov/pubmed/14667889 - a decrease in SHBG

Other things that increase free testosterone levels: Fructose, resistance exercise, tongkat ali (can be estrogenic though), BCAA (https://www.ncbi.nlm.nih.gov/pubmed/20300014), niacinamide, natural AIs (chrysin, naringenin, apigenin, etc.) and AI drugs (letrozole, exemestane, etc.), TRT.


Recommended books on the subject:

http://amzn.to/2iCsRYK

http://amzn.to/2iCp123

http://amzn.to/2i5p759


So if one were to build an experimental stack based on this research, it would look something like this:

Minerals:

Boron – 5-10mg/day, recommended brands: http://amzn.to/2iv4MUK, http://amzn.to/2iJJQZr

Magnesium – 400-600mg/day, recommended brands: http://amzn.to/2hx0HRA, http://amzn.to/2iv4k8S

Zinc – 25mg/day, http://amzn.to/2hA5xPn

Selenium – 200mcg/2-3x a week, http://amzn.to/2hRxOgu


Vitamins:

Vitamin E - 800 IU/day (Use mixed tocopherols instead of alpha tocopherol products)

Vitamin K2 - 5-10mg/day (Would have to use Thorne’s stuff to achieve milligram dosages)

Vitamin D – 2000-4000 IU/day, brand: http://amzn.to/2icCQqX

Amino – acids:

Taurine – 5g/day, http://amzn.to/2imzguS (cheap, well reviewed)

Glycine –10g/day, http://amzn.to/2iJLmKS

Hormones:

DHT – As far as I know it’s only available in cream form OTC, one can use creatine in it’s place though, combined with 5-ar enhancers (glycine), it should have the needed (similar) net effect. Here’s a study on creatine increasing DHT by 50%+: https://www.ncbi.nlm.nih.gov/pubmed/19741313

DHEA – 15mg/day (Must use with an AI like Nettle root/vit E to minimize conversion to estrogen)


Herbs and other:

Caffeine – 500mg/day (Can use caffeine capsules or just drink 4-5 cups of coffee)

Nettle root – 500-750 mg/day, http://amzn.to/2icKX73

Tribulus Terrestris – 500 mg/day (Again, use only with an AI, as it can be estrogenic, the OPPOSITE of what we want)


As you can see, the dosages I ‘recommend’ are quite high for some things (though some of the studies used even higher) , hence the word ‘experimental’. My recommendation is to do this as a test/loading phase only for a month or two(watch for effects and STOP, if they’re negative) and then cut all the recommended dosages in half for maintenance, with the exception of magnesium (400mg/day is a pretty standard dose). One also realistically wouldn’t use EVERYTHING on this list at once (though I can’t think of a reason why you couldn’t, theoretically).

 

[Such_Saturation]

I remember caffeine can increase SHBG? Also, Ray Peat thinks that carrier proteins can enter cells, and doesn't believe in free blood measurements.

 

[paymanz]

Thank you very much,these info all together is good reference.

Also I never knew ray's opinion on SHBG , thanks Such-Saturation!

 

[paymanz]

Some studies showing coconut oil also has good effect on T levels...

 

[matisvijs]

I remember caffeine can increase SHBG? Also, Ray Peat thinks that carrier proteins can enter cells, and doesn't believe in free blood measurements.

You seem to be right about that but it also increases the total T levels in multiple studies, so I'd argue that the net effect can still be positive, especially if combined with substances that would lower SHBG e.g. boron. Can you give some links/info on Peat's opinion about blood measurements? I'm definitely interested to read his POV on that.

 

[x-ray peat]

I really appreciate all the work!! good stuff

 

[Such_Saturation]

You seem to be right about that but it also increases the total T levels in multiple studies, so I'd argue that the net effect can still be positive, especially if combined with substances that would lower SHBG e.g. boron. Can you give some links/info on Peat's opinion about blood measurements? I'm definitely interested to read his POV on that.

Fats, functions and malfunctions.

The movement of proteins from the plasma into cells has often been denied, but there is clear evidence that a variety of proteins, including IgG, transferrin haptoglobin, and albumin can be found in a variety of cells, even in the brain (Liu, et al., 1989). Cells are lipophilic, and absorb molecules in proportion to their fattiness; this long ago led people to theorize that cells are coated with a fat membrane.


While the competition by PUFA for protein binding sites blocks the effects of thyroid hormone and vitamin A, the action of PUFA on the sex steroid binding protein (SBP, or SSBG, for sex steroid binding globulin) increases the activity of estrogen. That's because the SSBG neutralizes estrogen by binding it, keeping it out of cells; free PUFA keep it from binding estrogen (Reed, et al., 1986). People with low SSBG/estrogen ratio have an increased risk of cancer. When the SSBG protein is free of estrogen, it is able to enter cells, and in that estrogen-free state it probably serves a similar protective function, capturing estrogen molecules that enter cells before they can act on other proteins or chromosomes. Transthyretin, the main transporter of thyroid and vitamin A, and albumin (which can also transport thyroid hormone) are both able to enter cells, while loaded with thyroid hormone and vitamin A. Albumin becomes more lipophilic as it binds more lipid molecules, so its tendency to enter cells increases in proportion to its fat burden. Albumin in the urine is a problem associated with diabetes and kidney disease; albumin loaded with fatty acids passes from the blood into the urine more easily than unloaded albumin, and it is the fatty acids, not the albumin, which causes the kidney damage (Kamijo, et al., 2002). It's possible that SSBG's opposite behavior, entering cells only when it carries no hormones, is the result of becoming less lipophilic when it's loaded with estrogen.

Thyroid: Therapies, Confusion, and Fraud

The specific binding of T3 to albumin alters the protein's electrical properties, changing the way the albumin interacts with cells and other proteins. (Albumin becomes electrically more positive when it binds the hormone; this would make the albumin enter cells more easily. Giving up its T3 to the cell, it would become more negative, making it tend to leave the cell.) This active role of albumin in helping cells take up T3 might account for its increased uptake by the red cells when there were fewer cells in proportion to the albumin medium. This could also account for the favorable prognosis associated with higher levels of serum albumin in various sicknesses.

Natural Estrogens

Ann N Y Acad Sci 1988;538:257-264 Possible relevance of steroid availability and breast cancer. Bruning PF, Bonfrer JM Netherlands Cancer Institute (Antoni van Leeuwenhoekhuis), Amsterdam. “The as yet circumstantial evidence for a central role of estrogens in the promotion of human breast cancer is supported by many data. However, it has not been possible to identify breast cancer patients or women at risk by abnormally elevated estrogen levels in plasma. The concept of available, i.e., non-SHBG bound sex steroid seems to offer a better understanding than total serum steroid levels do. We demonstrated that sex steroid protein binding is decreased by free fatty acids.”


Where he bolded the last part of the citation. So it seems he thinks SHBG should be as high as possible to keep estrogen out of cells, and that it actually enters cells when it is unloaded, unlike albumin. He doesn't say anything about androgens on SHBG but if he claims it's less lipophilic when loaded with estrogen, I don't see why he wouldn't say it becomes more lipophilic when it's loaded with androgens.

 

[Ahanu]

Recommended books on the subject:

http://amzn.to/2iCsRYK

http://amzn.to/2iCp123

http://amzn.to/2i5p759

love the table of contents of the second book ,-)

 

[Parsifal]

Tribulus Terrestris raises nitric oxide as well.

 

[matisvijs]

Tribulus Terrestris raises nitric oxide as well.

Yes, again, one would want to combine things i.e. use it only with a NOS inhibitor (as well as an AI) to get the benefit, without much downside. Thanks for bringing that up, forgot to mention it in the post.

 

[tyler]

Awesome dude, really well put together. The collection of studies and your work of tying it all up is great.

 

[matisvijs]

Awesome dude, really well put together. The collection of studies and your work of tying it all up is great.

Thanks. Btw, I'm not suggesting anyone even follow the 'protocol' but base their decision making on their own views, I'm just putting forth some research that might help do that.

 

[Bahaa El wazzan]

@matisvijs

Interesting thank u


My t is on the high end of the normal range

Mg is good
But the problem of it
That it causes stomach irritations and diarrhea

Any suggestions guys ?

 

[Parsifal]

Yes, again, one would want to combine things i.e. use it only with a NOS inhibitor (as well as an AI) to get the benefit, without much downside. Thanks for bringing that up, forgot to mention it in the post.

Which inhibitors ould you advise?

 

[DaveFoster]

@matisvijs

Interesting thank u


My t is on the high end of the normal range

Mg is good
But the problem of it
That it causes stomach irritations and diarrhea

Any suggestions guys ?

Topical magnesium chloride can bypass the digestive system. What kind are you using, carbonate?

 

[mirc12354]

Good list overall just wondwring why are Vitamin A, thyroid and Aspirin not listed?

 

[LeeLemonoil]

In the thread "Boron: Essential for Peat health" @haidut stated this:

Boron is HIGHLY estrogenic. The bodybuilding community was crazy about it in the 1990s, but then they found out first hand that it raises estrogen (I think all 3 types) and dumped it. Boron has similar effects to cadmium, nickel, cobalt, etc and they are all estrogenic and carcinogenic in higher doses.
Peat is right that unless you are deficient you'd better not mess with it. See below for a study in men.

The effect of boron supplementation on its urinary excretion and selected cardiovascular risk factors in healthy male subjects

"...Supplementation with 10 mg B/d for 4 wk resulted in 84% of the supplemented dose being recovered in the urine. Plasma estradiol concentrations increased significantly as a result of supplementation (51.9±21.4 to 73.9±22.2 pmol/L;p<0.004) and there was a trend for plasma testosterone levels to be increased. However, there was no difference in plasma lipids or the oxidizability of low-density lipoprotein Our studies suggest that the absorption efficiency of B is very high and estimation of the urinary B concentration may provide a useful reflection of B intake. In addition, the elevation of endogenous estrogen as a result of supplementation suggests a protective role for B in atherosclerosis."

 

[matisvijs]

In the thread "Boron: Essential for Peat health" @haidut stated this:

Boron is HIGHLY estrogenic. The bodybuilding community was crazy about it in the 1990s, but then they found out first hand that it raises estrogen (I think all 3 types) and dumped it. Boron has similar effects to cadmium, nickel, cobalt, etc and they are all estrogenic and carcinogenic in higher doses.
Peat is right that unless you are deficient you'd better not mess with it. See below for a study in men.

The effect of boron supplementation on its urinary excretion and selected cardiovascular risk factors in healthy male subjects

"...Supplementation with 10 mg B/d for 4 wk resulted in 84% of the supplemented dose being recovered in the urine. Plasma estradiol concentrations increased significantly as a result of supplementation (51.9±21.4 to 73.9±22.2 pmol/L;p<0.004) and there was a trend for plasma testosterone levels to be increased. However, there was no difference in plasma lipids or the oxidizability of low-density lipoprotein Our studies suggest that the absorption efficiency of B is very high and estimation of the urinary B concentration may provide a useful reflection of B intake. In addition, the elevation of endogenous estrogen as a result of supplementation suggests a protective role for B in atherosclerosis."

Yeah, that's the study I quoted in the post. What about this one though: Comparative effects of daily and weekly boron supplementation on plasma steroid hormones and proinflammatory cytokines. - PubMed - NCBI -
'...After one week (in samples taken at 8.00 A.M, only), the mean plasma free testosterone increased and the mean plasma estradiol decreased significantly. Dihydrotestosterone, cortisol and vitamin D was elevated. Also, concentrations of all three inflammatory biomarkers decreased after supplementation. Of note, despite decreased proinflammatory cytokines, based on recent clinical data, this must be the first human study report to show an increase level of free testosterone after boron consumption.'

 

[Parsifal]

The problem with lowering SHGB is that it increases both T and estrogens. I wonder how to directly reduce estrogen production, not just by lowering aromatase.

 

[Bahaa El wazzan]

@DaveFoster
Im using the carbonate yea

They say magnesium carbonate mixed with glycine is absorbed very well
Donno if thats true

I will try mg chloride also