Pregnenolone, Progesterone And Androsterone Are Aromatase Inhibitors

Discussion in 'Scientific Studies' started by haidut, Apr 10, 2014.

  1. haidut

    haidut Member

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    I have seen some people in the forum claim that they thought pregnenolone increased their estrogen levels. According to this study, pregnenolone should in fact lower estrogen by inhibiting aromatase. Peat has already written extensively on progesterone being a known aromatase inhibitor, so that is no news:
    The concentrations of pregnenolone used were not high at all - 500nM inhibited aromatase by about 25%. Perhaps ore importantly, neither pregnenolone not progesterone could be used as a substrate for aromatase - i.e. they could not be used as source material for synthesizing more estrogen. Some people on the Internet keep claiming pregnenolone or progesterone gave them immediate estrogen symptoms. Well, this study suggests that this is unlikely as neither pregnenolone nor progesterone could be used as raw materials by aromatase for making more estrogen.
    Finally, the study also tested the 5-AR steroids commonly discussed on this forum - i.e. DHT, androsterone, androstanedione and androstanediol. They all inhibited aromatase in concentrations of 500nM and androsterone specifically inhibited aromatase by about 45%. A dose of about 2mg can achieve concentrations of 500nM. Another study posted in the androsterone threads showed that a twice as high concentration (1uM) inhibited aromatase by more than 90%. See attached images for more info.


    FSH-induced aromatase activity in porcine granulosa cells: non-competitive inhibition by non-aromatizable androgens. - PubMed - NCBI

    "...Other steroids such as pregnenolone and progesterone were inhibitory, but testosterone and diethylstilboestrol were stimulatory."

    "...As shown in Fig. 3, a 100-fold increase in oestradiol production was evident in cell culture containing FSH and testosterone during induction. All the other steroids were ineffective as substrates for aromatase. Similarly, during the test period the synthesis of oestradiol was significantly (p<0.05) enhanced in cells previously exposed to testosterone (160%) or DES (25%) and FSH, when compared with that of the FSH-stimulated ones. However, the presence of pregnenolone, progesterone and DHT (during the induction) significantly (p<0.05) decreased the FSH-induced aromatization of testosterone."

    "...To examine whether other 5-reduced C19 androgens also inhibit FSH-induced aromatase activity, granulosa cells were cultured for an initial induction period of 48h in the presence and absense of FSH with or without 0.5uM/L DHT, 5α-androsterone, 5α-androstane-3α,17β-diol, 5α-androstane-3α,17β-dione and 5β-androstane-3,17-dione. After the induction, the cells were incubated for an additional 6h. All the androgens tested were effective in significantly (p<0.05) reducing the aromatization of testosterone (Fig. 5). 5β-androstanedione was the most effective (57%) while DHT was the least (33%) when compared with cultures containing only FSH (Fig. 5, insert)."

    Here is another study referenced by the one above, which also found the 5-AR derived steroids to inhibit aromatase, even when used in low physiological concentrations.
    http://joe.endocrinology-journals.org.sci-hub.bz/content/84/3/409.long
     

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  2. j.

    j. Member

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    I wonder if people take too little. I wonder what would happen if they take 1 gram daily for a week.
     
  3. juanitacarlos

    juanitacarlos Member

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    Possibly. I take 300-500g when I dose, usually once weekly, and never noticed any estrogenic effects.
     
  4. Peata

    Peata Member

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    Why do you only take it once per week?
     
  5. juanitacarlos

    juanitacarlos Member

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    I just heard Peat say that one larger dose will generally work for about a week. I find that is accurate for me. Actually I think he might of said it would for him, last for ten days.

    I've been experimenting with larger doses a few times per week. I feel my stress hormones recede considerably when I take pregnenolone.
     
  6. Peata

    Peata Member

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    OK, thanks. I have pregnenolone ordered, should have it within a week. I'm doing some reading on people's experiences with it.
     
  7. Blossom

    Blossom Member

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    I took a large dose after work today and I must say I'm pleased. I've been taking it since discovering Peat but it had been awhile since I had used a large dose. I feel very calm and warm. I'm considering going back up on my daily dosage for awhile as it seems I still need more than I had previously been taking. I took 500mg today and I think I'll go to 100 daily for a bit. Thanks goes to haidut and j. for bringing this topic to the discussion today.
     
  8. Lin

    Lin Member

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    I thought progesterone increased my estrogen the first time I took it. But I was wrong. I tried again later, and it just made me feel good, hard to describe... I am taking 50 mg/day and thinking of increasing my dose.
     
  9. j.

    j. Member

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    Progesterone increases sensitivity to estrogen. So I think if you take a low dose, enough to increase the sensitivity to estrogen, but not enough to antagonize it, then it can have an overall estrogenic effect.

    Since pregnenolone is a precursor to progesterone, I wonder if a dose that is too low could have the same effect.
     
  10. charlie

    charlie The Law & Order Admin

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    I think I have enough to find out.
     
  11. Lin

    Lin Member

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    Sorry, j., that was a typo. I meant to say pregnenolone, not progesterone.
    But that's interesting about progesterone increasing sensitivity to estrogen. I have tried starting progesterone several times, and always have quit because it gives me such bad headaches.
    Pregnenolone, though, is no problem at all.
     
  12. Such_Saturation

    Such_Saturation Member

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    Sometimes if I double the 50mg amount one day, I start feeling adrenaline in my hands a little bit.
     
  13. Blossom

    Blossom Member

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    I took 100mg pregnenolone this morning and my feet have stayed warmer than usual. I do notice the face lifting effect Peat has written about when I take the higher doses. Perhaps I should let that be my guide in addition to how I feel in determining the correct dose for myself. I do that with Progest-e and the veins on my hands and it works out well.
     
  14. Blossom

    Blossom Member

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    Nearly 6 hours later the warmth is still with me! I'm constantly amazed at what a difference the simple things can make. I have been taking pregnenolone for nearly 8 months and was always happy with the results but obviously it was not enough for my situation. This positive change of events is quite encouraging to say the least. I guess somewhere deep down inside I thought I shouldn't need the higher dose but I was wrong. Work has been much more tolerable today too and I didn't think anything could have that result! :claporange
     
  15. j.

    j. Member

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    Interesting that your effects were so quick. I noticed effects from pregnenolone typically the next day, or a few days after taking it.
     
  16. Blossom

    Blossom Member

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    Yes, I've had that before when I took a large dose. I wonder if it is the powder I have or if I'm really just that in need of the pregnenolone? I'm happy regardless.
     
  17. Peata

    Peata Member

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    Nice to hear this, Blossom. I am really looking forward to getting my pregnenolone and starting it next week. Keep us updated.
     
  18. Blossom

    Blossom Member

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    Will do peata! I'm almost embarrassed since I've been using it and have it in my cabinet that I didn't try increasing the dose before now. Oh well, live and learn as the old saying goes. I'll be interested to hear about your pregnenolone experience too. :rockout
     
  19. Such_Saturation

    Such_Saturation Member

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    Have you noticed the increased color saturation after a couple hours? It's incredible, but also not really an increase in saturation, more like your brain able to do more with the color it gets. STRONGLY advise this substance of life with the coming season.
     
  20. j.

    j. Member

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    That's one effect I never got.
     
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