Pine Pollen Ancient Medicine for a New Millennium

Scientific

Oddly, given its extensive history in China, research on pine pollen in the West is still in its infancy. Nevertheless, it is, at the beginnings of the new millennium, starting to be discovered as an important nutritive and medicinal. The realization that it is a powerful phytoandrogen (that is, a plant that contains testosterone) has probably done the most to stimulate interest in the herb (on the part of mostly male researchers). Its androgenic actions are due to a number of substances in the pollen, not only the testosterone and other male steroids.

Pine pollen contains large quantities of sterols, steroid-like substances, that are exceptionally potent. In essence, they are plant steroids. Plants generally contain five major steroids (there are others, of course, but they are considered to be secondary steriodal compounds, i.e., chemicals such as testosterone). The five primary ones are auxins, cytokinins, gibberellins, brassinosteroids, and ethylene.

Plant steroids have generated interest in commercial agriculture because their use strongly stimulates plant growth. (This is similar to an athlete taking human steroids to quickly build up muscle tissue—just as with athletes, a lot of unforeseen problems occur later on.) Such plant steroids are often very potent. Brassinolide (only discovered in 1979), is a powerful growth stimulant—as little as one nanogram (a billionth of a gram) applied to a bean sprout can significantly increase its growth. Brassinolide (and other brassinosteroids) is, essentially, testosterone for plants. Basically, its use causes hyper growth in agricultural plants.

In general, brassinosteroids are highly active in and essential to plant growth and development. There are over thirty different types of brassinosteroids that have been found so far— many of them are in pine pollen, including three rather potent ones: brassinolide, castasterone, and typhasterol. Interestingly, they are very similar in structure to animal steroid hormones and are highly biologically active. Most types of pollen contain large quantities of them.

Because of their potent biological activity in plants, research in recent years has begun to explore the impacts of these kinds of plant steroids on human health and disease. Two forms of the brassinosteroid brassinolide have been found to enhance the function of liver microsomes—these are crucial to the transformation and safe disposal of xenobiotics, that is, foreign chemicals that end up in the body.

Brassinosteroids such as brassinolide and castasterone have shown antiviral activity, sometimes of exceptional strength, against a number of viruses. Among them are herpes simplex type one (HSV-1), measles, and arena viruses. They have been found to be “ten to eighteen times more potent than ribavirin, the main pharmaceutical antiviral.

In vivo studies have found that brassinosteroid compounds prevent HSV-1 in a dose-dependant manner with no cytotoxicity; that is, without damaging effects on healthy cells. They reduced the incidence of herpetic stromal keratitis, including inflammation, vascularization, and necrosis.

Castasterone (followed closely by epibrassinolide) has been found to be the most highly active brassinosteroid against common breast and prostate cancer lines in laboratory studies in micromolar concentrations (i.e., at extremely tiny doses), again without affecting healthy cells. It’s use inhibits cancer cell growth and stops proliferation of cancer cells. The brassinosteroids are considered to be highly novel steroidal compounds with unique anticancer actions while possessing very low toxicity.

Epibrassinolide, another steroid in this group, has been found to reduce the activity of 5 alpha reductase. 5 Alpha reductase is the enzyme that acts on testosterone to convert it into the more powerful androgen DHT. There is some evidence that abnormal DHT levels are involved in prostate enlargement and midlife hair loss. Researchers are now exploring its effectiveness in the treatment of benign prostatic hyperplasia (BPH) and androgen-related hair loss.

Early research indicates that brassinosteroids may be effective in the treatment of not only cancer but also Alzheimer’s disease, Huntington’s disease, steroid-induced osteoporosis, sexual differentiation disorders, hyperadrenocorticism associated with sex steroid excess, androgen insensitivity syndrome, glucocorticoid insensitive asthma, steroid induced cataracts, and deficiency of P450 oxidoreductase. They have shown some effectiveness in lowering serum cholesterol levels.

Pine pollen also contains very high concentrations of another family of plant steroids called gibberellins. These are plant hormones that are widely spread throughout the plant world; seventy-five have been identified so far. Numbered, rather unimaginatively, GA 1-75, they are especially abundant in the pollens, seeds, and young seedlings of plants. They stimulate the initial stages of germination, significantly enhancing seedling growth. Normal food plants, if sprayed with GA3, for “example, exhibit hyper growth—they significantly increase their size.

Gibberellins, also potent anti-inflammatories, decrease arachidonic acid release; decrease formation of leukotrienes, thromboxanes, prostaglandins, and prostacyclin (all involved in inflammation); and increase the stability of lysosomes. They increase the activity of cyclic AMP and GMP, which inhibits lymphocyte stimulation and the release of histamine and lysosomal enzymes.

They possess antitumor activity, have been found to be immunoactivating, and are effective in the treatment of BPH, psoriasis, and herpes simplex 1 and 2. In vivo trials found gibberellins (especially GA3 and GA7) to be highly effective in the topical treatment of burns, wounds, thromphlebitis, bronchitis, open fractures, peptic ulcer, aphthous ulcer, and decubitus.

Their impacts on the prostate are complex. They tend to act as prostate regulators rather than just reducing inflammation. If the prostate is enlarged they tend to reduce its size; if too small (as in castration of male rats) they increase its size or prevent atrophy. Dosing with 1 mg of GA4 resulted, in one human trial, of significant reduction of an enlarged prostate within an hour of administration.

But gibberellins are also stimulating interest because they are structurally very similar to testosterone; so close, in fact, that they bind to testosterone receptors in the human body. The physiological effects of testosterone are therefore mimicked by gibberellins; gibberellins are in essence testosterone mimics and thus androgen-like compounds. Like human androgens, they stimulate growth in both plants and animals. They possess both anabolic- and libido-enhancing activity, act as an adrenal and pituitary tonic, and are considered to be both androgenic and gonadotrophic. Because of their adrenal and pituitary actions, they stimulate androgen production in the body; energy levels increase. Gibberellins help prevent the atrophy that accompanies castration (in rats), which is one of the signs of strong androgenic action. They are present in most pollens at about 1 microgram per gram.

The gibberellins and brassinosteroids in pine pollen play integral parts in the health of the ecosystems of which pine trees and forests are a part. Pine pollen is “produced in much larger quantities than needed for pollination. The excess pine pollen falls to the ground and is absorbed by the plants that grow in those ecosystems, much to their benefit. It is, in fact, essential to the health of those ecosystems, and the plants, insects, and animals in them.

Pine pollen is also relatively high in arabinogalactan. It comprises about 1 percent of each pollen grain. Arabinogalactan is a polysaccharide abundant in the pine family. Most of the commercial forms are harvested from larch (Larix spp) trees, which have particularly high levels of the compound. Arabinogalactan has been generating a lot of interest of late as both an immune-stimulating supplement and as an adjunct in the treatment of cancer.

Arabinogalactan is approved as a dietary supplement by the FDA. It is a good source of dietary fiber and increases butyrate (and other short-chain fatty acid production) in the gut. Butyrate is essential for colon health and helps protect the intestinal mucosa against disease, including cancer. It has been found to be a probiotic in that it stimulates the production of bifidobacteria and lactobacillus in the GI tract. Arabinogalactan also prevents excess ammonia “buildup in the liver, something that can occur in diseases such as portal-systemic encephalopathy.

It is a useful adjunct in the treatment of cancer because of its immune stimulating actions. The polysaccharides of which the compound is composed stimulate the natural killer (NK) cell activity and cytotoxicity, increase gamma interferon production, stimulate general immune responses, and have been found to block metastasis of cancer cells to the liver. Arabinogalactan stimulates phagocytosis, competitive binding of bacterial fimbriae, and bacterial opsonization. It is especially effective against Gram-negative bacteria, including Klebsiella species. The supplement has been found helpful in chronic fatigue, hepatitis B and C, multiple sclerosis, and lyme disease. It will help to some extent in raising CD4 white blood cell counts which are often lowered in diseases such as AIDS.

Amino acid content is high in all pine pollens. For instance, chemical analysis of Pinus montana pollen has found that it contains the following: arginine (6.4 g/100 g), leucine (6.5 g/100 g), lysine (5.1 g/100 g), methionine “(1.5 g/100 g), phenylalanine (2.1 g/100 g), tryptophane (0.8 g/100 g), tyrosine (2.1 g/200 g), plus trace amounts of alanine, amino-butyric acid, aspartic acid, cystine, glutamic acid, glycine, hydroxyproline, isoleucine, proline, serine, threonine, valine.

The Pinus massonia and Pinus tabulaeformis combination that is often used in Chinese pine pollen tablets contains similar amino acids (per 100 grams): asparagic acid (1098 mg), threonine (492 mg), serine (522 mg), amino glutaric acid (1579 g), aminoacetic acid (698 mg), alanine (564 mg), isoleucine (539 mg), leucine (846 gm), tyrosine (365 mg), phenylalanine (572 mg), lysine (802 mg), histidine (189 mg), cystine (112 mg), valine (646 mg), merionin (166 mg), arginine (998 mg), proline (884 mg), and tryptophan (149 mg).

Phenylalanine is linked with neurotransmitters in the brain and affects mood and stimulates dopamine levels in the brain. Both phenylalanine and tyrosine are L-dopa precursors. L-dopa is metabolized into dopamine in both the heart and brain. Dopamine is a neurotransmitter without which neural communication in the brain would be impossible. L-dopa has also been found to increase sexual interest and activity and facilitate erections in men. It is specific for treating anorgasmia, a woman’s inability to have an orgasm. Essentially, L-dopa is a prosexual chemical. Tyrosine is also the precursor for epinephrine (adrenaline) and norepinephrine. Arginine is a precursor of nitric oxide (an erection stimulant) and possesses wound-healing and immune-enhancing functions (which is why pine pollen is so effective for skin conditions). Arginine boosts growth hormone release, improves fertility, and is spermigenic (that is, increases sperm production) at 4 g/day. “Much of the excitement surrounding pine pollen is, however, due to the presence of human androgens in the pollen: testosterone, androstenedione, dehydroepiandrosterone, androsterone, and epitestosterone. These, and the many other androgen stimulants or mimics that are present in pine pollen, make it one of the most potent natural phytoandrogens known and a welcome addition to the herbal pharmacopoeia.

Analysis of numerous pine pollens, including those from Pinus sylvestris, Pinus nigra, Pinus bungeana, and Pinus tabulaeformis has shown the presence of andro-androgenic constituents, including testosterone, in all the pollens.

Pinus nigra, or black pine, pollen contains the androgens: androstenedione (0.7-0.8 mcg per 10 g, .000009% by weight), testosterone (0.7 mcg per 10 g, approximately .000009% by weight), dehydroepiandrosterone (DHEA) (.0000015% by weight, about 0.1 mcg per 10 g), and androsterone (0.0000022% by weight, approx. 0.2 mcg per 10 g). The testosterone in Pinus bungeana pollen runs 11 ng per 0.1 gm dry weight (about 1.1 mcg per 10 g dry weight), while Pinus tabulaeformis runs 27 ng per 0.1 g dry weight (2.7 mcg per 10 g dry weight). Research on Scots–NOT Scotch–pine (Pinus sylvestris) pollen has found testosterone, epitestosterone, and androstenedione in the same kinds of micromolecular amounts. Testosterone is present at 0.8 mcg per 10 g dry weight, epitestosterone at 1.1 mcg per 10 g, and androstenedione at 5.9 mcg per 10 g dry weight. A microgram (mcg) is a millionth of a gram, a nanogram (ng) is a billionth of a gram. While those these amounts might seem extremely small it takes as little as four nanograms (one thousandth of a microgram, one billionth of a gram) to change an infant’s sex to male while it is developing in the womb. That figure can be mathematically represented by 0.004 mcg. In comparison to that figure Pinus nigra pollen contains 0.7 mcg per 10 grams of pollen. (And oral dosing in China runs from 5 to 10 grams per day, which, barring the problems of testosterone going through the GI tract, would give a comparatively high dose of testosterone every day.) Androgens are very potent chemicals. These amounts are enough, when pine pollen is taken by mouth as a tincture, to raise testosterone levels within a few minutes of ingestion.

Testosterone levels in the blood tend to peak in mid-morning, in mid-afternoon, and between 3:00 and 5:00 a.m. During aging the height of those peaks lowers, sometimes considerably, especially in those who are testosterone compromised. Taking pine pollen tincture upon rising, again at noon, and again before bed will help simulate the body’s normal patterns of testosterone production. Androstenedione, commonly present in pine pollen, is one of two androgens in the body that are converted directly into testosterone, making it a metabolic precursor of testosterone. The body converts DHEA to androstenedione and then converts that (usually) into testosterone or (sometimes) into estrone, an estrogen. Androstenedione and testosterone convert back and forth between each other using a specific (zinc-dependant) enzyme 17-beta-hydroxysteroid dehydrogenase, which is why zinc is essential to the diet for healthy androgen levels.

Androstenedione can also be made through an entirely different process in the body. Instead of using the pathway which begins with pregnenolone, 17a-hydroxypregnenolone, DHEA, andro, it is generated beginning with pregnenolone, then a conversion into progesterone, 17a-hydroxyprogesterone, and finally androstenedione to testosterone. For this second pathway the enzyme 17,20-lyase is used. Anything that reduces the levels of the particular enzyme (or the zinc it needs) that converts androstenedione to testosterone or that makes androstenedione in the first place results in lower levels of testosterone. Licorice, for instance, inhibits the 17,20-lyase enzyme and can reduce both serum testosterone and androstenedione levels.

Androstenedione, in comparison with testosterone, is a weak androgen. However, regular intake of androstenedione can and does increase testosterone levels in the blood.

While DHEA, again a common androgen in pine pollen, itself is only a mild androgen, it is the precursor for both androstenedione and androstenediol, two of the precursors of testosterone, making it essential for testosterone production. As well, research over the past twenty years has shown that it has significant effects on human health in almost every organ system in the body.

DHEA is the most abundant steroid in the human bloodstream; most of it (about 70 percent) is made from DHEA sulfate. The body essentially stores DHEA in a more stable form as DHEA sulphate (DHEAS) and converts it to DHEA (and then other androgens) whenever it is needed. During middle age, levels of testosterone and DHEA tend to decline. DHEA levels peak around a man’s twenty-fifth year and then decline by about 2 percent per year. By age eighty blood levels are only at 10–15 percent of that peak. Normal levels of DHEA in the blood are 250–650 micrograms per deciliter (about one tenth of a quart) of blood; DHEAS levels tend to be 500–1000 times higher. (DHEAS and DHEA can be considered interchangeable when talking about the health effects of DHEA.) People with levels of DHEA below 100 mcg/dl consistently show higher levels of cancer, heart disease, diabetes, and arthritis.

Most DHEA is synthesized in the adrenal glands; about 10 percent is made in the testes, while the rest is made in the brain, the heart, and the liver. Because of its synthesis in the brain DHEA is also considered to be a neurosteroid, having potent impacts on the central nervous system and brain function.

DHEA in peripheral tissues is often converted to more active androgens, and these levels never appear in the bloodstream. Basically, peripheral tissues in the human body make more active androgens from DHEA whenever they need them. Peripheral tissues in the body normally contain all the enzymes necessary to convert DHEA to androstenedione and then to testosterone. “This allows the more potent androgens to be used at the site where they are most needed in the exact levels needed; and perhaps this explains how DHEA is able to affect so many different parts of the body. In essence, the androgens synthesized from DHEA exert their effects within the same cells where synthesis takes place, and these synthesized androgens are rarely released into general blood circulation (thus never showing up in blood tests). The parts of the body that are engaging in androgen synthesis are essentially using an extremely sophisticated biofeedback loop to determine exactly what levels of androgens are necessary and then making exactly what they need from the DHEA that normally circulates in the body. At least 30–50 percent of the total androgens in men are synthesized in peripheral tissues in just this way. The enzymes that are used for this androgen synthesis (or metabolic conversion) and the basic androgenic precursors, especially DHEA, are, thus, absolutely necessary for overall health.

Because DHEA can be converted to the estrogens estrone and estradiol, some people feel that DHEA is a potential problem when used in androgen replacement therapy. No research has found this to occur; estrogen levels in men consistently remain unaffected by DHEA intake. For example, one study of sixty-to seventy-year-old men who received intramuscular DHEA injections showed increased levels of DHEA and androstenedione in their blood. No change was found in their levels of “estrone and estradiol. Even with extremely high oral dosing in young, healthy men (1600 mg per day), estrone, estradiol, and SHBG levels remain level.

DHEA supplementation will generally increase levels of DHEA in the blood as well as increasing serum androstenedione and testosterone. Overall, DHEA supplementation increases androgen levels in peripheral tissues, increases serum androstenedione, and improves functioning in most organ systems of the body. The majority of chronic diseases associated with male aging can be significantly helped with DHEA supplementation.

DHEA use has been shown to be associated with higher levels of energy and well-being, lower obesity/waist-to-hip ratio, enhanced libido and erectile ability, reduced depression, enhanced cognition, reduced death from coronary heart disease, and improved insulin sensitivity and glucose tolerance.

In short, pine pollen is a potent source of natural androgens, including testosterone and androgen mimics, it is a great nutritional source, especially of amino acids, vitamins, and minerals, and it is an excellent general tonic for the human body, useful in preventing or alleviating a number of conditions common to aging.

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