Botanical Description & Habitat
Pygeum africanum, prunus a
African Plum tree
Higher plateaus of southern Africa and Madagascar
A large evergreen tree. It has thick, oblong leaves, with small white flowers.
The fruit is a red berry, resembling a cherry.
Bark (red, brown or gray) which has an acid odor.
Historical Properties & Uses
Pygeum has come to the attention of the western world as a primary and very effective treatment for benign prostatic hypertrophy, and secondarily for prostatitis.
Although pygeum appears to have been described for the first time in botanical texts of the second half of the 18th century, its utilization as a medicinal plant presumably dates to some remote era, when it was the custom of certain isolated peoples of southern Africa to prepare teas by powdering the bark, dispersing it in water or milk, and administering it for both minor and serious complaints.
Research during the past two decades has not only attempted to elucidate and validate medicinal properties, but has been concerned with discovering effective extraction methods and ways of concentrating the active principles. In addition, analytical techniques were developed for the proper identification and standardization of the active principles in the dozens of different extracts being investigated.
It is now the leading treatment for BPH in France.
Method of Action
Clinical trials done during the early 1970's were generally pretty sloppy, as most early medical research tends to be. One finding these dozens of "pilot" studies had in common was pygeum consistently and reliably affected the course of benign prostatic hypertrophy.
Simultaneous with the early clinical trials, researchers were beginning to identify the different chemical fractions of the plant with suspected activity. Another series of animal and clinical trials was thereupon undertaken, the purpose of which was to clarify the action of each of the classes of constituents.
Pygeum contains three groups of lipid soluble components with effects on prostate disease. These are summarized as follows:
1. Phytosterols: beta-sitosterol, beta-sitosterol-3-0- glucoside, beta-sitosterone. Physiological action: anti-inflammatory.
2. Pentacyclic triterpenoids: ursolic acid, 2-alpha-hydroxyursolic
acid, oleanolic acid, crataegolic acid, friedelin. Physiological action: anti-edema.
3. Linear alcohols: n-tetra-cosanol, n-docosanol, and their particular ester derivatives, such as n-docosyl trans-ferulate. Physiological action: hypocholesterolemic.
Pharmacology of the Phytosterols
Most early research on individual pygeum fractions focused on the phytosterols, since past experience strongly suggested these were responsible for observed activity. Phytosterols, especially beta-sitosterol, are very prevalent in nature, occurring in variable percentages, in hundreds of plants: in half of the common grains, in oil of corn, in the oil of soy beans, in saw palmetto and pumpkin seeds, and in the bark of pygeum.
While it was formerly thought substances like beta-sitosterol were able to reduce the size of prostate adenoma, the main action turns out to be anti-inflammatory; subjectively, a decrease in inflammation could be perceived as an actual reduction in size.
The mode of action involves the inhibition of the biosynthesis of prostaglandins, mediators of the inflammatory process. The interference by beta-sitosterol on the metabolism of prostaglandins, especially epithelial levels of prostaglandins E2 and F2-alpha, have been well documented.
Patients with BPH normally show extremely elevated levels of prostaglandins; in a period of several days to several weeks under the influence of beta-sitosterol, these levels drop significantly.
Clinical studies using the phytosterol fraction of pygeum likewise normalize prostatic prostaglandin levels and are responsible for alleviating many cases of local hyperemia (excess blood) and vasal congestion.
Some authors maintain beta-sitosterol works by actively competing with some of the body's own substances having similar chemical structures during the metabolism of androgens, with the result of sensitizing prostatic cells to the hormonal stimulation. Result: a reawakening of sleeping gonadal activity. This assumes, of course, decreased gonadal activity is responsible for BPH, an important theory ascribed to by all investigators.
Recent research suggests the presence of phytosterols can not account for pygeum's total observed activity.
Pharmacology of the Pentacyclic Triterpenoids
These substances, particularly ursolic acid, and oleanolic acid, may be characterized by one special pharmacological action, evidenced by their response to traditional models of experimental inflammation: an effective anti-edema, or diuretic, action.
In addition, or in particular, the pentacyclic triterpenoids (TPs) have been found to inhibit the action of glucosil-transferase and of beta-glucuronidase, enzymes involved in the initial phases of the inflammation. The TPs strengthens the integrity of small veins and tiny capillaries, thereby putting on the brakes to some of the typical inflammatory processes resulting in edema. Specifically, the TPs halt the process of plasma exudation.
Exudation is the discharge of fluid from blood vessels during the inflammatory process. Small blood vessels passing through inflamed tissue become wider and more permeable, allowing fluids and cells to escape, resulting in swelling, or edema. Tissue glucosamino-glycans in fact attach in the initial stages of the inflammatory process to enzymes, especially glucose-transferase and beta-glucouronidase, biochemically breaking the bonds uniting disaccharides present in the polysaccharide structures of the vessel wall glucosamin-glycands, with the result vessel walls become very leaky.
In BPH, inflammation and edema are two of the major functional signs. They can range from hardly noticeable to very painful and obstructive. The gradual loss of the functional properties of the tissues supporting the vascular bed can be reversed by the application of pygeum pentacyclic triterpenoids.
The anti-exudative, and therefore anti-edema, action of the pygeum pentacyclic triterpenoids rests squarely on the capacity of ursolic acid and oleanolic acid to inactivate inflammatory enzymatic activity.
Therefore, pentacyclic triterpenoids have considerable power to complement the anti-prostaglandin activity of the phytosterols, even though at this time it would best to view their activity as ancillary and supportive.
Pharmacology of the Linear Alcohols and Ferulic Esters
The main activity of this class of compounds has been ascribed to the ferulic ester of docosanol and the ferulic ester of tetracosanol (commonly referred to as simply docosanol and tetracosanol). Of the two ferulic esters, docosanol appears to be the most active. Clinical research with docansol has shown this chemical alone can profoundly alter the course of BPH.
The real surprise came in discovering just how it works. No one really anticipated the outcome of pharmacological trials discovering docosanol inhibited the absorption and metabolism of cholesterol. It took some creative thinking and equally creative research to confirm cholesterol levels in enlarged prostates were not just coincidentally abnormally high, but in fact, the cholesterol contributed to the pathology. That particular concept had been around for awhile, largely overlooked, but has been revived as the result of research on pygeum.
And so a triad of pathological conditions emerges, each of which is ameliorated by one or more fractions of pygeum. The plant appears to be specially designed for fighting the symptom and causes of BPH. Ultimately all of the components of pygeum have been found to behave complementarily and synergistically in terms of their effects on BPH. For the first time, there is real hope of some reversal in this condition, not just control of symptoms.
Selected Clinical Research
A standardized lipophilic extract of pygeum, as a raw substance and under a couple of different trade names, has been subjected to scores of clinical trials, a few of which are reviewed here. The typical daily dose is 200mg, divided into two doses, over a period of 4 weeks to several months.
Later studies employ good protocol: double blind, placebo-controlled, statistically evaluated with attention being paid to both efficacy and safety, but even the earlier studies demonstrate strong pygeum effects.
Efficacy was established by observing and measuring effects on several parameters: dysuria, nocturia, diurnal and nocturnal polyuria (frequent urination), perineal (abdominal) heaviness, residual urine, volume of the prostate, voiding volume, peak flow and time mean. Safety was established by routine blood chemistry tests, clinical signs and self-report by patient.
1. 80% of 25 patients with BPH or cervico-prostatic adenomatosis showed significant improvement in symptoms (micturition and in 5 cases also the volume of the prostate) after 100mg/day for 30 days.
2. Thirteen of 18 patients with BPH, and 3 of 7 patients with prostatitis reported good results in amelioration of dysuria and polyuria.
3. In 27 patients with BPH and one with chronic prostatitis, all but three experienced significant symptomatic improvement after 6 weeks at 100mg/day. In general, the worse the symptoms, the less chance for recovery.
4. After 60 days of receiving 75mg/day in three divided doses, 60% of 20 patients reported significant improvement in dysuria and polyuria. 20% reported no improvement.
5. Out of 52 patients, 22 had very good regression, and 14 experienced acceptable regression of symptoms ranging from urinary disturbances, such as dysuria and polyuria, to signs of bladder neck urethral obstruction. All patients were surgical candidates. Treatment was 75mg divided into three administrations.
6. In a couple of the earliest trials on BPH patients, only 57-60% success was seen, but the treatment periods in most cases were fairly short, ranging from 10 to 50 days. Since that time, controls and protocol have steadily improved.
7. Against a placebo control, typical symptoms of BPH yielded significantly better to pygeum in 55 patients, aged 59-83. Only 10% of the patients reported no change, while a full 70% experienced very good results.
8. Out of 42 patients, aged 53-84, with obstructive urodynamic syndrome of prostatic origin, 19 experienced amelioration of diurnal polyuria, 31 experienced amelioration of nycturia and 21 showed improvement in residual urine after micturition. Treatment was 150mg daily for 45 days.
9. In a double blind, placebo-controlled study in 120 patients, significant findings were found in symptoms of nocturnal frequency, difficulty in starting micturition and incomplete emptying of the bladder. This study nicely portrayed confounding from placebo effects, since 50% of the placebo patients experienced improvement. It is very difficult under such circumstances to demonstrate statistical significance. Because the researchers were able to do so highlights the strength of the pygeum treatment.
10. In an open trial on 104 outpatients, aged 18-45, affected by prostatitis of different origin, secondary to infections, 89% experienced very good improvement in symptoms such as dysuria, polyuria, Strangury and pains in the pelvis.
11. Thirty typical elderly BPH patients were treated for three months with 100mg daily. All thirty experienced statistically significant improvement in symptoms.
12. In 39 cases of BPH 200mg daily for 60 days produced significant improvement in 75% of patients, compared to controls.
13. Twenty BPH patients, aged 51-89, divided into two groups: pygeum and control. Pygeum patients experienced significantly greater reduction in dysuric symptoms after 60 days with 200mg/day.
14. Another placebo-controlled trial, involving 40 men with prostatic hyperplasia (enlargement due to oversecretion of hormones), found significant improvement in more than 60-80% of the patients following 200mg daily treatment for 2 months.
15. In a recent open trial, the effects of pygeum on various male genital infections was assessed. Significant relief of symptoms and improvement in indices of a sexual and reproductive nature were observed.
Many other similar studies could be cited, but these should suffice to suggest the effectiveness of pygeum. BPH, prostatitis and related conditions, especially if functional in nature, are all amenable to safe and efficacious treatment with pygeum. Many patients even report improvement in such parameters as appetite, weight gain and mood. Four to six weeks of treatment are usually all that are necessary, but treatment may be repeated if desired.
Actually, a fourth class of potentially important chemicals exists, the C12-C24 fatty acids, but they appear to have no discernible effect on the prostate gland.
Drug Interactions & Precautions
The anti-inflammatory activity of this herb can be seriously inhibited by phenobarbital and certain other sedatives and hypnotics, meprobamate, chloral hydrate (aquachloral) etc., also beta-adrenergic blocking agents (propranolol).
Colchicine may increase sensitivity or enhance the response to pygeum.
Safety Factors & Toxicity
Tolerance for the herb was excellent in every study. No meaningful side effects of any kind were observed. Some gastric disturbances have been noted, but these do not amount to more 1% of the hundreds of patients treated. Even very elderly patients in generally poor condition could tolerate prolonged periods of treatment without side effects.
It has a low toxicity profile.
Pygeum has no contraindications, and its action is not hormone-like, and may therefore be used even in cases lacking a differential diagnosis between benign adenoma and cancer.
It is recommended that Pygeum be taken under professional supervision.
Preparation & Administration
Only available in capsules. Use 25-600mg daily, depending upon the seriousness of the problem.
The usual dosage for Pygeum Africanum Extract (PAE) is 100 mg/day in 6 - 8-week cycles.
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