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HERBAL AROMATASE INHIBITION

Kelly here,
      There is evidence indicating men with androgenetic hair loss in fact have *lower* testosterone levels than men who are not balding, (as if losing hair weren’t bad enough).

      It seems counterintuitive being that hair loss is actually androgen mediated. That being the case, the expected corollary would be that one would anticipate finging higher estrogen in those with hair loss. It was not at all surprising when we found a study showing that men with acne, (another classic”androgen mediated” disorder) indeed do have higher estrogen levels than men with no acne. The hormonal pathogenesis of acne is almost identical to that of MPB, i.e. elevated 5AR activity, increased sebum emission, inflammation, bacterial infiltrates etc .The available evidence indicates that MPB, like acne, involves higher levels of DHT and estrogen, and lower testosterone. Of additional interest is that it has been established that men with prostate disorders typically have higher estrogen as well.


Chin Med J (Engl). 1989 Mar;102(3):236-8.


Testosterone and estradiol serum levels in acne


      Fourty five acne patients and thirty eight healthy subjects were assayed for serum testosterone and estradiol levels by RIA. The results showed that serum testosterone levels of male patients were normal, but serum estradiol levels were significantly higher (40%) than in healthy males. In female patients, estradiol levels were normal, but testosterone levels were significantly higher (47%) than in healthy females. Of the 18 female patients, 16 had various degrees of menstrual dysfunction, and some even had slight hirsutism. Therefore, male acne patients should not be treated with estrogen and in female acne patients with ovarian dysfunction, artificial menstrual cycle therapy is recommended.

      Further evidence indicates that lowering DHT alone, as with Propecia and Avodart, is only partially effective at best for stopping the progression of MPB, and even then for a limited amount of time. Both Propecia and Avodart are known for raising estrogen as well as reducing serum DHT levels, thus compromising the full potential benefit of lowering DHT for scalp hair growth and prostate disorders.

      It’s a classic case of 2 steps forward and one and a half steps back for hair growth.

      This isn’t even taking into account the well established side effects of increased estrogen in men, i.e., increase in belly fat, decrease in libido, increased disposition to inflammation, decreased immunity, etc.

      The ideal solution to this dilemma is to simultaneously inhibit aromatase AND 5 alpha reductase, not just 5-alpha reductase alone. Aromatase, as many already know, is the enzyme that converts estrogens from androgens. Aromatase and consequently estrogen, increase as men age and is largely implicated in abdominal mass increase, prostate enlargement, hirsutism (body hair growth, particularly on back), and depression. This combination of medical problems, seen in the majority of American middle aged men has been termede the “Estrogen Syndrome” among endocrinologists.

      By inhibiting both 5 alpha reductase and aromatase, one increases testosterone and decreases both DHT and estrogen, optimizing the hormone profile for muscle mass maintenance, libido, bodyfat, and for our purposes, hair growth.

      How to inhibit aromatase???
      There are several compounds, both herbal, and pharmaceutical, that are useful.

      Arimidex is an aromatase inhibiting drug that is used in the treatment of breast cancer. It has been in vogue for years in the bodybuilding community who found that it generally prevents breast enlargement among anabolic steroid users. It has interestingly also been used to increase final adult height in children, (for those sports parents). Its drawback is its cost- typically $280.00 or more a month. Insurance will only cover in certain cases of diagnosed breast cancer.

      Alternatives do exist.
      Several compounds, some of which are already recommended in our treatment protocol, have been shown to inhibit aromatase and have additional benefits for health, anti-aging, and hair growth. Most notable among these compounds are Green Tea Extract, Grape Seed/Resveratrol Extract, Pomegranate Extract, Melatonin, and Chrysin/piperine (Chrysin without piperine is useless , as it is not absorbed).


Cancer Res. 2006 Jun 1;66(11):5960-7.

Grape seed extract is an aromatase inhibitor and a suppressor of aromatase expression.
      Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California, USA.

      Aromatase is the enzyme that converts androgen to estrogen. It is expressed at higher levels in breast cancer tissues than normal breast tissues. Grape seed extract (GSE) contains high levels of procyanidin dimers that have been shown in our laboratory to be potent inhibitors of aromatase. In this study, GSE was found to inhibit aromatase activity in a dose-dependent manner and reduce androgen-dependent tumor growth in an aromatase-transfected MCF-7 (MCF-7aro) breast cancer xenograft model, agreeing with our previous findings. We have also examined the effect of GSE on aromatase expression. Reverse transcription-PCR experiments showed that treatment with 60 mug/mL of GSE suppressed the levels of exon I.3-, exon PII-, and exon I.6-containing aromatase mRNAs in MCF-7 and SK-BR-3 cells. The levels of exon I.1-containing mRNA, however, did not change with GSE treatment. Transient transfection experiments with luciferase-aromatase promoter I.3/II or I.4 reporter vectors showed the suppression of the promoter activity in a dose-dependent manner. The GSE treatment also led to the down-regulation of two transcription factors, cyclic AMP-responsive element binding protein-1 (CREB-1) and glucocorticoid receptor (GR). CREB-1 and GR are known to up-regulate aromatase gene expression through promoters I.3/II and I.4, respectively. We believe that these results are exciting in that they show GSE to be potentially useful in the prevention/treatment of hormone-dependent breast cancer through the inhibition of aromatase activity as well as its expression.


Breast Cancer Res Treat. 2002 Feb;71(3):203-17


Chemopreventive and adjuvant therapeutic potential of pomegranate (Punica granatum) for human breast cancer.


      Department of Pharmacy, Pusan National University, Korea.

      Fresh organically grown pomegranates (Punica granatum L.) of the Wonderful cultivar were processed into three components: fermented juice, aqueous pericarp extract and cold-pressed or supercritical CO2-extracted seed oil. Exposure to additional solvents yielded polyphenol-rich fractions ('polyphenols') from each of the three components. Their actions, and of the crude whole oil and crude fermented and unfermented juice concentrate, were assessed in vitro for possible chemopreventive or adjuvant therapeutic potential in human breast cancer. The ability to effect a blockade of endogenous active estrogen biosynthesis was shown by polyphenols from fermented juice, pericarp, and oil, which inhibited aromatase activity by 60-80%. Fermented juice and pericarp polyphenols, and whole seed oil, inhibited 17-beta-hydroxysteroid dehydrogenase Type 1 from 34 to 79%, at concentrations ranging from 100 to 1,000 microg/ml according to seed oil >> fermented juice polyphenols > pericarp polyphenols. In a yeast estrogen screen (YES) lyophilized fresh pomegranate juice effected a 55% inhibition of the estrogenic activity of 17-beta-estradiol; whereas the lyophilized juice by itself displayed only minimal estrogenic action. Inhibition of cell lines by fermented juice and pericarp polyphenols was according to estrogen-dependent (MCF-7) >> estrogen-independent (MB-MDA-231) > normal human breast epithelial cells (MCF-10A). In both MCF-7 and MB-MDA-231 cells, fermented pomegranate juice polyphenols consistently showed about twice the anti-proliferative effect as fresh pomegranate juice polyphenols. Pomegranate seed oil effected 90% inhibition of proliferation of MCF-7 at 100 microg/ml medium, 75% inhibition of invasion of MCF-7 across a Matrigel membrane at 10 microg/ml, and 54% apoptosis in MDA-MB-435 estrogen receptor negative metastatic human breast cancer cells at 50 microg/ml. In a murine mammary gland organ culture, fermented juice polyphenols effected 47% inhibition of cancerous lesion formation induced by the carcinogen 7,12-dimethylbenz[a]anthracene (DMBA). The findings suggest that clinical trials to further assess chemopreventive and adjuvant therapeutic applications of pomegranate in human breast cancer may be warranted.


Food Chem Toxicol. 2002 Jul;40(7):925-33


Inhibition of aromatase activity by green tea extract catechins and their endocrinological effects of oral administration in rats.


    Department of Toxicology, The Tokyo Metropolitan Research Laboratory of Public Health, 24-1 Hyakunincho 3 chome, Shinjuku-ku, Japan. sato@tokyo-eiken.go.jp

    We orally administered polyphenone-60 (P-60), green tea extract catechins, in the diet (0, 1.25 and 5%) to male rats for 2, 4 and 8 weeks initiated at 5 weeks old. It was found that a 5% dose to male rats for 2-8 weeks induced goiters and decreased weights of the body, testis and prostate gland. Endocrinologically, elevating plasma thyroid stimulating hormone (TSH), luteinizing hormone (LH) and testosterone levels and decreasing tri-iodothyronine (T(3)) and thyroxine (T(4)) levels were induced by this treatment. We also found that P-60 as a whole and some of its constituents exhibited inhibitory effects on human placental aromatase activity by in vitro assay. The concentration of P-60 that required producing 50% inhibition of the aromatase activity (IC(50) value) was 28 microg/ml. The IC(50) values of (-)-catechin gallate (Cg), (-)-epigallocatechin (EGC), (-)-epigallocatechin gallate (EGCg) and (-)-gallocatechin gallate (GCg) were 5.5 x 10(-6), 1.0 x 10(-4), 6.0 x 10(-5) and 1.5 x 10(-5) M, respectively. (-)- Epicatechin gallate (ECg) at 1.0 x 10(-4) M produced 20% inhibition. (-)-Epicatechin (EC) and (+)-catechin (CT) exhibited no effects on aromatase activity. The endocrinological changes observed in vivo were in conformity with antithyroid effects and aromatase inhibition effects of P-60 and its constituents.


Melatonin modulates aromatase activity in MCF-7 human breast cancer cells.


    Department of Physiology and Pharmacology, School of Medicine, University of Cantabria, Santander, Spain.

    Most of the current knowledge about the mechanisms by which melatonin inhibits the growth of breast cancer cells point to an interaction of melatonin with estrogen-responsive pathways, thus behaving as an antiestrogenic hormone. However, a possible effect of melatonin on the local synthesis of estrogens had not been examined. The objective of this work was to study whether melatonin may modify the aromatase activity in MCF-7 breast cancer cells thus modulating the local estrogen biosynthesis. In MCF-7 cells cultured with testosterone in estradiol-free media, melatonin (1 nM) counteracts the testosterone-induced cell proliferation dependent on the local biosynthesis of estrogens from testosterone by the aromatase activity of the cells. We found that melatonin reduces the aromatase activity (measured by the tritiated water release assay) of MCF-7 cells both at basal conditions and when aromatase activity was stimulated by cAMP or cortisol. The greatest inhibition of the aromatase activity was obtained with 1 nm melatonin, the same concentration that gives the highest antiproliferative and anti-invasive effects of MCF-7 cells. Finally, by RT-PCR, we found that melatonin downregulates aromatase expression at the transcriptional level in the MCF-7 cells. We conclude that melatonin, at physiological concentrations, decreases aromatase activity and expression in MCF-7 cells. This aromatase inhibitory effect of melatonin, together with its already known antiestrogenic properties interacting with the estrogen-receptor, makes this indoleamine an interesting tool to be considered in.

      When used in full or partial combination, one would obtain the benefits of aromatase inhibition without having to resort to Arimidex, and would get a plethora of health and hair growth promoting benefits in the process.

      When used in conjunction with Propecia or Avodart, the side effects of these drugs would significantly diminish, and their benefit for hair growth enhanced. Feedback from the steroid using bodybuilding community, (often a source of good information) has been positive about the ability of these herbal/supplements to prevent “gyno” or breast enlargement.

      To reiterate-5 AR inhibition plus aromatase inhibition equals better hair growth and better health.





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