1-Androsterone DSHEA Information

Author: Proprietary Wellness LLC

We contend that 1-dehydroepiandrosterone (1-DHEA) is legal to sell under US law as a dietary supplement and that is it totally naturally occurring and in the food supply as an article used for food, where that article has not been chemically altered. It is a metabolite of naturally occurring products in addition to being in the food supply as an article used for food itself. It is a naturally occurring dietary ingredient and a metabolite of existing known dietary ingredients. It is present in the food supply as food in bovine tissue, via the natural conversion process of 1-Androstenediol which was found endogenously in pork tissue (1) and also as a metabolite of human metabolism(10).

5alpha-androst-1-ene-3beta,17beta-diol has been shown in the literature to naturally occur in Pig adipose tissue and was widely accepted to be a dietary substance (1). Additionally, 1-DHEA is a natural metabolite of 1,4 Androstadiene-3,17-dione via the 5aReductase enzyme. 1,4 Androstadiene-3,17-dione has been proven in countless papers to appear naturally in bovine tissue and has been on the US market since 2001 as a dietary supplement. Several papers have confirmed the endogenous production of boldenone and boldione in mammals with numerous theories of how the animal creates this hormone (16,17) 17a-Boldenone was found in untreated animals further confirming the presence of endogenous 1,4 androstadienes (17). This is consistent with the findings of Velle, that ruminants excrete most of their steroidal agents into the feces and in the 17a configuration(18). This all supports the conclusion that cattle and pigs can produce androstadiene steroids from a variety of sources (19). Via 5aReductase, and 3b-Hydroxysteroid dehydrogenase, both plentiful in the bodies of pigs and cattle, 1,4 Androstadiene-3,17-dione can be converted to 1-DHEA in the body of both the bovine and pig. The human body has also been shown to produce 1-ene hormones from exogenous sources such as DHEA supplementation(15). As shown, exogenous hormone administration can yield 1-ENE metabolites (14) which further supports the position that 1-ene hormones are byproducts of mammalian metabolism of which 1-DHEA is included.

According to DSHEA, a metabolite of a dietary ingredient is therefore allowed under DHSEA regulations and tissue concentrations and extracts are and have been used for thousands of years to promote health and vitality along with extractions of food born supplements. 1-ene hormones have been shown to occur in humans, pigs and other species and 1-DHEA is a natural metabolite of those hormones(1,9,10,11,12,13,14,21). Specifically 1-DHEA is a metabolite of 5alpha-androst-1-ene-3beta,17beta-diol by virtue of the action of 17-beta hydroxysteroid dehydrogenase which has been shown to be present in pigs (2,3) and also a metabolite of 1,4 Androstadiene-3,17-dione via 5aReductase and 3a/b hydroxysteroid dehydrogenase. This product is not intended to treat or cure any disease, but it can be used to augment hormone levels in men wishing to increase their levels. Both beef and pig flesh are articles that are sold as food and are in the food supply. Recently their hormone levels have been shown to influence excretion ratios of natural hormones in humans(15) showing potential activity as a nutritional supplement.

Structure

Routes of Metabolic Formation

This section explains the conversion process that occurs in mammals via Hydroxysteroid-dehydrogenases to verify that indeed 1-Androstenediol can convert into 1-DehydroEpiAndrosterone (better known as 1-DHEA). Hydroxysteroid dehydrogenases are known to be bi-directional and this paper shows just one example (which exactly parallels the 1-ene system). This process is known to happen in isomers and utilizing the same enzymatic systems in humans and pigs to bi-directionally convert adrenal steroids to active androgens via this pathway:

This bi-directional nature of 17bHSD type 4 can be verified in the attached paper from which this excerpt was taken(20).

“The activity of 17b-HSD is in fact responsible for the interconversion of 17-ketosteroids (e.g., dehydroepiandrosterone, androstenedione, and estrone) with the corresponding 17b-hydroxysteroids (e.g., androst-5-ene-313,17b-diol, testosterone, and 17b-estradiol). The reduction step catalyzed by the various 17b-HSDs is thus essential for the formation of the active estrogens, 17b-estradiol (E2) and androst-ene-3b,17b-diol (5-diol), as well as for the biosynthesis of the active androgen testosterone, and the oxidative reaction catalyzed by other 17b-HSDs inactivates the potent sex steroids into compounds having no or low biological activity. 17b-HSD is thus the key enzyme involved in the development, growth, and function of all reproductive tissues in both males and females.”

“and type 4, 17b-HSD mainly degrades 17b-estradiol into estrone and androst-5-ene-3b, 17b-diol into dehydroepiandrosterone.”

“The human type 4 17b-HSD is a 736-amino acid protein of MW 80 kDa that shares 84% identity with the corresponding porcine enzyme and transforms E2 into El and 5-diol into DHEA.”

The presence of a precursor to 1-DHEA in porcine tissues as well as the necessary metabolic enzyme systems protects 1-DHEA as a nutritional supplement. ‘

Safety of the ingredient

Using 5-DHEA as a model, we expect the exogenous use of 1-DHEA to be extremely safe, since 1-DHEA would have many improvements in safety over standard 5-DHEA which can be found at thousands of nutrition stores across the country. 5-DHEA has a long history of use in healthy and dieased humans and has been shown to be safe in doses up to 200 mg per day for 24 weeks (22) and 2250 mg for 16 weeks (23) with minimal side effects. The side effects that are encountered are due, in large part to the formation of estrogen and potent 5-alpha reduced metabolites (24,22). DHEA has been shown in the literature to convert via the aromatase enzyme to estrogens (25) which would not happen with the 1-DHEA isomer, vastly increasing it’s safety profile.

References

  1. McGregor SJ, Erickson AJ. Identification of 5alpha-androst-1-ene-3beta,17beta-diol in the fat of Sus scrofa L.: a "nutritional supplement" not found previously in the food supply. J Nat Prod. 2003 Sep;66(9):1147-8.
  2. Ohno S, Nakajima Y, Nakajin S. Triphenyltin and Tributyltin inhibit pig testicular 17beta-hydroxysteroid dehydrogenase activity and suppress testicular testosterone biosynthesis. Steroids. 2005 Aug;70(9):645-51.
  3. Chen G, Bourneuf E, Marklund S, Zamaratskaia G, Madej A, Lundström K. Gene expression of 3beta-hydroxysteroid dehydrogenase and 17beta-hydroxysteroid dehydrogenase in relation to androstenone, testosterone, and estrone sulphate in gonadally intact male and castrated pigs. J Anim Sci. 2007 Oct;85(10):2457-63.
  4. Chang DM, Lan JL, Lin HY, Luo SF. Dehydroepiandrosterone treatment of women with mild-to-moderate systemic lupus erythematosus: a multicenter randomized, double-blind, placebo-controlled trial. Arthritis Rheum. Nov;46(11):2924-7, 2002
  5. Dyner TS, Lang W, Geaga J, Golub A, Stites D, Winger E, Galmarini M, Masterson J, Jacobson MA. An open-label dose-escalation trial of oral dehydroepiandrosterone tolerance and pharmacokinetics in patients with HIV disease. J Acquir Immune Defic Syndr. May;6(5):459-65, 1993
  6. Gilad S, Chayen R, Tordjman K, Kisch E, Stern N. Assessment of 5 alpha-reductase activity in hirsute women: comparison of serum androstanediol glucuronide with urinary androsterone and aetiocholanolone excretion. Clin Endocrinol (Oxf). Apr;40(4):459-64, 1994
  7. Acacio BD, Stanczyk FZ, Mullin P, Saadat P, Jafarian N, Sokol RZ. Pharmacokinetics of dehydroepiandrosterone and its metabolites after long-term daily oral administration to healthy young men. Fertil Steril. Mar;81(3):595-604, 2004
  8. Longcope C, Bourget C, Flood C. The production and aromatization of dehydroepiandrosterone in post-menopausal women. Maturitas. Dec;4(4):325-32, 1982
  9. Counsel et al., “Anabolic Agents. Derivatives of 5alpha-Androst-1-ene”, J. Org. Chem., 27 (1962), 248-251
  10. Galletti and Gardi, “Metabolism of 1-Dehydroandrostanes in Man”, J Steroid Biochem, 3 (1972), 933-936
  11. Langecker, “Beziehungen Zwischen Substitution im Ring A und Abbau im Stoffwechsel bei Verwandten des Testosterons”, Acta Endocrin, 41 (1962), 494-506
  12. Lieberman et al., J. Biol. Chem, 182 (1950), 299
  13. Galletti and Gardi, “Metabolism of 1-Dehydroandrostanes in Man”, J Steroid Biochem, 3 (1972), 933-936
  14. Kohler M, Parr MK, Opfermann G Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites. Institute of Biochemistry, German Sport University of Cologne, Carl-Diem-Weg 6, 50933 Cologne, Germany. maxie@biochem.dshs-koeln.de
  15. Le Bizec B, Gaudin I, Monteau F, Andre F, Impens S, De Wasch K, De Brabander H Consequence of boar edible tissue consumption on urinary profiles of nandrolone metabolites. I. Mass spectrometric detection and quantification of 19-norandrosterone and 19-noretiocholanolone in human urine. Rapid Commun Mass Spectrom. 2000;14(12):1058-65.
  16. De Brabander, H. F., S. Poelmans, R. Schilt, R. W. Stephanyl, B. Le Bizec, R. Draisci, S. S. Sterk, L. A. van Glink, D. Courtheyn, N. van Hook, A. Macri, K. De Wasch (2004) Presence and metabolism of the anabolic steroid boldenone in various animal species: A review. Food Additives and Contaminants 21(6):515-525.
  17. Le Bizec, B, F. Courant, I. Gaudin, E. Bichon, B. Destrez, R. Schildt, R. Draisci, F. Monteau, F. Andre (2006) Criteria to distingush between natural situations and illegal use of boldenone, boldenone esters and boldione in cattle 1. Metabolite profiles of boldenone, boldenone esters and boldione in cattle urine. Steroids 71:1078-1087.
  18. 1.Velle W. Endogenous anabolic agents in farm animals. Environ Qual Saf Suppl. 1976;(5):159-70.
  19. Poelmans S, De Wasch K, Noppe H, Van Hoof N, Van Cruchten S, Le Bizec B, Deceuninck Y, Sterk S, Van Rossum HJ, Hoffman MK, De Brabander HF. Food Addit Contam. 2005 Sep;22(9):808-15. Links Endogenous occurrence of some anabolic steroids in swine matrices.
  20. Fernand Labrie, Van Luu-The, Sheng-Xiang Lin, Claude Labrie, Jacques Simard, Roch Breton, and Alain BrlangerMRC Group in Molecular Endocrinology, CHUL Research Center and Laval University, Ste-Foy, QuObec, Canada The key role of 17b -hydroxysteroid dehydrogenases in sex steroid biology
  21. Lieberman Seymore, Fukushima David, Sloan Kettering Institute For Cancer Research, August 29, 1949 Studies In Steroid Metabolism: Identification and Characterization of Ketosteroids Isolated From Urine of Healthy and Diseased Persons
  22. Chang DM, Lan JL, Lin HY, Luo SF. Dehydroepiandrosterone treatment of women with mild-to-moderate systemic lupus erythematosus: a multicenter randomized, double-blind, placebo-controlled trial. Arthritis Rheum. Nov;46(11):2924-7, 2002
  23. Dyner TS, Lang W, Geaga J, Golub A, Stites D, Winger E, Galmarini M, Masterson J, Jacobson MA. An open-label dose-escalation trial of oral dehydroepiandrosterone tolerance and pharmacokinetics in patients with HIV disease. J Acquir Immune Defic Syndr. May;6(5):459-65, 1993
  24. Gilad S, Chayen R, Tordjman K, Kisch E, Stern N. Assessment of 5 alpha-reductase activity in hirsute women: comparison of serum androstanediol glucuronide with urinary androsterone and aetiocholanolone excretion. Clin Endocrinol (Oxf). Apr;40(4):459-64, 1994
  25. Longcope C, Bourget C, Flood C. The production and aromatization of dehydroepiandrosterone in post-menopausal women. Maturitas. Dec;4(4):325-32, 1982

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