Vitamin E (tocopherol) Is A Potent Aromatase Inhibitor

[haidut]

honeybee,

Isn't the Healthnatura Palm Oil Vitamin E marketed for its tocotrienol content(which I believe is high)? I thought I read somewhere on the forum that tocotrienols were to be avoided according to RP and the tocopherols is what we want.

I have not tried the HealthNatura product yet, but yes, Ray has cautioned against tocotrienol use since they are unsaturated (unlike tocopherols) and have been shown to cause liver enlargement in animals. Here is the Ray quote:
http://raypeat.com/articles/articles/vitamin-e.shtml
"...Besides antagonizing some of the end effects of the toxic fatty acids, vitamin E inhibits lipolysis, lowering the concentration of free fatty acids (the opposite of estrogen’s effect), and it also binds to, and inactivates, free fatty acids. The long saturated carbon chain is very important for its full functioning, and this saturated chain might allow it to serve as a substitute for the omega -9 fats, from which the Mead acid is formed. The unsaturated tocotrienols have hardly been tested for the spectrum of true vitamin E activity, and animal studies have suggested that it may be toxic, since it caused liver enlargement."

 

[ziton]

Philomath/Haidut do either of you happen to know what is the UI amount for say 1/4 tsp of the Lotioncrafter E? There doesn't seem to be any info on their site. The E is also marked 'external use' although you both take it orally? TIA

 

[raypeatclips]

I, personally, managed to fix a very large varicose vein on my right leg with topical vitamin E.

Just saw this post of yours from 2014 haidut. Do you think topical vitamin E applied to a testicle with a varicocele would be able to fix the problem?

 

[haidut]

Just saw this post of yours from 2014 haidut. Do you think topical vitamin E applied to a testicle with a varicocele would be able to fix the problem?

It may, a least probably no harm in trying it. Progesterone or even DHT on the testicle may also help.

 

[Wagner83]

Any thoughts on the anti androgenic activity of vitamin E? (gave links in pansterone thread)

 

[haidut]

Any thoughts on the anti androgenic activity of vitamin E? (gave links in pansterone thread)

Vitamin E has a very strong pro-progesterone effect in higher doses, so that may be the reason. I don't think vitamin E is a direct androgen antagonist itself.

 

[Wagner83]

Vitamin E has a very strong pro-progesterone effect in higher doses, so that may be the reason. I don't think vitamin E is a direct androgen antagonist itself.

Vitamin E succinate inhibits the function of androgen receptor and the expression of prostate-specific antigen in prostate cancer cells
Not sure how relevant vit E succinate is:

Many factors may influence AR function, including interrupting production of the AR at the mRNA or protein levels, ligand binding, dimerization, nuclear translocation, the presence of AR-associated proteins, etc. Our data indicate that VES has a delayed and marginal inhibiting effect on the transcription of AR (Fig. (Fig.3),3), with no obvious effects on ligand binding, nuclear translocation, and the interaction between the N terminus and the C terminus of AR (Fig. (Fig.4).4). VES, however, influences AR function by down-regulating the efficiency of its translation in LNCaP cells (Fig. (Fig.5).5). This could represent a previously unreported mechanism for regulating AR function.

An other compound of vitamin E mentioned here:
Pansterone - Liquid Dietary Supplement For Rejuvenation

 

[Wagner83]

More discussion here and the following posts
https://raypeatforum.com/community/...ent-for-rejuvenation.7426/page-39#post-225767

https://www.ncbi.nlm.nih.gov/pubmed/15084515
Lycopene and vitamin E interfere with autocrine/paracrine loops in the Dunning prostate cancer model.
"Vitamin E reduced androgen signaling without affecting androgen metabolism"

As haidut said the vitamin E has a long tracking record of boosting T rather than the opposite, however I'm curious about potential effects on AR.

 

[Dobbler]

Do i need to eat vitamin e with fat? Im currently following PUFA depletion protocol and eating 0 fat so is it pointless to take high dose vitamin e?

 

[ddjd]

isnt the regular health natura vitamin e product ok? not the palm one i mean to say

 

[Mateo Wiechers]

Hi all,

As you know Ray has written extensively on the benefits of Vitamin E though its actions as an estrogen antagonist. I opsted some studies that show that tocopherols act directly like estrogen "receptor" antagonist and this may explain some of their anti-estrogenic properties. However, receptor antagonists (e.g. cyproheptadine) typically do not decrease plasma levels of the hormone/substance they are antagonizing. So, I was wondering how come several studies with mixed tocopherols (escpecially a mix with high gamma contents) reduced plasma levels of estrogen. I just found this study that appears to confirm that in addition to being an estrogen "receptor" antagonist, tocopherols are also aromatase inhibitors - i.e. they also reduce the synthesis of new estrogen "in vivo".

http://www.fasebj.org/content/early/200 ... e.full.pdf

This would make vitamin E even more attractive substance for Peat-minded people since reducing estrogen (AKA the "shock hormone") is one of the main goals of the Peat-style diets and regimens. Interestingly, tocopherols were also found to suppress androgen signaling WITHOUT suppressing androgen metabolism. So, what other substance is known to have this effect - i.e. estrogen receptor antagonist, aromatase inhibitor, and anti androgenic? The answer is - progesterone!
And of course, not surprisingly, Peat and others scientists working with vitamin E have written extensively about its progesterone-like qualities and progesterone-sparing effects. So, in a sense, vitamin E is a surrogate for progesterone.
The study compared vitamin E to lycopene in terms of prostate cancer inhibition and found that lycopene has 5-alpha reductase inhibiting properties, while vitamin E did not. So, lycopene works similarly to the well-known "chemical castration" drugs like Finasteride (i.e. Propecia) while vitamin E does not.
I strongly recommend reading the full study, but for those that do not have the patience here are some notable quotes:

"...In contrast to lycopene supplementation, vitamin E treatment did not influence steroid 5-α-reductase expression in the prostate tumors. Vitamin E, however, significantly reduced aromatase expression, suggesting reduced estrogen synthesis. Also, in contrast to lycopene treatment, neither IGF-I nor the ROS generating iNOS or NADPH oxidase were affected by vitamin E. "

"...In the vitamin E-treated group, the reduced androgen target gene expression is in agreement with studies demonstrating that vitamin E inhibits the androgen receptor (25). In addition, vitamin E affected estrogen metabolism by down-regulating aromatase expression."

"...Vitamin E reduced androgen signaling without affecting androgen metabolism. Lycopene interfered with local testosterone activation by down-regulating 5-α-reductase and consequently reduced steroid target genes expression (cystatin-related protein 1 and 2, prostatic spermine binding protein, prostatic steroid binding protein C1, C2 and C3 chain, probasin)."

The human equivalent dosage for achieving these effects is about 7mg/kg - 9 mg/kg vitamin E. This is close to the human equivalents of 1g - 1.5g daily reported by the studies using the high-gamma mixed tocopherols (γ-TmT) for breast cancer listed below. Also of note, is the fact the vitamin E used was only alpha-tocopherol, not mixed tocopherols. This is in line with the other study I posted showing alpha-tocopherol to be an estrogen receptor antagonist.
Vitamin E is an estrogen receptor antagonist
Furthermore, the above dose of about 1.5g for a person of 100kg weight, matches well with yet another study on using gamma-tocopherol rich mixture to treat prostate cancer.
Dietary tocopherols inhibit PhIP-induced prostate carcinogenesis in CYP1A-humanized mice. - PubMed - NCBI
"...In the present study, we investigated the effects of different preparations of tocopherols on PhIP-induced prostate carcinogenesis. The dosages of γ-TmT (0.3% in diet) or δ-T, γ-T and α-T (0.2% in diet) were selected from the optimal doses observed in previous studies and correspond to the intake of 1.5 g or 1.0 g of tocopherols, respectively, for a person consuming 500 g of diet per day [20–22,27]. These doses, although higher than the nutritional level, have been reported to be nontoxic [28]. Dietary γ-TmT and δ-T were found to inhibit the development of mPIN lesions and related molecular events, while γ-T and α-T were less effective. The results suggest that the inhibitory effect of tocopherols involves the reduction in cellular oxidative and nitrosative stress and inhibition of the PI3K/ AKT signaling pathway."

Btw, the vitamin E used in this study was dl-alpha-tocopheryl acetate (Rovimix E50 brand). Peat wrote that DL-alpha-tocopheryl acetate has only about 50% of the activity of pure alpha-tocopherol. This suggests that if pure alpha-tocopherol is used, a person may be able to achieve the same effects with only half the dose used in the study.

Finally, since lycopene is found primarily in tomatoes and bright-colored vegetables like bell peppers - that may another reason to take it easy on the vegetable intake. Ray talks about tomatoes containing serotonin, and when you add lycopene with its "castration" properties I think this makes the case for avoiding the nightshades plants family even stronger.

Thoughts?

Hi, if you where to take a high dose of Vitamin E, say 1500 mg/day for Estrogen Reduction, would it be better to split te dose across the Day or to get a single dose with the main meal ?

 

[haidut]

Hi, if you where to take a high dose of Vitamin E, say 1500 mg/day for Estrogen Reduction, would it be better to split te dose across the Day or to get a single dose with the main meal ?

I don't think that such a high dose is needed. Several recent studies found that a dose of around 500mg daily optimally suppresses estrogen and at that dose it can be taken in a single sitting with a large meal to reduce risk of GI irritation.

 

[Lyall]

@haidut Is that 500mg of the dL-tocopherol?

 

[haidut]

@haidut Is that 500mg of the dL-tocopherol?

No, 500mg of D-tocopherols. Natural mixed tocopherols are of the D-type. The L-isomer is probably inactive.

 

[Lyall]

Thank you

 

[Peatogenic]

@haidut when you say progesterone surrogate does this mean that Vit E literally raises progesterone levels, or just creates the feel of progesterone? I wonder the same about "thyroid surrogates".

 

[haidut]

@haidut when you say progesterone surrogate does this mean that Vit E literally raises progesterone levels, or just creates the feel of progesterone? I wonder the same about "thyroid surrogates".

It has been shown to "spare" progesterone by opposing estrogen and is also used as a tocolytic agent - i.e. prolongs pregnancy. The latter is the main effects of progesterone in pregnant women, so vitamin E seems to have strong parallels to progesterone in terms of effects. Whether it directly acts on the progesterone "receptor" - that I don't know.

 

[Peatogenic]

It has been shown to "spare" progesterone by opposing estrogen and is also used as a tocolytic agent - i.e. prolongs pregnancy. The latter is the main effects of progesterone in pregnant women, so vitamin E seems to have strong parallels to progesterone in terms of effects. Whether it directly acts on the progesterone "receptor" - that I don't know.

Thank you.

 

[GeoX]

I only used it topically for about a month to fix the varicose vein. Afterwards I started taking it orally. If you mix vitamin E with olive oil it will absorb very well through the skin. It absorbs poorly only when you apply it without oil.

Hi @haidut : Today I purchased Tocovit to see if I can fix a small varicose vein and a damaged blue vein spot on my calf (from a minor farming broadfork injury) before trying progesterone. Although Tocovit has MCT, do you recommend adding some olive oil for better topical absorption? I plan to take Tocovit topically and orally. Any rather recommendations regarding this experiment? Thanks for all your help and great products!

 

[Vinny]

Search for "magnesium bicarbonate".

I searched too but could not find it