The Diagnosis and Treatment of Male Andropause in Your Practice – Part II

by Dr. Greg Fors, DC – Board Certified Neurologist DIBCN Posted On: 08/12/2011

In my previous article, ‘The Diagnosis and Treatment of Male Andropause in Your Practice – Part One’ I laid the foundation for the understanding and diagnosis of male Andropause. Please refer to part one for any clarification on symptomatology and diagnostic criteria in the treatment of this very common disorder. The primary symptoms of Male Andropause include increased abdominal fat, decreased muscle mass, irritability, depression, anxiety, difficulty concentrating, and decreased facial and leg hair. Recall that the underlying metabolic cause of this disorder in aging male patients is too little free testosterone and too much estrogen. Please refer to my first article for optimal laboratory levels when diagnosing and following appropriate treatment protocols.

Raising Testosterone Levels Naturally The best botanical agent known to raise testosterone levels in aging males is the plant known as Tribulus Terrestris, a flowering plant that grows throughout India, Pakistan and Sri Lanka. Indian Ayurvedic practice utilizes this plant as a primary male tonic. The key compounds found in Tribulus Terrestris are extracted from the aerial parts of the plant. The subsequent extract contains a whole host of phytoactive and phytodynamic ingredients, the most important being protodioscin and its related steroidal saponins.

Independent studies have shown that Tribulus Terrestris steroidal saponin extracts increase hormone levels, but not outside the normal range. These steroidal saponins increase testosterone levels by increasing Gonadotropin-Releasing Hormone (GnRH) production within the hypothalamus. This in turn stimulates the production of Luteinizing Hormone (LH) and Follicle-Stimulating hormone (FSH) in the anterior pituitary gland. In males, LH stimulates Leydig cell production of testosterone and FSH stimulates spermatogenesis in the testes. This regulatory system controlling testosterone is often referred to as the hypothalamic-pituitary-testicular axis.

Research has now established that the primary steroidal saponin in Tribulus Terrestris that creates these physiological effects is protodioscin. Protodioscin has been shown to directly elevate testosterone by increasing the production of LH(1) and by increasing testosterone precursors such as dehydroepiandrosterone(2) and dehydroepiandrosterone sulphate.(3) Unfortunately, most Tribulus based supplements contain none or only negligible amounts of this protodioscin, therefore, benefits to your patient are questionable. This is not the case if your Tribulus formula is standardized to contain a specific content of protodioscin of at least 10%. However, this is only half the problem; once testosterone has been elevated you must make certain that at least 2% consists of the free unbound form and isn’t converted to estrogen.

Keeping Testosterone Free An herbal extract known for its beneficial effect on free testosterone levels is nettle root; specifically, extracts of the species Urtica dioica containing active amounts of 3, 4-divanillyltetrahydrofuran. Nettle root research is now focusing on several in vivo pharmacological studies designed to determine the nature and extent of beneficial effects on testosterone. As previously discussed in part one, protein globulins like SHBG actively inhibit the level of free testosterone by binding to it and rendering it biologically inactive. This research has found that specific nettle root extracts have a greater affinity for SHBG than does testosterone.(4) When nettle root contains 3, 4-divanillyltetrahydrofuran it has the ability to increase free testosterone by actively binding to SHBG as well as inhibiting the aromatase enzyme(5), thereby increasing the level of free testosterone. Also 3, 4-divanillyl THF actively inhibits SHBG, increasing the rate at which androgens enter the cell and activate metabolic transcription factors. This “nettle effect” presents some very stunning biological ramifications. As a result, any quality male support formula should contain the very highest quality Urtica dioica standardized to a specific level of bioactive 3, 4-divanillyltetrahydrofuran.

Optimizing the Testosterone to Estrogen Ratio Recall from part one that the primary hormonal issue in the aging male is not just decreased free testosterone but also the ratio of testosterone to estrogen. The enzyme aromatase is highly concentrated within intra-abdominal fat where it converts testosterone into estrogen. Increased abdominal fat and subsequently increased activity of aromatase can cause men receiving testosterone therapy to produce excess estrogens, leading to many health issues. Specific extracts of nettle root not only increase free testosterone but also actively inhibit the aromatase enzyme.(6) Therefore, you only want to use formulations that utilize the highest quality Urtica dioica extracts to assist in achieving a proper free testosterone to estrogen ratio.

Chrysin is still promoted by many nutritional companies as an aromatase inhibitor; however, there is growing evidence that Chrysin elicits no effect on the estrogen levels of neither animals nor humans.(7) Multiple studies have now determined that cell membranes block Chrysin from entering the cells and producing any effect on estrogen levels in vivo.(8), (9) However, evidence is available that Chrysin may inhibit thyroid function.(10) Therefore, practitioners should avoid formulas including Chrysin, especially given the superior results found with specific extracts of stinging nettle root.

Finally, research has shown that intake of DIM increases the conversion of estradiol to the healthier estriol, and beneficially increases the 2-hydroxy estrogen (2OHE) metabolites. The 2OHE promoted by DIM also increases testosterone synthesis by turning off the estradiol negative feedback loop on testosterone production. Therefore, a quality formula for men should provide 150 mg to 200 mg of Bioactive DIM.

1. Koumanov, F., Bozadzhieva, E., Andreeva, M.(1982) Clinical trial of the drug “Tribestan”. Savr.Med 4: 211-215.
2. Adimoelja,A., (1997) Protodioscin from herbal plant Tribulus terrestris L improves male sexual function possibly via DHEA. Int.J.Impot.Res 9 (1).
3. Adaikan, P.G., et. al. (2001) History of herbal medicines with an insight on the pharmacological properties of Tribulus terrestris. Aging Male 4: 163 – 169.
4. Legssyer A, et al. Cardiovascular effects of Urtica dioica L. in isolated rat heart and aorta. Phytother Res 2002 Sep;16(6):503-7.
5. Schöttner M, Gansser D, Interaction of lignans with human sex hormone binding globulin (SHBG). ” Z Naturforsch [C]”. 1997 Nov–Dec;52(11–12):834–43.
6. Gansser D, Spiteller G Aromatase inhibitors from Urtica dioica roots. Planta Med. 1995 Apr; 61(2):138-40.
7. Dean, W.Chrysin: Is It An Effective Aromatase Inhibitor?
8. Campbell DR, Kurzer MS “Flavonoid inhibition of aromatase enzyme activity in human preadipocytes”. J. Steroid Biochem. Mol. Biol. 46 (3): 381–8.
9. Saarinen N, Joshi SC, Ahotupa M, et. al.(2001). “No evidence for the in vivo activity of aromatase-inhibiting flavonoids”. J Steroid Biochem Mol Biol. 78 (3): 231.
10. Koehrle J, Auf’mkolk M, Spanka M, Irmscher K, et. al. (1986). “Iodothyronine deiodinase is inhibited by plant flavonoids”. Prog. Clin. Biol. Res. 213: 359–71.