Extracts from Pygeum africanum and other ethnobotanical species with antiandrogenic activity.
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.
Schleich
Sonja
S
Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marburg, Germany.
Papaioannou
Maria
M
Baniahmad
Aria
A
Matusch
Rudolf
R
D000726:Androgen Antagonists / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D028464:Cucurbita / Q000737:chemistry; D017930:Genes, Reporter; D000882:Haplorhini; D008156:Luciferases / Q000032:analysis; D009828:Oleanolic Acid / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D000068218:Prunus africana / Q000737:chemistry*; D028024:Serenoa / Q000737:chemistry; D012855:Sitosterols / Q000494:pharmacology; D013449:Sulfonamides / Q000302:isolation & purification / Q000494:pharmacology*; D014315:Triterpenes / Q000494:pharmacology; D000097245:Ursolic Acid; D000096926:Benzenesulfonamides
D000726:Androgen Antagonists; D008156:Luciferases; D009828:Oleanolic Acid; D010936:Plant Extracts; D012855:Sitosterols; D013449:Sulfonamides; D014315:Triterpenes; D000097245:Ursolic Acid; C025473:gamma-sitosterol; C065565:N-butylbenzenesulfonamide; D000096926:Benzenesulfonamides