Many plants contain
compounds that directly or indirectly affect hormones or hormone activity
in the body. Since phytoestrogens (i.e., "Plant Estrogens")
are far weaker than their animal counterparts, they can be used effectively
to manage overabundant or deficient amounts of estrogen. The molecular
structure of phytoestrogens is so similar to those in animals that they
readily bind with estrogen receptors, in some cases even more readily
than the actual animal steroids. Becase the plant steroids are so much
less "reactive," though, they occupy the receptor while only
performing some (or none) of the job. The animal estrogen is swept on
in the bloodstream to either bind with some other receptor, a blood
protein, or ultimately to be destroyed in the liver or excreted from
the body altogehter. In this way, plant hormones can be used to "block"
the direct activity of free, unbound estrogen in the body. If there
is a deficiency the small amount of stimulation from the plant hormones
can cause a mild estrogenic effect and in this way act as an estrogen
USE IN TRANSGENDER
If you are a Male-to-Female
transgendered person who have come to this page in search of information
on over-the-counter natural/herbal hormones for the purpose of feminizing
your body, you need to be aware that the effectiveness of the few herbals
the DO exert estrogenic actions is extremely minimal because phytoestrogens
tend to be only about 1/1000th as strong as animal estrogens. These
herbal drugs may work well to help balance a biological females peri-menopausal
or post-menopausal endocrine system, but they are wholly insufficient
for over-riding a biological male's testosterone dominance. The amounts
of herb that would have to be consumed would be dangerous if not outright
toxic. While some people do report some minor effect from certain herbal
formulations (such as gynecomastia or a small amount of fat redistribution)
the majority of transgender people who've tried them will tell you that
herbals are ineffective and a waste of money if your goal is to fully
feminize your body. Only prescription-grade
hormones will provide adequate feminization results
(some of which are bio-identical to what your body produces - i.e.,
I am not a medical nor naturopathic doctor. This is
all based on months of research I did myself trying to find out if herbal
supplements might help my own hormone imbalance. I provide it here for
informational purposes only.
sativa) - The hormonal activity of alfalfa was first observed in
Veterinary Medicine. Animals observed grazing on alfalfa developed traits
similar to animals treated with synthetic estrogens. Alfalfa contains
three major plant estrogens: coumestrol, genistein, and formonetin (as
well as the lesser diadzein and biochanin A). Coumestrol is the most
active with a relative activity of 5% that of a natural estradiol estrogen.
Genistein's activity is about 1%, and formonetin is .01% or less. The
amount of "active" phytoestrogens varies with the growing
season. It is highest during the full blooming and seeding stages. Also,
keep in mind that these are the active percentages for EXTRACTED phytoestrogens
as compared to an equal amount of true estrogen - the amounts consumed
in plant form will vary widely and will likely be in much smaller concentrations.
From the Journal
of Naturapathic Medicine, Volume 1, Number 1:
importance of the phytoestrogens lies with their ability to alter
the biological response to endogenous estrogen. Estradiol receptors
will bind to a diverse group of chemical compounds, including other
steroids, isoflavones and phytoestrogens. When phytoestrogens bind
to estrogen receptors on cells, they translocate to the nucleus and
stimulate cell growth in a manner similar to estradiol. Despite the
apparently weak relative binding capacity of the phytoestrogens, they
can have significant hormonal effects. This is due to their lower
affinity for the serum estrogen binding proteins, this resulting in
a net effect of enhancing the concentration of available phytoestrogen
at the target tissue sites.
The relative weakness
of their estrogenic action means that these compounds will have an
"alterative" or "balancing" effect. Thus, phytoestrogens may be used
therapeutically in both hypoestrogenism and hyperestrogenism states.
It is precisely this quality that makes them so useful therapeutically,
especially in a naturopathic setting.
of hypoestrogenism [lack of estrogen] the plant estrogens will bind
directly to estrogen receptors and provide a mild estrogenic effect.
This is enhanced by the tendency of the phytoestrogens to concentrate
in reproductive tissues, in preference to the serum proteins.
. . . .When we
use these plants medicinally as an alternative to synthetic drugs,
it is essential to remember that we are utilizing the specific plant
components in order to produce pharmacological actions. Thus, we would
be well advised to utilize the most concentrated sources available.
In the case of Medicago the preferred forms are solid extracts, fluid
extracts and concentrated tinctures. Teas and tablets may not deliver
enough active ingredient to be effective.
It should also be
noted that alfalfa contains a seperate and distinct "anti-estrogen"
compound that is reported to be about 12% as strong as the phytoestrogens,
so there is some "attrition" of effectiveness when this compound
is also present (the compound is apparently chloroform-soluable, but
I don't know if that means it can be eliminated).
Sage, Soy, Red
Cover, Black Cohosh - large amounts of phytoestrogenic compounds.
Black Cohosh (Cimicifuga
racemosa or Cimicifugae racemosae rhizoma), also known
as "Snakeroot" can be toxic in large doses. The best info
I could find was not to take more than about 2000mg/day of the ground
root. If you get nausea, you're taking to much and should cut back
your dosage. It is one of only a couple plant steroids known to have
a direct hormonal effect within the human body (source).
Red Clover contains
high levels of isoflavone compounds such as Genistein, which have
Sage and Soy also
have phytoestrogenic isoflavonoids in them, but not to the extent
of Black Cohosh or Red Clover.
Tree/Berry) - has no phytoestrogenic or other direct hormone effect.
Stimulates LH (Leutenizing Hormone) production, which can in turn increase
levels of progesterone secreted by the endocrine system. However, a
component of Black Cohosh also has a LH suppressing action, so if these
two are taken together they can end up working against one another.
- clinical tests performed by Kaiser Permanente showed it has NO estrogenic
or phytoestrogenic effects. Another component acts as a muscle relaxant,
which explains why it helps ease PMS cramps for women. As a component
of HRT, however, it was no more effective than the placebo.
- also has lots of phytoestrogenic compounds but side effects and long
term toxicity preclude it's value as a Hormone Replacer. In fact, it
is one of the very few plants that has a direct hormonal action in the
human body (source).
It's generally used short-term as a treatment for Asthma or other bronchial
problems in that it acts as an expectorant. It also can cause high blood
pressure if used for extended periods.
added 4 January 2002]
Here are some additional
cautionary notes on the over-use of Licorice (glycyrrhiza glabra):
act as an anti-coagulant, preventing blood clots. This can be a benefit
for someone who is prone to thrombosis (a potential risk of taking
exogenous estrogen compounds). However, it also leaves the person
risk to hemmorraging and hematomas. "Glycyrrhizin prolonged thrombin
and fibrinogen clotting times, and inhibited thrombin-induced, but
not collagen-, PAF- or convulxin-induced platelet aggregation."
Francischetti IM, Monteiro RQ, Guimaraes JA, Francischetti B. Department
of Medical Biochemistry, ICB/CCS, Federal University of Rio de Janeiro,
as a corticosteroid and abuse or long term use has similar effects,
one of which can be corticosteroid-induced Cushing's
Syndrome. "Urine cortisol excretion more than doubled (33
to 83 microgm) in 10 of 13 people taking 100 or 200 g licorice for
1-4 weeks. Levels typical of Cushing's syndrome were seen in 7 subjects
and remained high for a week after licorice stopped." Epstein
MT, Espiner EA, Donald RA, Hughes H, Cowles RJ, Lun S. (source)
levels, increased thirst, increased blood pressure, and a craving
for salty foods are also common with Licorice abuse. "Increases
in potassium loss, water intake and appetite for salt were found after
glycyrrhizic acid blocking of 11 beta-OHSD (EC 18.104.22.168) in rats.
Results resembled effect of mineralocorticoid" Cooney AS,
Fitzsimons JT. Physiological Laboratory, Cambridge, UK. (source)
Note on purchasing Licorice Below)
- "Testosterone decreased 35% and 17-hydroxyprogesterone increased
21% in 7 men taking 7 g/d licorice (500 mg glycyrrhizic acid) for a
week; returning to normal 4 days later. This indicates inhibition of
17B-hydroxysteroid dehydrogenase and 17,20-lyase" Armanini D,
Bonanni G, Palermo M.(source)
Note on Purchasing Licorice: There are actually two forms
of this herbal available on the market. One is labeled as being "De-glycyrrhizinated"
(abbreviated "DGL") and does not carry the health risks
of non-DGL licorice but also does not contain the glycyrrhizic acid
(the active ingredient) of interest to anyone taking Licorice as part
of an herbal HRT regimen. If you plan to use Licorice for HRT purposes
(either as an anti-androgen, phytoestrogen, or both) make
sure that you purchase the non-DGL kind.
- often listed with as an herbal anti-androgen. VERY weak compared to
true antiangrogens, and to gain a similar effectiveness would have to
be consumed in toxic amounts. It supposedly reduces the amount of 5-alpha-reductase
which in turn reduces the amount of testosterone that is converted to
DHT (dihydrotestosterone). DHT, in part, causes prostate swelling, and
estrogen inhibits the body's ability to remove DHT. Results were usually
attributed to administration of an EXTRACT from the plant. There may
be no truth to this claim, however. Here were the results of one study
which compared an estract of Saw Palmetto (Sernoa repens) to
the pharmaceutical drug Finasteride:
of finasteride (Proscar) and Serenoa repens (Permixon) in the inhibition
of 5-alpha reductase in healthy male volunteers.
Strauch G; Perles P; Vergult G; Gabriel M; Gibelin B; Cummings S;
Malbecq W; Malice MP, Eclimed Pharmacologie Clinique, Hopital Universitaire
Cochin, Paris, France.
Eur Urol (SWITZERLAND)
1994, 26 (3) p247-52, ISSN 0302-2838
A total of 32
healthy male volunteers (age range 20-30 years) were enrolled in a
1-week open, randomized, placebo-controlled study comparing finasteride
(Proscar), a 5 alpha-reductase inhibitor, with Permixon, the plant
extract of Serenoa repens. The objective of the study was to evaluate
the effect of single and multiple doses of the drugs on the inhibition
of 5 alpha-reductase as assessed by serum dihydrotestosterone level
determination. Following baseline measurements on day 1, the subjects
were randomized to finasteride 5 mg once a day (n = 10), Permixon
80 mg x 2 twice a day (n = 11), or to placebo once a day (n = 11)
for 7 days. Serum testosterone and dihydrotestosterone levels, were
determined on day 1 (baseline and 12 h) and on days 2 (24 h), 3 (48
h), 4 (72 h), 6 (120 h), and 8 (168 h). After 12 h, a single dose
of finasteride 5 mg reduced the serum dihydrotestosterone level by
65% (p = 0.01). The decreases ranged from -52 to -60% with multiple
doses of finasteride 5 mg once a day (p = 0.01). As in the
placebo group, there was no effect of Permixon on the serum dihydrotestosterone
level. No significant difference was detected between finasteride
and Permixon or between finasteride and placebo with respect to serum
testosterone, except on days 3 and 6, respectively (p = 0.05).
However, the corresponding serum testosterone levels remained within
the normal ranges.
So it appears lab
testing found Saw Palmetto (even in concentrated extract form) to be
completely ineffective as an anti-androgen. Saw Palmetto may have an
anti-estorgenic effect, but I could not locate any studies. If you're
trying to ADD estrogen to your body, and the rumour that is can be an
anti-estrogen is true, Saw Palmetto can work against that goal.
- known to interfere with androgenic hormones. Another herb with a number
of positive health benefits, but some undesirable side-effects as well.
Plus, in many places it is an illegal controlled substance - but I point
it out here because it IS an herb, it IS widely available (albeit, often
illegally), and it IS a known androgen blocker.
Yam (Dioscorea mexicana)- Contains "diosgenin"
which, when processed, yeilds progesterone. But this compound (diosgenin)
cannot be converted by the body, this must be done pharmaceutically.
Also extracted from the Mexican Wild Yams is DHEA (Dihydroepiandrosterone)
which is a naturally occuring, weak androgenic steroid (read: MALE HORMONE)
produced by the adrenal gland. Orally ingested DHEA is also converted
to DHEAS (S=sulfate), with a smaller fraction being converted to androstenedione,
and even smaller fraction converted to testosterone. Subsequent testing
of plants in the Dioscorea family have also found that Dioscorea
composita and Dioscorea floribunda also contain large amounts
- Another popular "female hormone" that contains diosgenin.
Appears to have beneficial effects on blood pressure and as a preventitive
measure against diabetes. Traditionally given as something to quiet
an upset stomach or to "relax" the uterus. The conversion
of diosgenin to progesterone suffers the same impossibility as Mexican
Following are two
of the most pressing risks associated with pharmaceutical grade hormone
use. Although there is no evidence that phytoestrogens pose similar
risks, there is also no evidence that they do not.
Here's some information
about the risk factor (this is in relation to post-menopausal women,
by the way, but I think it might be reasonable to assume that men might
have at least a similar risk, if not more-so since cardiovascular problems
are much more prevelant among the male population).
NEW YORK, March
14, 2000 (Reuters) -- Women who take estrogen after menopause have
a greater risk of developing blood clots in the legs or lungs in the
first year of hormone use, a new study suggests. The association holds
true whether a woman takes estrogen by pill or patch, alone or in
combination with other hormones, or in high or low doses. However,
the risk drops sharply after the one-year mark. After that, a
hormone-user appears to be at no greater risk of blood clots than
other women, according to the report in the March 15 issue of the
British Medical Journal.
woman has a 1.3 in 10,000 risk of developing such clots, which
can be life-threatening if they lodge in the lungs. A woman's risk
of clots rises to roughly 3 to 4 in 10,000 if she is taking estrogen,
reported researchers from Madrid and Barcelona, Spain. When used for
extended periods, estrogen replacement therapy (ERT) is thought to
greatly lower the risk of heart disease and the bone-thinning disorder,
osteoporosis. In the short term, ERT can help reduce menopausal symptoms,
such as hot flashes and night sweats.
does increase the risk of uterine cancer, most women also take progestin,
a hormone that helps to reduce that risk. The new study included 292
women, aged 50 to 79, who were diagnosed with lung or leg clots. The
researchers compared the women to 10,000 other randomly selected women
the same age. Overall, women have four to five times greater risk
of developing a clot in the first 6 months of taking hormones, and
a three times greater risk at 6 to 12 months of taking estrogen.
Other risk factors for such clots include a history of varicose veins,
removal of both ovaries, obesity, and smoking. A leg clot, or deep
vein thrombosis, is characterized by pain, swelling and warmth, and
discoloration of the skin on the affected leg. A lung clot can cause
shortness of breath, chest pain and fever.
What can you do
to prevent the possibility of blood clots? Well, don't smoke, make sure
to excercise regularly, and eat right. If there is a history of coronary
problems in your family, you're most likely a contender for cardiovascular
problems as well and should take that into consideration. A couple aspirin
a day is supposed to be healthy and prevent clotting because it acts
as a blood thinner.
The liver is the
largest organ inside your body and it performs over 500 functions and
is the primary "detox" center of your body, seperating the
good stuff from the bad stuff and then passing on the good stuff to
the rest of the body while sending the bad stuff to the gall bladder
and kidneys for further processing and disposal (that is a VERY simplistic
version of the process, by the way). And that literally means EVERYTHING
that winds up in your blood or stomach - alcohol, pesticides on foods
you eat, chemicals absorbed through your skin, fumes inhaled, etc. We
live in a VERY toxic world, and your liver is putting in a lot of Over
Time just trying to deal with it. Even things we normally don't think
of as "toxic" can be if the liver is overworked or malfunctioning.
A high protein diet can, for example, lead to unwanted Amonia in your
bloodstream (it is a byproduct of metabolizing proteins). Too much amonia
in the blood can lead to dementia, among other things. Okay, now that
the scare is on and you're ready to live in a bubble, you should also
know that the liver can do it's job even when 80% of it's tissues are
damaged. That doesn't mean you shouldn't care what you do to it, though.
As part of its "detox
duties" it also has to deal with a number of hormones. For example,
it is supposed to clear out extra insulin. If it doesn't, the insulin
remains in circulation and continues to do its job of lowering blood
sugar. Failure to dispose of adrenaline (the "fight" or"flight" hormone)
after it has outlived its usefulness may lead to chronic irritability
and temper explosions.
All products absorbed
through digestion initially pass through the liver. THIS is why ingested
hormones CAN POTENTIALLY damage the liver. The liver is supposed to
take care of "excess" hormone production. Ideally, if you
are trying to infuse your system with hormones, you want them to make
a complete circuit through your body, bonding to receptors along the
way, BEFORE the blood gets to the liver. Otherwise there are just too
many hormones for the liver to deal with. But it is also important to
consider WHICH hormones actually do damage. It is well-documented that
synthetic anabolic steroids or testosterone derivitives damage the liver.
I had difficulty understanding exactly HOW they damage it, but I gathered
that the enzymes employed in breaking down the "natural" hormones
into harmless compounds often "accidently" break synthetics
down into toxic substances that cause cellular-level damage. But what
about estrogen? In some cases, even as little as two or three weeks
of use have been documented to ruin the ability of the liver to detoxify
natural estrogen. The livers of women on B vitamin/protein deficient
diets may have difficulty metabolizing estrogen to non-toxic estriol,
leaving it instead in the form of liver toxic estradiol. Estradiol is
the form associated with hyper emotional states including explosive
temper and obsessive-compulsive tendencies (essentially, PMS).
The main problem
with taking hormones orally is that the hormones are passed into the
liver as part of the process of digestion. Not only will some of the
hormones be destroyed in the process, the liver is designed to deal
with small amounts of "left overs" and will be inundated by
the large amount of hormones - some of which will likely be liver-toxic
and cause cellular damage to the organ. Whatever the liver can't handle
will ultimately be washed out the "downstream" side of the
liver into the cardiovascular circuit where the hormones will be pushed
all around the body, binding to receptors as they go, before the blood
returns to the liver. The problem with this scenario is that it is the
REVERSE of the process for hormones produced within the body.
So, obviously, if
you are going to have estrogen passing through your liver BEFORE it
gets into the rest of your bloodstream, you'd avoid liver-toxic (i.e.,
liver damaging) effects if the hormones were "ESTRIOL" in
form instead of "ESTRADIOL." However, phytoestrogen most closely
bear a chemical resemblence to "estradiol" estrogens, meaning
that you wouldn't particularly want a lot of them being processed through
your liver. How much is too much? That's unknown and would vary person
to person and also depend on the concentrations of phytoestrogen consumed.
Even though the phytoestrogens are comparatively weaker than true estrogens,
studies of women on birth control pills have indicated that damage to
the liver's ability to process estradiol is compromised relatively quickly.
There appears to
be some debate over the value of "Diosgenin" as a hormone
in plants like Mexican Wild Yam, Fenugreek, Agave, Soy, and
Yucca. The herbal supplement industry is walking a very thin line
of legality in their labeling practices and has contributed to much
of the confusion surrounding this "herbal hormone." The herbal
supplement industry also likes to use the terms "disogenin,"
"hormone precursor," and "phytoestrogen" interchangably.
Here is the scientific
fact: The human body does not have the enzymes necessary to synthesize
Diosgenin into Progesterone or any other hormone.
Diosgenin is not
really a hormone anyway. It is what is called a "Saponin."
Saponins mimic hormones because they have molecular structures that
are similar to natural hormones.
steroids are formed by the polymerization of 5-carbon isoprene subunits
into tetracyclic triterpenoid compounds during complex metabolic pathways
inside plant cells. All steroids have the same fundamental structure
of four (tetracyclic) carbon rings called the steroid backbone or
steroid nucleus. The addition of different chemical groups at different
places on this backbone leads to the formation of many different steroidal
compounds, including the sex hormones progesterone and testosterone,
the anti-inflammatory steroid cortisone, and the cardiac steroids
digoxin and digitoxin. (source)
As you can see from
the three images below, the "Steroid Backbone" for hormones
is the same whether it is a male or female hormone. What is different
is what is molecularly bound to that backbone - which determines the
molocule's chemical interactivity inside the body:
just having the "back bone" molocule isn't sufficient. It
HAS to have the other carbon, hydrogen, and oxygen atoms hanging off
of it in the right places. Complicating matters is that this useful
"backbone" molucule is already "bound" in the plant
cell as "diosgenin." It is essentially non-reactive and not
bio-available for use by the human body.
it can be used by the human body it must be pre-processed. As mentioned
previously, the human body does not have the chemical mechanisms (enzymes)
to break the complex diosgenin molocule apart, nor to reassemble the
pieces into a useful hormone. This MUST be done outside the human body.
you were hoping there was some easy procedure to pre-process diosgenin
containing plants and produce your own supply of progesterone (or other
hormones), you're outta luck.
process was developed in the 1940s by Dr. Russell Marker, which is why
it is called "Marker Degredation." Using a multi-step process
involving specific enzymes and recombinant agents he was able to extract
the diosgenin molucules, break the down with enzymes and other chemicals,
and with other enzymes and chemicals get the carbon, hydrogen, and oxygen
atoms to bond to the steroid backbone and produce pure, pharmaceutical-grade
progesterone. Because it came from plant materials and is molecularly
identical to what the human body produces, it is called "Natural
Progesterone" even though it is synthesized from plant material
in a laboratory. (source)
Dr. Marker's early trials the process took over 30 steps, which made
synthesis from plant saponins economically unviable. Eventually he wittled
it down to about 6 steps, which made it less expensive than other methods
of hormone synthesis or harvesting. Although I've found numerous references
to the history of this process and Dr. Marker's problems finding someone
to fund his research, I have not been able to locate any source online
that details WHAT enzymes and chemicals are used, or what constitutes
the 6 steps of the synthesis process. I'm not looking for that information
for the purpose of making my own - I'm no chemist or biologist and to
attempt to make pharmaceuticals yourself is stupid and dangerous - I'm
just curious about the process and materials involved, as I'm sure you
are too if you're bothering to read this stuff. Cortisol is also extracted
from diosgenin, but through a different process involving stigmasterol
and bacterial culturing. It is also worthy to note that one researcher
found that no company producing pharmaceutical-grade progesterone has
used Yams or the "Marker Degradation" method in about 20 years
This being due to other methods of production and laboratory synthesis,
usually using an inexpensive Soy-oil "starter" and stigmasterol.
isn't to say that there is NO effect in using diosgenin containing plant
extracts. Anytime you put something into your body, your body is going
to attempt to break it down and process it. One also has to remember
that if the plant materials have been pre-processed in any manner, it
is likely that some of the long-chain molucules have been broken up
in the mashing, chopping, or other processes likely to "degrade"
molecular bonds. It is possible that a limited (an EXTREMELY LIMITED)
amount of diosgenin is accidently broken down to the "Steroid Backbone"
or some other form that will mimic the actions of a real hormone or
will bond to hormone receptors - which may just have the effect of occupying
the "seat" or it may have the desired biochemical effect.
But this is a complete "crap shoot" as to how much diosgenin
is broken down into something useful and exactly what form it takes.
I bring up the possibility only because there have been some studies
of women using plant-derived topical ointments in large concentrations
who HAVE shown a progesterone-like effect, but nothing comparable to
the use of pharmaceutical-grade progesterone.
of the topical creams DO contain low concentrations of pharmaceutical-grade
progesterone, however. I recently found out that in the United States
these concentrations are limited to less than 3% if the product is to
be non-prescription and sold as a "cosmetic" and that the
inclusion of any concentration of pharmacuetical-grade progesterone
in a cream was banned by Canadian law. The preferred method of delivery
for progesterone is as a topical ointment. This allows the hormone to
enter the bloodstream and be both circulated and bioavailable to receptors
in body tissues. Oral consumption is the least effective, as progesterone
is destroyed by acids in the stomach and whatever isn't destroyed is
passed to the liver where, if you're lucky, up to 5% will be absorbed
into the bloodstream. Sublingual (under the tongue) is much more effective
at about 90% absorbtion, but are ruputedly hard to find. Injectibles
are considered 100%, but most people don't like the injections. Transdermal
delivery (by skin patch or creams) is more than 90% efficient - depending
upon the method of delivery and the transfer agent (source).
- Diosgenin is
compound with a steroidal structure similar to natural hormones
- The human body
cannot process diosgenin into any other substance
- Diosgenin must
be pre-processed into hormones in a laboratory and you can't do it
at home in your kitchen.
- Many diosgenin-containing
plants have other, non-hormonal, benefits.
- Orally consumed
progesterone is mostly destroyed by digestion.
IS available in some products at low, non-prescription (but often
is best introduced to the body Transdermally, Sublingually, or by