14 Ways to Decrease and Inactivate Estrogen Receptors

Lowering estrogen can be done via a variety of methods, such as inhibiting the aromatase, increasing estrogen detoxification, and inhibiting/decreasing estrogen receptors.

If lowering estrogen seems like “mission impossible”, try lowering its receptors.

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
• Mood swings
• Aggression
• High serotonin symptoms (A)
• High cortisol/adrenal symptoms (A)

Blocking estrogen receptors will be a great way to reduce estrogenic symptoms, while you focus on improving the root cause of high estrogen.

Here are 14 ways to lower estrogen receptors

1) Fatty acid synthase inhibitors

Fatty acid synthase (FAS) is an enzyme that creates fats and cholesterol. FAS blockade knocks down estrogen receptor alpha (ERα) likely via degradation through the ubiquitination-proteasome pathway and/or inhibition of ERα gene expression (1). Plus, FAS uses NADPH as a cofactor.

So first you can reduce NADPH availability to reduce FAS activity, or you can directly inhibit FAS.

NADPH is created by the enzyme glucose 6 phosphate dehydrogenase. DHEA is one of the most potent natural G6PDH inhibitors that will reduce NADPH production, which in turn will reduce FAS.

To directly inhibit FAS, here is a bunch of effective natural inhibitors, namely: Ursolic acid, theaflavin (found in black tea), epigallocatechin-3-gallate (EGCG), extra virgin olive oil derived phenolics (lignans, secoiridoids, and flavonoids), leaves from orange trees, luteolin, quercetin, amentoflavone and Ginkgolic acid (found in Ginkgo biloba), ellagic acid, α-mangostin and γ-mangostin (from mangosteen), curcumin, diosgenin, etc (2).

2) Vitamin E

Vitamin E (alpha-tocopherol) potently reduces estrogen receptors and reduces estrogen sensitivity (3). Gamma-tocopherol is also anti-estrogen, but the alpha-tocopherol is the most hormonally active and is the most effective at lowering prolactin and increasing testosterone. More on vitamin E here…

• Unique E – 400IU α-tocopherol + 432mg blend on γ-tocopherol, δ-tocopherol and β-tocopherol per cap, 30 caps

3) Vitamin A

Vitamin A (retinol), when converted to retinoic acid, binds to retinoic acid receptors, RAR and RXR, which decreases the expression of estrogen receptors (4). But don’t go too crazy, as too much vitamin A can increase CRH, which is inflammatory, which would contribute to inflammatory conditions, such as psoriasis, arthritic symptoms, etc, depression, cortisol excess and so on. More on vitamin A here…

• Vitamin A – 5000IU per cap, 100 caps

4) Vitamin D

Vitamin D (from the diet, sunlight or supplementation) is not merely a vitamin but the essential precursor to the potent steroid hormone, 1,25(OH)₂D₃ or calcitriol. Vitamin D, and calcitriol, inhibits the aromatase and decreases estrogen receptors (5, 6, 7). More on vitamin D here…

• Vitamin D – 1000IU per cap, 180 caps

5) Dihydrotestosterone (DHT)

DHT competes with estradiol for binding (inverse agonist) to the cytosolic estrogen receptor, thus reducing the availability of estrogen receptors (8). DHT doesn’t activate the estrogen receptors, but blocks estrogen from binding to it, thus reducing the potency of estrogen.

DHT treatment is also shown to reduce estrogens’ action, even after estrogen has already bound to its receptor, as DHT significantly reduces estrogen-induced RNA transcription (9). More on boosting DHT here…

6) Caffeine

Caffeine significantly reduces estrogen receptors in a dose-dependent manner (10), and also lowers the aromatase, increase testosterone and DHT as well as androgen receptors. More of coffee/caffeine here…

• Caffeine – 200mg per cap, 100 caps

7) Curcumin

Curcumin, the principal curcuminoid of turmeric, downregulates estrogen receptors activity (11).

8) Prunella Vulgaris

Prunella Vulgaris contains a few active constituents, with ursolic acid (UA) and betulinic acid (BA) being the two responsible for its anti-estrogenic action. The ingestion of UA and BA reduces both mRNA and protein levels of ERα (12).

9) Conjugated linoleic acid (CLA)

CLA has anti-estrogenic properties, as it prevents the phosphorylation of estrogen receptors. Meaning, CLA prevents estrogen receptors from exerting it’s action, even when estrogen has bound to the receptor (13). This does not count for normal linoleic acid, as other polyunsaturated fats, such as linoleic acid, actually activate estrogen receptors, exerting an estrogenic effect (14).

Beef and dairy fat is a good source of CLA.

10) Progesterone

Progesterone decreases the expression of both ERα and ERβ and, as a consequence, also reduces the ER-dependent transcriptional activity (15).

Supplemental pregnenolone is a great way to increase progesterone if it’s low.

• Pregnenolone – 100mg per cap,
• Progestene – 20mg per 12 drops, 30 servings

11) Zinc

It’s been shown that rats that are deficient in zinc have significantly more estrogen receptors, low testosterone and high estrogen, which is indicative of high aromatase activity (16).

Also, a zinc deficiency increases estrogen sensitivity, indicative of more estrogen receptors. Supplemental zinc reverses the sensitivity (17).

• Zinc glycinate – 22mg per cap, 250 caps

12) Iodine

Iodine increases peroxidase activity, which is inversely related to ERα concentration, thus restricting estrogen’s action. Plus, 2-5mg/day of iodine supplementation diminished the translocation of the ERα into the nucleus, preventing its action (18, 19, 20).

• Kelp – 225mcg per cap, 500 caps

13) Niacinamide

Niacinamide is anti-estrogenic by decreasing ERs via SIRT1 inhibition (21). Thus, anything that promotes SIRT1, such as resveratrol, actually increases estrogen receptors.

• Niacinamide – 500mg per cap, 100 caps

14) Histone deacetylase inhibition

Histone deacetylase (HDAC) inhibitors are used to treat cancer and have been found to significantly reduce estrogen receptors (22).

Natural substances that inhibit HDAC include, short-chain fatty acids, such as butyric acid and valeric acid (also found in valerian root), Trichostatin A, niacinamide, biotin, lipoic acid, garlic, vitamin E, CLA, nicotine, curcumin, etc.