Male Hormone Restoration
Boost Testosterone and Suppress Estrogen Levels Naturally
For men who choose not to (or are advised not to) use hormone replacement therapy, nutrients can play a vital role in a comprehensive program designed to reduce the impact of aging on sex hormone production and metabolism. The following is a list of nutrients that are part of the Life Extension Foundation’s comprehensive male hormone restoration program:
Essential nutrients for optimal testosterone production:
Zinc: This mineral is involved in almost every aspect of male reproduction, including testosterone metabolism, sperm formation, and sperm motility (Ali et al 2005). A prime example of the usefulness of zinc was illustrated in a study of 37 infertile men with decreased testosterone levels and associated low sperm counts (Netter et al 1981). The men were given 60 mg of zinc daily for 45-50 days. In the majority of patients, testosterone levels significantly increased and mean sperm count rose from 8 million to 20 million. Some men require higher levels of zinc to adequately suppress aromatase.
L-Carnitine. L-Carnitine is an amino acid derivative that may be more active than testosterone in aging men who have sexual dysfunction and depression caused by an androgen deficiency (Cavallini G et al 2004). Both testosterone and carnitine improve sexual desire, sexual satisfaction, and nocturnal penile tumescence, but carnitine is more effective than testosterone in improving erectile function, nocturnal penile tumescence, orgasm, and general sexual well-being. L-Carnitine was also more efficacious than testosterone for treating depression (Cavallini G et al 2004).
DHEA: DHEA is an important hormone that tends to be depleted steadily with age (Basar NM et al 2005). A 2006 study assessing DHEA supplementation in men of average 65 years of age found that the men experienced significant increases in testosterone and significant decreases in low-density lipoprotein (Martina et al 2006).
Tribulus: Tribulus terrestris, also known as puncture vine, contains the active ingredient protodioscin, which is reportedly converted to DHEA in the body (Adimoelja A 2000). This DHEA-boosting activity may account for puncture vine’s reputation as an aphrodisiac in its native Europe and Asia. While some animal studies appear to confirm the ability of tribulus to improve sexual function, no reliable human trials have taken place (Gauthaman et al 2003; Milasius et al 2009).
Antioxidants: One reason testosterone production may decline with advancing age is oxidative damage in the tissues that produce testosterone. A study examining the role of antioxidants in male hormone imbalance in aging men noted that antioxidant supplements (including vitamins A and E, zinc and selenium) all supported testosterone production (He et al 2005).
Natural products keep aromatase and/or sex hormone-binding globulin (SHBG) in check:
Chrysin: The bioflavonoid chrysin is a natural aromatase inhibitor (Kellis et al 1984). Bodybuilders have used chrysin as a testosterone-boosting supplement, because it minimizes the conversion of testosterone to estrogen. Although chrysin has low oral bioavailability (Walle et al 2001), its bioavailability may be significantly enhanced by co-administration with the black pepper extract, piperine, thus enhancing its actions as an aromatase inhibitor (Srinivasan et al 2007).
Quercetin: One study showed that red wine inhibits aromatase, thus inhibiting the conversion of testosterone to estrogen. The study attributed this effect to the quercetin and other ingredients (Eng et al 2002).
Nettle root: Lignans contained in nettle root extract may help prevent the binding of sex hormone-binding globulin to testosterone. This may help ensure that free testosterone is available for promoting male vitality and youthful sexual function (Anon 2007, Chrubasik et al 2007). Nettle root extract is used extensively, either in combination with saw palmetto (Lopatkin 2005) or by itself (Safarinejad 2005) for relief of BPH symptoms.
Fish oil: A study examined how the essential fatty acids EPA and DHA affected SHBG levels in men 43 to 88 years of age (Nagata et al 2000). After controlling for other variables, the researchers concluded that both EPA and DHA decreased levels of SHBG in middle-aged and elderly men.
Protein: While adequate protein consumption is vital to maintaining muscle mass, it is also important in maintaining testosterone levels. A study examined the relationship between diet and SHBG, and found that diets low in protein in men 40-70 years old may lead to elevated SHBG levels and consequently decreased testosterone bioactivity (Longcope et al 2000).
Natural products to support sexual function
Muira Puama: Muira puama, Ptychopetalum olacoides, grows in the Amazon region of Brazil. It is considered an aphrodisiac and an effective treatment for impotence. It has been studied by Dr. Jacques Waynberg (Waynberg 1990), a prominent medical sexologist at the Institute of Sexology in Paris. In one of his studies, men with loss of libido received 1.5 grams/day of muira puama for 2 weeks. 62% rated the treatment as having a dynamic effect, and 52% with erectile dysfunction rated the treatment as beneficial. In another study, muira puama treatment was given to 100 men, aged 18 years or older, with impotence and/or loss of libido. A significantly increased frequency of intercourse was reported in 66% of the men. Of the 46 men who complained of loss of desire, 70% reported libido intensification. The stability of erection during intercourse was restored in 55% of men, and 66% of men reported a reduction in fatigue. Other reported beneficial effects included improved sleep and morning erections.
Maca: Maca has been used among indigenous people in the Andes region for centuries. It is a reputed aphrodisiac and fertility enhancer. Peruvian researchers conducted a randomized, placebo-controlled double-blind study on a small group of men aged 21-56. Results showed that, versus placebo, maca improved subjective reports of male sexual desire. Subjects consumed either 1,500 mg or 3,000 mg of maca, or placebo, for three months. After eight weeks, improvements were noted in sexual desire among the subjects who consumed maca (Gonzales et al 2002).
Natural products to support prostate health
Indole-3-carbinol (I3C): I3C protects against dangerous estrogen metabolites and subsequent prostate cancer. An adequate intake of I3C, through vegetables such as broccoli, Brussels sprouts, and cabbage, or via supplements, may be very helpful for aging men in both keeping undesirable estrogen metabolites such as 16-alphahydroxyestrone in check and decreasing their risk of prostate cancer. Studies have demonstrated that I3C increases the ratio of 2-hydroxyestrone to 16-alpha-hydroxyestrone. For men, this very well might mean a decrease in prostate cancer risk (Sepkovic et al 2001, Bradlow 2008). In a study that examined the association of prostate cancer risk with estrogen metabolism, the authors said, “results of this case-control study suggest that the estrogen metabolic pathway favoring 2-hydroxylation over 16-alpha-hydroxylation may reduce risk of clinically evident prostate cancer” (Muti et al 2002).
Pygeum: A bark extract from the native African cherry tree Pygeum africanum, has been used in Europe to treat BPH since 1960, and is currently the most commonly used therapeutic agent for this condition in France (Buck 2004). One theory for the anti-BPH action of pygeum involves the conversion of testosterone to dihydrotestosterone (DHT), a potent testosterone metabolite that may exacerbate BPH, via the enzyme 5-a-reductase (Wilt et al 2002). A recent study identified that N-butylbenzene-sulfonamide (NBBS) was isolated from P. africanum as a specific androgen receptor (AR) antagonist. NBBS inhibits AR- and progesterone receptor (PR)- mediated transactivation, as well as endogenous PSA expression and growth of human prostate cancer cells (Papaioannou et al 2009).
Saw Palmetto: In Europe, saw palmetto (Serenoa repens) has been used extensively as a drug for reducing symptoms of (BPH). Saw palmetto has multiple mechanisms of action: inhibition of 5-alpha-reductase; inhibition of DHT binding to the androgen receptor; reduction of the inflammatory component of prostate growth (by inhibiting COX-2 and an enzyme called 5-lipoxygenase); induction of apoptosis and inhibition of prostate cell proliferation (Debruyne 2002; Goldmann et al 2001; Paubert-Braquet et al 1997; Vacherot et al 2000). Its clinical benefits for prostate enlargement include reduced nocturnal urinary urgency (Pavone et al 2010), decreased residual urine volume in the bladder (Giannakopoulos et al 2002), and less discomfort from urination symptoms (Mantovani 2010).
Testosterone and Prostate Cancer: The Myth
For more than 6 decades, the medical establishment erroneously conjectured that testosterone replacement therapy increases one’s risk of developing prostate cancer. This fear has made it standard practice for physicians to deprive hypogonadal male patients of testosterone replacement that could otherwise provide them with a world of cardiovascular, musculoskeletal, cognitive, metabolic and other health benefits, as discussed above.
Remarkably, though, it appears that, in most cases, the opposite is true—lower levels of endogenous testosterone present a greater risk of prostate cancer than higher levels (Morgentaler 2009). A review of data from the National Institutes of Health revealed that, in men of advancing age, “high testosterone levels are not associated with an increased risk of prostate cancer, nor are low testosterone levels protective against prostate cancer” (Morgentaler 2006).
A collaborative review of 18 prospective studies compared serum concentrations of androgen and estrogen in 3,886 men with prostate cancer with those in 6,438 healthy controls. The results showed no significant associations between the risk of prostate cancer and sex hormone levels (Roddam et al 2008).
In more than 500 men diagnosed with prostate cancer (followed over a mean of 8.7 years), high androgen levels were actually associated with a decreased risk of aggressive prostate disease, compared with no change in the risk of non-aggressive disease. Overall, levels of any steroid hormones (except estradiol) were not correlated with the risk of aggressive prostate cancer (Severi et al 2006).
Dr. Abraham Morgentaler, an associate clinical professor at the Harvard Medical School, in his book Testosterone for Life, convincingly makes the case for the benefits and safety of high testosterone vs. the dangers of low testosterone. He also goes back to the original 1941 Nobel Prize-winning research (Huggins et al 1941) about testosterone and shows how these data have been misinterpreted and unquestioned for over 70 years.
Life Extension Recommendations
Step One: Testing
It is critical that men undergo comprehensive medical testing before embarking on a hormone modulation program. First, a baseline blood PSA must be taken to rule out existing prostate cancer (for more information, please see the chapter on prostate cancer). Then, free and total testosterone and estradiol tests are needed to make sure that testosterone is not being excessively converted into estrogen. If estrogen levels are too high, the use of aromatase inhibitors can reduce the rate at which testosterone converts to estrogen in the body. Follow-up testing for estrogen, testosterone, and PSA levels are needed to rule out prostate cancer and fine-tune your program. Additional tests that should be considered include:
- Complete blood cell count and chemistry profile, including liver and kidney function, glucose, minerals, lipids and thyroid-stimulating hormone (TSH)
- DHEA
- Luteinizing hormone (LH) (optional)
- SHBG (optional)
- Dihydrotestosterone (optional)
Blood for these tests may be drawn at your physician’s office or directly at a laboratory in your area. Information about ordering these tests on your own may be obtained by calling 1-800-208-3444. These tests will yield crucial information that can help you design a program tailored to your unique situation.
Step Two: Interpreting the Results
Free testosterone: The Life Extension Foundation believes that direct testing for free testosterone is the best way to test for testosterone activity, as free testosterone is the active form of the hormone and comprises only about 2% of total testosterone.
The Life Extension Foundation recommends that men strive for a free testosterone level that is in the upper one-third range for men aged 21 to 49 years. The range of free testosterone serum level is 20 to 25 picograms per milliliter (pg/mL), using our current testing methodology.
There are five reasons that free testosterone levels may be low:
- Too much testosterone is being converted to estrogen through the activity of aromatase.
- Too much free testosterone is being bound by SHBG. This would be especially apparent if a man’s total testosterone level is in the high normal range but his free testosterone level is low.
- The pituitary gland, which controls testosterone production through the production of luteinizing hormone (LH), is not secreting enough LH to stimulate gonadal production of testosterone. In this case, total testosterone would be low.
- The testicles (gonads) have lost their ability to produce testosterone, despite adequate amounts of LH. In this case, the level of LH would be high despite a low testosterone level.
- DHEA level is abnormally low.
Estrogen: Measured as estradiol, should be kept in a range of 20 to 30 pg/ml. If a man’s estrogen level is elevated, it could be associated with:
- Increased aromatase activity, often caused by increased abdominal fat.
- The liver is failing to remove excess estrogen, possibly because of heavy alcohol intake. In men, heavy alcohol intake has been shown to boost estrogen levels within the liver (Colantoni et al 2002).
If a man’s estradiol level is higher than 30 pg/mL, it should be reduced by using aromatase-inhibiting drugs or nutrients. (Optimal estradiol levels are between 20-30 pg/mL.)
Step Three: Correcting Abnormal Levels
Ultimately, the ideal program will depend on the results of various tests. Below are some common scenarios and solutions to correct hormone imbalances.
Low Free Testosterone, High Estradiol, Mid Total Testosterone: This situation suggests excessive aromatase activity, which converts free testosterone to estrogen. Inhibition of aromatase and reduction in aromatase-containing tissue (fat) is indicated. Suggestions include:
- Chrysin: 1,500 mg daily
- Piperine: 10 mg daily to enhance absorption of chrysin
- Zinc: 50 – 90 mg daily
- Acetyl-L-carnitine: 1,000 – 2,000 mg daily
- Muira puama: 850 mg daily
- Quercetin: 500 – 1,000 mg daily
- Lose weight to reduce aromatase activity.
- Reduce or eliminate alcohol intake to enable excess estrogen removal by the liver.
- Review all current medications to see if they might be interfering with healthy liver function. Common medications that affect liver function are nonsteroidal anti-inflammatory drugs (NSAIDs) (e.g., naproxen, ibuprofen, acetaminophen, and aspirin); the statin class of cholesterol-lowering drugs (e.g., simvastatin, atorvastatin); some heart medications; some blood pressure-lowering medications; and some antidepressants. Drugs being prescribed to treat the symptoms of testosterone deficiency (such as the statins and certain antidepressants) may actually aggravate the testosterone deficit, thus making the cholesterol problem or depression worse. However, do not discontinue any prescription medicine without consulting your physician.
- If all of the above fail to increase free testosterone and lower excess estradiol, consider discussing with your physician the use of the aromatase inhibitor anastrozole (Arimidex) at the very low dose of 0.5 mg twice per week.
Low Free Testosterone, Low Estrogen, High Total Testosterone: This situation suggests excessive SHBG levels, making sufficient testosterone unavailable to target tissues. The elevation of SHBG explains why some older men who are on testosterone replacement therapy do not report a long-term beneficial effect, that is, the administered testosterone becomes bound by SHBG and is not bioavailable to cellular receptor sites where it would normally produce an effect. Suggestions include:
- Inhibit aromatase by following some of the recommendations in the previous section, since low testosterone and high estrogen are involved in excess SHBG activity.
- Take the following supplements:
Low Free Testosterone, Low Estrogen, Low Testosterone: This situation suggests low production of testosterone, with resultant low conversion to estrogen. Suggestions include:
- Use testosterone patches or creams. Do not use testosterone injections or tablets. If tests reveal low levels of LH, ask your physician about the possibility of using human chorionic gonadotropin (HCG). HCG functions in a manner similar to that of LH, thus helping to stimulate the leydig cells of the testes to produce more testosterone.
- Take DHEA: 15 – 75 mg daily
- Tribulus fruit extract (40% saponins): 450 mg daily
General Nutrients to Boost Sexual Function
A number of nutrients have been studied for their ability to boost testosterone and/or treat conditions such as erectile dysfunction and loss of libido. This nutrient group includes antioxidants, which may function by reducing oxidative damage to testosterone-producing tissues.
Product Availability
All the nutrients and supplements discussed in this protocol are available through the Life Extension Foundation Buyers Club, Inc. For ordering information, call anytime toll-free 1-800-544-4440, or visit us online at www.LifeExtension.com.
The blood tests discussed in this section are available through Life Extension National Diagnostics, Inc. For ordering information, call anytime toll-free 1-800-208-3444, or visit us online at www.LifeExtension.com. |
Male Hormone Restoration Safety Caveats
An aggressive program of dietary supplementation should not be launched without the supervision of a qualified physician. Several of the nutrients suggested in this protocol may have adverse effects. These nutrients include:
Acetyl-L-carnitine
- For some people, L-carnitine, especially acetyl-L-carnitine, may have a stimulating effect. Therefore, it may be unwise to take it in the evening.
Chrysin
- Do not take chrysin if you have prostate cancer. Chrysin can also increase the effects of aromatase inhibitors, such as aminoglutethimide, anastrozole, and letrozole.
DHEA
- Do not take DHEA if you have prostate cancer. DHEA can also cause androgenic effects, such as acne, deepening of the voice, and facial hair growth.
Piperine
- This can inhibit such drugs as propranolol, theophylline, phenytoin, sulfadiazine, rifampicin, isoniazid, ethambutol, pyrazinamide, and dapsone, all of which are metabolized by cytochrome P450 enzymes in the liver.
Zinc
- Supplemental zinc can inhibit the absorption and availability of copper. If more than 50 mg of supplemental zinc is taken daily, 2 mg of supplemental copper should also be taken to prevent deficiency. Chronic ingestion of more than 100 mg of zinc daily may be toxic.
For more information see the Safety Appendix. |
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