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A Proposed Anabolic Mechanism Of Tribulus Terrestris (TT)

Discussion in 'Scientific Studies' started by haidut, Oct 26, 2018.

  1. haidut

    haidut Member

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    Some people on the forum like @Wagner83 myself and a few others have tried the infamous herb TT with the hope of raising androgens and improving body composition. Despite Wikipedia bashing TT and raising doubts about its effectiveness, there is plenty of evidence from human trials shows the herb does have an effect. Its main effects seem to be on body composition, libido, steroid levels, and mental health. The proposed main active ingredient is the saponin protodioscin (PTD), even though there are others like diosgenin, tigogenin, 3-OH-5a-sapogenin, etc.
    Protodioscin - Wikipedia

    If you look at the molecular structure of PTD you will quickly see that it is identical to the molecule of DHEA except for several sugary molecules attached to positions C-3 and C-22. One of the known effects of TT is that it raises mostly DHT and DHEA, and less so total/free T. This is pretty much what DHEA does as well when taken on its own. Another known effect of TT is that is increases androgen receptor density in various tissues like muscle and brain, which DHEA is also known to do. However, unlike DHEA, the saponins in TT do not seem to convert into estrogen or raise it much when ingested. Several studies suggest such DHEA-like effect of TT.
    Evaluation of the efficacy and safety of Tribulus terrestris in male sexual dysfunction-A prospective, randomized, double-blind, placebo-controlled... - PubMed - NCBI
    "...The exact mechanism of action of protodioscin is still unclear. Some authors affirm that improvement of sexual desire and enhancement of the erection is due to the conversion of protodioscin to dehydroepiandrosterone (DHEA) [11]. Recently, a hypothesis was reported that the induced relaxation of the corpus cavernosum is probably due to the involvement of the nitric oxide synthase pathway and the endothelium of the corpus cavernosum [1]."

    I don't think that PTD converts to DHEA, but rather that PTD acts like DHEA due to its structure but without the estrogenic metabolism of DHEA. So, if the main active ingredients in TT are mostly non-aromatizable DHEA analogs then how can this explain the anabolic effects and increase in strength it has in people who take it? Well, as I explained in another thread, steroids known to be anabolic for muscle (and brain) have pronounced anti-glucocorticoid effects.
    Structural Requirements For An Optimal Anti-Catabolic Steroid

    DHEA is a known anti-glucocorticoid and I have posted quite a few studies about its effects on inhibiting cortisol synthesis. It also appears to antagonize cortisol at the receptor and possibly centrally (CRH->ACTH).
    Anti-glucocorticoid effects of dehydroepiandrosterone (DHEA). - PubMed - NCBI

    A human study found a 3-fold increase in DHEA from taking TT, which corroborates it being a plant source of DHEA-type steroid.
    Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men. - PubMed - NCBI

    Even more impressively, the TT treatment dropped the prolactin levels of the males from 17 down to 7 - a whopping 60% drop! So, it appears TT is also anti-estrogenic, at least in humans. See further comments down this thread for more discussion on this study. The drop in prolactin is consistent with the dopaminergic effects of TT.
    Evaluation of anti-depressant and anxiolytic activity of Rasayana Ghana Tablet (A compound Ayurvedic formulation) in albino mice
    "...The studies on Tribulus terrestris (Gokshura) suggest that the harmine content of Tribulus acts as Monoamine Oxidase (MAO) inhibitor, leading to higher levels of dopamine in the brain. Due to higher levels of dopamine, the mood is elevated slowly and the stronger and better is the feeling."

    So, if TT contains a non-metabolizable analog of DHEA its primary effects should be through antagonizing cortisol. The study below shows exactly this to be the case and the cortisol antagonism can explain most of the anabolic effects of TT on body and brain, as well as its known anti-depressant effects and improving digestion. As the study below shows, TT was even more effective than Prozac (fluoxetine) in lowering CRH and especially cortisol (fluoxetine effect on cortisol was not significant). The effective doses used in the study seem high but this was plain TT powder, not an extract. Good extracts on the market are usually in potency of 20:1 or even 50:1. With 20:1 potency extracts, the doses used in the study correspond to about 1g-1.5g, which is exactly the dose used clinically with extracts like the Bulgarian prescription drug Tribestan.
    The last study also found strong decrease in cortisol combined with increases in T during overtraining, and a much higher T/cortisol ratio then either training or sedentary groups. The dose that lead to these effects was also equivalent to about 1.2g-1.5g TT extract daily.


    So, anybody else experience cortisol-lowering effects from TT? Any improvements in cognition or mood (as the study below found)?

    Effect of tribulus terrestris saponins on behavior and neuroendocrine in chronic mild stress depression rats. - PubMed - NCBI
    "...As shown in Table 2, Compared with vehicle group, the CMS procedure induced serum CRF levels of model rats a significantly higher (P<0.05). After 4-week treatment, TTS at 0.75 and 2.25 g/kg significantly reduced serum CRF levels in the stressed animals (P< 0.05). Fluoxetine also produced a significant reduce in serum CRF levels (P<0.05). However, TTS at 0.375 g/ kg was failed to alter serum CRF levels in the stressed animals."

    "...As shown in Table 2, Compared with vehicle group there was a significant increase in CORT levels in CMS rats (P<0.05). TTS at 0.375 g/kg slightly but not remarkably reduced serum CORT levels in the CMS-treated rats (P>0.05), and TTS at 0.75and 2.25 g/kg significantly attenuated the CMS-induced increase in CORT levels (P<0.05). Fluoxetine exhibited a tendency to significantly decrease these levels of CMS-treated animals (P<0.05)."

    "...Our results found that CMS can reduced scores of crossing, rears and time of grooming, increased time of staying in central square in OFT, decreased body weight and reduced sucrose preference in SPT, the present result was in agreement to the findings of other similar studies.9,10 All of these symptoms induced by CMS procedure was significantly attenuated by chronic treatment with TTS at 0.75 and 2.25 g/kg, but not at 0.375 g/kg, which confirmed that CMS can affect rats behavior and cause depression, TTS (0.75 and 2.25 g/kg) can antagonism on it and has antidepressant-like effects."

    "...Thus normalization of HPA axis activity is a cure key and an indication of depression relief. In the present study, the CMS procedure resulted in increases of serum CRF and CORT in rats, indicating that CMS might cause HPA axis hyperactivity. CRF is the most potent ACTH secretagogue, but in the present study, the CMS procedure rendered no relative differences on serum ACTH concentrations in rats. This dissociation between CRF and ACTH was found in other similar studies.18 These may be due to the origin of serum CRF was a confounding factor in these determinations, hence peripheral concentrations of CRF were difficult to interpret. In this study, we found TTS at 0.75 and 2.25 g/kg but not at 0.375 g/ kg significantly attenuated the CMS-induced serum CRF and CORT levels. It supported the hypothesis that TTS could exert its antidepressant effect by normalizing HPA axis hyperactivity through CRF and CORT levels regulation."

    tribulus_crf_cortisol_blocking.png

    Effects of Tribulus terrestris saponins on exercise performance in overtraining rats and the underlying mechanisms. - PubMed - NCBI
    "...As shown in Fig. 3, serum level of testosterone was decreased significantly to about 70% of control while serum level of corticosterone was unchanged after six weeks of overtraining. Treatment of rats with TT saponins during overtraining dramatically increased the serum level of testosterone to about 150% of control and 216% of overtraining group respectively and led to a significant decrease in serum level of corticosterone, and consequently a much higher T/C ratio."
    tribulus_testosterone_cortisol_ratio.jpg
     
  2. Wagner83

    Wagner83 Member

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    Thanks. I'm not sure what is the relevance of the ratio of extractions, what may matter more is the amount of protodioscin found in the final product, that is, without lies from the companies (which removes 99% of the products). By the way, I recently contacted the guy who was taking big doses of TT daily to overcome low T and he is still doing it and loving it, I think it takes more time to kick in (and in his case bigger doses) than what a lot of people do. It'd be interesting to know if you run an experiment over a few months, from what I remember reading 3 months was a common minimum course of tribestan.
     
  3. paymanz

    paymanz Member

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    thanks haidut.

    do you guys think its good idea to buy the herb itself and extract it myself? like with ethanol for example?
     
  4. OP
    haidut

    haidut Member

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    The problem is that we don't know of PTD is the only active ingredient. In studies with Maral Root, the extracts performed MUCH better than the isolated 20-ecdysteroid.
    I am currently using only it and plan on doing a 4 week course and then doing blood tests. Will post my results when done.
     
  5. OP
    haidut

    haidut Member

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    I think it would be best to do your own if you find quality herb. There are Youtube videos on how to do a water/ethanol (vodka) extract and studies showed that this type of extract performed much better than ethyl acetate or methanol extracts.
     
  6. Cameron

    Cameron Member

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    Are you planning on making a tt product for the time being what producers seem to have a great product? Lost empire herbs? I've heard great experiences with proper extracts
     
  7. OP
    haidut

    haidut Member

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    Not planning a TT product for now. There are plenty of vendors selling this out there and unless I manage to get a large amount of good Bulgarian herb I don't wan to risk it.
    Here is one vendor I have used and had good results with. Not endorsing it in any way and not getting royalties from them.
    Tribulus Terrestris Saponins Extract | BadmonkeyBotanicals.com
     
  8. Cameron

    Cameron Member

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    Ordering gonna give an ounce a try thanks exactly the right extract
     
  9. Cameron

    Cameron Member

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    Are you taking the 250mgs three times a day or a gram to gram and a half??
     
  10. OP
    haidut

    haidut Member

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    I am taking 750mg once daily.
     
  11. Cameron

    Cameron Member

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    Non aromitazing dhea sounds pretty androgenic right there. Are you still using Androsterone?
     
  12. Cameron

    Cameron Member

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    Non aromitazing dhea sounds pretty androgenic right there. Are you still using Androsterone?
     
  13. OP
    haidut

    haidut Member

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    From time to time, as needed. For the next month I want to try only TT and see if changes cortisol, androgens, and prolactin.
     
  14. Cameron

    Cameron Member

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    Is there a human dht study on tt or just primates couldn't find much on humans and what dht increase there was unless I've overlooked something
     
  15. OP
    haidut

    haidut Member

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    There are several, but most of them published in Bulgarian, Iranian, Indian or Chinese journals. Here is one published in a better known Western journal.
    Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men. - PubMed - NCBI

    That study above is whack though. It considered a 3-fold increase in DHEA and a drop of prolactin from 17 down to 7 to be both non-significant, which is impossible to take seriously! Anybody who experiences such dramatic improvements in DHEA and prolactin will just laugh at the notion of the P-value and statistics.

    @Wagner83 - have you seen this study?

    I am starting to suspect that many TT studies in Western journals are purposefully mis-reported or designed in a way to show no effect from TT. A powerful OTC cortisol blocker that can treat hypogonadism, depression and obesity could decimate drug sales. Since cortisol is often a cause of female hypogonadism as well, the threat to Big Pharma from such a cheap herbal tonic with no known serious side effects ([406 cases of angina pectoris in coronary heart disease treated with saponin of Tribulus terrestris]. - PubMed - NCBI) cannot be overstated.
    tribulus_effects_human_males.png
     
  16. Cameron

    Cameron Member

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    That's increadible especially knowing the mechanism of action that results like that are being down played as insignificant
     
  17. OP
    haidut

    haidut Member

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    Btw, the dose in that study was quite modest. The men took 250mg x 3 daily. The extract had about 15% PTD, whch amounted to about 112.5mg PDT daily. Many commercial extracts provide that much PTD in a single tablet of 250mg, so it should be very easy and cheap to replicate the study design.

    "...All participating men underwent an initial evaluation (Day 0) then started treatment with TT extract in the form of a commercially prepared pill (Androsten® [Herbarium Laboratório Botânico Ltda., Brazil]). Each pill contained 250 mg of extract, including 37.5 mg (15%) of steroidal saponins (protodioscin), according to the manufacturer. Starting on Day 1, the men were instructed to take one pill orally every 8 hr, thus providing 112.5 mg of protodioscin per day."

    Here are other human studies that also found increases in androgens as a result of TT supplementation.
    Tribulus terrestris versus placebo in the treatment of erectile dysfunction and lower urinary tract symptoms in patients with late-onset hypogonadi... - PubMed - NCBI
    Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men. - PubMed - NCBI
    Pilot Study on the Effect of Botanical Medicine (Tribulus terrestris) on Serum Testosterone Level and Erectile Function in Aging Males With Partial... - PubMed - NCBI
    http://www.tribumen.lt/assets/Pdf/K...tris-L-improves-the-male-sexual-functions.doc
    The influence of the Tribulus terrestris extract on the parameters of the functional preparedness and athletes' organism homeostasis. - PubMed - NCBI
    Efficacy of Tribulus Terrestris for the treatment of premenopausal women with hypoactive sexual desire disorder: a randomized double-blinded, place... - PubMed - NCBI
    Efficacy of Tribulus terrestris for the treatment of hypoactive sexual desire disorder in postmenopausal women: a randomized, double-blinded, place... - PubMed - NCBI
     
  18. aguilaroja

    aguilaroja Member

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    Agreed @haidut that some findings, esp. DHEA and prolactin changes, were quite notable. It's hard to read between and outside the lines of the provided data. The standard deviations and ranges were high. The study was done at a private infertility clinic. In such settings, data analysis resources may have been limited. Maybe number crunching just brought judgements about "statistical" "significance".

    Even doing their best, other factors may have figured in: subjects taking different amounts of Tribulus than directed, subjects doing other maneuvers, clinical staff less familiar with research protocol.... Lacking full data set, it is hard to guess how numbers were skewed, how outlier findings were interpreted, and so on. It could be that, as a fertility clinic using assisted reproduction, the improvement in sperm count and motility was the main focus.

    With dramatic responses seen, a well capitalized institution would be doing extended studies. The major prolactin drop happened in less than 28 days. What if it really happened much faster?
     
  19. paymanz

    paymanz Member

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    I see , i think ingesting powder in capsules probably also has persorption risk.
     
  20. rei

    rei Member

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    What is your opinion on Iron Maxx Tribulus Terrestris Ultra Strong? This is the only sanely priced product available locally, worth a try or is 1600mg way too much extract in one tablet?
     
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