Written by Victor R. Prisk, M.D.
Boosting Testosterone
Four Ways to Get Huge Faster
Muscular Development is always on the cutting edge when it comes to performance enhancement. Now you have the opportunity to learn the truth about how some of the greats built their massive physiques. It is no surprise that this involved “supplementation” with testosterone and its anabolic counterparts. Whether they’re used legally or under-the-table, these compounds are commonplace in professional sports arenas.
I’d like to review the stacking options from the “natural” side of things. Stacks often include testosterone-boosting agents, estrogen-limiting agents, GH/IGF axis boosters and insulin sensitizers. In the following subsets, I will present to you the “natural stack” with the most scientific promise to achieve the physiologic optimization of your anabolic potential.
1) Testosterone Booster:
Eurycoma longifolia (Tongkat Ali, TA)
The bioactive compound eurycomanone has been shown to increase testosterone levels and sperm production in animal models.5 TA extracts work via a few mechanisms.5 One is by enhancing the enzymes that produce DHEA, a precursor of testosterone. More interestingly, eurycomanone appears to act as an aromatase inhibitor, thus preventing the conversion of testosterone to estrogen.6 This action also reduces feedback on the pituitary by estrogen, in turn raising luteinizing hormone (LH) production to boost testosterone levels.5
Studies in humans have demonstrated a performance-enhancing effect of 100 milligrams of an aqueous extract of TA in both men and women, increasing strength and muscle circumference.5 Treatment with 400 milligrams of TA extract for five weeks resulted in significant increases in total and free testosterone concentrations and muscular force in senior-aged men.7
2) Estrogen/DHT Blockers:
Androsta-3,5-diene-7,17-dione (AD)
AD is a metabolite of 7-Keto DHEA. Although DHEA and 7-Keto DHEA do not seem to result in significant androgenic effects, AD appears to act as an aromatase inhibitor and is marketed as an estrogen blocker. Laboratory studies suggest that androgens may act as aromatase inhibitors.8 Caution: even though this is a derivative of the relatively safe DHEA and 7-Keto DHEA, studies in humans are scarce.
Astaxanthin + Saw Palmetto
This is an herbal combination that inhibits the enzyme reductase (converts testosterone to DHT, or dihydrotestosterone) and aromatase. In one study, this supplement produced increases in serum testosterone levels up to 60 percent while decreasing estrogen and DHT.9 Doses of 800 milligrams and 2,000 milligrams were shown to equally raise testosterone levels, while the 2,000-milligram dose suppressed estrogen levels. A recent study has demonstrated that this combination of compounds decreases estrogen levels at a proprietary dosage of 1,200 milligrams per day.10 Caution: industry-sponsored studies could lead to bias.
3) GH/IGF-1 Boosters:
Ecdysterone (20-hydroxyecdysone, Ecdy)
Ecdy is an insect steroid that is marketed as a testosterone and performance-boosting supplement. Unfortunately, a human supplementation study in 2006 at a dose of 200 milligrams per day failed to show any improvements in body composition or training adaptations.11 However, more recent studies in animal models suggest otherwise. A study in rats recently suggested that Ecdy could boost muscle growth through increasing serum IGF-1 and decreasing estrogen levels.12 Further evaluation showed that Ecdy acted on a specific estrogen receptor on muscle cells in culture. This could mean that Ecdy would still activate estrogen-driven muscle growth while decreasing systemic estrogen levels.
Melatonin
Melatonin is a sleep aid that increases deep sleep onset. Growth hormone is released during deep sleep. IGF-1 is a hormone that is produced in response to growth hormone secretion, and is an important player in muscle anabolism.
A study by Oner et al. comparing supplementation of melatonin to supplementation of testosterone in rats produced fascinating results.13 Castrating rats induces muscle atrophy caused by a loss of the anabolic effect of testosterone produced by the testicles. In their study, the scientists found that melatonin supplementation increased soleus (calf) muscle weight and fiber diameter in castrated rats just as well as supplemental testosterone. The researchers noted that there was a strong IGF-1 presence within the melatonin-treated muscles. This study concluded that melatonin is as effective as testosterone in the prevention of muscle atrophy through action on the IGF-1 axis.
Furthermore, in a 2007 study, Willoughby and colleagues at Baylor University showed that single-dose melatonin supplementation could affect the GH/IGF-1 axis.14 In this study, a dose of five milligrams of melatonin significantly increased GH levels and lowered the competing hormone, somatostatin. Although IGF-1 levels were not affected, the levels of IGFBP-3 were increased in males. IGFBP-3, or insulin-like growth factor binding protein-3, is a binding protein that helps prolong the IGF-1 in the plasma. Melatonin has long been a mainstay in my evening supplement regimen.
4) Insulin Sensitizers:
Fenugreek (Trigonella foenum-graecum)
Fenugreek is known to have anti-diabetic properties and an ability to boost testosterone levels. It also contains an unusual amino acid, 4-hydroxyisoleucine, so far found only in fenugreek, which has anti-diabetic properties of enhancing insulin secretion and sensitivity under hyperglycemic conditions.15,16 Its ability to raise testosterone levels and improve insulin action explains its ability to produce an anabolic effect in humans and rats.16 In addition to doubling testosterone levels, fenugreek has even been shown at a dose of 500 milligrams to significantly impact both upper- and lower-body strength and body composition, compared to a placebo in a double-blind, controlled trial.17
Vitamin D
Vitamin D is a hormone made from cholesterol, just like testosterone. Vitamin D also turns on a nuclear receptor just like anabolic steroids. You must think of this “vitamin” as a vital hormone. Its function goes way beyond simply improving calcium absorption for healthy bones.
Multiple studies have shown how important vitamin D supplementation is for improving muscle strength, especially in vitamin D-deficient older individuals. Vitamin D levels in the blood have been correlated to muscle cell contractility, strength and postural stability. Vitamin D deficiency has also been correlated to insulin resistance and metabolic dysfunction. Supplementation with vitamin D3 at 1,000 to 2,000 IU per day may improve the actions of leucine and insulin in boosting muscle protein synthesis.18
Conclusion
There are a large number of testosterone-boosting supplements out there that count on the placebo effect in unsuspecting bodybuilders. The interesting thing about most of these herbal supplements is that they feel like they work. For instance, although the science is weak for Tribulus terrestris in producing increases in testosterone, it actually has beneficial effects in boosting sex drive and erectile function. Although it may not make your muscles harder, it makes you feel harder elsewhere. Just because a supplement acts as an aphrodisiac doesn’t mean it acts like testosterone in building muscle.
Dr. Victor Prisk is a board certified orthopaedic surgeon and IFBB professional bodybuilder in Pittsburgh, PA. Dr. Prisk is an active member of the GNC Medical Advisory Board and creator of the “G.A.I.N. Plan.” He is an NCAA All-American gymnast, champion swing dancer and NPC Welterweight National Champion.
References:
1. Amory JK, et al. Preoperative supraphysiological testosterone in older men undergoing knee replacement surgery. J Am Geriatr Soc 2002;Oct;50(10):1698-701.
2. Metcalfe D, et al. Anabolic steroids in patients undergoing total knee arthroplasty. BMJ Open 2012;Sep 22;2(5). pii: e001435.
3. Bhasin S, et al. Testosterone dose response relationships in healthy young men. Am J Physiol Endocrinol Metab 2001;281:E1172-E1181.
4. Sinha-Hikim I, et al. Testosterone-induced increase in muscle size in healthy young men is associated with muscle fiber hypertrophy. Am J Physiol Endocrinol Metab 2002;283:E154-E164.
5. George A, Henkel R. Phytoandrogenic properties of Eurycoma longifolia as natural alternative to testosterone replacement therapy. Andrologia 2014;Sep;46(7):708-21.
6. Low BS, et al. Eurycomanone, the major quassinoid in Eurycoma longifolia root extract increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis. J Ethnopharmacol 2013;Aug 26;149(1):201-7.
7. Henkel RR, et al. Tongkat Ali as a potential herbal supplement for physically active male and female seniors— a pilot study. Phytother Res 2014;Apr;28(4):544-50.
8. Nagaoka M, et al. Structure-activity relationships of 3-deoxy androgens as aromatase inhibitors. Synthesis and biochemical studies of 4-substituted 4-ene and 5-ene steroids. Steroids 2003;Aug;68(6):533-42.
9. Angwafor F, et al. An open label, dose response study to determine the effect of a dietary supplement on dihydrotestosterone, testosterone and estradiol levels in healthy males. J of the Int Soc of Sports Nutr 2008; 5:12.
10. Anderson ML. Evaluation of Resettin on serum hormone levels in sedentary males. J Int Soc Sports Nutr 2014;Aug 23;11:43.
11. Wilborn CD, et al. Effects of methoxyisoflavone, ecdysterone, and sulfo-polysaccharide supplementation on training adaptations in resistance-trained males. J Int Soc Sports Nutr 2006;Dec 13;3:19-27.
12. Parr MK, et al. Estrogen receptor beta is involved in skeletal muscle hypertrophy induced by the phytoecdysteroid ecdysterone. Mol Nutr Food Res 2014;Sep;58(9):1861-72.
13. Oner et al. Melatonin is as effective as testosterone in the prevention of soleus muscle atrophy induced by castration in rats. Anat Rec (Hoboken) 2008;Apr 291(4):448-55.
14. Nassar E et al. Effects of a single dose of N-Acetyl-5-methoxytryptamine (Melatonin) and resistance exercise on the growth hormone/IGF-1 axis in young males and females. J Int Soc Sports Nutr 2007;Oct 23 (4):14.
15. Haeri MR, et al. Non-insulin dependent anti-diabetic activity of (2S, 3R, 4S) 4-hydroxyisoleucine of fenugreek (Trigonella foenum graecum) in streptozotocin-induced type 1 diabetic rats. Phytomedicine 2012;May 15;19(7):571-4
16. Aswar U, et al. Effect of furostanol glycosides from Trigonella foenum-graecum on the reproductive system of male albino rats. Phytother Res 2010;Oct;24(10):1482-8.
17. Poole C, et al. The effects of a commercially available botanical supplement on strength, body composition, power output, and hormonal profiles in resistance-trained males. J Int Soc Sports Nutr 2010;Oct 27;7:34
18. Salles J, et al. 1,25(OH)2-vitamin D3 enhances the stimulating effect of leucine and insulin on protein synthesis rate through Akt/PKB and mTOR mediated pathway in murine C2C12 skeletal myotubes. Mol Nutr Food Res 2013;Dec;57(12):2137-46.
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