Inhibit Aromatase: 31 Potent Supplements

Estrogen, the female hormone, or the modern man hormone?

Men always had estrogen more on the low side of the normal ranges, but nowadays, estrogen is rapidly on the rise and men do experience high estrogen symptoms.

It’s not only due to the rapid conversion of testosterone to estrogen, but also the significant amounts of estrogenic compounds that are found in nature, such as phytoestrogens ( natural estrogens certain foods, such as soy and flax), mold, herbicides, food colorants, especially red colourant, birth control in the water, plastics, and so much more.

But apart from the estrogens in nature, we also convert a lot more testosterone into estrogen than we used to a few decades ago. This is due to a couple of reasons that we’ll discuss below.

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

There is increasing controversy whether estrogen is actually very desirable for men and that men on testosterone replacement therapy (TRT) need high estrogen, which is “protective”. What most estro-philes that promote TRT don’t tell you is that TRT lowers LH. LH signals the testes to produce what? Testosterone? Now you’re jumping the gun. First and foremost, pregnenolone is created, then progesterone and DHEA and then testosterone. What if I told you pregnenolone, progesterone and DHEA is actually the primary cardioprotectors and not estrogen? But that is for another article.

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
• Gynecomastia
• Fatigue and depression
• Poor memory
• Mood swings
• Low libido

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.

Estrogen:

• potently lowers steroidogenesis, much more potent than DHT
• inhibits DHEA production by inhibiting 17 alpha-hydroxylase and (or) C17-C20 lyase activity (R)
• can promote thyroid dysfunction as well as autoimmunity by enhancing NADPH oxidase and excess free radical production (R)
• promotes excess lipolysis that leads to elevated free fatty acids and insulin resistance
• increases IL-17 (R), an inflammatory cytokine, which is potently correlated with anhedonia and autoimmune disease.
• increase the risk of stroke and thrombosis (R), by promoting excess blood clotting
• promotes anxiety
• increases serotonin production and potentiates the effect of serotonin
• creates gyno
• increases total and free cortisol. This effect is blunted by progesterone (R, R)
• elevates prolactin
• promotes aldosterone, which causes water retention (R)
• increases adipogenesis (creation of new fat cells) (R)
• increases thyroxine-binding globulin, which decreases free thyroid hormones (R)
• increases fat uptake in the adipose tissue by increasing PPARγ and fatty acid-binding protein (R).
• increases brain excitation and can contribute to seizures. Aromatase inhibitors are useful against epilepsy (R)
• Reduces bile flow from the liver to the gallbladder, which can lead to intrahepatic cholestasis (R). This can lead to the skin and whites of the eyes looking yellow, the skin itches, urine is dark, and stools may become light-coloured and smell foul.
• increases lactate production from glucose which is a very ineffective method of producing energy. Lactate itself also possesses many negative effects (R).
• promotes migraines (R)
• causes testicular degeneration (R)
• decreases FGF21, which result in lower thermogenesis and energy expenditure (R)

Pretty shocking if you ask me.

Now let’s discuss how to lower it. First I’ll discuss a few free methods on how to control/lower aromatase and then I’ll jump into the supplements.

#1 Increase DHT

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

> How to increase DHT

#2 Stabilize Blood sugar

Cortisol, noradrenaline and adrenaline are involved in blood sugar regulation and if blood sugar drops too low, these hormones are released to pick it back up and prevent low blood sugar. Thing is, these hormones promote the aromatase, increase estrogen and actually causes insulin resistance in the first place which causes blood sugar roller coasters. It’s not sugar or glucose, it’s cortisol dysregulation that’s causing it.

So the first thing you can do to fix cortisol is to prevent blood sugar roller coasters. One way to do this is to snack every hour, but this is not feasible or desired for most.

A few simple tricks are to:

• Avoid insulinogenic foods in the morning. A low protein, low GI, high-fat breakfast would work perfectly here. Nuts, fruit and gelatin can work perfectly for this. A simple smoothie recipe includes 1-2 cups of coconut milk, 1 tbsp cocoa powder, 1 tbsp raw honey (or monk fruit sweetener), 2 tbsp hydrolyzed gelatin, a handful of berries and a small mango.
• A moderate protein and carb lunch.
• A moderate protein and high carb dinner.

The reason for this is that most people with cortisol dysregulation are most insulin resistant in the morning and insulin sensitivity improve later in the day. Doing a training session before dinner is also a great way to improve insulin sensitivity before the high carb meal.

I’m not pro-low carb at all, but I’m all about finding foods and following a routine that doesn’t take you on a blood sugar roller coaster. Very low carb intake will further increase cortisol to pick blood sugar up again, so you do need carbs. About 100-200 grams daily while recovering is a good start. 

You can also do things to improve your blood sugar along the way. Check out my Facebook post on it:

#3 Lose excess fat

The more fat you have, the more aromatase you’ll have (R). Also, the less fat you have the more testosterone you’ll have due to less inhibitory feedback from estrogen.

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 want to maximize 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 Eat lots of nutrients dense foods

Eating the right diet for you is fundamental for keeping estrogen low. Apart from stabilizing blood sugar, the nutrients in the food are also very important for keeping estrogen low.

A calcium deficiency is associated with significantly higher estradiol as well as elevated aromatase (R). 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… If you don’t tolerate milk very well, goats milk is a great alternative and is tolerated by most. Getting used to the taste might take some time though.

Vitamin A as retinol and all-trans retinoic acid significantly blocks the aromatase (R). Instead of supplementing it, you can rather eat vitamin A rich foods, such as leafy greens, pumpkin, butternut, liver, eggs, papaya, oranges, etc.

Men low in zinc have reduced testosterone levels and an elevated estrogen to testosterone ratio. Eating more zinc-rich foods or supplementing zinc increases testosterone, inhibits the aromatase and lowers estrogen.

Selenium lowers the aromatase and boosts the metabolic rate.

Flavonoids, such as apigenin, hesperidin, kaempferol, quercetin and naringenin are potent inhibitors of the aromatase and are found in food like parsley, camomile tea, onions, potatoes, citrus fruit, etc.

#5 Get ample sunlight

Sunlight is fantastic for your health and we often get way too little direct sunlight on our skins. Vitamin D, that is synthesized from the rays on the sun, is a potent aromatase inhibitor. Men with low vitamin D often have elevated estrogen.

#6 Lower stress

Stress increases cortisol, which increases the aromatase. 

> Lower cortisol article

# 7 Lower inflammation

Inflammation, together with elevated cortisol and insulin, is the major drivers of the aromatase and can boost it many fold. If you want to lower inflammation, check out this article where I discuss some of the most common inducers of inflammation.

> 4 most important things for health, androgens and longevity

Now, let’s discuss some supplements that are effective at lowering aromatase.

#1 Androsterone

Androsterone is structurally very similar to the aromatase inhibitor Aromasin and is almost equally potent at inhibiting the aromatase. Although no human studies have been done yet, many men have used this an reported that it’s potent anti-estrogen even in low doses. A dose as low as 1mg can have an effect and doses up to 15mg is safe.

I’d recommend that if you are estrogen dominant that you use 15mg daily for about 2-4 weeks and then taper off to 5mg daily and then stick to that dose.

• Androsterone – (IdealabsDC)

#2 Nicotine

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

#3 Caffeine/coffee

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

Coffee intake is associated with lower estrogen levels, as coffee powerfully inhibits the aromatase activity (R).

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.

> Coffee, the manliest drink 

#4 White button mushrooms

Certain compounds found in the white button mushrooms (WBM), namely beta D glucans, powerfully inhibit the aromatase (R). You can saute a bunch of mushrooms in butter and/or coconut oil for 20+ minutes and then store it in the fridge and have a tbsp per day or eat all of it. Eat a bunch of sauteed mushrooms every day or every other day should have a potent anti-estrogenic effect.

#5 Grape seed extract

Grape seed extract exerts antioxidant properties and increases microcirculation. It’s able to protect testosterone against oxidative stress and inhibit the aromatase (R). 2g 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. 

#6 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 (R, R).

#7 Stinging nettle

Stinging nettle is a very common and popular supplement used to lower DHT. However, it can also lower 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 (R, R).

If you want to maximize DHT, which is a good idea, then stinging nettle might not be the best choice for lowering estrogen. 

#8 Chrysin

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

Now before you just exit this article because you know chrysin is ineffective, hear me out.

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.

This study (R) claims that:

“…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” 

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 (R). So don’t waste your money on plain chrysin, get yourself the methylated version (Amazon). 5,7-dimethoxyflavone is also naturally found in Thai black ginger.

#8 Hesperidin

A citrus bioflavonoid, found in the peel of an orange, is a very potent aromatase inhibitor (R). 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.

#9 Naringenin

Another flavonoid found predominantly in grapefruit, is one of the most potent natural aromatase inhibitors (R). However, I do not recommend 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 (R). (Amazon)

#10 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 (R). It’s very safe and very well tolerated. (Amazon)

#11 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 than men that eat a zinc-sufficient diet. It also has a potent anti-aromatase effect (R). Raw oysters would be the best food source.

> Zinc article

• Zinc glycinate – (Amazon, iHerb)

#12 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 (R).

#13 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) (R, R). Smaller doses, around 500mg or less, 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 – (Amazon, iHerb)

#14 Olive leaf extract

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

• Olive leaf extract – (Amazon, iHerb)

#15 Aspirin

I’m personally a huge fan of aspirin. It’s able to significantly lower excess cortisol and potently inhibit the aromatase and boost testosterone production. Just 800mg twice daily for 10 days is enough to gain significant benefits. (Amazon)

#16 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 (R). Vitamin E is also known to suppress COX-2 and synergizes with aspirin at opposing estrogen. More on vitamin E here…

• Vitamin E – (Amazon, iHerb, IdealabsDC (product: TocoVit))

#17 Vitamin D

Vitamin D is a potent aromatase inhibitor. Vitamin D also helps with mood, increases dopamine (well-being), testosterone, DHT, lowers inflammation and much more (R).

> Vitamin D: the steroid vitamin

• Vitamin D – (Amazon, iHerb)

#18 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 (R).

> Vitamin K2 article 

• Vitamin K2 – (Amazon, iHerb)

#19 Selenium

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 (R). So basically, selenium inhibits the cortisol, LH and prostaglandins induced activation of the aromatase.

• Selenium – (Amazon, iHerb)

#20 Magnesium

Aromatase activity is decreased in the presence of magnesium (R). 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 as well as being in a low energy state. Optimal energy production in the body aids in the retention of magnesium and if you have low ATP production, chances are that your body is just wasting the magnesium away. 

> Magnesium article

• Oral magnesium – (Amazon, iHerb)
• Topical magnesium – (Amazon, iHerb, IdealabsDC (product: Magniol))

#21 Tongkat Ali

Tongkat Ali is a great testosterone/libido 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 (R).

> Tongkat Ali article

• Tongkat Ali – (Amazon)

#22 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 (R). Gingko Biloba also increases blood circulation in the whole body as well as to the brain. 

• Ginkgo Biloba – (Amazon, iHerb, NeuroActive (use the link to get 10% off))

#23 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 (R), however, resveratrol itself is highly estrogenic so I would not recommend using it.

#24 Methylene blue

In vitro studies show that methylene blue inhibits the aromatase, but no in vivo studies have been done yet to show its hormone-altering effect. I’m personally also a huge fan of methylene blue as it can rescue energy production, increase the NAD/NADH ratio, improve tissue oxygenation, act as a nootropic, lower oxidative stress, lower excess nitric oxide production, lower inflammation and act as an anti-viral just to name a few.