Naringenin, Naringin Supplements?

[Koveras]

RP has said the opposite. He thinks they are fairly powerful anti-estrogens. I think haidut has posted some studies about this too.

When did Ray say that? I never saw that heard that read that. Maybe he did, but I am positive, 100%, looking at studies, that it is a phytoestrogen. There are many many studies showing this. It may in some cases not be estrogenic but it is not a simple matter.

"Breast Cancer
Orange juice and guavas contain aromatase inhibitors, and aspirin and progesterone are other inhibitors. Aspirin and progesterone also oppose the effects of HER2/neu on aromatase and estrogen. (Reference)"

Ray Peat Email Exchanges - Ray Peat Forum Wiki

 

[Giraffe]

RP has said the opposite. He thinks they are fairly powerful anti-estrogens.

When did Ray say that? I never saw that heard that read that.

There is a clip posted here: KMUD: Fasting, Alzheimers, Fish oil, Testosterone,...

 

[BibleBeliever]

Effect of Citrus Flavonoids, Naringin and Naringenin, on Metabolic Syndrome and Their Mechanisms of Action


Effect of Citrus Flavonoids, Naringin and Naringenin, on Metabolic Syndrome and Their Mechanisms of Action

 

[ddjd]

When did Ray say that? I never saw that heard that read that. Maybe he did, but I am positive, 100%, looking at studies, that it is a phytoestrogen. There are many many studies showing this. It may in some cases not be estrogenic but it is not a simple matter.

Double directional adjusting estrogenic effect of naringin from Rhizoma drynariae (Gusuibu). - PubMed - NCBI


Naringenin-type flavonoids show different estrogenic effects in mammalian and teleost test systems. - PubMed - NCBI

CONCLUSIONS:
Naringin and naringenin revealed a double directional adjusting function of estrogenic and anti-estrogenic activities. Both of them showed estrogenic agonist activity at low concentration or lack of endogenous estrogen. On the other hand, they also acted as estrogenic antagonists at high concentrations or too much endogenous estrogen. They produced estrogenic and anti-estrogenic effects primarily through selectively binding with ERβ, which could prevent and treat osteoporosis with the mechanism of estrogenic receptor agitation. This paper confirmed the estrogenic and anti-estrogenic activity of naringin and naringenin, and further studies were still essential to study their dose-effect relationship and the anti-osteoporosis mechanism for Rhizoma drynariae in the treatment of osteoporosis and other estrogen deficiency-related diseases.

have you not heard about Melanon. Main ingredient is Naringenin, as an anti estrogen -

http://raypeat.com/articles/articles/th ... trix.shtml
"...Substances that inhibit inflammation are likely to also inhibit excessive collagen synthesis, serotonin secretion, and the formation of estrogen. Besides aspirin, some effective substances are apigenin and naringenin, found in oranges and guavas. These flavonoids also inhibit the formation of nitric oxide and prostaglandins, which are important for inflammation and carcinogenesis (Liang, et al., 1999). Increased CO2, which has a variety of anti-inflammatory effects, can decrease collagen formation and tissue collagen content significantly (Ryu, et al., 2010)."

Naringenin:
Citrus flavanone naringenin enhances melanogenesis through the activation of Wnt/β-catenin signalling in mouse melanoma cells. - PubMed - NCBI
Hydrolysates of citrus plants stimulate melanogenesis protecting against UV-induced dermal damage. - PubMed - NCBI
Enhancement of transglutaminase activity and polyamine depletion in B16-F10 melanoma cells by flavonoids naringenin and hesperitin correlate to red... - PubMed - NCBI
In vitro cytotoxic activity of extracts and isolated constituents of Salvia leriifolia Benth. against a panel of human cancer cell lines. - PubMed - NCBI
Stimulation of melanogenesis by the citrus flavonoid naringenin in mouse B16 melanoma cells. - PubMed - NCBI
Update on uses and properties of citrus flavonoids: new findings in anticancer, cardiovascular, and anti-inflammatory activity. - PubMed - NCBI
Naringenin Inhibits UVB Irradiation-Induced Inflammation and Oxidative Stress in the Skin of Hairless Mice. - PubMed - NCBI
Chemopreventive and therapeutic potential of "naringenin," a flavanone present in citrus fruits. - PubMed - NCBI
Induction of apoptosis and antiproliferative activity of naringenin in human epidermoid carcinoma cell through ROS generation and cell cycle arrest. - PubMed - NCBI
Myricetin and naringenin inhibit human squamous cell carcinoma proliferation and migration in vitro. - PubMed - NCBI
Tumor growth attenuating effects of naringenin. - PubMed - NCBI
Inhibitory effect of GB-2a (I3-naringenin-II8-eriodictyol) on melanogenesis. - PubMed - NCBI
Preparation and Characterization of Naringenin-Loaded Elastic Liposomes for Topical Application. - PubMed - NCBI
The inhibitory effect of naringenin on atopic dermatitis induced by DNFB in NC/Nga mice. - PubMed - NCBI
Protective effects of fermented Citrus unshiu peel extract against ultraviolet-A-induced photoageing in human dermal fibrobolasts. - PubMed - NCBI
Naringenin protects HaCaT human keratinocytes against UVB-induced apoptosis and enhances the removal of cyclobutane pyrimidine dimers from the genome. - PubMed - NCBI
Inhibition of mammalian collagenase, matrix metalloproteinase-1, by naturally-occurring flavonoids. - PubMed - NCBI
Correlation of in vitro chemopreventive efficacy data from the human epidermal cell assay with animal efficacy data and clinical trial plasma levels. - PubMed - NCBI

 

[Inaut]

I just ordered some naringenin powder and want to make a topical solution... What kind of solvent would be recommended? Not a big fan of dmso but I don’t know what my other options are.

Also, looking forward to Georgi’s new naringenin product ?

 

[lilsticky]

Orange and camomile oils are probably a good concentration of those things. If those are food grade and used safely etc

 

[Inaut]

Orange and camomile oils are probably a good concentration of those things

Really???!! I thought it was mainly terpenes ?

 

[Mito]

Are there any supplements out there which contain only Naringenin and/or Naringin ?

Naringin

Shop the Best Naringin Extract Powder at Bulk Supplements. What is Naringin, When to take, health benefits, dosage, side effects, and customer reviews.

www.bulksupplements.com

 

[johnwester130]

I just ordered some naringenin powder and want to make a topical solution... What kind of solvent would be recommended? Not a big fan of dmso but I don’t know what my other options are.

Also, looking forward to Georgi’s new naringenin product ?

I think this is the new product by haidut. At leasst it contains an interesting ignredient

Virtus

Iron Legions Revolutionary New Aromatase Inhbitor

iron-legion.com

 

[ddjd]

Are there any supplements out there which contain only Naringenin and/or Naringin ?

I get some good effects from OJ, unfortunately I also seem to have an allergy to oranges, with sneezing, runny nose, short breath... Since no other fruit juices produce the beneficial effects of orange juice, I'm assuming either naringenin or naringin could be responsible for the good effects. However, all the supplements I have seen on the market with these two flavonoids also contain something like a dozen other ingredients.

Is it even possible to get them in pure powder form or something like that?

i found this on the french amazon website. a private seller. probably from china. but im slightly suspicious because real naringenin should be much much more expensive- 60 euros is way too cheap for Naringenin.
its probably the regular naringin and theyve mislabelled it- but slightly odd because they put the correct naringenin CAS on the packaging.

maybe someone out there wants to try it out??

 

[Beatrix_]

Just a warning note

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence | British Journal of Nutrition | Cambridge Core

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence - Volume 123 Issue 10

www.cambridge.org

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence
Published online by Cambridge University Press: 20 February 2020

Abstract
The study of polyphenols’ effects on health has been gaining attention lately. In addition to reacting with important enzymes, altering the cell metabolism, these substances can present either positive or negative metabolic alterations depending on their consumption levels. Naringenin, a citrus flavonoid, already presents diverse metabolic effects. The objective of this work was to evaluate the effect of maternal naringenin supplementation during pregnancy on the tricarboxylic acid cycle activity in offspring’s cerebellum. Adult female Wistar rats were divided into two groups: (1) vehicle (1 ml/kg by oral administration (p.o.)) or (2) naringenin (50 mg/kg p.o.). The offspring were euthanised at 7th day of life, and the cerebellum was dissected to analyse citrate synthase, isocitrate dehydrogenase (IDH), α-ketoglutarate dehydrogenase (α-KGDH) and malate dehydrogenase (MDH) activities. Molecular docking used SwissDock web server and FORECASTER Suite, and the proposed binding pose image was created on UCSF Chimera. Data were analysed by Student’s t test. Naringenin supplementation during pregnancy significantly inhibited IDH, α-KGDH and MDH activities in offspring’s cerebellum. A similar reduction was observed in vitro, using purified α-KGDH and MDH, subjected to pre-incubation with naringenin. Docking simulations demonstrated that naringenin possibly interacts with dehydrogenases in the substrate and cofactor binding sites, inhibiting their function. Naringenin administration during pregnancy may affect cerebellar development and must be evaluated with caution by pregnant women and their physicians.

 

[ddjd]

Just a warning note

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence | British Journal of Nutrition | Cambridge Core

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence - Volume 123 Issue 10

www.cambridge.org

Tricarboxylic acid cycle dehydrogenases inhibition by naringenin: experimental and molecular modelling evidence
Published online by Cambridge University Press: 20 February 2020

Abstract
The study of polyphenols’ effects on health has been gaining attention lately. In addition to reacting with important enzymes, altering the cell metabolism, these substances can present either positive or negative metabolic alterations depending on their consumption levels. Naringenin, a citrus flavonoid, already presents diverse metabolic effects. The objective of this work was to evaluate the effect of maternal naringenin supplementation during pregnancy on the tricarboxylic acid cycle activity in offspring’s cerebellum. Adult female Wistar rats were divided into two groups: (1) vehicle (1 ml/kg by oral administration (p.o.)) or (2) naringenin (50 mg/kg p.o.). The offspring were euthanised at 7th day of life, and the cerebellum was dissected to analyse citrate synthase, isocitrate dehydrogenase (IDH), α-ketoglutarate dehydrogenase (α-KGDH) and malate dehydrogenase (MDH) activities. Molecular docking used SwissDock web server and FORECASTER Suite, and the proposed binding pose image was created on UCSF Chimera. Data were analysed by Student’s t test. Naringenin supplementation during pregnancy significantly inhibited IDH, α-KGDH and MDH activities in offspring’s cerebellum. A similar reduction was observed in vitro, using purified α-KGDH and MDH, subjected to pre-incubation with naringenin. Docking simulations demonstrated that naringenin possibly interacts with dehydrogenases in the substrate and cofactor binding sites, inhibiting their function. Naringenin administration during pregnancy may affect cerebellar development and must be evaluated with caution by pregnant women and their physicians.

@haidut should people be cautious using your Melanon product during pregnancy based on this study?

 

[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.

NATURAL AROMATASE INHIBITORS

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...

raypeatforum.com

 

[LucH]

Is it even possible to get them in pure powder form or something like that?

I won't do that.
Naringin and naringenin are potent inhibitors of cytochrome P450 3A4 (Cytochrome P3A4 or CY P3A4) and to a lesser extent of CYP1A2 and CYP3A5. Naringenin from grapefruit and certain polyphenols, such as polyphenols from red wine, slow down the activity of an enzyme, especially CY P3A4, which is very useful in the first phase of hepatic detoxification. Note, however, that some genetically predisposed people are more sensitive than others on this point (factor varying from 1 to 8).

Grapefruit juice, and grapefruit in general, is therefore a powerful inhibitor of the CYP3A4 enzyme. Half-life of the CYP3A4 enzyme Human CYP3A4 turnover varies widely depending on location. At the hepatic level, the half-life in vivo is between 70 and 140 hours. At the intestinal level, the half-life of cytochromes is linked to the turnover/renewal of the intestinal cells themselves. Otherwise expressed: The process is reversible. We can recover normal functioning as soon as the inhibitors are stopped... It is also dose-dependent.

36% of drugs are metabolized by the CYP450 3A4 enzyme. Almost half of the drugs metabolized are via CYP3A4.

Explained differently, naringin and naringenin prolong the half-life of quite a few drugs/toxins, which can overtax the liver and kidneys.

 

[Rinse & rePeat]

Are there any supplements out there which contain only Naringenin and/or Naringin ?

I get some good effects from OJ, unfortunately I also seem to have an allergy to oranges, with sneezing, runny nose, short breath... Since no other fruit juices produce the beneficial effects of orange juice, I'm assuming either naringenin or naringin could be responsible for the good effects. However, all the supplements I have seen on the market with these two flavonoids also contain something like a dozen other ingredients.

Is it even possible to get them in pure powder form or something like that?

Marmalade and candied orange peels may be a more tolerable way to get naringenin. I made candied orange peels the other day and they were easier than I had imagined. I posted my recipe for them in one of my recipe threads linked below, on page 8…

“Source and occurrence of naringenin
Naringenin is present in citrus fruits like grapefruits (115–384 mg/L), sour orange (> 100 mg/L), tart cherries, tomatoes (0.68 ± 0.16 mg/100 g), Greek oregano [59]. In smaller quantities it is also found in bergamot, cocoa, water mint, Drynaria, as well as in beans”

“Naringenin​

Naringenin (Fig. 11.5) (4′,5,7-trihydroxy flavanone) is a flavanone bioactive present in grapefruit”

“5.2.4 Naringenin​

Naringenin (Fig. 11.17), a flavanone, is basically found in tomato's skin and other citrus fruits like grapes. It has many pharmacological properties such as antidiabetic, antidyslipidemic, antinecrotic, antifibrotic, and antiobesity.”

“17.4.4 Naringenin​

Naringenin is a naturally occurring, predominant flavone present in citrus fruits such as grapes, oranges, bergamots, lemons, etc. Owing to its high antioxidant, anti-inflammatory, anti-diabetic, anti-tumor, DNAprotective, immunomodulatory, memory improving, and neuroprotective properties, it has been extensively studied for the cure of several disorders”

https://www.sciencedirect.com/topics/chemistry/naringenin#:~:text=Bioactive%20Natural%20Products&text=Naringenin%20is%20present%20in%20citrus,as%20in%20beans%20%5B60%5D.

Navel orange peel hydroethanolic extract, naringin and naringenin have potent anti-hyperglycemic, anti-hyperlipidemic and anti-oxidant effects in NA/STZ-induced type 2 diabetic rats.

https://www.sciencedirect.com/science/article/abs/pii/S0753332217326100

"Peaty" Fruits & Vegetables - Easy Step By Step Recipes (Photos)

SCALLOPED POTATOES This is my favorite splurge meal nowadays! To keep from gaining weight with this meal, I just have a good plate of them as the main course, without any sides. I sleep so good on the nights I have these for dinner! I make my scalloped potatoes with half red potatoes and half...

raypeatforum.com