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PHYTOESTROGENS

Sharol Tilgner N.D.

 

The term phytoestrogen is used loosely in the herbal community. There is no

current agreed upon definition for this term. Basically the term is used for any

plant that has one or more constituents with similar chemical structure to

estrogen or is changed into a similar compound in vivo or clinically produces

effects that the clinician would expect from giving exogenous estrogens.

 

Plants may have compounds that are structurally similar to human endogenous

estrogens that mimic estrogenic activity or effect estrogen metabolism. Some

plants may show an estrogenic effect in laboratory studies, animal studies or in

clinical settings but the specific constituent or mode of action has not been

identified.

 

It is thought that the weaker phytoestrogens can compete for estrogen receptors

with the more potent endogenous estrogens thereby decreasing the overall

estrogenic activity when it is deemed to be too high.

When endogenous estrogens are low and phytoestrogens are used in large

quantities phytoestrogens have been shown to exert an estrogenic effect in

animals.

 

The phytoestrogens can take up receptor sites that are empty due to low estrogen

levels.

 

Most of the identified phytoestrogen constituents consist of sterols, coumestans

and isoflavones.

 

There are more than 300 plants, which have been identified as possessing

estrogenic or uterotropic activity. 282 Phytoestrogens compete with estradiol

for estrogen binding sites in the reproductive tracts of animals in vivo and in

human breast cancer cells in vitro. 220-2222, 223

 

Phytoestrogens will produce similar results to estrogens such as growth and

increased weight of the uterus. Research measuring weight increase of uteri in

mice showed sterols to have the most activity, followed by coumestans and then

isoflavones. 224, 291

 

Coumestans have a high affinity for the human estrogen receptor.

 

They are estimated to be 200 times less potent than estrone and 3000 times less

potent than diethylstilbestrol, and 30-100 times more potent than isoflavones.

 

Animal studies have shown coumestans can reduce follicle-stimulating hormone and

lutenizing hormone levels. Coumestans produce uterine growth in rats at natural

dietary levels and competitively inhibit binding to the estrogen receptors.

 

Not all isoflavones have estrogenic effects, but many of them do.

 

Some of them need to be converted by gut bacteria to other compounds to be

effective.

 

If a person is using antibiotics or ingesting other substances that destroy gut

flora, there would be decreased isoflavone conversion in the gut, and the herb

would not work as expected. The isoflavone, Genistein, has shown

antiproliferative effects against estrogen-dependent and independent human

breast carcinoma cell lines.

 

 

180 Phytoestrogens can act as anti-estrogens to compete with estradiol for

cytoplasmic receptors in estrogen-sensitive tissues. Non-gmo soybeans, which

also contain estrogenic isoflavones, have been implicated as being responsible

for the low incidence of breast and other female reproductive cancers in

Japanese woman who consume large amounts of soybean products.

 

183 Studies show a correlation between high levels of urninary lignans and

isoflavonoid phytoestrogens, specifically genistein, and a low incidence of

hormone-dependent cancers such as breast and prostate cancer.

 

In vitro studies show genistein and daidzein inhibit growth of both estrogen

receptor-positive and estrogen receptor-negative human breast cancer cell lines

(IC50=24-44um).

 

Dietary phytoestrogenes dilute xenoestrogen-type *carcinogens* by binding at

the receptor sites and acting as antiestrogens.

 

The phytoestrogens genistein and daidzein tend towards normalizing estrogen and

progesterone levels.

 

Lignans are phenolic compounds with weak estrogenic activity. They have been

linked to a lowered incidence of breast cancer.

The highest concentrations of estrogenically-active lignans are in the defatted

portion of flax seeds.

 

They are converted by gut bacteria to mammalian lignans, the primary ones being

enterolactone and enterodiol.

 

They are structurally similar to estrogen and bind with low affinity to estrogen

receptors. They also increase sex hormone binding protein.

 

The most potent phytoestrogens are the phytosterols. Common foods, which contain

phytosterols, are chestnuts, sesame, safflower, sunflower and pumpkin seeds.

 

Phytosterols are most common in organic whole grains, nuts, seeds and legumes.

The sterol, beta-sitosterol has phytoestrogen activity as well as

anti-inflammatory activity and antipyretic activity.

 

It can be found in Achillea millefolium, Anemone pratensis, Angelica sinensis,

Calendula officinalis, Glycyrrhiza glabra, Hypericum perforatum, Larrea spp.,

Panax spp., Piscidia erythrina, Plantago psyllium, Serenoa repens, Symphytum

spp., Taraxacum officinale, Trifolium pratense, Turnera spp., Tussilago farfara,

Valeriana officinalis, Viburnum prunifolium. 289, 290

A fat soluble extract of Humulus lupus was found to contain small amounts of

estradiol. 225 Water-soluble glycoproteins from Hops strobiles are

antigonadotropic and suppress progesterone production by luteal cells in rats.

226,227

 

Dioscorea species contain the steroidal sapogenin called diosgenin. Diosgenin is

manipulated chemically in laboratories to create estrone, testosterone, and

progesterone as well as adrenocortical hormones.

 

In current research on animals, it appears that diosgenin usually turns into

smilagenin due to action on it by gut flora 230 Both animals and humans poorly

absorb diosgenin itself.

 

When diosgenin was given orally to female rats they had an increase in uterine

weight, vaginal opening and vaginal cornification. 232 When injected into

ovariectomized mice there was a growth of mammary epithelium. 233 Chamaelirium

and Aletris both contain diosgenin and have produced estrogenic activity in

rats.

 

Cimicifuga (Black cohosh) contains the isoflavone formononetin and two other

unidentified endocrine-active compounds, which appear to have estrogenic

activity via competition for estrogen receptors.

 

Black cohosh has been shown to suppress luteinizing hormone secretion in

menopausal woman and competes in vitro with 17-beta-estradiol for estrogen

receptor binding sites. 37

 

Black Cohosh has an inhibitory activity in vitro and in vivo on bone resorption

in ovariectomized rats as well as rats on low calcium diets. 265, 266 The active

constituents in black cohosh are thought to be 1.) Triterpene glycosides,

principally actein, 27-deoxyactein, cimicifugoside and cimigenol

3-O-alpha-L-arabinopyranoside and related aglycones, 2.) Isoflavones including

formonoetin,

 

3.) Aromatic acids including isoferulic acid, ferulic acid, and salicylic acid.

281 Legumes are a good source of edible phytoestrogens. Soybeans and other beans

are the most highly researched source of phytoestrogens. They are currently

thought to be one of the best sources of edible phytoestrogens.

 

Additionally, soybean sprouts have the highest concentration of isoflavones.

Health care practitioners have been concerned about giving plants with

phytoestrogens to patients that have estrogen sensitive breast cancer.

 

Research has shown that women consuming high amounts of phytoestrogens in their

diet have had a decreased incidence of breast cancer rates.

 

Practitioners should be cautious giving phytoestrogens to patients on tamoxifen

or other anti-estrogenic drugs since the phytoestrogens could (theory, not

known) interfere with the drug therapy.

 

Sharol Tilgner (Author of Herbal Medicine: From the Heart of the Earth:)

 

Wise Acres

stilgner

www.planetherbs.com

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