11-05-2014, 22:36
taken from GID.info
http://www.hemingways.org/GIDinfo/herbal.htm
HERBAL HORMONES
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 supplement.
USE IN TRANSGENDER FEMINZATION
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., "natural") .
Disclaimer: 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.
PHYTOESTROGENS
Alfalfa (Medicago 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:
The practical 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.
In conditions 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 estrogenic properties.
Sage and Soy also have phytoestrogenic isoflavonoids in them, but not to the extent of Black Cohosh or Red Clover.
Vitex (Chaste 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.
Don Quai - 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.
Licorice - 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.
[following information added 4 January 2002]
Here are some additional cautionary notes on the over-use of Licorice (glycyrrhiza glabra):
Licorice can 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, Brazil. (source)
Licorice acts 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)
Lowered potassium 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 1.1.1.146) in rats. Results resembled effect of mineralocorticoid" Cooney AS, Fitzsimons JT. Physiological Laboratory, Cambridge, UK. (source)
(See Note on purchasing Licorice Below)
ANDROGEN BLOCKERS
Licorice - "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)
A 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.
Saw Palmetto - 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:
Comparison 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
Languages: ENGLISH
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.
Cannabis - 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.
PROGESTERONE SUPPLEMENTS
Mexican Wild 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 of diosgenin.
Fenugreek - 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 Wild Yam.
WARNINGS!
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.
BLOOD CLOTS
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.
Overall, a 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.
While estrogen 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.
LIVER DAMAGE
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.
DIOSGENIN EXPLAINED
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.
Natural plant 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:
Unfortunately, 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.
BEFORE 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.
If 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.
The 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)
In 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 (source). This being due to other methods of production and laboratory synthesis, usually using an inexpensive Soy-oil "starter" and stigmasterol.
This 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.
Some 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).
To summarize:
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.
Progesterone IS available in some products at low, non-prescription (but often ineffective) dosages.
Progesterone is best introduced to the body Transdermally, Sublingually, or by Injection.
