Vitis vinifera (grape)
This article was written by Eric Yarnell, ND, RH(AHG) and is protected by copyright, 2020.
Last updated April 2020.
Numerous herbal medicines have been reported to inhibit aromatase. The following is a list of reports of herbal aromatase inhibitors (also called botanical aromatase inhibitors) for easy reference. Note that these are in vitro or animal studies and thus cannot be directly extrapolated to human beings. None of these or any other herbal substance has been shown to inhibit aromatase in human beings, and some have notably failed to do so (see Vitis vinifera and chrysin below). Note that isolated compounds may be found in plants other than those indicated, but the one listed is the specific herb from which it was extracted in the study cited.
Abbreviations used: IC50 = a measure of strength based on the concentration at which half of the activity of aromatase is inhibited; Ki = a measure of strength of binding of a substances to the aromatase enzyme; µM = micromolar; µmol = micromol; PMID = PubMed ID Number.
Last updated April 2020.
Numerous herbal medicines have been reported to inhibit aromatase. The following is a list of reports of herbal aromatase inhibitors (also called botanical aromatase inhibitors) for easy reference. Note that these are in vitro or animal studies and thus cannot be directly extrapolated to human beings. None of these or any other herbal substance has been shown to inhibit aromatase in human beings, and some have notably failed to do so (see Vitis vinifera and chrysin below). Note that isolated compounds may be found in plants other than those indicated, but the one listed is the specific herb from which it was extracted in the study cited.
Abbreviations used: IC50 = a measure of strength based on the concentration at which half of the activity of aromatase is inhibited; Ki = a measure of strength of binding of a substances to the aromatase enzyme; µM = micromolar; µmol = micromol; PMID = PubMed ID Number.
Crude Herbal Extracts
* Agaricus bisporus (button mushrooms) in vitro and in mice (PMID 17178902)
* Alcea rosea (hollyhock) flower (PMID 12502186)
* Artemisia annua (sweet Annie) root ethanol extract IC50 24.33 μg/ml, methylene chloride extract IC50 2.2 μg/ml (PMID 29909120)
* Brassica oleracea (cabbage) juice or sauerkraut juice (PMID 23090135)
* Brassica rapa (rape) pollen (PMID 19336936)
* Corydalis yanhusuo (yan hu suo) root (PMID 20657498)
* Epilobium parviflorum (fireweed) leaf and flower (PMID 19526676)
* Euonymus alatus (burning bush) (PMID 15518167)
* Glycine max (soy) extract, more potent when fermented by Aspergillus awamori (PMID 2864496)
* Glycyrrhiza uralensis (Asian licorice) root, multiple constituents (PMID 23265493)
* Humulus lupulus (hops) strobiles in beer (PMID 16608212)
* Mammaea siamensis (saraphi) flower methanol extract IC50 16.5 µg/mL (PMID 27373643)
* Mangifera indica (mango) peel extract (PMID 27585256)
* Olea europaea (olive) leaf extract (PMID 27585256)
* Piper cubeba (cubeb) fruit ethanol extract, IC50 30 µg/ml (PMID 18219597)
* Punica granatum (pomegranate) fruit pulp and pericarp polyphenol extracts, IC50 0.02-0.04 µg/ml (PMID 12002340 )
* Scutellaria barbata (Chinese skullcap) root (PMID 15518167)
* Turnera diffusa (damiana), methanol extract IC50 63.1 µg/ml (PMID 18948180)
* Urtica dioica (nettle) root extract, ED50 3.58 mg/ml, combined with Prunus africanum (pygeum) bark extract ED50 0.24 mg/d (PMID 23194959)
* Vitis vinifera (grape) seeds (proanthocyanidins), Ki 6 µM (PMID 14679019); proanthocyanidins inhibit aromatase expression at 60 µg/ml (PMID 16740737)
Clinical trial: n=46 postmenopausal women, double-blind randomized trial comparing grape seed extract 200, 400, 600, or 800 mg qd x 12 weeks, no difference in serum estrogen or androgen precursor levels in any group, so no evidence of aromatase inhibition (PMID 24670122)
* Zingiber officinale (ginger) rhizome methylene chloride extract extract IC50 52.7 μg/ml (PMID 29909120)
* Alcea rosea (hollyhock) flower (PMID 12502186)
* Artemisia annua (sweet Annie) root ethanol extract IC50 24.33 μg/ml, methylene chloride extract IC50 2.2 μg/ml (PMID 29909120)
* Brassica oleracea (cabbage) juice or sauerkraut juice (PMID 23090135)
* Brassica rapa (rape) pollen (PMID 19336936)
* Corydalis yanhusuo (yan hu suo) root (PMID 20657498)
* Epilobium parviflorum (fireweed) leaf and flower (PMID 19526676)
* Euonymus alatus (burning bush) (PMID 15518167)
* Glycine max (soy) extract, more potent when fermented by Aspergillus awamori (PMID 2864496)
* Glycyrrhiza uralensis (Asian licorice) root, multiple constituents (PMID 23265493)
* Humulus lupulus (hops) strobiles in beer (PMID 16608212)
* Mammaea siamensis (saraphi) flower methanol extract IC50 16.5 µg/mL (PMID 27373643)
* Mangifera indica (mango) peel extract (PMID 27585256)
* Olea europaea (olive) leaf extract (PMID 27585256)
* Piper cubeba (cubeb) fruit ethanol extract, IC50 30 µg/ml (PMID 18219597)
* Punica granatum (pomegranate) fruit pulp and pericarp polyphenol extracts, IC50 0.02-0.04 µg/ml (PMID 12002340 )
* Scutellaria barbata (Chinese skullcap) root (PMID 15518167)
* Turnera diffusa (damiana), methanol extract IC50 63.1 µg/ml (PMID 18948180)
* Urtica dioica (nettle) root extract, ED50 3.58 mg/ml, combined with Prunus africanum (pygeum) bark extract ED50 0.24 mg/d (PMID 23194959)
* Vitis vinifera (grape) seeds (proanthocyanidins), Ki 6 µM (PMID 14679019); proanthocyanidins inhibit aromatase expression at 60 µg/ml (PMID 16740737)
Clinical trial: n=46 postmenopausal women, double-blind randomized trial comparing grape seed extract 200, 400, 600, or 800 mg qd x 12 weeks, no difference in serum estrogen or androgen precursor levels in any group, so no evidence of aromatase inhibition (PMID 24670122)
* Zingiber officinale (ginger) rhizome methylene chloride extract extract IC50 52.7 μg/ml (PMID 29909120)
Isolated Botanical Constituents
* (9Z,11E)-13-hydroxy-9,11-octadecadienoic acid from Urtica dioica (nettle) root, (PMID 17238068)
* 14-octacosanol from Urtica dioica (nettle) root, (PMID 17238068)
* 2-Methoxy-5-acetoxyfruranogermacr-1(10)-en-6-one from Commiphora molmol (myrrh) resin, IC50 0.21 µM (PMID 19101885)
* (2S)-2',4'-dihydroxy-2' '-(1-hydroxy-1-methylethyl)dihydrofuro[2,3-h]flavanone, a flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.1 µM (PMID 11678652 )
* (2S)-abyssinone II, a prenylated flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.4 µM (PMID 11678652 )
* 3'-[gamma-hydroxymethyl-(E)-gamma-methylallyl]-2,4,2',4'-tetrahydroxychalcone 11'-O-coumarate, a chalcone, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.5 µM (PMID 11678652 )
* 8-Prenylnaringenin, a prenylated flavonoid, from Humulus lupulus (hops) strobile, IC50 0.065-0.08 µM (PMID 17643984, PMID 16608212)
* Acacetin, a flavonoid from Turnera diffusa (damiana) leaf, IC50 18.7 µM (PMID 18948180)
* Apigenin, a flavonoid from from Matricaria recutita (chamomile) flower, IC50 10 µM (PMID 18192087)
* Benzoflavone, a flavonoid, from Passiflora incarnata (passionflower) leaf; IC50 not reported (PMID 12511112 )
* Biflavonoids, notably morreloflavone, from Garcinia gardneriana (bacupari) branches; IC50 1.35–7.67 μM (PMID 31393836)
Biochanin A, an isoflavone, from Trifolium pratense (red clover) flower, inhibits aromatase expression at 25 µM (PMID 17761019 )
* Capsaicin, a vanilloid, from Capsicum spp (cayenne) fruit, inhibits aromatase at 13.6 µM (PMID 21663483 )
* Cardamonin, a chalcone from Desmos cochinchinensis (dwarf ylang ylang) leaf, inhibits aromatase at IC50 0.9 µM (PMID 21802698 )
* Chrysin, a flavonoid, IC50 4.6 µM; Ki 2.4 µM (PMID 9831487), IC50 0.25 µg/ml (PMID 29909120)
Clinical trial: a propolis and honey supplement (containing chrysin, amount ?) was given to n=21 young men for 3 weeks, it had no effect on serum testosterone levels (PMID 14977449)
The following combination has been studied in at least two clinical trials in men: androstenedione 300 mg, dehydroepiandrosterone 150 mg, Tribulus terrestris 750 mg, chrysin 625 mg, indole-3-carbinol 300 mg, Serenoa repens 540 mg (daily oral doses)
Trial 1, randomized, placebo-controlled, blinding?: n=20 young men doing weight training thrice weekly, after 8 wk on the supplement there was a significant increase in serum estradiol, estrone, and androstenedione compared to placebo, with no effect on serum free or total testosterone, which if anything suggests an increase in aromatase activity (PMID 10997957)
Trial 2, randomized, placebo-controlled, blinding?, n=55 men aged 30–59 yr, after 4 wk on the supplement there was a significant rise in serum androstenedione, free testosterone, dihydrotestosterone, and estradiol and a significant decline in HDL cholesterol levels compared to placebo, again if anything suggesting a stimulation of aromatization (PMID 11725694)
* Coumarins from Mammea siamensis (saraphi) flower, IC50 3.1–21.0 µg/ml (PMID 27373643)
* Dehydroabietic acid from Commiphora molmol (myrrh) resin, IC50 0.32 µM (PMID 19101885)
* Desmosflavans A and B, flavanochalcone hybrids, from Desmos cochinchinensis (dwarf ylang ylang) leaf, inhibits aromatase at IC50 1.8--3.3 µM (PMID 21802698 )
* Ellagitanins from Punica granatum (pomegranate) rind (PMID 20051378)
* Flavonoids and isoflavones, various, from Glycyrrhiza uralensis (gan cao) root, 20 µg/ml (PMID 23265493 )
* Genistein, an isoflavone, from Trifolium pratense (red clover) flower, inhibits aromatase expression (PMID 17761019)
* Ginsenosides Rk1, Rg5, Rs5, 20R-Rg3, and Rs4 from Panax ginseng (Asian ginseng), inhibit aromatase activity (PMID 28027838)
* Hesperetin, a flavonoid from various citrus fruit, IC50 5 µM (PMID 22209285 )
* Indole-3-carbinol, a glucosinolate, from Brassica oleracea (cabbage) leaf (PMID 23090135 )
* Isolicoflavonol, a flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.1 µM (PMID 11678652 )
* Isoliquiritigenin, a flavonoid, from Glycyrrhiza glabra (licorice) root in mice with Ki 3 µM (PMID 19065667)
* Isoxanthohumol, a flavonoid, from Humulus lupulus (hops) strobile, IC50 25.4-139.7 µM (PMID 17643984 , PMID 16608212 )
* Mammeasins C and D, geranylated coumarins from Mammea siamensis, IC50 2.7 µM and
3.6 µM (PMID 27373643)
* γ-Mangostin, a xanthone, from Garcinia mangostana (mangosteen) pericarp, IC 4.97 µM (PMID 18558747)
* α-Naphthoflavone, a flavonoid, IC50 0.5 muM; Ki 0.2 µM (PMID 9831487)
* Oenotherin A and B, ellagitannins, from Epilobium spp (small-flowered willow herb) leaf and flower (PMID 9140222)
* Oleanolic acid from Urtica dioica (nettle) root, (PMID 17238068)
* Pinocembrin, a flavonoid from Turnera diffusa (damiana) leaf, IC50 10.8 µM (PMID 18948180)
* Secoisolariciresinol, a lignan, from Urtica dioica (nettle) root, (PMID 17238068)
* Triptolide, a diterpenoid from Tripterygium wilfordii (thunder duke vine) leaf, IC50 0.035 muM (PMID 22282961)
* Urolithin B, an ellagitannin metabolite, from Punica granatum (pomegranate) rind, Ki 5 µmol/L (PMID 20051378)
* Ursolic acid, a ubiquitous phytosterol, IC50 32 µmol (PMID 18192087, PMID 17238068)
* Xanthohumol, a flavonoid, from Humulus lupulus (hops) strobile, IC50 3.2-20.3 µM (PMID 17643984, PMID 16608212)
* 14-octacosanol from Urtica dioica (nettle) root, (PMID 17238068)
* 2-Methoxy-5-acetoxyfruranogermacr-1(10)-en-6-one from Commiphora molmol (myrrh) resin, IC50 0.21 µM (PMID 19101885)
* (2S)-2',4'-dihydroxy-2' '-(1-hydroxy-1-methylethyl)dihydrofuro[2,3-h]flavanone, a flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.1 µM (PMID 11678652 )
* (2S)-abyssinone II, a prenylated flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.4 µM (PMID 11678652 )
* 3'-[gamma-hydroxymethyl-(E)-gamma-methylallyl]-2,4,2',4'-tetrahydroxychalcone 11'-O-coumarate, a chalcone, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.5 µM (PMID 11678652 )
* 8-Prenylnaringenin, a prenylated flavonoid, from Humulus lupulus (hops) strobile, IC50 0.065-0.08 µM (PMID 17643984, PMID 16608212)
* Acacetin, a flavonoid from Turnera diffusa (damiana) leaf, IC50 18.7 µM (PMID 18948180)
* Apigenin, a flavonoid from from Matricaria recutita (chamomile) flower, IC50 10 µM (PMID 18192087)
* Benzoflavone, a flavonoid, from Passiflora incarnata (passionflower) leaf; IC50 not reported (PMID 12511112 )
* Biflavonoids, notably morreloflavone, from Garcinia gardneriana (bacupari) branches; IC50 1.35–7.67 μM (PMID 31393836)
Biochanin A, an isoflavone, from Trifolium pratense (red clover) flower, inhibits aromatase expression at 25 µM (PMID 17761019 )
* Capsaicin, a vanilloid, from Capsicum spp (cayenne) fruit, inhibits aromatase at 13.6 µM (PMID 21663483 )
* Cardamonin, a chalcone from Desmos cochinchinensis (dwarf ylang ylang) leaf, inhibits aromatase at IC50 0.9 µM (PMID 21802698 )
* Chrysin, a flavonoid, IC50 4.6 µM; Ki 2.4 µM (PMID 9831487), IC50 0.25 µg/ml (PMID 29909120)
Clinical trial: a propolis and honey supplement (containing chrysin, amount ?) was given to n=21 young men for 3 weeks, it had no effect on serum testosterone levels (PMID 14977449)
The following combination has been studied in at least two clinical trials in men: androstenedione 300 mg, dehydroepiandrosterone 150 mg, Tribulus terrestris 750 mg, chrysin 625 mg, indole-3-carbinol 300 mg, Serenoa repens 540 mg (daily oral doses)
Trial 1, randomized, placebo-controlled, blinding?: n=20 young men doing weight training thrice weekly, after 8 wk on the supplement there was a significant increase in serum estradiol, estrone, and androstenedione compared to placebo, with no effect on serum free or total testosterone, which if anything suggests an increase in aromatase activity (PMID 10997957)
Trial 2, randomized, placebo-controlled, blinding?, n=55 men aged 30–59 yr, after 4 wk on the supplement there was a significant rise in serum androstenedione, free testosterone, dihydrotestosterone, and estradiol and a significant decline in HDL cholesterol levels compared to placebo, again if anything suggesting a stimulation of aromatization (PMID 11725694)
* Coumarins from Mammea siamensis (saraphi) flower, IC50 3.1–21.0 µg/ml (PMID 27373643)
* Dehydroabietic acid from Commiphora molmol (myrrh) resin, IC50 0.32 µM (PMID 19101885)
* Desmosflavans A and B, flavanochalcone hybrids, from Desmos cochinchinensis (dwarf ylang ylang) leaf, inhibits aromatase at IC50 1.8--3.3 µM (PMID 21802698 )
* Ellagitanins from Punica granatum (pomegranate) rind (PMID 20051378)
* Flavonoids and isoflavones, various, from Glycyrrhiza uralensis (gan cao) root, 20 µg/ml (PMID 23265493 )
* Genistein, an isoflavone, from Trifolium pratense (red clover) flower, inhibits aromatase expression (PMID 17761019)
* Ginsenosides Rk1, Rg5, Rs5, 20R-Rg3, and Rs4 from Panax ginseng (Asian ginseng), inhibit aromatase activity (PMID 28027838)
* Hesperetin, a flavonoid from various citrus fruit, IC50 5 µM (PMID 22209285 )
* Indole-3-carbinol, a glucosinolate, from Brassica oleracea (cabbage) leaf (PMID 23090135 )
* Isolicoflavonol, a flavonoid, from Broussonetia papyrifera (paper mulberry) herb, IC50 0.1 µM (PMID 11678652 )
* Isoliquiritigenin, a flavonoid, from Glycyrrhiza glabra (licorice) root in mice with Ki 3 µM (PMID 19065667)
* Isoxanthohumol, a flavonoid, from Humulus lupulus (hops) strobile, IC50 25.4-139.7 µM (PMID 17643984 , PMID 16608212 )
* Mammeasins C and D, geranylated coumarins from Mammea siamensis, IC50 2.7 µM and
3.6 µM (PMID 27373643)
* γ-Mangostin, a xanthone, from Garcinia mangostana (mangosteen) pericarp, IC 4.97 µM (PMID 18558747)
* α-Naphthoflavone, a flavonoid, IC50 0.5 muM; Ki 0.2 µM (PMID 9831487)
* Oenotherin A and B, ellagitannins, from Epilobium spp (small-flowered willow herb) leaf and flower (PMID 9140222)
* Oleanolic acid from Urtica dioica (nettle) root, (PMID 17238068)
* Pinocembrin, a flavonoid from Turnera diffusa (damiana) leaf, IC50 10.8 µM (PMID 18948180)
* Secoisolariciresinol, a lignan, from Urtica dioica (nettle) root, (PMID 17238068)
* Triptolide, a diterpenoid from Tripterygium wilfordii (thunder duke vine) leaf, IC50 0.035 muM (PMID 22282961)
* Urolithin B, an ellagitannin metabolite, from Punica granatum (pomegranate) rind, Ki 5 µmol/L (PMID 20051378)
* Ursolic acid, a ubiquitous phytosterol, IC50 32 µmol (PMID 18192087, PMID 17238068)
* Xanthohumol, a flavonoid, from Humulus lupulus (hops) strobile, IC50 3.2-20.3 µM (PMID 17643984, PMID 16608212)