“Extracts from PYGEUM AFRICANUM, SERENOA REPENS and CUCURBITA PEPO are used in the treatment of benign prostatic hyperplasia (BPH) and prostate cancer (PCa).

The activity of the androgen receptor (AR) is known to control growth of the prostate. Here, we examined extracts of these plants for their antiandrogenic activity using an AR responsive reporter gene assay for drug discovery.

A selective dichloromethane extract from the stem barks of PYGEUM AFRICANUM revealed the highest antiandrogenic effect.

Bioactivity-directed fractionation of this extract led to the isolation of N-butylbenzenesulfonamide (NBBS) indicating that extracts of the stem bark of P. AFRICANUM harbour androgen antagonistic activity. This compound may provide a novel approach for the prevention and treatment of BPH and human PCa. ”
Reference: Planta Med. 2006 Jun 19
Extracts from Pygeum africanum and Other Ethnobotanical Species with Antiandrogenic Activity.
Schleich S, Papaioannou M, Baniahmad A, Matusch R.
Institut fur Pharmazeutische Chemie, Philipps-Universitat Marburg, Marburg, Germany.

Related studies

Planta Med. 2006 Apr;72(6):547-51.Activity-Guided Isolation of an Antiandrogenic Compound of Pygeum africanum.
Schleich S, Papaioannou M, Baniahmad A, Matusch R.
Institut fur Pharmazeutische Chemie, Philipps-Universitat Marburg, Marburg, Germany.

Nonsteroidal antiandrogens of natural and synthetic origin for the treatment of prostate cancer
Schleich, Sonja. Fachbereich Pharmazie, Universität Marburg.

“N-Butyl-4-nitro-3-trifluoromethylbenzenesulfonamide revealed the highest antiandrogenic activity, scilicet an inhibition of the androgen induced luciferase activity of 75% at a concentration of 1 µM. The leadstrucures were also analysed for their receptor binding specificity and the growth inhibition of LNCaP prostate cancer cells leading to the conclusion that NBBS and atraric acid both have a high affinity to the androgen receptor and only to some extent to the progesterone receptors A and B, while other steroid receptors were unaffected by these substances. Treatment of LNCaP cells with NBBS and atraric acid inhibited potently LNCaP proliferation.”

Cochrane Database Syst Rev. 2002;(1):CD001044. Pygeum africanum for benign prostatic hyperplasia [BPH]. Wilt T, Ishani A, Mac Donald R, Rutks I, Stark G. General Internal Medicine (111-0), Minneapolis VA/VISN 13 Center for Chronic Disease Outcomes Research, One Veterans Drive, Minneapolis, Minnesota 55417, USA.

For men taking it for urinary symptoms of benign enlarged prostate (BPH). “Pygeum africanum provided a moderately large improvement in the combined outcome of urologic symptoms and flow measures …. Men using Pygeum africanum were more than twice as likely to report an improvement in overall symptoms…. Nocturia was reduced by 19%, residual urine volume by 24% and peak urine flow was increased by 23%. Adverse effects due to Pygeum Africanum were mild and comparable to placebo.”

“REVIEWER’S CONCLUSIONS: A standardized preparation of Pygeum africanum may be a useful treatment option for men with lower urinary symptoms consistent with benign prostatic hyperplasia. However, the reviewed studies were small in size, were of short duration, used varied doses and preparations and rarely reported outcomes using standardized validated measures of efficacy. Additional placebo-controlled trials are needed as well as studies that compare Pygeum africanum to active controls that have been convincingly demonstrated to have beneficial effects on lower urinary tract symptoms related to BPH. These trials should be of sufficient size and duration to detect important differences in clinically relevant endpoints and use standardized urologic symptom scale scores.”