Activity-guided isolation of an antiandrogenic compound of Pygeum africanum.
| Title | Activity-guided isolation of an antiandrogenic compound of Pygeum africanum. |
| Publication Type | Journal Article |
| Year of Publication | 2006 |
| Authors | Schleich, S., Papaioannou M., Baniahmad A., & Matusch R. |
| Journal | Planta Med |
| Volume | 72 |
| Issue | 6 |
| Pagination | 547-51 |
| Date Published | 2006 May |
| ISSN | 0032-0943 |
| Keywords | Androgen Antagonists, Dose-Response Relationship, Drug, Humans, Hydroxybenzoates, Male, Phytotherapy, Plant Bark, Plant Extracts, Prostatic Neoplasms, Prunus africana, Receptors, Androgen, Structure-Activity Relationship |
| Abstract | Inactivation of the androgen receptor (AR) through androgen ablation and treatment with antiandrogens is a major goal in the therapy for prostate hyperplasia and prostate cancer. Bioactivity-directed fractionation of a selective dichloromethane extract from the stem bark of Pygeum africanum led to the isolation of the antiandrogenic compound atraric acid. Its activity was examined by an androgen receptor responsive reporter gene assay. For lead structure optimization we transformed the natural occurring compound atraric acid into its ethyl, N-propyl and N-butyl esters and their antiandrogenic activities were examined as well. In addition, benzoic acid was isolated. The structures of all compounds were determined and characterized by means of 1H- and 13C-NMR, HR-EI-mass, IR and UV spectroscopy. |
| DOI | 10.1055/s-2006-941472 |
| Alternate Journal | Planta Med |
| PubMed ID | 16773539 |
