http://www.hemingways.org[...]bal.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.
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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.
Cristine
This post was edited by Cristine Jennifer Shye. BL at December 7, 2020 2:05 PM GMT