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Published in: Journal of the International Society of Sports Nutrition 1/2007

Open Access 01-12-2007 | Research article

Effects of eight weeks of an alleged aromatase inhibiting nutritional supplement 6-OXO (androst-4-ene-3,6,17-trione) on serum hormone profiles and clinical safety markers in resistance-trained, eugonadal males

Authors: Dan Rohle, Colin Wilborn, Lem Taylor, Chris Mulligan, Richard Kreider, Darryn Willoughby

Published in: Journal of the International Society of Sports Nutrition | Issue 1/2007

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Abstract

The purpose of this study was to determine the effects of 6-OXO, a purported nutritional aromatase inhibitor, in a dose dependent manner on body composition, serum hormone levels, and clinical safety markers in resistance trained males. Sixteen males were supplemented with either 300 mg or 600 mg of 6-OXO in a double-blind manner for eight weeks. Blood and urine samples were obtained at weeks 0, 1, 3, 8, and 11 (after a 3-week washout period). Blood samples were analyzed for total testosterone (TT), free testosterone (FT), dihydrotestosterone (DHT), estradiol, estriol, estrone, SHBG, leutinizing hormone (LH), follicle stimulating hormone (FSH), growth hormone (GH), cortisol, FT/estradiol (T/E). Blood and urine were also analyzed for clinical chemistry markers. Data were analyzed with two-way MANOVA. For all of the serum hormones, there were no significant differences between groups (p > 0.05). Compared to baseline, free testosterone underwent overall increases of 90% for 300 mg 6-OXO and 84% for 600 mg, respectively (p < 0.05). DHT underwent significant overall increases (p < 0.05) of 192% and 265% with 300 mg and 600 mg, respectively. T/E increased 53% and 67% for 300 mg and 600 mg 6-OXO, respectively. For estrone, 300 mg produced an overall increase of 22%, whereas 600 mg caused a 52% increase (p < 0.05). Body composition did not change with supplementation (p > 0.05) and clinical safety markers were not adversely affected with ingestion of either supplement dose (p > 0.05). While neither of the 6-OXO dosages appears to have any negative effects on clinical chemistry markers, supplementation at a daily dosage of 300 mg and 600 mg for eight weeks did not completely inhibit aromatase activity, yet significantly increased FT, DHT, and T/E.
Literature
1.
go back to reference Bhasin S, Storer T, Berman N, Yarasheski K, Clevenger B, Phillips J, Lee W, Bunnell T, Casaburi R: Testosterone replacement increases fat-free mass and muscle size in hypogonadal men. J Clin Endocrinol Metab. 1997, 82: 407-13. 10.1210/jc.82.2.407.PubMed Bhasin S, Storer T, Berman N, Yarasheski K, Clevenger B, Phillips J, Lee W, Bunnell T, Casaburi R: Testosterone replacement increases fat-free mass and muscle size in hypogonadal men. J Clin Endocrinol Metab. 1997, 82: 407-13. 10.1210/jc.82.2.407.PubMed
2.
go back to reference Bhasin S, Storer T, Javanbakht M, Berman N, Yarasheski K, Phillips J, Dike M, Sinha-Hikim I, Shen R, Hays R, Beall G: Testosterone replacement and resistance exercise in HIV-infected men with weight loss and low testosterone levels. JAMA. 2000, 283: 763-70. 10.1001/jama.283.6.763.PubMedCentralCrossRefPubMed Bhasin S, Storer T, Javanbakht M, Berman N, Yarasheski K, Phillips J, Dike M, Sinha-Hikim I, Shen R, Hays R, Beall G: Testosterone replacement and resistance exercise in HIV-infected men with weight loss and low testosterone levels. JAMA. 2000, 283: 763-70. 10.1001/jama.283.6.763.PubMedCentralCrossRefPubMed
3.
go back to reference Bhasin S, Woodhouse L, Casaburi R, Singh A, Bhasin D, Berman Chen X, Yarasheski K, Magliano L, Dzekov C, Dzekov J, Bross R, Phillips J, Sinha-Hikim I, Shen R, Storer T: Testosterone dose-response relationships in healthy young men. Am J Physiol Endocrinol Metab. 2001, 281: E1172-81.PubMed Bhasin S, Woodhouse L, Casaburi R, Singh A, Bhasin D, Berman Chen X, Yarasheski K, Magliano L, Dzekov C, Dzekov J, Bross R, Phillips J, Sinha-Hikim I, Shen R, Storer T: Testosterone dose-response relationships in healthy young men. Am J Physiol Endocrinol Metab. 2001, 281: E1172-81.PubMed
4.
go back to reference Bhasin S, Woodhouse L, Storer T: Proof of the effect of testosterone on skeletal muscle. J Endocrinol. 2001, 170: 27-38. 10.1677/joe.0.1700027.CrossRefPubMed Bhasin S, Woodhouse L, Storer T: Proof of the effect of testosterone on skeletal muscle. J Endocrinol. 2001, 170: 27-38. 10.1677/joe.0.1700027.CrossRefPubMed
5.
go back to reference Sinha-Hikim I, Artaza J, Woodhouse L, Gonzalez-Cadavid N, Singh A, Lee M, Storer T, Casaburi R, Shen R, Bhasin S: Testosterone-induced increase in muscle size in healthy young men is associated with muscle fiber hypertrophy. Am J Physiol Endocrinol Metab. 2002, 283 (1): E154-E164.CrossRefPubMed Sinha-Hikim I, Artaza J, Woodhouse L, Gonzalez-Cadavid N, Singh A, Lee M, Storer T, Casaburi R, Shen R, Bhasin S: Testosterone-induced increase in muscle size in healthy young men is associated with muscle fiber hypertrophy. Am J Physiol Endocrinol Metab. 2002, 283 (1): E154-E164.CrossRefPubMed
6.
go back to reference Sinha-Hikim I, Roth S, Lee M, Bhasin S: Testosterone-induced muscle hypertrophy is associated with an increase in satellite cell number in healthy, young men. Am J Physiol Endocrinol Metab. 2003, 285: E197-E205.CrossRefPubMed Sinha-Hikim I, Roth S, Lee M, Bhasin S: Testosterone-induced muscle hypertrophy is associated with an increase in satellite cell number in healthy, young men. Am J Physiol Endocrinol Metab. 2003, 285: E197-E205.CrossRefPubMed
7.
go back to reference Schroeder E, Terk M, Sattler F: Androgen therapy improves muscle mass and strength but not muscle quality: results from two studies. Am J Physiol Endocrinol Metab. 2003, 285: E16-24.CrossRefPubMed Schroeder E, Terk M, Sattler F: Androgen therapy improves muscle mass and strength but not muscle quality: results from two studies. Am J Physiol Endocrinol Metab. 2003, 285: E16-24.CrossRefPubMed
8.
go back to reference Brown G, Martini E, Roberts S, Vukovich M, King D: Acute hormonal response to sublingual androstenediol intake in young men. J Appl Physiol. 2002, 92: 142-46.CrossRefPubMed Brown G, Martini E, Roberts S, Vukovich M, King D: Acute hormonal response to sublingual androstenediol intake in young men. J Appl Physiol. 2002, 92: 142-46.CrossRefPubMed
9.
go back to reference Brown G, McKenzie D: Acute resistance exercise does not change the hormonal response to sublingual androstenediol intake. Eur J Appl Physiol. 2006, 97: 404-12. 10.1007/s00421-006-0194-9.CrossRefPubMed Brown G, McKenzie D: Acute resistance exercise does not change the hormonal response to sublingual androstenediol intake. Eur J Appl Physiol. 2006, 97: 404-12. 10.1007/s00421-006-0194-9.CrossRefPubMed
10.
go back to reference Broeder C, Quindry J, Brittingham K, Panton L, Thomson J, Appakondu S: Physiological and hormonal influences on androstenedione supplementation in men 35 to 65 years old participating in a high-intensity resistance training program. Arch Intern Med. 2000, 160: 3093-104. 10.1001/archinte.160.20.3093.CrossRefPubMed Broeder C, Quindry J, Brittingham K, Panton L, Thomson J, Appakondu S: Physiological and hormonal influences on androstenedione supplementation in men 35 to 65 years old participating in a high-intensity resistance training program. Arch Intern Med. 2000, 160: 3093-104. 10.1001/archinte.160.20.3093.CrossRefPubMed
11.
go back to reference King D, Sharp R, Vukovich M, Brown G, Reifenrath T, Uhl N, Parsons K: Effect of oral androstenedione on serum testosterone and adaptations to resistance training in young men. JAMA. 1999, 281: 2020-28. 10.1001/jama.281.21.2020.CrossRefPubMed King D, Sharp R, Vukovich M, Brown G, Reifenrath T, Uhl N, Parsons K: Effect of oral androstenedione on serum testosterone and adaptations to resistance training in young men. JAMA. 1999, 281: 2020-28. 10.1001/jama.281.21.2020.CrossRefPubMed
12.
go back to reference Beckham S, Earnest C: Four weeks of androstenedione supplementation diminishes the treatment response in middle aged men. Br J Sports Med. 2003, 37: 212-18. 10.1136/bjsm.37.3.212.PubMedCentralCrossRefPubMed Beckham S, Earnest C: Four weeks of androstenedione supplementation diminishes the treatment response in middle aged men. Br J Sports Med. 2003, 37: 212-18. 10.1136/bjsm.37.3.212.PubMedCentralCrossRefPubMed
13.
go back to reference Mauras N, O'Brien K, Klein K, Hayes V: Estrogen suppression in males: metabolic effects. J Clin Endocrinol Metab. 2000, 85: 2370-77. 10.1210/jc.85.7.2370.PubMed Mauras N, O'Brien K, Klein K, Hayes V: Estrogen suppression in males: metabolic effects. J Clin Endocrinol Metab. 2000, 85: 2370-77. 10.1210/jc.85.7.2370.PubMed
14.
go back to reference Mauras N, Lima J, Patel D, Rini A, diSalle E, Kwok A, Lippe B: Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. J Clin Endocrinol Metab. 2003, 88: 5951-56. 10.1210/jc.2003-031279.CrossRefPubMed Mauras N, Lima J, Patel D, Rini A, diSalle E, Kwok A, Lippe B: Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. J Clin Endocrinol Metab. 2003, 88: 5951-56. 10.1210/jc.2003-031279.CrossRefPubMed
15.
go back to reference Taxel P, Kennedy D, Fall P, Willard A, Clive J, Raisz L: The effect of aromatase inhibition on sex steroids, gonadotropins, and markers of bone turnover in older men. J Clin Endocrinol Metab. 2001, 86: 2869-74. 10.1210/jc.86.6.2869.PubMed Taxel P, Kennedy D, Fall P, Willard A, Clive J, Raisz L: The effect of aromatase inhibition on sex steroids, gonadotropins, and markers of bone turnover in older men. J Clin Endocrinol Metab. 2001, 86: 2869-74. 10.1210/jc.86.6.2869.PubMed
16.
go back to reference Willoughby D, Wilborn C, Taylor L, Campbell B: Eight weeks of aromatase inhibition using the nutritional supplement Novedex XT: Effects on steroid hormones, body composition, and clinical safety markers in young, eugonadal men. Int J Sport Nutr Exerc Metab. 2007, 17 (1): 92-108.PubMed Willoughby D, Wilborn C, Taylor L, Campbell B: Eight weeks of aromatase inhibition using the nutritional supplement Novedex XT: Effects on steroid hormones, body composition, and clinical safety markers in young, eugonadal men. Int J Sport Nutr Exerc Metab. 2007, 17 (1): 92-108.PubMed
17.
go back to reference Numazawa M, Tsuji M, Mutsumi A: Studies on aromatase inhibition with 4-androstene-3,6,17-trione: its 3 beta-reduction and time-dependent irreversible binding to aromatase with human placental microsomes. J Steroid Biochem. 1997, 28: 337-44. 10.1016/0022-4731(87)91028-4.CrossRef Numazawa M, Tsuji M, Mutsumi A: Studies on aromatase inhibition with 4-androstene-3,6,17-trione: its 3 beta-reduction and time-dependent irreversible binding to aromatase with human placental microsomes. J Steroid Biochem. 1997, 28: 337-44. 10.1016/0022-4731(87)91028-4.CrossRef
18.
go back to reference Numazawa M, Mutsumi A, Tachibana M: Mechanism for aromatase inactivation by a suicide substrate, androst-4-ene-3,6,17-trione. The 4 beta, 5 beta-epoxy-19-oxo derivative as a reactive electrophile irreversibly binding to the active site. Biochem Pharmacol. 1996, 52: 1253-59. 10.1016/0006-2952(96)00479-0.CrossRefPubMed Numazawa M, Mutsumi A, Tachibana M: Mechanism for aromatase inactivation by a suicide substrate, androst-4-ene-3,6,17-trione. The 4 beta, 5 beta-epoxy-19-oxo derivative as a reactive electrophile irreversibly binding to the active site. Biochem Pharmacol. 1996, 52: 1253-59. 10.1016/0006-2952(96)00479-0.CrossRefPubMed
19.
go back to reference Leder B, Rohrer J, Rubin S, Gallo J, Longcope C: Effects of aromatase inhibition in elderly men with low or borderline-low serum testosterone levels. J Clin Endocrinol Metab. 2004, 89: 1174-80. 10.1210/jc.2003-031467.CrossRefPubMed Leder B, Rohrer J, Rubin S, Gallo J, Longcope C: Effects of aromatase inhibition in elderly men with low or borderline-low serum testosterone levels. J Clin Endocrinol Metab. 2004, 89: 1174-80. 10.1210/jc.2003-031467.CrossRefPubMed
20.
go back to reference O'Connor K, Stip E, Pélissier M, Aardema F, Guay S, Guadette M, Van Haaster I, Robillard S, Grenier S, Careau Y, Doucet P, Leblanc V: Treating delusional disorder: a comparison of cognitive-behavioural therapy and attention placebo control. Can J Psychiatry. 2007, 52 (3): 182-190.PubMed O'Connor K, Stip E, Pélissier M, Aardema F, Guay S, Guadette M, Van Haaster I, Robillard S, Grenier S, Careau Y, Doucet P, Leblanc V: Treating delusional disorder: a comparison of cognitive-behavioural therapy and attention placebo control. Can J Psychiatry. 2007, 52 (3): 182-190.PubMed
21.
go back to reference Hossian A, Hornick C: Androgenic modulation of lipid metabolism at subcellular sties in cholestatic rats. Horm Metab Res. 1994, 26: 19-25.CrossRef Hossian A, Hornick C: Androgenic modulation of lipid metabolism at subcellular sties in cholestatic rats. Horm Metab Res. 1994, 26: 19-25.CrossRef
22.
go back to reference Mauras N, Rini A, Welch S, Sager B, Murphy SP: Synergistic effects of testosterone and growth hormone on protein metabolism and body composition in prepubertal boys. Metabolism. 2003, 52 (8): 964-969. 10.1016/S0026-0495(03)00163-X.CrossRefPubMed Mauras N, Rini A, Welch S, Sager B, Murphy SP: Synergistic effects of testosterone and growth hormone on protein metabolism and body composition in prepubertal boys. Metabolism. 2003, 52 (8): 964-969. 10.1016/S0026-0495(03)00163-X.CrossRefPubMed
23.
go back to reference Harden C, MacLusky N: Aromatase inhibition, testosterone, and seizures. Epilepsy Behav. 2004, 5: 260-63. 10.1016/j.yebeh.2003.12.001.CrossRefPubMed Harden C, MacLusky N: Aromatase inhibition, testosterone, and seizures. Epilepsy Behav. 2004, 5: 260-63. 10.1016/j.yebeh.2003.12.001.CrossRefPubMed
24.
go back to reference Incledon T: The chronic effects of androst-4-ene-3,6,17-trione on endocrine responses in resistance-trained men. Unpublished observations. 2003 Incledon T: The chronic effects of androst-4-ene-3,6,17-trione on endocrine responses in resistance-trained men. Unpublished observations. 2003
25.
go back to reference Meinhardt U, Mullis P: The aromatase cytochrome P-450 and its clinical impact. Horm Res. 2002, 57: 145-52. 10.1159/000058374.CrossRefPubMed Meinhardt U, Mullis P: The aromatase cytochrome P-450 and its clinical impact. Horm Res. 2002, 57: 145-52. 10.1159/000058374.CrossRefPubMed
26.
go back to reference Hayes F, Seminara S, Decruz S, Boepple P, Crowley W: Aromatase inhibition in the human male reveals a hypothalamic site of estrogen feedback. J Clin Endocrinob Metab. 2000, 85: 3027-35. 10.1210/jc.85.9.3027. Hayes F, Seminara S, Decruz S, Boepple P, Crowley W: Aromatase inhibition in the human male reveals a hypothalamic site of estrogen feedback. J Clin Endocrinob Metab. 2000, 85: 3027-35. 10.1210/jc.85.9.3027.
27.
go back to reference Schnorr J, Bray M, Veldhuis J: Aromatization mediates testosterone's short-term feedback restraint of 24-hour endogenously driven and acute exogenous gonadotropin-releasing hormone-stimulated luteinizing hormone and follicle-stimulating hormone secretion in young men. J Clin Endocrinol Metab. 2001, 86: 2600-06. 10.1210/jc.86.6.2600.PubMed Schnorr J, Bray M, Veldhuis J: Aromatization mediates testosterone's short-term feedback restraint of 24-hour endogenously driven and acute exogenous gonadotropin-releasing hormone-stimulated luteinizing hormone and follicle-stimulating hormone secretion in young men. J Clin Endocrinol Metab. 2001, 86: 2600-06. 10.1210/jc.86.6.2600.PubMed
Metadata
Title
Effects of eight weeks of an alleged aromatase inhibiting nutritional supplement 6-OXO (androst-4-ene-3,6,17-trione) on serum hormone profiles and clinical safety markers in resistance-trained, eugonadal males
Authors
Dan Rohle
Colin Wilborn
Lem Taylor
Chris Mulligan
Richard Kreider
Darryn Willoughby
Publication date
01-12-2007
Publisher
BioMed Central
DOI
https://doi.org/10.1186/1550-2783-4-13

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