| Title |
NBBS isolated from Pygeum africanum bark exhibits androgen antagonistic activity, inhibits AR nuclear translocation and prostate cancer cell growth
|
|---|---|
| Published in |
Investigational New Drugs, September 2009
|
| DOI | 10.1007/s10637-009-9304-y |
| Pubmed ID | |
| Authors |
Maria Papaioannou, Sonja Schleich, Daniela Roell, Undine Schubert, Tamzin Tanner, Frank Claessens, Rudolf Matusch, Aria Baniahmad |
| Abstract |
Extracts from Pygeum africanum are used in the treatment of prostatitis, benign prostatic hyperplasia (BPH) and prostate cancer (PCa). The ligand-activated human androgen receptor (AR) is known to control the growth of the prostate gland. Inhibition of human AR is therefore a major goal in treatment of patients. Here, we characterize the compound N-butylbenzene-sulfonamide (NBBS) isolated from P. africanum as a specific AR antagonist. This antihormonal activity inhibits AR- and progesterone receptor- (PR) mediated transactivation, but not the related human glucocorticoid receptor (GR) or the estrogen receptors (ERα or ERβ). Importantly, NBBS inhibits both endogenous PSA expression and growth of human PCa cells. Mechanistically, NBBS binds to AR and inhibits its translocation to the cell nucleus. Furthermore, using a battery of chemically synthesized derivatives of NBBS we revealed important structural aspects for androgen antagonism and have identified more potent AR antagonistic compounds. Our data suggest that NBBS is one of the active compounds of P. africanum bark and may serve as a naturally occurring, novel therapeutic agent for treatment of prostatic diseases. Thus, NBBS and its derivatives may serve as novel chemical platform for treatment prostatitis, BPH and PCa. |
Mendeley readers
The data shown below were compiled from readership statistics for 47 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 2% |
| Unknown | 46 | 98% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 10 | 21% |
| Student > Master | 9 | 19% |
| Lecturer | 3 | 6% |
| Student > Bachelor | 3 | 6% |
| Professor > Associate Professor | 3 | 6% |
| Other | 8 | 17% |
| Unknown | 11 | 23% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 11 | 23% |
| Pharmacology, Toxicology and Pharmaceutical Science | 6 | 13% |
| Agricultural and Biological Sciences | 6 | 13% |
| Biochemistry, Genetics and Molecular Biology | 5 | 11% |
| Environmental Science | 4 | 9% |
| Other | 4 | 9% |
| Unknown | 11 | 23% |
Attention Score in Context
This research output has an Altmetric Attention Score of 9. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 08 June 2023.
All research outputs
#3,925,670
of 23,967,950 outputs
Outputs from Investigational New Drugs
#130
of 1,222 outputs
Outputs of similar age
#15,200
of 95,601 outputs
Outputs of similar age from Investigational New Drugs
#3
of 17 outputs
Altmetric has tracked 23,967,950 research outputs across all sources so far. Compared to these this one has done well and is in the 83rd percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 1,222 research outputs from this source. They receive a mean Attention Score of 4.8. This one has done well, scoring higher than 89% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 95,601 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 84% of its contemporaries.
We're also able to compare this research output to 17 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 88% of its contemporaries.