|5 alpha Reductase (5AR) is the enzyme that converts testosterone into dihydrotestosterone (DHT). DHT has been conclusively implicated in the pathogenesis of MPB, Acne, Hirsutism and Prostate Enlargement, which are generally referred to as “Androgen Mediated” disorders. Lowering DHT levels to a point in humans will over time, reliably halt and to some degree, reverse the course of MPB. Reducing DHT levels can be readily accomplished by inhibiting the enzyme 5AR, which is the mechanism of action for both Propecia (finasteride) and Avodart (dutasteride). Both Propecia and even more so, Avodart, are established to have fairly reliable hair growth effects. Unfortunately both come with a side effect price tag, including loss/reduction of libido, erectile dysfunction, depression, insomnia, and anxiety. Post Finasteride Syndrome is a newly coined diagnosis for symptoms of reduced libido and erectile dysfunction that persist years after discontinuation of these 5AR inhibiting drugs. It is however possible to inhibit 5AR in a way that is not only side effect free, but in a way that actually enhances both mood and male function. A team of researchers found in 3 successive (abstracts below) studies, 2 published in the prestigious Journal of the International Society for Sports Nutrition, that the combination of Astaxanthin with Saw Palmetto achieved a 98% inhibition of 5 alpha reductase. |
J Herb Pharmacother 2005;5(1):17-26.
A preliminary investigation of the enzymatic inhibition of 5alpha-reduction and growth of prostatic carcinoma cell line LNCap-FGC by natural astaxanthin and Saw Palmetto lipid extract in vitro AbstractInhibition of 5alpha-reductase has been reported to decrease the symptoms of benign prostate hyperplasia (BPH) and possibly inhibit or help treat prostate cancer. Saw Palmetto berry lipid extract (SPLE) is reported to inhibit 5alpha-reductase and decrease the clinical symptoms of BPH. Epidemiologic studies report that carotenoids such as lycopene may inhibit prostate cancer. In this investigation the effect of the carotenoid astaxanthin, and SPLE were examined for their effect on 5alpha-reductase inhibition as well as the growth of prostatic carcinoma cells in vitro. These studies support patent #6,277,417 B1. The results show astaxanthin demonstrated 98% inhibition of 5alpha-reductase at 300 microg/mL in vitro. Alphastat, the combination of astaxanthin and SPLE, showed a 20% greater inhibition of 5alpha-reductase than SPLE alone n vitro. A nine day treatment of prostatic carcinoma cells with astaxanthin in vitro produced a 24% decrease in growth at 0.1 mcg/mL and a 38% decrease at 0.01 mcg/mL. SPLE showed a 34% decrease at 0.1 mcg/mL.Conclusions: Low levels of carotenoid astaxanthin inhibit 5alpha-reductase and decrease the growth of human prostatic cancer cells in vitro. Astaxanthin added to SPLE shows greater inhibition of 5alpha-reductase than SPLE alone in vitro.
J Int Soc Sports Nutr2008 Aug 12;5:12. An open label, dose response study to determine the effect of a dietary supplement on dihydrotestosterone, testosterone and estradiol levels in healthy males AbstractBackground: Maintaining endogenous testosterone (T) levels as men age may slow the symptoms of sarcopenia, andropause and decline in physical performance. Drugs inhibiting the enzyme 5alpha-reductase (5AR) produce increased blood levels of T and decreased levels of dihydrotestosterone (DHT). However, symptoms of gynecomastia have been reported due to the aromatase (AER) enzyme converting excess T to estradiol (ES). The carotenoid astaxanthin (AX) from Haematococcus pluvialis, Saw Palmetto berry lipid extract (SPLE) from Serenoa repens and the precise combination of these dietary supplements, Alphastat(R) (Mytosterone(trade mark)), have been reported to have inhibitory effects on both 5AR and AER in-vitro. Concomitant regulation of both enzymes in-vivo would cause DHT and ES blood levels to decrease and T levels to increase. The purpose of this clinical study was to determine if patented Alphastat(R) (Mytosterone(trade mark)) could produce these effects in a dose dependent manner.
Methods: To investigate this clinically, 42 healthy males ages 37 to 70 years were divided into two groups of twenty-one and dosed with either 800 mg/day or 2000 mg/day of Alphastat(R) (Mytosterone(trade mark)) for fourteen days. Blood samples were collected on days 0, 3, 7 and 14 and assayed for T, DHT and ES. Body weight and blood pressure data were collected prior to blood collection. One-way, repeated measures analysis of variance (ANOVA-RM) was performed at a significance level of alpha = 0.05 to determine differences from baseline within each group. Two-way analysis of variance (ANOVA-2) was performed after baseline subtraction, at a significance level of alpha = 0.05 to determine differences between dose groups. Results are expressed as means +/- SEM.
Results: ANOVA-RM showed significant within group increases in serum total T and significant decreases in serum DHT from baseline in both dose groups at a significance level of alpha = 0.05. Significant decreases in serum ES are reported for the 2000 mg/day dose group and not the 800 mg/day dose group. Significant within group effects were confirmed using ANOVA-2 analyses after baseline subtraction. ANOVA-2 analyses also showed no significant difference between dose groups with regard to the increase of T or the decrease of DHT. It did show a significant dose dependant decrease in serum ES levels.
Conclusion: Both dose groups showed significant (p = 0.05) increases in T and decreases in DHT within three days of treatment with Alphastat(R) (Mytosterone(trade mark)). Between group statistical analysis showed no significant (p = 0.05) difference, indicating the effect was not dose dependent and that 800 mg/per day is equally effective as 2000 mg/day for increasing T and lowering DHT. Blood levels of ES however, decreased significantly (p = 0.05) in the 2000 mg/day dose group but not in the 800 mg/day dose group indicating a dose dependant decrease in E levels.
J Int Soc Sports Nutr2014 Aug 23;11:43. Evaluation of Resettin® on serum hormone levels in sedentary males AbstractBackground: Comparisons of hormones such as dihydrotestosterone (DHT), estradiol (E2), and testosterone indicate their impact on metabolism and body composition. While less is known regarding DHT and E2, testosterone is an androgenic metabolic hormone capable of positively regulating a variety of anabolic and androgenic processes in the body. Accordingly, it has been postulated that the age-related reduction in serum testosterone levels leads to reductions in lean muscle mass, bone mineral density, and other physical conditions that impair physical performance and decrease quality of life. Preliminary studies suggest that key ingredients found in Resettin®/MyTosterone™, a natural supplement containing the carotenoid astaxanthin from Haematococcus pluvialis and Saw Palmetto berry lipid extract from Serenoa repens, could positively impact testosterone levels. To investigate the clinical efficacy of Resettin®, the serum profiles of testosterone, E2 and DHT in healthy sedentary males before and after Resettin® treatment were evaluated in a randomized, placebo controlled clinical trial.
Method: Twenty healthy, sedentary men between the ages of 21 and 70 were randomized into either an 800 mg/day or 1200 mg/day Resettin®/MyTosterone™ treatment group or lecithin, which was used as the placebo. After a 14-day treatment period, there was a 14-day washout period. After the wash-out period, participants were crossed over within their respective group to either Resettin®/MyTosterone™ or the lecithin placebo for 14 days.
Results: After 14 days, participants receiving 800 mg per day of Resettin® had significantly reduced baseline-subtracted serum DHT levels in comparison to the placebo control group. While after 14 days, participants receiving 1200 mg per day of Resettin® had significantly reduced baseline-subtracted serum DHT and E2 levels in comparison to the placebo control group. Moreover, participants receiving 1200 mg per day of Resettin® experienced a 38% increase in serum testosterone levels in comparison to the placebo control group, but the effect did not reach statistical significance.
Conclusion: Although additional studies will be required to evaluate how Resettin® may promote proper testosterone regulation, these findings indicate that Resettin® can favorably influence serum hormone profiles in men.
The combination used in these was also patented and trademarked (Resettin) as both a Prostate Treatment and an endocrine modulating intervention for aging males, who progressively become more androgen deficient. It reduces DHT and Estrogen, but which become more elevated in men in what is considered “normal” aging. If that weren’t enough, it also increases testosterone to a high normal level which many androgen deficient middle aged men can only attain through either testosterone patches or injections.
Astaxanthin has additionally been demonstrated to help maintain lean body mass, as detailed in a just published review in a medical journal:
Effects of Astaxanthin on the Protectionof Muscle Health
Astaxanthin also helps reduce wrinkling, maintain skin firmness, and protect from ultra violet light insult from the inside out.
Effects of Astaxanthin Supplementation on Skin Health:A Systematic Review of Clinical Studies
I have been using the combination of Saw Palmetto/Beta sitosterol and Astaxanthin (4 mg.) for over 10 years, and have a high testosterone level along with a low level of bodyfat. Although I use numerous other supplements for anti-aging, health and hair, this is one core combination with unique effects on Testosterone, Estrogen and DHT I would not do without, especially since going off Propecia over a decade ago.
Due to its unique mechanisms, this combination has reportedly been used in conjunction with Propecia (finasteride) and Avodart (dutasteride) to both accentuate their hair growth effects and mitigate side effects.
This combination simply consists of one soft gel each of both Astaxanthin and Palmetto Guard. Our Astaxanthin is compounded with phospholipids for significantly enhanced absorption. Palmetto Guard combines the standardized critical CO2 extract of Saw palmetto AND Beta-Sitosterol, which in addition to inhibiting 5 alpha reductase, inhibits androgen binding at receptor sites. Both are low cost and easily integrated into any existing regime.