Inhibit Aromatase: 31 Potent Supplements

Blocking the aromatase is crucial for decreasing estrogen, whether you have high testosterone or not. The less aromatase leaves more testosterone to bind with androgen receptors as well as to be converted to DHT via 5-AR (5 alpha reductase).

High Estrogen symptoms include:

  • Pelvic pain
  • Night wakings and sweats (can’t sleep through the night)
  • Hot flashes
  • Edema, puffiness, water retention
  • Increased risk of a migraine
  • Low body temp (can also be low thyroid)
  • Brain fog
  • Frequent urination during the night (small bladder feeling)
  • Struggle to build muscle
  • Gyneostema
  • Fatigue and depression
  • Poor memory (estrogen antagonize brain-derived neurotrophic factor (BDNF))

High estrogen in men increases the risk of prostate cancer, autoimmune diseases, diabetes and many other things…

Keep in mind, estrogen and prolactin go hand in hand and some of these symptoms might be the same. More on lowering prolactin here. Estrogen also increases serotonin and inhibits 5-alpha reductase.

Estrogen is classified as a stress hormone. It increases in times of stress, both physical and emotional. Exercise, on the other hand, is a healthy stressor, and actually helps rid the body of estrogen.

Listed below are 31 ways to inhibit the aromatase.

 

1) Increase DHT

DHT, the most powerful androgen, which cannot be aromatized, and is also a powerful aromatase inhibitor itself.

More on boosting DHT here

 

2) Eliminate stress & stabilize blood sugar

Cortisol and noradrenaline increase aromatase and decrease 5-AR activity (1). These two stress hormones are secreted during periods of stress and during low blood sugar. When blood sugar drops, cortisol is secreted to increase blood sugar again. But when an individual has adrenal fatigue and is not producing enough cortisol, adrenaline is secreted instead to raise blood sugar. Signs of high cortisol include: inability to fall asleep, irritability, weight gain, muscle weakness, cognitive dysfunction, inability to detox, etc. Signs of low cortisol include: waking up tired in the mornings, low blood sugar, hypo-tension, fatigue, weak immune system etc.

You can stabilize your blood sugar by eating more protein, less insulinogenic foods (such as starch, glucose rich foods, with the exception of fructose which is not insulinogenic) and more fats. Dietary healthy fats (like coconut oil, butter, cream, etc…) this will provide your body with more stable energy for much longer during the day. Also, eat breakfast – (no oats/breads/cereals) Dairy/meat/eggs with a fruit is a good choice. Get an adaptogen to lower cortisol and which will enable you to become more resilient to stress and balance blood sugar levels. More on lowering cortisol here

 – Ashwagandha – this amazing adaptogen herb could help you with more stable energy through the day, aid in sleep, is also pro-androgens, anti-estrogen and anti-cortisol. More on ashwagandha here…

 

3) Lower the fat

The more fat you have, the greater the aromatase effect (3). So testosterone levels will also automatically increase when you lose body fat (4), as the aromatase enzyme will then be decreased.

Adipose tissue is like a factory that converts testosterone into estrogen, and breaks DHT down to its inactive form.

Having too much body fat is really something you don’t want if you’re wanting to increase testosterone and lower estrogen.

In order to lose weight, you need to follow a healthy meal plan with the right amount of calories and nutrients that will help recover your hormones, fix your glands (thyroid, adrenal gland, etc), and speed up your metabolism. As a result, your testosterone will escalate from being healthier, as well as from the decrease in body fat.

 

4) Coffee/caffeine

Coffee is for sure one of the best beverages of all times.

Lower estrogen is associated with greater coffee intake, as coffee powerfully inhibits the aromatase activity. (5)

In this study, coffee consumption (5 cups a day, for 8 weeks) increased total testosterone and lowered total and free estrogen. Decaffeinated coffee, however, did not have the same effect. Caffeine also increases DHT. More on coffee here

 

5) Tobacco leaf extract/nicotine

The ingredients in tobacco leaves, namely nicotine as well as other tobacco alkaloids, strongly inhibit the aromatase. (5, 6) Purification of nicotine gives n-n-octanoylnornicotine, which inhibits the aromatase more powerfully than just nicotine. (7) Nicotine is a potent stimulant and can increase dopamine, but it can also be addictive, even in capsule form, so proceed with caution.

 

6) White button mushroom extract 

Certain compounds found in the white button mushrooms (WBM), namely beta D glucans, powerfully inhibit the aromatase. (8) Some people saute a bunch of mushrooms in butter and/or coconut oil for 10+ minutes to make a paste and then take a tbsp or more each day, and reported very positive effects in regards to lower estrogen symptoms.

 

7) Grape seed extract

Grape seed extract exerts antioxidant properties and increases microcirculation. Its able to protect testosterone against oxidative stress and inhibit the aromatase. (92g of GSE is needed for sufficient absorption, but the amount taken can be less when black pepper extract is added, as it significantly increases the absorption thereof.

  • GSE – 200mg per cap, 100 caps

 

8) Mangosteen

Four (namely garcinone D, garcinone E, α-mangostin, and γ-mangostin) of the twelve xanthone constituents found in the mangosteen fruit has shown to inhibit the aromatase in a dose dependent manner. Of these 4 xanthone compounds, γ-mangostin is the most potent in inhibiting the aromatase. (10, 11)

  • Mangosteen – 187.5mg Mangosteen Fruit Rind Extract per serving, 60 tablets. (XanoMax standardized to 95% flavonoids and 40% mangostins providing 75 mg of xanthones as mangostins).

 

9) Stinging nettle

This is actually a common weed in most places, especially in South Africa, and it contains histamine on its leaves, that can make you itch and burn when you touch it. It can be used in salads or other dishes, after it’s been washed, as a substitute for lettuce or spinach.

However, it’s not the leaf but the root that inhibits the aromatase. A few compounds in the root, namely secoisolariciresinol, oleanolic and ursolic acid, exert an inhibitory effect on the aromatase, but it appears to be only moderate. (12, 13)

I personally would not use it, as it’s quite a potent 5-AR inhibitor and decreases DHT levels.

  • Nettle root tincture – 2oz (lost empire herbs). Start with 30 drops twice a day under the tongue.

 

10) Chrysin

Chrysin is a flavonoid found in high concentration in raw honey, bee pollen and propolis, which exert an anti-aromatase effect.  (14)

Chrysin has very poor absorption and studies show no increase in testosterone even after 400mg has been ingested. People comment that even 1000mg per serving does nothing in regards to lowering estrogen. “…unmethylated flavones…chrysin (5,7-dihydroxyflavone)…were rapidly eliminated because of extensive glucuronidation and/or sulfation…” However “The methylated flavones showed approximately 5- to 8-fold higher apparent permeability” (15) So unmethylated chrysin (5,7-dihydroxyflavone), doesn’t work in humans, but methylated chrysin (5,7-dimethoxyflavone) could actually work. Methylated chrysin possesses potent anti-inflammatory comparable to aspirin. (16)

  • Chrysin – 500mg per serving, 30 servings

 

11) Hesperidin

A citrus bioflavonoid, found in the peel of an orange, is a very potent aromatase inhibitor. (17) It also increases circulation, is anti-inflammatory and anti-diabetic and has a protective effect on the eyes. 500mg daily would be a good dose to start with.

 

12) Naringenin

Another flavonoid found predominantly in grapefruit, is one of the most potent natural aromatase inhibitors. (18) However, I do not advise eating grapefruit for its flavonoid, as the fruit as a whole inhibits the excretion of estrogen. Naringenin also inhibits adipogenesis (fat formation) and decreases glucose uptake by adipose tissue, and works well with fat burners. (19)

 

13) Apigenin 

This flavonoid is found in very high concentrations in dried parsley, chamomile and a few other foods/herbs. It’s good against anxiety (acts in GABA receptors), contains sedative properties at very high doses and is also able to lower cortisol. It increases steroidogenic acute regulatory protein (StAR) expression (rate limited step), which increases cholesterol transport into the mitochondria to be synthesized to testosterone. Apigenin is also a powerful aromatase inhibitor. (20) It’s very safe and very well tolerated.

 

14) Zinc

Zinc is one of the most important minerals for testosterone production. It increases steroid synthesis, improves thyroid function, lowers SHBG and boosts DHT. Men that are zinc deficient have significantly lower testosterone that men that eat a zinc-sufficient diet. It also has a potent anti-aromatase effect. (21) Raw oysters would be the best food source. Start with 22mg a day. More on zinc here

 

15) Pregnenolone

Pregnenolone is the first endogenous steroid and precursor/metabolic intermediate synthesized from cholesterol. Pregnenolone is proven to lower prolactin, and prolactin in the blood (determined by blood tests) tends to be reliable and the most accurate way to measure estrogen in tissue. Studies show pregnenolone and its metabolites increase dopamine. Lower prolactin levels indicate lower estrogen in tissue (which blood tests cannot measure) as well as lower aromatase activity.

  • IdealabsDC StressNon/Pansterone – 20mg pregnenolone per serving, 30 servings per container for StressNon and 5mg/5mg pregnenlone/DHEA per serving for Pansterone, 90 servings.

 

16) Brassaiopsis glomerulata

This is a small tree that mostly grows in Indonesia. And in India, an indigenous tribe called the Nagas to drink the juice extract of the tree’s bark to aid in digestion and to alleviate constipation. The extract from this tree’s leaves is also shown to be a potent aromatase inhibitor. (22)

 

17) Curcumin

Curcumin, the yellow pigment of turmeric which is its active ingredient, has potent anti-inflammation and anti-cancer properties. Black pepper extract greatly increases its absorption. A very high dose of curcumin is estrogenic and anti-androgenic as it inhibits 17beta-HSD3 (the final enzyme in testosterone synthesis) and 5AR (the enzyme that converts testosterone to DHT). (23, 24) Smaller doses, however, do not have this estrogenic and anti-androgenic effect. It also appears that curcumin reduces the catalytic activity of the aromatase as well as blocks the effect of estrogen at their receptors (tested on animals only). Human studies are needed to confirm this, but many people use curcumin as a potent aromatase inhibitor.

  • Curcumin (with black pepper extract) – 500mg per serving, 120 servings

 

18) Rotenone

Rotenone is a naturally occurring compound extracted from the roots of several tropical plants. It’s been used as a natural insecticide and pesticide. It’s also a very potent aromatase inhibitor.  (25)

 

19) Oleuropein

Oleuropein naturally occurs in olive leaves and olive oil, and is a very a potent aromatase inhibitor which also rivals aromatase inhibitory drugs. It’s “comparable to that of the reference anti-aromatase drug aminoglutethimide“. (26) Olive leaf extract (OLE) is also used to improve thyroid health and metabolism and has many good testimonies.

 

20) Aspirin

The inflammatory marker, COX-2, increases prostaglandin synthesis, which in turn increases the aromatase.

Aspirin is an antioxidant that protects against lipid peroxidation. It inhibits abnormal cell division and prevents excitotoxic nerve injury. It also stimulates mitochondrial respiration which increases energy production, promotes normal cell division and increases learning ability (brain function). The active ingredient in aspirin is salicylic acid, which is protective of the stomach, intestine, and other organs and is a potent anti-inflammatory agent.  Aspirin can very effectively lower cortisol and also COX-2 and thus aromatase.

 

21) Vitamin E

Vitamin E is a fat-soluble vitamin that acts similar to a steroid hormone. It protects and aid in the synthesize of androgens, while powerfully decreasing estrogen and prolactin. It antagonizes estrogen receptors and also inhibits the aromatase. (27) Vitamin E is also known to suppress COX-2, and synergizes with aspirin at opposing estrogen. More on vitamin E here

  • Idealabs TocoVit – 400IU per serving, 30 servings, very pure wheat germ extract with no additives
  • Vitamin E – 400IU per serving, 120 caps. Mixed tocopherol.

 

22) Calcium

A calcium deficiency is associated with significantly higher estradiol as well as elevated aromatase. (28) Calcium is also able to increase energy expenditure, aid in muscle contraction, testosterone synthesis, etc. You can easily make your own calcium supplement from eggshells like I do

 

23) Vitamin A

Vitamin A as retinol and all-trans retinoic acid, significantly blocks the aromatase. (29)

Vitamin A is also great for many other things, check it out here

  • IdealabsDC Retinil – There are two options – retinyl acetate which provides 2,400 IU per drop with 340 drops per container, and retinyl palmitate which provides 5,000 IU per drop with 340 drops per container. The palmitate version is dissolved in MCT and the other in ethanol/water. Both are high purity vitamin A
  • Vitamin A – 2000IU per serving, 100 tablets

 

24) Vitamin D

Vitamin D is a potent aromatase inhibitor, by inhibiting prostaglandins. Vitamin D also helps with mood, increases dopamine (well-being), testosterone, DHT, lowers inflammation and much more. (30) More on vitamin D here

  • Calcirol – 1000IU per serving, 240 servings. High topical absorption
  • Vitamin D – 1000IU per cap, 180 caps

 

25) Vitamin K2

Vitamin K2 (MK-4) is a potent aromatase inhibitor and decreases estradiol levels. Vitamin K2 can increase testosterone significantly when applied topically on the scrotum. (31) More on vitamin K2 here

  • IdealabsDC Kuinone – 1.5mg vitamin K2 (MK-4) per serving, 720 servings, dissolved in SFA (saturates fatty acids) and ethanol for enhanced absorption. This product, while consisting entirely of food-grade ingredients, is sanctioned for external use only (Apply directly on the scrotum to increase testosterone synthesis and inhibit the aromatase)
  • Thorne vitamin K2 (MK-4) – 1mg per drop, 1200 drops

 

26) Selenium

Selenium, a very essential trace mineral, which is involved in the glutathione redox cycle (master anti-oxidant defense of the body), improves thyroid health as well as increases thyroid hormone T4 conversion to T3 (the active thyroid hormone that exert the important functions, such as increase metabolism and steroid synthesis).

Methylseleninic acid (MSA), a second-generation selenium compound, can effectively suppress the aromatase. MSA suppression of aromatase activation is not mediated via direct inhibition of aromatase enzymatic activity. Rather, it is attributable to a marked downregulation of promoters PI.4- (cortisol activation) and PII-specific (activated by FSH, LH and prostaglandin) aromatase mRNA expression, and thereby a reduction of aromatase protein. (32) So basically, selenium inhibits the cortisol, LH and prostaglandins induced activation of the aromatase.

  • Selenium – 200mcg as selenomethionine per serving, 180 servings

 

27) Magnesium

Aromatase activity is decreased in the presence of magnesium. (33) A deficiency in magnesium increases aromatase, and most people are deficient in this nutrient. Even if individuals eat lots of magnesium-rich foods, they can still have a deficiency due to anti-nutrients in the food that binds to magnesium, making it unavailable for absorption. I’d always be very sure to get adequate amounts of this nutrient as it’s involved in more than 300 processes in the body, including steroidogenesis, recovery from exercise, muscle relaxation, mood, etc. as its receptors are found in every tissue in the body. More on magnesium here

 

28) Eurycoma Longifolia Jack

Also known as Tongkat Ali, is a great testosterone boosting herb, that does so by inhibiting the aromatase and increasing free testosterone. Eurycomanone, the major quassinoid in Tongkat Ali is responsible for this effect. (34)

 

29) Ginkgo biloba

Three flavonoids found in ginkgo biloba (kaempferol, quercetin, and isorhamnetin) synergistically inhibit estrogen biosynthesis through aromatase inhibition, by decreasing aromatase mRNA, and suppressing aromatase transcriptional (reduce gene expression). Kaempferol has the most potent effect, however, the inhibitory effect is even greater when the whole herb is taken together, rather than just one of the isolated ingredients. (35) Gingko biloba also increases blood circulation in the whole body as well as to the brain.

 

30) Resveratrol

Resveratrol is a polyphenolic compound that can be isolated from grape peels. Resveratrol inhibits the aromatase at both the enzyme and mRNA levels, similar to gingko biloba. (36) However, resveratrol is estrogenic in itself so I would not advise it.

 

31) Methylene blue

Methylene blue is a very potent aromatase inhibitor with IC50 values of 0.04 and 0.55uM. An oral dose of about 10mg should achieve concentrations of at least 0.5uM in most people, and in fact probably closer to 1uM. Methylene blue also uncouples the mitochondria at concentrations of 0.5uM, which will increase your body temperature, energy expenditure and might aid in weight loss, while you also reap the anti-estrogen benefits with a fairly low dose.

  • Oxidal – 400mcg methylene blue per drop, 240 drops. 12-13 drops will give you 5mg methylene blue.

17 thoughts on “Inhibit Aromatase: 31 Potent Supplements

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