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Vitamin E (tocopherol) Is A Potent Aromatase Inhibitor

Discussion in 'Scientific Studies' started by haidut, Jan 29, 2014.

  1. haidut

    haidut Member

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    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?
     
  2. solaire_of_astora

    solaire_of_astora Member

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    I took maybe half a tablepoon worth of A.C. Grace's liquid E about a week ago. I only took it that one time because it had pretty much ran out and I was draining the leftovers out of the bottle. I think it might have increased my libido a bit, but it's too hard to say with just a one-time large dose. I'll probably get some more in the coming weeks and see what massive doses do for me.
     
  3. OP
    haidut

    haidut Member

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    The AC Grace vitamin E product might not be the best one for this purpose. Several months ago I posted a discussion where I said they might have changed the formula. If it's not too much trouble, try the LotionCrafter or Swanson products, or any of the other tocopherol products listed in the Supplements section. I get big drop in estrogen from a proper vitamin E supplement, but I got bad reactions from AC Grace.
     
  4. Ben

    Ben Member

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    What kind of reactions did you get from it, and was the drop in estrogen from Unique E smaller than from the other products? I don't understand what could be changed about the "formula", it's just vitamin E, glycerin, and gelatin.
     
  5. OP
    haidut

    haidut Member

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    This is discussed at length at another thread:
    viewtopic.php?f=3&t=1949

    Bottom line - AC Grace seems to have changed the formula and dilutes it with some kind of vegetable oil that essentially nullifies the good effect I had from it circa 2011. I still have a bottle of the "old" AC Grace product and it is much much darker in color than the "new" one.
    Anyways, with the other vitamin E brands my estrogen drops by about 62%-74% of the average monthly plasma estrogen for the last 3 months, while with AC Grace I don't see that effect. Blood tests may be unreliable, but they are consistent in what they show. So, a big drop in estrogen by using some brands and no drop in estrogen using AC Grace. I can also tell subjectively, since AC Grace does not give any boost in libido while the other brands I use (most of which are 95% purity or higher) give a dramatic boost in libido. Also, on AC Grace I seem to retain water and that is classic symptom of estrogen dominance. Using any other brand makes me as dry as a desert shrub.
    The list is long, but for me there is no doubt what works and what doesn't (for me at least).
     
  6. Ben

    Ben Member

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    Man, it would make life so much easier if users could edit their posts, such as the OP in the supplement thread or in your vitamin E thread. Which brand did you get the best cost-benefit ratio from?

    http://www.tkoskin.com/Vitamin-E_p_57.html
    http://www.bulknaturaloils.com/Products ... erols.aspx
    http://www.lotioncrafter.com/vitamin-e- ... ls-95.html

    Vitamin E being so anti-estrogenic, can it be applied to areas of the body such as the legs to reduce water retention, or doesn't the focal application help? This is something my mom has a problem with.
     
  7. OP
    haidut

    haidut Member

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    I think LotionCrafter is the biggest bang for the buck and also the highest concentration (95%+). It also has a CoA. The TKO is a very nice product but expensive and I thin it is pure alpha-tocopherol, not mixed with gamma and the rest of the isomers.
    If you prefer pills, I had very good experience with the Swanson high gamma product.
    http://www.swansonvitamins.com/swanson- ... l-30-sgels

    Vitamin E can be applied externally to skin. I know women who removed stretch marks and C-section scars with vitamin E dissolved in olive oil. Ray recommends it taken that way too. For water retention, magnesium and sodium are best. So, I'd recommend you search the forum for my post on how to make magnesium bicarbonate water and drop some Alka-Seltzer in it, or add salt. It is great for removing excess water. The vitamin E can do it too but it would take about a week taken orally to get you that effect.
    I, personally, managed to fix a very large varicose vein on my right leg with topical vitamin E (it has progesterone-like effects and progesterone is used for varicose veins).
    I hope that info helps.
     
  8. jyb

    jyb Member

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    Do you get your vit E topically for general purposes (estrogen), or just for local skin healing purposes? For vitamins it seems like only a small % topical gets absorbed.
     
  9. OP
    haidut

    haidut Member

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    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.
     
  10. Ben

    Ben Member

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    I thought stretch marks are a form of fibrosis and impossible to reverse. So the cell gets collagenized, how can vitamin E reverse collagenization of the cells? It's frequently said that stretch marks and scars are impossible to remove, and it's only possible to cover them up. I know estrogen is involved in fibrosis, but I don't know what reverses it, if something can reverse it.

    I have stretch marks and I can do before and after photos for reference.
     
  11. aguilaroja

    aguilaroja Member

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    The lore about vitamin E or wheat germ oil reducing scars and/or stretch marks goes back at least several decades.

    I have seen examples of it working in myself and more than a dozen others. In some cases, the Kenogen/Progest-E oil got additional results after vitamin E "alone" was tried first. Many more people are willing to try the suggestion of vitamin E alone than to use a hormone with E oil.I have not seen good accounts about whether it (vitamin E) works in controlled trials, or how it works. Of course, there is some touting of vitamin E as an antioxidant.

    The replacement of fibrosed or scarred cells by "livelier" ones seems significant. It is telling about research enterprises if this happens and is not much investigated.

    I have not recently looked over the accounts by Perricone and other nutrient-touting dermatologists to know their views.

    The Shutes wrote about it:

    Shute, Vogelsang, Skelton and Shute (1948) Surg., Gyn. and Obst. 86:1.
    "It prevents scar contraction as wounds heal."
    http://www.doctoryourself.com/shute_protocol.html

    And there are other mid-20th century articles:
    Steinberg (1948) Med. Clin. N. America 30:221, 1946. (occasionally lyses scar tissue)

    BELLANTI F. , Rass Int Clin Ter. 1949 Sep 15-30;29(17-18):322-7.
    [Use of alpha-tocopherol in the prevention of postoperative pathologic peritoneal adhesions: experimental research]. [Article in Italian]PMID: 15394366
     
  12. solaire_of_astora

    solaire_of_astora Member

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    The bottle I used was from back when the stuff was still good, but I plan to get the LotionCrafter brand sometime soon.
     
  13. BingDing

    BingDing Member

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    Great post, haidut, thanks.

    I was just looking at Lotioncrafters site about their 95% product. Under the "formulary" tab they have a note "You can substitute Mixed Tocopherols 99% for the D-alpha Tocopherol, as these are pure tocopherols without the soybean added to dilute them".

    That sure got my attention, I've never seen 99%. A google search didn't turn up anything. Thought you might have the contacts to find out more.
     
  14. OP
    haidut

    haidut Member

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    Are you asking where to get 99% tocopherol? It's possible but in small quantities and it is very expensive. Simga-Aldrich sells it as does Fisher Scientific. But 95% is pure enough for most purposes.
     
  15. marikay

    marikay Member

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    haidut..I searched for your post on magnesium water but couldn't find it. Can you re-post? Thanks
     
  16. OP
    haidut

    haidut Member

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    Search for "magnesium bicarbonate".
     
  17. himsahimsa

    himsahimsa Member

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    Magnesium carbonate + soda water. Unlike sodium bicarb, Mg and Ca bicarbonates are only maintained in solution.
     
  18. bradley

    bradley Member

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    I've made magnesium water by mixing milk of magnesia with a high quality high bicarbonate content sparkling water such as apollinaris. Works wonders.
     
  19. Ben

    Ben Member

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    Have you ever witnessed anyone curing their rosacea, which RP recently wrote an article about? I read the article and I'm taking niacinamide and thiamine, and I've been eating the Peaty way for 2 years. About 1 year in, my nose started getting red when I was stressed out, then it became persistently light red, and stayed that way until now. I applied progest-E to my nose, but the redness didn't fade. I also applied the unique-E brand of vitamin E on my nose, to no avail either. So I wonder if the good brands of vitamin E can help treat it.
     
  20. Jib

    Jib Member

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    FWIW, my dad has nummular eczema. I finally convinced him to let me rub some of the Lotion Crafter 95% vitamin E oil and some coconut oil on an inflamed part of his leg near his ankle.

    It's been a few days since I applied it and he said it hasn't bothered him or itched at all since. If I can convince him to make a regular habit out of this it seems like it might have some potentially promising results.

    I've made the magnesium bicarbonate. You just funnel in 3 tablespoons of milk of magnesia into a liter bottle of seltzer (slowly, so it doesn't overflow), replace the cap, shake it up, refrigerate it, wait 30 minutes, shake it again, back in the fridge, and once it becomes crystal clear again it's ready to go.

    I've had loose bowel movements every time I've used it. Even in small amounts, like a tablespoon or half a tablespoon mixed into a cup of coffee. That is really not a lot of magnesium considering that only 3 tablespoons of magnesium hydroxide are diluted in an entire liter.

    I don't know anyone else that's had that problem and I also can't tolerate even small amounts of magnesium glycinate. I just stick to epsom salt baths. But if someone can tolerate it I do think the magnesium bicarbonate water can probably be a very huge help.
     
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