NATURAL AROMATASE INHIBITORS

[Logan-]

Through research and experience, I’ve come to the conclusion that aromatase inhibition is crucial for having high testosterone. Many who take DHEA, DHT, T. etc. and don’t experience the expected conditions of having high T, may benefit from the inhibition of aromatase.

Well cooked button mushrooms are well-known aromatase inhibitors. Their effects in this regard are easily noticeable.

IIRC, Ray has talked about OJ in this regard.

I‘ve read in numerous studies that ginger consumption increases testosterone, but I cannot remember if it was due to aromatase inhibition or some other mechanisms.

What are some other safe and natural ways to decrease the conversion of T into estrogen?

It’s also been mentioned numerous times that good laxatives like cascara sagrada, and things like carrot salad, bamboo shoots decrease estrogen.

 

[ddjd]

- nettle root
- green tea
- mangosteen
- German chamomile
- orange juice/ peel
- oregano
- tarragon
- grape seed extract (Pycnogenol)
- raw onion
- guava (apigenin is an AI)
- watercress
- turmeric
- coriander
- brocolli sprout
- rosemary
- sage
- marjoram
- chasteberry
- Dandelion root
- parsley
- wasabi root powder

 

[learnedhelpless]

Vitamin E (tocopherol) Is A Potent Aromatase Inhibitor

Hi all, As you know Ray has written extensively on the benefits of Vitamin E though its actions as an estrogen antagonist. I opsted some studies that show that tocopherols act directly like estrogen "receptor" antagonist and this may explain some of their anti-estrogenic properties. However...

raypeatforum.com

I think methylene blue and very high doses of cheap alpha tocopherol, would be the best natural ones ( I am not sure if methylene blue is natural though)

 

[youngsinatra]

White button mushrooms are very powerful. I cannot eat them regularly, because it drops my estradiol too much and I get low estrogen symptoms. (flat mood, apathy, destroyed libido, joint pains)

 

[ecstatichamster]

I think aspirin is good for this.

 

[Bozidar]

Haha, I must laugh.
Somebody wrote in some other thread: I realized we went 17 minutes without discussing aromatase inhibitor and then he posted an article on aromatase inhibition.
Explored that topic myself, there is really so much resources here on aromatase inhibition.
I have nettle root, mangosteen and grape seed extract scheduled to try out. To bad I don't find white button mushroom as a supplement for that purpose.

 

[Marcia]

Dr. Chi from Chi Enterprises sells a product named Myomin, that is quite effective.

 

[Logan-]

I have long suspected this considering the peculiar side effects of some AI drugs, but was not able to find concrete evidence...until now. The study below demonstrates that one of the most widely used AI - anastrozole - is a potent estrogen receptor activator/agonist, and at low concentrations too. At higher concentrations, the estrogenic effects seem to disappear but those concentrations are not achievable with clinically used doses. As such, for most people taking anastrozole in the clinically-approved 1mg-2mg (or lower) doses daily, the drug is a potent estrogen activator, which likely negates most of the benefit of inhibiting aromatase. While the closely-related analog letrozole apparently did not have estrogenic effects, structurally the drugs are very similar and produce very similar side effects. As such, I suspect letrozole also has at least partial estrogen agonism. The steroidal AI exemestane did not display estrogenic effects, and it also happens to not produce the side effects associated with the *zole drugs. Several studies have demonstrated that exemestane metabolizes into the potent androgen 17-beta-OH-6-methylene-boldenone, and that metabolite has anti-estrogenic effects similar to other androgens such as testosterone, DHT, Masteron, etc., all of which have been successfully used in the past for treating breast cancer. IMO, this androgenic property makes steroidal AI drugs such as exemestane, formestane, and atamestane less risky than the *zoles, especially if the steroidal AI are combined with endogenous anti-estrogens such as progesterone.

Anastrozole has an Association between Degree of Estrogen Suppression and Outcomes in Early Breast Cancer and is a Ligand for Estrogen Receptor α - PubMed

"...Results: Women with E1 ≥1.3 pg/mL and E2 ≥0.5 pg/mL after 6 months of AI treatment had a 2.2-fold increase in risk (P = 0.0005) of an EBCE, and in the anastrozole subgroup, the increase in risk of an EBCE was 3.0-fold (P = 0.001). Preclinical laboratory studies examined mechanisms of action in addition to aromatase inhibition and showed that only anastrozole could directly bind to estrogen receptor α (ERα), activate estrogen response element-dependent transcription, and stimulate growth of an aromatase-deficient CYP19A1-/- T47D breast cancer cell line. Conclusions: This matched case-control clinical study revealed that levels of estrone and estradiol above identified thresholds after 6 months of adjuvant anastrozole treatment were associated with increased risk of an EBCE. Preclinical laboratory studies revealed that anastrozole, but not exemestane or letrozole, is a ligand for ERα. These findings represent potential steps towards individualized anastrozole therapy."

"...However, in CYP19A1 KO T47D cells, only anastrozole at 0.1–10 nM resulted in increased cell proliferation, with a decrease in cell proliferation when anastrozole concentrations increased to 100–500 nM (Fig. 2B). In CYP19A1 KO T47D cells, treatment with exemestane or letrozole at the same concentrations (0.1 to 500 nM) did not affect cell proliferation compared with vehicle-treated cells (Supplementary Fig. S8B)."

Damiana extract has Acacetin.
Aromatase inhibitors and estrogen blockers: Nature's answer to xenoestrogens and aging
Acacetin (4'methoxy-5,7-dihydroxyflavone) is one of natural aromatase inhibitors isolated from the damiana plant which may suppress up to 63 percent of aromatase activity. Unlike some other natural AI's, it has no estrogenic activity at all.

Some aromatase inhibitors (AI) are estrogenic

I have long suspected this considering the peculiar side effects of some AI drugs, but was not able to find concrete evidence...until now. The study below demonstrates that one of the most widely used AI - anastrozole - is a potent estrogen receptor activator/agonist, and at low concentrations...

raypeatforum.com

 

[PopSocket]

I recently decided to experiment with mushrooms eating a big amount at least once a day and they are indeed extremely powerful.

Just like @youngsinatra said - total blow on the libido. And I thought my libido was low due to methylene blue,thyroid and other peaty foods/supplements but mushrooms killed it completely. Feeling like a small child. But very calm. I even tried raising my NO with a good dose cialis and it did not work.

 

[Logan-]

I recently decided to experiment with mushrooms eating a big amount at least once a day and they are indeed extremely powerful.

Just like @youngsinatra said - total blow on the libido. And I thought my libido was low due to methylene blue,thyroid and other peaty foods/supplements but mushrooms killed it completely. Feeling like a small child. But very calm. I even tried raising my NO with a good dose cialis and it did not work.

I have also been consuming mushrooms every day (for gut health and as a copper source), and I have never experienced erectile dysfunction with them. If anything, aromatase inhibition should improve sexual function. Ray said high estrogen can cause insatiable sexual desire, but at the same time estrogen worsens sexual functioning in men.

 

[PopSocket]

I have also been consuming mushrooms every day (for gut health and as a copper source), and I have never experienced erectile dysfunction with them. If anything, aromatase inhibition should improve sexual function. Ray said high estrogen can cause insatiable sexual desire, but at the same time estrogen worsens sexual functioning in men.

I already have very low E levels without using anything. When I add vit E, k2, mushrooms, MB, OJ and other stuff it gets too low I think. It is normally needed in small amounts for sexual function and libido.

 

[Logan-]

I already have very low E levels without using anything. When I add vit E, k2, mushrooms, MB, OJ and other stuff it gets too low I think. It is normally needed in small amounts for sexual function and libido.

Have you ever checked your serum E, PRL, T, SHBG, cortisol levels?

 

[Pete Rey]

Funny thing. I view testosterone cream as self-regulating for me personally, because beyond replacement levels I quickly get side effects. But when I first tried thyroid I noticed that threshold went up quite a bit. I was able to run it hot for a few days just to see what it felt like.

 

[PopSocket]

Have you ever checked your serum E, PRL, T, SHBG, cortisol levels?

yes, E is undetectable no matter how low the lab tests for, even 1/3 of the lower range, still nothing shows up, prl is normal low range, T is usually at the top of the range, cortisol is normal low range, even when I do topical T cycles and bump my T 2-3x the normal range E is still undetectable. Never done tissue analysis. No idea what is going on with E. SHBG used to be high, now it is at the top of the range or slightly above.

 

[PopSocket]

Funny thing. I view testosterone cream as self-regulating for me personally, because beyond replacement levels I quickly get side effects. But when I first tried thyroid I noticed that threshold went up quite a bit. I was able to run it hot for a few days just to see what it felt like.

What sides do you get from too much topical T ?

 

[Logan-]

yes, E is undetectable no matter how low the lab tests for, even 1/3 of the lower range, still nothing shows up, prl is normal low range, T is usually at the top of the range, cortisol is normal low range, even when I do topical T cycles and bump my T 2-3x the normal range E is still undetectable. Never done tissue analysis. No idea what is going on with E. SHBG used to be high, now it is at the top of the range or slightly above.

What, do you think, causes/contributes to the most about this state of yours? What are the things that you do and don’t do that cause you to be in this condition? A little context would help; i.e. your age, weight, height, lifestyle etc., if you don’t mind sharing.

 

[Pete Rey]

What sides do you get from too much topical T ?

High blood pressure, cystic acne, soreness behind the nipple (I know that's a prolactin thing, but an AI seems to resolve it).

 

[Logan-]

Anti-aromatase activity of phytochemicals in white button mushrooms (Agaricus bisporus)​

Shiuan Chen et al. Cancer Res. 2006.

Abstract​

White button mushrooms (Agaricus bisporous) are a potential breast cancer chemopreventive agent, as they suppress aromatase activity and estrogen biosynthesis. Therefore, we evaluated the activity of mushroom extracts in the estrogen receptor-positive/aromatase-positive MCF-7aro cell line in vitro and in vivo. Mushroom extract decreased testosterone-induced cell proliferation in MCF-7aro cells but had no effect on MCF-10A, a nontumorigenic cell line. Most potent mushroom chemicals are soluble in ethyl acetate. The major active compounds found in the ethyl acetate fraction are unsaturated fatty acids such as linoleic acid, linolenic acid, and conjugated linoleic acid. The interaction of linoleic acid and conjugated linoleic acid with aromatase mutants expressed in Chinese hamster ovary cells showed that these fatty acids inhibit aromatase with similar potency and that mutations at the active site regions affect its interaction with these two fatty acids. Whereas these results suggest that these two compounds bind to the active site of aromatase, the inhibition kinetic analysis indicates that they are noncompetitive inhibitors with respect to androstenedione. Because only conjugated linoleic acid was found to inhibit the testosterone-dependent proliferation of MCF-7aro cells, the physiologically relevant aromatase inhibitors in mushrooms are most likely conjugated linoleic acid and its derivatives. The in vivo action of mushroom chemicals was shown using nude mice injected with MCF-7aro cells. The studies showed that mushroom extract decreased both tumor cell proliferation and tumor weight with no effect on rate of apoptosis. Therefore, our studies illustrate the anticancer activity in vitro and in vivo of mushroom extract and its major fatty acid constituents.

Chen S, Oh SR, Phung S, Hur G, Ye JJ, Kwok SL, Shrode GE, Belury M, Adams LS, Williams D. Anti-aromatase activity of phytochemicals in white button mushrooms (Agaricus bisporus). Cancer Res. 2006 Dec 15;66(24):12026-34. doi: 10.1158/0008-5472.CAN-06-2206. PMID: 17178902.

 

[Logan-]

White button mushroom phytochemicals inhibit aromatase activity and breast cancer cell proliferation​

B J Grube et al. J Nutr. 2001 Dec.

Abstract​

Estrogen is a major factor in the development of breast cancer. In situ estrogen production by aromatase/estrogen synthetase in breast cancer plays a dominant role in tumor proliferation. Because natural compounds such as flavones and isoflavones have been shown to be inhibitors of aromatase, it is thought that vegetables that contain these phytochemicals can inhibit aromatase activity and suppress breast cancer cell proliferation. Heat-stable extracts were prepared from vegetables and screened for their ability to inhibit aromatase activity in a human placental microsome assay. The white button mushroom (species Agaricus bisporus) suppressed aromatase activity dose dependently. Enzyme kinetics demonstrated mixed inhibition, suggesting the presence of multiple inhibitors or more than one inhibitory mechanism. "In cell" aromatase activity and cell proliferation were measured using MCF-7aro, an aromatase-transfected breast cancer cell line. Phytochemicals in the mushroom aqueous extract inhibited aromatase activity and proliferation of MCF-7aro cells. These results suggest that diets high in mushrooms may modulate the aromatase activity and function in chemoprevention in postmenopausal women by reducing the in situ production of estrogen.

Grube BJ, Eng ET, Kao YC, Kwon A, Chen S. White button mushroom phytochemicals inhibit aromatase activity and breast cancer cell proliferation. J Nutr. 2001 Dec;131(12):3288-93. doi: 10.1093/jn/131.12.3288. PMID: 11739882.

 

[Logan-]

Table 1​

Previous literature reports of natural product extracts tested for aromatase inhibition

Species Name​	Common Name​	Family​	Type​	Extraction Solvent​	Assay Type​	Activity​	Ref.(s)​
Aesculus glabra​	Ohio buckeye​	Hippocastanaceae​	plant​	methanol (CHCl3partition)​	microsomes​	42.0​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	baby button mushroom​	Agaricaceae​	fungus​	water reflux​	microsomes​	~58​	PCA at 100 μL​	[115]​
Agaricus bisporus​	crimini mushroom​	Agaricaceae​	fungus​	water reflux​	microsomes​	~46​	PCA at 100 μL​	[115]​
Agaricus bisporus​	portobello mushroom​	Agaricaceae​	fungus​	water reflux​	microsomes​	~45​	PCA at 100 μL​	[115]​
Agaricus bisporus​	stuffing mushroom​	Agaricaceae​	fungus​	water reflux​	microsomes​	~20​	PCA at 100 μL​	[115]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water reflux​	microsomes​	~35​	PCA at 100 μL​	[115]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water reflux​	MCF-7aro cells​	14​	at 10 μL/mL​	[115]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (air dried)​	microsomes​	83.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (air dried, hexane partition)​	microsomes​	71.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (air dried, CHCl3partition)​	microsomes​	51.7​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (air dried, water partition)​	microsomes​	63.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (air dried, butanol partition)​	microsomes​	82.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (dehydrated)​	microsomes​	94.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (dehydrated, hexane partition)​	microsomes​	55.3​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (dehydrated, CHCl3 partition)​	microsomes​	54.7​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (dehydrated, water partition)​	microsomes​	73.5​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (dehydrated, butanol partition)​	microsomes​	55.0​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (fresh)​	microsomes​	66.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (fresh, hexane partition)​	microsomes​	72.7​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (fresh, CHCl3 partition)​	microsomes​	78.8​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (fresh, water partition)​	microsomes​	89.6​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (fresh, butanol partition)​	microsomes​	79.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	acetone (fresh)​	microsomes​	59.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	acetone (fresh, hexane partition)​	microsomes​	38.3​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	acetone (fresh, CHCl3 partition)​	microsomes​	39.2​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	acetone (fresh, water partition)​	microsomes​	81.5​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	acetone (fresh, butanol partition)​	microsomes​	85.3​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water (reflux)​	microsomes​	96.2​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water (reflux, hexane partition)​	microsomes​	80.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water (reflux, CHCl3 partition)​	microsomes​	56.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water (reflux, water partition)​	microsomes​	79.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	water (reflux, butanol partition)​	microsomes​	65.3​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (sautéed)​	microsomes​	85.8​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (sautéed, hexane partition)​	microsomes​	53.5​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (sautéed, CHCl3partition)​	microsomes​	68.2​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (sautéed, water partition)​	microsomes​	83.8​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	methanol (sautéed, butanol partition)​	microsomes​	57.1​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	white button mushroom​	Agaricaceae​	fungus​	Dichloromethane​	microsomes​	54.4​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	cremini mushroom​	Agaricaceae​	fungus​	Dichloromethane​	microsomes​	65.7​	PCA at 20 μg/mL​	[143]​
Agaricus bisporus​	portobella mushroom​	Agaricaceae​	fungus​	Dichloromethane​	microsomes​	59.1​	PCA at 20 μg/mL​	[143]​
Agaricus blazei(1SY16)​	almond mushroom​	Agaricaceae​	fungus​	Unknown​	microsomes​	87.7​	PCA at 20 μg/mL​	[143]​
Agaricus blazei​	almond mushroom​	Agaricaceae​	fungus​	Methanol​	microsomes​	75.2​	PCA at 20 μg/mL​	[143]​
Agaricus blazei​	almond mushroom​	Agaricaceae​	fungus​	methanol (hexane partition)​	microsomes​	72.5​	PCA at 20 μg/mL​	[143]​
Agaricus blazei​	almond mushroom​	Agaricaceae​	fungus​	methanol (dichloromethane partition)​	microsomes​	82.1​	PCA at 20 μg/mL​	[143]​
Agaricus blazei​	almond mushroom​	Agaricaceae​	fungus​	methanol (water partition)​	microsomes​	88.4​	PCA at 20 μg/mL​	[143]​
Agaricus blazei​	almond mushroom​	Agaricaceae​	fungus​	Dichloromethane​	microsomes​	74.5​	PCA at 20 μg/mL​	[143]​
Allium sp.a​	green onion​	Liliaceae​	plant​	water reflux​	microsomes​	~75​	PCA at 100 μL​	[115]​
Allium sp.a​	green onions​	Liliaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Allium sp.a​	spanish onions​	Liliaceae​	plant​	70% ethanol​	microsomes​	310​	units/100 g​	[113]​
Allium sp.a​	white onions​	Liliaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Alpinia purpurata​	red ginger​	Zingerberaceae​	plant​	75% MeOH reflux​	microsomes​	~78​	% inhib.​	[105]​
Althaea roseavar. nigra​	hollyhock​	Malvaceae​	plant​	Nd​	immunocytochemistry in Leydig cells​	weak​	​	[181]​
Apium graveolens a​	celery​	Apiaceae​	plant​	water reflux​	microsomes​	~80​	PCA at 100 μL​	[115]​
Apium graveolens a​	celery​	Apiaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Asparagus officinalis a​	asparagus​	Liliaceae​	plant​	70% ethanol​	microsomes​	1300​	units/100 g​	[113]​
Auricularia sp.​	woodear mushroom​	Auriculariaceae​	fungus​	water reflux​	microsomes​	~86​	PCA at 100 μL​	[115]​
Brassaiopsis glomerulata(leaves)​	none​	Araliaceae​	plant​	methanol (hexane partition)​	microsomes​	6.9​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(leaves)​	none​	Araliaceae​	plant​	methanol (ethyl acetate partition)​	microsomes​	59.3​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(leaves)​	none​	Araliaceae​	plant​	methanol (water partition)​	microsomes​	98.2​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(leaves)​	none​	Araliaceae​	plant​	methanol (hexane partition)​	SK-BR-3 cells​	7.2​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(leaves)​	none​	Araliaceae​	plant​	methanol (ethyl acetate partition)​	SK-BR-3 cells​	37.0​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(twigs)​	none​	Araliaceae​	plant​	methanol (hexane partition)​	microsomes​	35.6​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(twigs)​	none​	Araliaceae​	plant​	methanol (ethyl acetate partition)​	microsomes​	46.6​	PCA at 20 μg/mL​	[143]​
Brassaiopsis glomerulata(twigs)​	none​	Araliaceae​	plant​	methanol (water partition)​	microsomes​	95.8​	PCA at 20 μg/mL​	[143]​
Brassica junceaa​	mustard (greens)​	Brassicaceae​	plant​	70% ethanol​	microsomes​	2700​	units/100 g​	[113]​
Brassica oleracea a​	broccoli​	Brassicaceae​	plant​	water reflux​	microsomes​	~85​	​	[115]​
Brassica oleracea a​	broccoli​	Brassicaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Brassica oleracea a​	broccoli (leaves)​	Brassicaceae​	plant​	70% ethanol​	microsomes​	3600​	units/100 g​	[113]​
Brassica oleracea a​	cabbage​	Brassicaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Brassica oleracea a​	cauliflower​	Brassicaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Brassica oleracea a​	collards​	Brassicaceae​	plant​	70% ethanol​	microsomes​	8500​	units/100 g​	[113]​
Brassica oleracea a​	kale​	Brassicaceae​	plant​	70% ethanol​	microsomes​	4700​	units/100 g​	[113]​
Brassica rapavar. rapaa​	turnips​	Brassicaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Camellia sinensis a​	black tea​	Theaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Camellia sinensis a​	green tea​	Theaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Camellia sinensis a​	green tea (polyphenone-60)​	Theaceae​	plant​	Nd​	microsomes​	28​	μg/mL IC50​	[112]​
Camellia sinensis a​	tea​	Theaceae​	plant​	70% ethanol​	microsomes​	27000​	units/100 g​	[113]​
Cantharellus sp.​	chanterelle mushroom​	Cantharellaceae​	fungus​	water reflux​	microsomes​	~80​	PCA at 100 μL​	[115]​
Capsicum annuuma a​	bell pepper​	Solanaceae​	plant​	water reflux​	microsomes​	~89​	PCA at 100 μL​	[115]​
Capsicum sp.a​	pepper (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	2800​	units/100 g​	[113]​
Capsicum sp.a​	peppers​	Solanaceae​	plant​	70% ethanol​	microsomes​	330​	units/100 g​	[113]​
Cestrum sp.​	none​	Solanaceae​	plant​	75% MeOH reflux​	microsomes​	~40​	% inhib.​	[105]​
Chrysanthemum partheniuma a​	feverfew​	Asteraceae​	plant​	Nd​	​	>50​	% inhib.​	[182]​
Cichorium endivia a​	endive​	Asteraceae​	plant​	70% ethanol​	microsomes​	850​	units/100 g​	[113]​
Cichorium endivia a​	escarole​	Asteraceae​	plant​	70% ethanol​	microsomes​	830​	units/100 g​	[113]​
Citrus × limonaa​	lemons​	Rutaceae​	plant​	70% ethanol​	microsomes​	660​	units/100 g​	[113]​
Citrus paradisia​	grapefruit (juice)​	Rutaceae​	plant​	Nd​	microsomes​	~68​	PCA at 25 μL​	[183]​
Citrus sinensis a​	orange​	Rutaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Citrus sinensis a​	orange (juice)​	Rutaceae​	plant​	Nd​	microsomes​	~90​	PCA at 25 μL​	[183]​
Coccothrinaxsp.​	none​	Arecaceae​	plant​	75% MeOH reflux​	microsomes​	~70​	% inhib.​	[105]​
Coffea sp.a​	coffee​	Rubiaceae​	plant​	70% ethanol​	microsomes​	13000​	units/100 g​	[113]​
Coix lachrymal-jobi var. ma-yuen​	adlay or Job's tears​	Poaceae​	plant​	Methanol​	rat granulose cells​	inhibits​	activity at 100 μg/mL​	[184]​
Cucumis melo a​	cantaloupe​	Cucurbitaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Cucumis sativusa​	cucumber​	Loasaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Curcuma longaa​	turmeric​	Zingiberaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Cycas cairnsiana​	none​	Cycadaceae​	plant​	75% MeOH reflux (ethyl acetate partition)​	microsomes​	69​	% inhib.​	[104]​
Cycas revoluta​	sago palm​	Cycadaceae​	plant​	75% MeOH reflux (methanol partition)​	microsomes​	79​	% inhib.​	[104]​
Cycas revoluta​	sago palm​	Cycadaceae​	plant​	75% MeOH reflux (ethyl acetate partition)​	microsomes​	86​	% inhib.​	[104]​
Cycas rumphii​	none​	Cycadaceae​	plant​	75% MeOH reflux (methanol partition)​	microsomes​	90​	% inhib.​	[104]​
Cycas rumphii​	none​	Cycadaceae​	plant​	75% MeOH reflux (ethyl acetate partition)​	microsomes​	15​	% inhib.​	[104]​
Daucus carota a​	carrot​	Apiaceae​	plant​	water reflux​	microsomes​	~74​	PCA at 100 μL​	[115]​
Daucus carota a​	carrot​	Apiaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Dioon spinulosum​	none​	Zamiaceae​	plant​	75% MeOH reflux (methanol partition)​	microsomes​	40​	% inhib.​	[104]​
Dioon spinulosum​	none​	Zamiaceae​	plant​	75% MeOH reflux (ethyl acetate partition)​	microsomes​	97​	% inhib.​	[104]​
Encephalartos ferox​	bread palm​	Zamiaceae​	plant​	75% MeOH reflux (methanol partition)​	microsomes​	45​	% inhib.​	[104]​
Encephalartos ferox​	bread palm​	Zamiaceae​	plant​	75% MeOH reflux (ethyl acetate partition)​	microsomes​	97​	% inhib.​	[104]​
Epilobium capense​	willowherb​	Onagraceae​	plant​	aqueous methanol​	microsomes​	60​	% inhib. at 200 μg​	[130]​
Epilobium capense​	willowherb​	Onagraceae​	plant​	Methanol​	microsomes​	54​	% inhib. at 200 μg​	[130]​
Euonymus alatus​	“gui-jun woo”​	Celastraceae​	plant​	water reflux​	microsomes​	11​	μg/mL IC50​	[111]​
Euonymus alatus​	“gui-jun woo”​	Celastraceae​	plant​	water reflux​	myometrial cells​	0.80​	μg/mL IC50​	[111]​
Euonymus alatus​	“gui-jun woo”​	Celastraceae​	plant​	water reflux​	leiomyonal cells​	0.07​	μg/mL IC50​	[111]​
Flammulina velutipes​	enoki mushroom​	​	fungus​	water reflux​	microsomes​	~78​	PCA at 100 μL​	[115]​
Fragaria sp.a​	strawberry (juice)​	Rosaceae​	plant​	Nd​	microsomes​	~52​	PCA at 25 μL​	[183]​
Fragaria sp.​	strawberry​	Rosaceae​	plant​	Methanol​	microsomes​	84.8​	PCA at 20 μg/mL​	[143]​
Fragaria sp.​	strawberry​	Rosaceae​	plant​	Acetone​	microsomes​	65.8​	PCA at 20 μg/mL​	[143]​
Fragaria sp.​	strawberry​	Rosaceae​	plant​	methanol/acetone​	microsomes​	84.3​	PCA at 20 μg/mL​	[143]​
Garcinia mangostana​	mangosteen​	Clusiaceae​	plant​	Methanol​	microsomes​	18.9​	PCA at 20 μg/mL​	[109]​
Garcinia mangostana​	mangosteen​	Clusiaceae​	plant​	methanol (CHCl3partition)​	microsomes​	29.8​	PCA at 20 μg/mL​	[109]​
Garcinia mangostana​	mangosteen​	Clusiaceae​	plant​	Methanol​	SK-BR-3 cells​	24.1​	PCA at 20 μg/mL​	[109]​
Garcinia mangostana​	mangosteen​	Clusiaceae​	plant​	methanol (CHCl3partition)​	SK-BR-3 cells​	16.5​	PCA at 20 μg/mL​	[109]​
Glycyrrhiza glabra a​	licorice​	Fabaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Glyxine max a​	soy (infant formulas)​	Fabaceae​	plant​	Nd​	in vivo brain aromatase​	none​	​	[185]​
Hericium erinaceus​	lion's mane mushroom​	Hericiaceae​	fungus​	Dichloromethane​	microsomes​	57.9​	PCA at 20 μg/mL​	[143]​
Hordeum vulgare Humulus lupulus​	alcohol free beer​	Poaceae Cannabaceae​	plant​	Nd​	choriocarcinoma-derived JAR cells​	65.27​	PCA​	[114]​
Hordeum vulgare a Humulus lupulus a​	lager beer​	Poaceae Cannabaceae​	plant​	Nd​	choriocarcinoma-derived JAR cells​	75.8​	PCA​	[114]​
Hordeum vulgare a Humulus lupulus a​	stout​	Poaceae Cannabaceae​	none​	Nd​	choriocarcinoma-derived JAR cells​	33.9​	PCA​	[114]​
Hordeum vulgare a Humulus lupulus a​	xanthohumol-rich stout​	Poaceae Cannabaceae​	nd​	Nd​	choriocarcinoma-derived JAR cells​	26.4​	PCA​	[114]​
Isodon excisusvar. coreanus​	none​	Lamiaceae​	plant​	methanol (diethyl ether partition)​	microsomes​	13.7​	μg/mL IC50​	[110]​
Lactuca sp.a​	iceberg lettuce​	Asteraceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Lactuca sp.a​	romaine lettuce​	Asteraceae​	plant​	70% ethanol​	microsomes​	560​	units/100 g​	[113]​
Larrea tridentata a​	chaparral​	Zygophyllaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Lentinula edodes​	shiitake mushroom​	Marasmiaceae​	fungus​	water reflux​	microsomes​	~62​	PCA at 100 μL​	[115]​
Lentinus edodes​	shiitake mushroom​	Marasmiaceae​	fungus​	Dichloromethane​	microsomes​	76.5​	PCA at 20 μg/mL​	[143]​
Lycopersicon esculentum a​	tomato​	Solanaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Lycopersicon esculentum a​	tomato (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	6000​	units/100 g​	[113]​
Morinda citrifolia​	noni​	Rubiaceae​	plant​	Nd​	nd​	inhibits​	​	[131]​
Murraya paniculata​	mock orange​	Rutaceae​	plant​	75% MeOH reflux​	microsomes​	~68​	% inhib.​	[105]​
Musa sp.a​	banana​	Musaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Nicotiana tabacum a​	cigarette smoke​	Solanaceae​	plant​	aqueous trap​	microsomes​	0.25​	cigarette equivalents​	[113]​
Nicotiana tabacum a​	cigarette smokea​	Solanaceae​	plant​	methylene chloride trap​	microsomes​	0.07​	cigarette equivalents​	[113]​
Nicotiana tabacum a​	tobacco (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	0.025​	cigarette equivalents​	[113]​
Nicotiana tabacum a​	tobacco (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	590​	units/100 g​	[113]​
Opuntia sp.a​	cactus flower​	Cactaceae​	plant​	water (autoclaved) (dichloromethane-methanol partition)​	microsomes​	~20​	PCA at 100 μL​	[186]​
Opuntia sp.a​	cactus flower​	Cactaceae​	plant​	water (autoclaved) (diethyl ether subfraction)​	microsomes​	~17​	PCA at 100 μL​	[186]​
Opuntia sp.a​	cactus flower​	Cactaceae​	plant​	water (autoclaved) (petroleum ether-diethyl ether subfraction)​	microsomes​	~10​	PCA at 100 μL​	[186]​
Persea americana a​	avocado (meat)​	Lauraceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Persea americana a​	beet (greens)​	Amaranthaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Petroselinum crispum a​	parsley​	Apiaceae​	plant​	70% ethanol​	microsomes​	1200​	units/100 g​	[113]​
Piper cubeba​	none​	Piperaceae​	plant​	96% ethanol​	enzyme​	<10​	μg/mL IC50​	[187]​
Pleurotus ostreatus​	oyster mushroom​	Tricholomataceae​	fungus​	water reflux​	microsomes​	~94​	PCA at 100 μL​	[115]​
Pleurotus sp.​	Italian brown mushroom​	Tricholomataceae​	fungus​	water reflux​	microsomes​	~36​	PCA at 100 μL​	[115]​
Plumbago capensis​	leadwort​	Plumbaginaceae​	plant​	75% MeOH reflux​	microsomes​	~8​	% inhib.​	[105]​
Prunus persicaa​	peach (juice)​	Rosaceae​	plant​	Nd​	microsomes​	~89​	PCA at 25 μL​	[183]​
Prunus persicaa​	peach (juice)​	Rosaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Prunus sp.a​	plum (juice)​	Rosaceae​	plant​	Nd​	microsomes​	~70​	PCA at 25 μL​	[183]​
Prunus sp.a​	plum​	Rosaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Pternandra azurea​	none​	Melastomataceae​	plant​	methanol (CHCl3partition)​	microsomes​	70.1​	PCA at 20 μg/mL​	[143]​
Punica granatum​	pomegranate​	Punicaceae​	plant​	fermented juice​	microsomes​	51​	% inhib.​	[188]​
Punica granatum​	pomegranate​	Punicaceae​	plant​	pericarp polyphenols​	microsomes​	24​	% inhib.​	[188]​
Pyrus malus a​	apple (juice)​	Rosaceae​	plant​	Nd​	microsomes​	~79​	PCA at 25 μL​	[183]​
Pyrus malus a​	apple​	Rosaceae​	plant​	70% ethanol​	microsomes​	<80​	units/100 g​	[113]​
Renealmia sp.​	none​	Bromeliaceae​	plant​	75% MeOH reflux​	microsomes​	~18​	% inhib.​	[105]​
Riedelia sp.​	none​	Ericaceae​	plant​	75% MeOH reflux​	microsomes​	~97​	% inhib.​	[105]​
Rubus occidentalis​	black raspberry​	Rosaceae​	plant​	none (dried fruit)​	microsomes​	80.8​	PCA at 20 μg/mL​	[143]​
Salix sp.a​	willow bark​	Salicaceae​	plant​	nd​	nd​	>50​	% inhib.​	[182]​
Scutellaria barbata​	skullcap​	Lamiaceae​	plant​	water reflux​	microsomes​	23​	μg/mL IC50​	[111]​
Scutellaria barbata​	skullcap​	Lamiaceae​	plant​	water reflux​	myometrial cells​	15.00​	μg/mL IC50​	[111]​
Scutellaria barbata​	skullcap​	Lamiaceae​	plant​	water reflux​	leiomyonal cells​	1.01​	μg/mL IC50​	[111]​
Solanum melongena a​	eggplant​	Solanaceae​	plant​	70% ethanol​	microsomes​	190​	units/100 g​	[113]​
Solanum melongena a​	eggplant (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	800​	units/100 g​	[113]​
Solanum tuberosum a​	potato​	Solanaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Solanum tuberosum a​	potato (leaves)​	Solanaceae​	plant​	70% ethanol​	microsomes​	4500​	units/100 g​	[113]​
Spinacia oleracea a​	spinach​	Amaranthaceae​	plant​	water reflux​	microsomes​	~83​	PCA at 100 μL​	[115]​
Spinacia oleracea a​	spinach​	Amaranthaceae​	plant​	70% ethanol​	microsomes​	2400​	units/100 g​	[113]​
Taraxacum officinale a​	dandelion (greens)​	Asteraceae​	plant​	70% ethanol​	microsomes​	2900​	units/100 g​	[113]​
Theobroma cacao a​	chocolate​	Sterculiaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Theobroma cacao a​	cocoa​	Sterculiaceae​	plant​	70% ethanol​	microsomes​	9000​	units/100 g​	[113]​
Trifolium pratense​	red clover (flowers)​	Fabaceae​	plant​	Nd​	MCF-7 dual assay for AI and estrogenicity​	inhibits​	aromatase​	[116]​
Uncaria tomentosa a​	cat's claw​	Rubiaceae​	plant​	Nd​	nd​	>50​	% inhib.​	[182]​
Vallaris sp.​	none​	Apocynaceae​	plant​	75% MeOH reflux​	microsomes​	~20​	% inhib.​	[105]​
Viscum album​	mistletoe​	Viscaceae​	plant​	75% MeOH reflux​	microsomes​	~94​	% inhib.​	[105]​
Vitis sp.a​	black grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~23​	PCA at 25 μL​	[189]​
Vitis sp.a​	Cabernet Sauvignon, Glen Ellen Proprietor's Reserve (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	7.7​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Cabernet Sauvignon, San Andrés (Lontué Valley, Chile)​	Vitaceae​	plant​	Nd​	microsomes​	0.36​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Cabernet Sauvignon, Tanglewood (France)​	Vitaceae​	plant​	Nd​	microsomes​	0.29​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Champagne grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~90​	PCA at 25 μL​	[189]​
Vitis sp.a​	Chardonnay, Santa Rita Reserve (Casablanca Valley, Chile)​	Vitaceae​	plant​	Nd​	microsomes​	80​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Chardonnay, Woodbridge (Woodbridge, CA)​	Vitaceae​	plant​	Nd​	microsomes​	99.1​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Christmas rose grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~40​	PCA at 25 μL​	[189]​
Vitis sp.a​	Christmas rose grape (seed)​	Vitaceae​	plant​	Nd​	microsomes​	~10​	PCA at 25 μL​	[189]​
Vitis sp.a​	Fumé Blanc, Domaine Napa (Napa Valley, CA)​	Vitaceae​	plant​	Nd​	microsomes​	112.5​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	grape (seed)​	Vitaceae​	plant​	Water​	MCF-7aro cells​	70.4​	% inhib. at 40 μg/mL​	[85]​
Vitis sp.a​	grape (seed)​	Vitaceae​	plant​	Water​	in vivo MCF-7aro xenograft​	reduced​	tumor weight​	[85]​
Vitis sp.a​	grape (seed)​	Vitaceae​	plant​	Water​	MCF-7aro cells​	80.5​	% inhib. at 60 μg/mL​	[85]​
Vitis sp.a​	grape (seed)​	Vitaceae​	plant​	Water​	in vivo MCF-7aro xenograft​	reduced​	tumor weight​	[85]​
Vitis sp.a​	green seedless grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~38​	PCA at 25 μL​	[189]​
Vitis sp.a​	Merlot, Forest Ville (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.46​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Merlot, Hacienda, 1997 (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	3.29​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Merlot, Hacienda, 1998 (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.9​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Merlot, JW Morris Winery (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.42​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Pinot Noir, Cambiaso (Healdburg, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.34​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Pinot Noir, Hacienda (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	2.16​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Pinot Noir, Hacienda (Sonoma, CA)​	Vitaceae​	plant​	Nd​	microsomes​	~8​	PCA at 25 μL​	[86, 106, 107]​
Vitis sp.a​	Pinot Noir, Hacienda (Sonoma, CA)​	Vitaceae​	plant​	Nd​	in vivo mouse​	inhibits​	​	[86, 106, 107]​
Vitis sp.a​	red globe grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~78​	PCA at 25 μL​	[189]​
Vitis sp.a​	red seedless grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~29​	PCA at 25 μL​	[183]​
Vitis sp.a​	red seedless grape (juice)​	Vitaceae​	plant​	Nd​	MCF-7aro cells​	inhibits​	aromatase​	[183]​
Vitis sp.a​	red seedless grape (juice)​	Vitaceae​	plant​	Nd​	in vivo MCF-7aro xenograft​	70​	% reduced tumor size​	[183]​
Vitis sp.a​	red seedless grape (juice)​	Vitaceae​	plant​	Nd​	microsomes​	~30​	PCA at 25 μL​	[189]​
Vitis sp.a​	Sauvignon Blanc, Turning Leaf (Modesto, CA)​	Vitaceae​	plant​	Nd​	microsomes​	106.5​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	seedless grape​	Vitaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
Vitis sp.a​	Zinfandel, Black Mountain (San Diego, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.39​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.a​	Zinfandel, Sequoia Ridge (Graton, CA)​	Vitaceae​	plant​	Nd​	microsomes​	0.39​	PCA at 50 μL​	[86, 106, 107]​
Vitis sp.​	grape​	Vitaceae​	plant​	none (dried fruit)​	microsomes​	75.7​	PCA at 20 μg/mL​	[143]​
Zingiber officinale a​	ginger (root)​	Zingerberaceae​	plant​	70% ethanol​	microsomes​	0​	units/100 g​	[113]​
none​	propolis​	none​	misc.​	Nd​	nd​	>50​	%inhib.​	[182]​

aGenus and species not provided by author.
nd = no data

Natural Products as Aromatase Inhibitors

With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating also the potential of natural products as AIs. Natural products ...

www.ncbi.nlm.nih.gov

Table 2​

Previous literature reports of natural product flavones tested for aromatase inhibition

Compound Name​	Assay Type​	Activity​	Ref.(s)​
apigenin (8)​	microsomes​	1.2​	μM IC50​	[122]​
apigenin (8)​	microsomes​	2.9​	μM IC50​	[123]​
apigenin (8)​	microsomes​	4.2​	μM IC50​	[190]​
apigenin (8)​	microsomes​	10​	μM IC50​	[177]​
apigenin (8)​	microsomes​	15​	μM IC50​	[136]​
apigenin (8)​	microsomes​	0.9​	μg/mL IC50​	[121]​
apigenin (8)​	microsomes (modified)​	2.9​	μM IC50​	[124]​
apigenin (8)​	spectrophotometric w/microsomes​	0.9​	Ks​	[120]​
apigenin (8)​	trout ovarian aromatase​	84.0​	μM IC50​	[128]​
apigenin (8)​	JEG-3 cells​	0.18​	μM IC50​	[125]​
apigenin (8)​	Arom+HEK 293 cells​	1.4​	μM IC50​	[125]​
apigenin (8)​	H295R adrenocortical carcinoma cells​	20​	μM IC50​	[127]​
apigenin (8)​	granulose-luteal cells​	inhibited​	at 10 μmol/L for 24 h​	[129]​
ayanin (9)​	microsomes​	69.6​	PCA at 20 μg/mL​	[143]​
broussoflavonol F (10)​	microsomes​	7.3​	PCA at 20 μg/mL​	[143]​
broussoflavonol F (10)​	microsomes​	9.7​	μM IC50​	[135]​
broussoflavonol F (10)​	SK-BR-3 cells​	28.4​	PCA at 50 μM​	[143]​
chrysin (11)​	microsomes​	0.5​	μM IC50​	[122]​
chrysin (11)​	microsomes​	0.7​	μM IC50​	[123]​
chrysin (11)​	microsomes​	1.1​	μM IC50​	[191]​
chrysin (11)​	microsomes​	8.9​	μM IC50​	[136]​
chrysin (11)​	microsomes​	1.1​	μg/mL IC50​	[121]​
chrysin (11)​	microsomes​	1​	Ki​	[118]​
chrysin (11)​	microsomes​	2.6​	Ki​	[119]​
chrysin (11)​	microsomes (modified)​	0.7​	μM IC50​	[124]​
chrysin (11)​	spectrophotometric w/microsomes​	0.5​	Ks​	[120]​
chrysin (11)​	trout ovarian aromatase​	>1004​	μM IC50​	[128]​
chrysin (11)​	JEG-3 cells​	0.5​	μM IC50​	[125]​
chrysin (11)​	Arom+HEK 293 cells​	0.6​	μM IC50​	[125]​
chrysin (11)​	human preadipocyte cells​	4.6​	μM IC50​	[126]​
chrysin (11)​	H295R adrenocortical carcinoma cells​	7​	μM IC50​	[127]​
chrysin (11)​	MCF-7 dual assay for AI and estrogenicity​	inhibits​	​	[116]​
chrysin (11)​	endometrial stromal cells​	none​	​	[118]​
chrysin (11)​	nd​	11​	μM IC50​	[192]​
3',4'-dihydroxyflavone (12)​	microsomes​	90​	μM IC50​	[132]​
3',4'-dihydroxyflavone (12)​	microsomes​	100​	μM IC50​	[136]​
3',4'-dihydroxyflavone (12)​	microsomes​	>200​	μM IC50​	[132]​
5,4'-dihydroxyflavone (13)​	microsomes​	120​	μM IC50​	[132]​
6,4'-dihydroxyflavone (14)​	microsomes​	90​	μM IC50​	[132]​
7,4'-dihydroxyflavone (15)​	microsomes​	2​	μM IC50​	[132]​
7,4'-dihydroxyflavone (15)​	trout ovarian aromatase​	200.0​	μM IC50​	[128]​
7,8-dihydroxyflavone (16)​	microsomes​	8​	μM IC50​	[123]​
7,8-dihydroxyflavone (16)​	microsomes​	2.2​	μg/mL IC50​	[121]​
7,8-dihydroxyflavone (16)​	microsomes​	10​	Ki​	[119]​
7,8-dihydroxyflavone (16)​	nd​	55​	μM IC50​	[192]​
3',4'-dimethoxyflavone (17)​	microsomes​	42​	μM IC50​	[136]​
fisetin (18)​	microsomes​	8.5​	μg/mL IC50​	[121]​
fisetin (18)​	JEG-3 cells​	55​	μM IC50​	[125]​
flavone (19)​	microsomes​	8​	μM IC50​	[122]​
flavone (19)​	microsomes​	10​	μM IC50​	[132]​
flavone (19)​	microsomes​	48​	μM IC50​	[123]​
flavone (19)​	microsomes​	67​	μM IC50​	[136]​
flavone (19)​	microsomes​	375.0​	μM IC50​	[128]​
flavone (19)​	microsomes (modified)​	48.0​	μM IC50​	[124]​
flavone (19)​	trout ovarian aromatase​	731.0​	μM IC50​	[128]​
flavone (19)​	human preadipocyte cells​	68​	μM IC50​	[126]​
flavone (19)​	JEG-3 cells​	>100​	μM IC50​	[125]​
flavone (19)​	H295R adrenocortical carcinoma cells​	none​	​	[127]​
galangin (20)​	microsomes​	95​	Ki​	[119]​
galangin (20)​	JEG-3 cells​	12​	μM IC50​	[125]​
3-hydroxyflavone (21)​	microsomes​	140​	μM IC50​	[132]​
3'-hydroxyflavone (22)​	microsomes​	73​	μM IC50​	[136]​
4'-hydroxyflavone (23)​	microsomes​	180​	μM IC50​	[132]​
5-hydroxyflavone (24)​	microsomes​	100​	μM IC50​	[132]​
6-hydroxyflavone (25)​	microsomes​	80​	μM IC50​	[132]​
6-hydroxyflavone (25)​	JEG-3 cells​	5.5​	μM IC50​	[125]​
7-hydroxyflavone (26)​	microsomes​	0.2​	μM IC50​	[123]​
7-hydroxyflavone (26)​	microsomes​	0.5​	μM IC50​	[132]​
7-hydroxyflavone (26)​	microsomes​	8.2​	μM IC50​	[136]​
7-hydroxyflavone (26)​	microsomes​	30.5​	μg/mL IC50​	[121]​
7-hydroxyflavone (26)​	microsomes (modified)​	0.21​	μM IC50​	[124]​
7-hydroxyflavone (26)​	trout ovarian aromatase​	>1001​	μM IC50​	[128]​
7-hydroxyflavone (26)​	JEG-3 cells​	0.35​	μM IC50​	[125]​
7-hydroxyflavone (26)​	H295R adrenocortical carcinoma cells​	4​	μM IC50​	[127]​
isolicoflavonol (27)​	microsomes​	0.1​	μM IC50​	[135]​
kaempferide (28)​	JEG-3 cells​	80​	μM IC50​	[125]​
kaempferol (29)​	microsomes​	32​	% inhib. at 50 μM​	[130]​
kaempferol (29)​	JEG-3 cells​	11​	μM IC50​	[125]​
kaempferol (29)​	preadipose cells​	61​	μM IC50​	[134]​
kaempferol 7,4'-dimethyl ether (30)​	microsomes​	45.6​	PCA at 20 μg/mL​	[143]​
kaempferol 7,4'-dimethyl ether (30)​	SK-BR-3 cells​	99.2​	PCA at 50 μM​	[143]​
luteolin (31)​	microsomes​	8.6​	μM IC50​	[136]​
luteolin (31)​	microsomes​	3.3​	μg/mL IC50​	[121]​
luteolin (31)​	microsomes (modified)​	1.2​	μM IC50​	[133]​
luteolin (31)​	spectrophotometric w/microsomes​	1.0​	Ks​	[120]​
luteolin (31)​	JEG-3 cells​	2​	μM IC50​	[125]​
luteolin (31)​	preadipose cells​	25​	μM IC50​	[134]​
7-methoxyflavone (32)​	microsomes​	3.2​	μM IC50​	[123]​
7-methoxyflavone (32)​	microsomes (modified)​	3.2​	μM IC50​	[124]​
7-methoxyflavone (32)​	H295R adrenocortical carcinoma cells​	none​	​	[127]​
morin (33)​	spectrophotometric w/microsomes​	5.0​	Ks​	[120]​
myricetin (34)​	microsomes​	5.6​	μg/mL IC50​	[121]​
myricetin (34)​	microsomes​	41​	% inhib. at 50 μM​	[130]​
myricetin (34)​	spectrophotometric w/microsomes​	5.6​	Ks​	[120]​
oxyayanin B (35)​	microsomes​	83.0​	PCA at 20 μg/mL​	[143]​
prunetin (36)​	microsomes​	none​	μM IC50​	[123]​
prunetin (36)​	microsomes​	7.8​	μg/mL IC50​	[121]​
quercetin (37)​	microsomes​	12​	μM IC50​	[122]​
quercetin (37)​	microsomes​	35​	% inhib. at 50 μM​	[130]​
quercetin (37)​	spectrophotometric w/microsomes​	4.7​	Ks​	[120]​
quercetin (37)​	trout ovarian aromatase​	139.0​	μM IC50​	[128]​
quercetin (37)​	JEG-3 cells​	>100​	μM IC50​	[125]​
quercetin (37)​	H295R adrenocortical carcinoma cells​	none​	​	[127]​
quercetin (37)​	human preadipocyte cells​	none​	​	[126]​
quercetin (37)​	granulose-luteal cells​	none​	at 10 μmol/L for 24h​	[129]​
quercetin (37)​	nd​	~85​	% inhib. at 100 μM​	[107]​
quercetin (37)​	nd​	nd​	​	[131]​
robinetin (38)​	microsomes​	45.7​	μg/mL IC50​	[121]​
rutin (39)​	human preadipocyte cells​	none​	​	[126]​
rutin (39)​	nd​	~120​	% inhib. at 100 μM​	[107]​
7,3',4',5'-tetrahydroxyflavone (40)​	microsomes​	45​	μM IC50​	[136]​
5,7,2',4'-tetrahydroxy- 3-geranylflavone (41)​	microsomes​	24.0​	μM IC50​	[135]​
7,3',4'-trihydroxyflavone (42)​	microsomes​	38​	μM IC50​	[136]​
5,7,3'-trihydroxy-4'- methoxyflavone (43)​	microsomes​	27​	μM IC50​	[136]​
5,7,4'-trihydroxy-3'- methoxyflavone (44)​	microsomes​	7.2​	μM IC50​	[136]​

nd = no data

Natural Products as Aromatase Inhibitors

With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating also the potential of natural products as AIs. Natural products ...

www.ncbi.nlm.nih.gov

Table 3​

Previous literature reports of natural product flavanones tested for aromatase inhibition

Compound Name​	Assay Type​	Activity​	Ref.(s)​
(2S)-abyssinone II (45)​	microsomes​	0.4​	μM IC50​	[135]​
3',4'-dihydroxyflavanonea(46)​	microsomes​	160​	μM IC50​	[132]​
5,7-dihydroxyflavanonea(47)​	microsomes​	10​	μM IC50​	[136]​
7,8-dihydroxyflavanonea(48)​	microsomes (modified)​	8.0​	μM IC50​	[124]​
(2S)-2',4'-dihydroxy-2”-(1-hydroxy-1-methylethyl)dihydrofuro[2,3-h]flavanone (49)​	microsomes​	0.1​	μM IC50​	[135]​
eriodictyola (50)​	microsomes​	5.3​	μM IC50​	[136]​
eriodictyola (50)​	microsomes (modified)​	0.6​	μM IC50​	[133]​
(2S)-euchrenone a7 (51)​	microsomes​	3.4​	μM IC50​	[135]​
flavanonea (52)​	microsomes​	8​	μM IC50​	[122]​
flavanonea (52)​	microsomes​	8​	μM IC50​	[132]​
flavanonea (52)​	microsomes​	28.5​	μM IC50​	[137]​
flavanonea (52)​	microsomes​	32​	μM IC50​	[136]​
flavanonea (52)​	microsomes​	250.0​	μM IC50​	[128]​
flavanonea (52)​	microsomes​	8.7​	μg/mL IC50​	[121]​
flavanonea (52)​	microsomes (modified)​	13.8​	μM IC50​	[133]​
flavanonea (52)​	trout ovarian aromatase​	>1000​	μM IC50​	[128]​
hesperetina (53)​	microsomes​	1.0​	μg/mL IC50​	[121]​
hesperetina (53)​	microsomes (modified)​	3.3​	μM IC50​	[133]​
hesperidina (54)​	microsomes​	40.9​	μg/mL IC50​	[121]​
4'-hydroxyflavanonea (55)​	microsomes​	10​	μM IC50​	[132]​
7-hydroxyflavanonea (56)​	microsomes​	3.8​	μM IC50​	[138]​
7-hydroxyflavanonea (56)​	microsomes​	10​	μM IC50​	[136]​
7-hydroxyflavanonea (56)​	microsomes (modified)​	2.4​	μM IC50​	[133]​
7-hydroxyflavanonea (56)​	H295R adrenocortical carcinoma cells​	65​	μM IC50​	[127]​
isoxanthohumola (57)​	choriocarcinoma-derived JAR cells​	139.7​	μM IC50​	[114]​
isoxanthohumola (57)​	SK-BR-3 cells​	25.4​	μM IC50​	[139]​
7-methoxyflavanonea (58)​	microsomes​	8.0​	μM IC50​	[137]​
7-methoxyflavanonea (58)​	microsomes (modified)​	2.6​	μM IC50​	[124]​
7-methoxyflavanonea (58)​	H295R adrenocortical carcinoma cells​	none​	​	[127]​
naringenin (59a)​	microsomes​	2.9​	μM IC50​	[191]​
naringenin (59a)​	microsomes​	9.2​	μM IC50​	[123]​
(2S)-naringenin (59)​	microsomes​	17.0​	μM IC50​	[135]​
naringenin (59a)​	microsomes​	0.3​	Ki​	[118]​
naringenin (59a)​	microsomes​	5.1​	Ki​	[119]​
naringenin (59a)​	microsomes (modified)​	9.2​	μM IC50​	[124]​
naringenin (59a)​	JEG-3 cells​	1.4​	μM IC50​	[125]​
naringenin (59a)​	Arom+HEK 293 cells​	3.2​	μM IC50​	[125]​
naringenin (59a)​	H295R adrenocortical carcinoma cells​	85​	μM IC50​	[127]​
naringenin (59a)​	MCF-7 dual assay for AI and estrogenicity​	inhibits​	​	[116]​
naringenin (59a)​	rat granulose cells​	inhibits​	​	[184]​
naringenin (59a)​	endometrial stromal cells​	none​	​	[118]​
naringin (60)​	microsomes​	1.8​	μg/mL IC50​	[121]​
pinostrobina (61)​	JEG-3 cells​	4​	μM IC50​	[125]​
8-prenylnaringenina (62)​	microsomes​	0.2​	μM IC50​	[191]​
8-prenylnaringenina (62)​	choriocarcinoma-derived JAR cells​	0.065​	μM IC50​	[114]​
8-prenylnaringenina (62)​	SK-BR-3 cells​	0.08​	μM IC50​	[139]​
8-prenylnaringenina (62)​	breast adipose fibroblast cells​	0.3​	μM IC50​	[191]​
(2S)-5,7,2',4'-tetrahydroxyflavanone (63)​	microsomes​	2.2​	μM IC50​	[135]​
5,7,4'-trihydroxy-3'-methoxyflavanone (64)​	microsomes​	25​	μM IC50​	[136]​

aOptical sign not provided by authors.

Natural Products as Aromatase Inhibitors

With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating also the potential of natural products as AIs. Natural products ...

www.ncbi.nlm.nih.gov

From: Balunas MJ, Su B, Brueggemeier RW, Kinghorn AD. Natural products as aromatase inhibitors. Anticancer Agents Med Chem. 2008 Aug;8(6):646-82. PMID: 18690828; PMCID: PMC3074486.

Natural Products as Aromatase Inhibitors

With the clinical success of several synthetic aromatase inhibitors (AIs) in the treatment of postmenopausal estrogen receptor-positive breast cancer, researchers have also been investigating also the potential of natural products as AIs. Natural products ...

www.ncbi.nlm.nih.gov

There are many other similar tables in the article. Quite extensive.