
PYGEUM (bark)
Pygeum is an herbal remedy derived from the bark of the Pygeum africanum tree that has been used since ancient times to treat bladder problems. Some natives of various South African tribes still use the remedy by boiling the bark of the tree to make a tea. In the 1960s, the Europeans began using a pygeum bark extract to treat mild to moderate BPH. Since then pygeum bark extract has caught the attention of nontraditional healers in other countries.
The major active components of the bark are fat-soluble sterols (phytosterols) and fatty acids. Phytosterols can inhibit the production of DHT (dihydrotestosterone), a hormone that increase the risk of BPH and prostate cancer. Pygeum also reduces the number of receptor sites where DHT can attach to cells.
Virtually all of the research on Pygeum has featured a Pygeum extract standardized to contain 14% triterpenes including beta-sitosterol and 0.5% n-docosanol. This extract has been extensively studied in both experimental animal studies and clinical trials, and a dose of 100 mg daily has been found to be most effective.
Pygeum and BPH Studies, Pre-2000
An early animal study evaluated the effect of Pygeum africanum in rat prostatic fibroblast proliferation. The investigators found that “therapeutic effect of Pygeum africanum may be due at least in part to the inhibition of growth factors [bFGF, EGF, IGF-I] responsible for the prostatic overgrowth in man.” (Yablonsky 1997)
In an early human study, the efficacy of a Pygeum africanum extract was tested in 263 men who had BPH. The multicenter, double-blind trial was conducted in eight centers in Europe and lasted 60 days. Capsules containing 50 mg of Pygeum africanum extract or placebo were administered twice daily, once in the morning and once in the evening. At the end of the trial, men who had taken Pygeum extract showed a “marked clinical improvement” in urinary factors (e.g., residual urine, uroflowmetry, nighttime urination), with a 66 percent improvement in urination compared with 31 percent in the placebo group. (Barlet 1990)
Urology published a study in which men with symptomatic BPH participated in a two-month randomized, parallel-group, double-blind, comparative phase (group A received 50 mg of Pygeum daily; group B received 100 mg once daily), followed by a ten-month, open phase, during which men were given 100 mg of Pygeum once daily. A total of 209 men completed the comparative phase and 174 finished the open phase. Results and safety were similar between groups A and B: both groups had similar improvements in the International Prostate Symptom Score (38% and 35%, respectively), quality of life (28% in both), and maximum urinary flow rate (increase of 16% and 19%, respectively). The authors concluded that “P. africanum extract at 50 mg twice daily and 100 mg once daily proved equally effective and safe at 2 months.” (Chatelain 1999)
A multicenter trial conducted in central Europe explored the efficacy and safety of Pygeum africanum extract (available as Tadenan) in men aged 50 to 75 years who had mild to moderate BPH. During the two-month study, the men were administered 50 mg of Pygeum africanum extract twice daily. This phase was followed by a one-month period during which none of the men took Pygeum. Eighty-five men completed the entire study. After the two-month phase, International Prostate Symptom Score (IPSS) improved 40 percent and quality of life, 31 percent. Nighttime frequency was reduced by 32 percent. These improvements persisted after one month without taking Pygeum. No changes were reported in either prostatic volume or quality of sexual life throughout both phases of the study, and no adverse effects related to use of Pygeum were noted. The authors concluded that “under conditions of daily practice, Pygeum africanum extract induces significant improvement in IPSS and uroflowmetry parameters.” (Breza 1998)
Pygeum and BPH Studies, Post-2000
Researchers from the Minneapolis Veterans Affairs Center evaluated 18 randomized controlled trials that involved a total of 1,562 men who had BPH. All but one of the trials were double-blinded, and none compared Pygeum to standard pharmacologic approaches such as 5-alpha-reductase inhibitors. Overall, the reviewers found that compared with men who took a placebo, Pygeum provided a “moderately large improvement” in urinary symptoms and urinary flow measures. Specifically men who used Pygeum africanum were more than twice as likely to report improvement in overall symptoms: residual urine volume improved by 24 percent, peak urine flow increased by 23 percent, and nocturia declined by 19 percent. The conclusion of the researchers was that “a standardized preparation of Pygeum africanum may be a useful treatment option for men with lower urinary symptoms consistent with benign prostatic hyperplasia.” (Wilt 2002)
A review of two studies, conducted at the University of Milan, reported on the results of 70 men who had BPH and who were administered either 320 mg of saw palmetto for 30 days (study 1) or 100 mg Pygeum africanum plus 320 mg of saw palmetto for 30 days (study 2). The results of both studies were positive, showing an improvement of about 50 percent in dysuria (painful urination) and frequent urination, and “about a 50% increase in micturition rate with positive effects also in terms of reduction of the micturition rate and of prostate size.” (Mantovani 2010)
Pygeum, BPH, Prostatitis, and Prostate Cancer
In a more recent study, investigators reported on the effects of atraric acid (AA), which they isolated from the bark of Pygeum and they found to have an impact on prostate health. The ligand-activated human androgen receptor (AR) plays a key role in supporting the growth of the prostate gland. Thus inhibition of the androgen receptor is a main goal in management of patients. Investigators at the Institute of Human Genetics and Anthropology found that atraric acid has anti-androgenic activity and inhibits the “transactivation mediated by the ligand-activated human AR.” Specifically, the scientists found that atraric acid can repress the broth of androgen-dependent LNCaP and androgen-independent C402 Pca cells, but not prostate cancer cells that lack AR. The authors concluded that their study findings “may serve as a basis for AA derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases.” (Papaioannou 2009)
In a subsequent study by many of the same researcher team, the scientists identified the compound N-butylbenzene-sulfonamide (NBBS), isolated from Pygeum africanum, as a specific androgen receptor antagonist. They noted that NBBS has antihormonal activity and the ability to inhibit endogenous PSA expression and the growth of prostate cancer cells. The authors concluded that “NBBS and its derivatives may serve as a novel chemical platform for treatment of prostatitis, BPH and PCa [prostate cancer].” (Papaioannou 2010)
For treatment of BPH, the suggested dosage is 75 to 200 mg capsules of standardized pygeum extract (bark; 13% total sterols) taken daily either as a single dose or divided into two equal doses. Possible side effects of pygeum include nausea, loss of appetite, and abdominal pain. (University of Maryland)
References
Barlet A et al. Efficacy of Pygeum africanum extract in the treatment of micturational disorders due to benign prostatic hyperplasia. Evaluation of objective and subjective parameters. A multicenter, randomized, double-blind trial. Wein Klin Wochenschr 1990;102:667–73.
Breza J et al. Efficacy and acceptability of tadenan (Pygeum africanum extract) in the treatment of benign prostatic hyperplasia (BPH): a multicentre trial in central Europe. Curr Med Res Opin 1998; 14(3):127-39.
Chatelain C et al. Comparison of once and twice daily dosage forms of Pygeum africanum extract in patients with benign prostatic hyperplasia: a randomized, double-blind study, with long-term open label extension. Urology 1999 Sep; 54(3):473-78.
Mantovani F. Serenoa repens in benign prostatic hypertrophy: analysis of 2 Italian studies. Minerva Urol Nefrol 2010 Dec; 62(4): 335-40
Papaioannou M et al. NBBS isolated from Pygeum africanum bark exhibits androgen antagonistic activity, inhibits AR nuclear translocation and prostate cancer cell growth. Invest New Drugs 2010 Dec; 28(6): 729-43
Papaioannou M et al. The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate cancer cell growth. J Cell Mol Med 2009 Aug; 13(8B): 2210-23
University of Maryland Medical Center: http://www.umm.edu/altmed/articles/benign-prostatic-000018.htm
Wilt T et al. Pygeum africanum for benign prostatic hyperplasia. Cochrane Databases of Systematic Reviews 2002; (1)CD001044
Yablonsky FP et al. Antiproliferative effect of Pygeum africanum extract on rat prostatic fibroblasts. J Urol 1997; 157:2381-87.







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