The natural compounds atraric acid and N-butylbenzene-sulfonamide as antagonists of the human androgen receptor and inhibitors of prostate cancer cell growth.

Extracts from the plant Pygeum africanum are widely used in the therapy of benign prostate hyperplasia (BPH) and in combinational therapy for prostate cancer, the second leading cause of cancer death and the mostly diagnosed form of cancer in men. The androgen receptor (AR) plays a crucial role in the development of the prostate as well as in prostate diseases. Even though the extracts from P. africanum are considered as beneficial for prostate diseases in clinical trials, and some active compounds for treatment of BPH could be identified, compounds responsible for AR inhibition and the molecular mechanism for inhibition of prostatitis need to be identified. Recently, atraric acid and N-butylbenzene-sulfonamide were isolated from a selective dichlormethane extract of P. africanum as two novel AR antagonistic compounds. The molecular mechanisms of AR inhibition were analyzed and are summarized here. Both compounds are the first known natural, complete and specific AR antagonist.
AuthorsDaniela Roell, Aria Baniahmad
JournalMolecular and cellular endocrinology (Mol Cell Endocrinol) Vol. 332 Issue 1-2 Pg. 1-8 (Jan 30 2011) ISSN: 1872-8057 [Electronic] Ireland
PMID20965230 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
CopyrightCopyright © 2010 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • AR protein, human
  • Androgen Receptor Antagonists
  • Hydroxybenzoates
  • Plant Extracts
  • Receptors, Androgen
  • Sulfonamides
  • atraric acid
  • N-butylbenzenesulfonamide
  • Androgen Receptor Antagonists (chemistry, therapeutic use)
  • Cell Line, Tumor
  • Humans
  • Hydroxybenzoates (chemistry, therapeutic use)
  • Male
  • Molecular Structure
  • Plant Extracts (chemistry, therapeutic use)
  • Prostatic Hyperplasia (drug therapy)
  • Prostatic Neoplasms (drug therapy)
  • Receptors, Androgen (metabolism)
  • Sulfonamides (chemistry, therapeutic use)

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