Article Abstract

Pharmacologically relevant concentrations of berberine transiently stimulate dihydrotestosterone-inducible androgen receptor-mediated luciferase activity in human prostate cancer cells

Authors: Ondrej Zenata, Zdenek Dvorak, Radim Vrzal


Background: Herbal medicines containing berberine have a wide spectrum of usage. However, the effect on androgen receptor (AR) activity at plasmatic relevant concentrations is omitted. Therefore, the effect of berberine on AR activity in prostate cancer cell lines was investigated.
Methods: We used the reporter gene assay (RGA) and polymerase chain reaction (qPCR) for monitoring the activity of AR. Moreover, we monitored the proliferation of two prostate cancer cell lines treated with Berberine.
Results: Berberine significantly potentiated dihydrotestosterone (DHT)-inducible AR-dependent luciferase activity in RGA. It also significantly decreased basal KLK3 mRNA level in 22Rv1 cells, but DHT-inducible KLK3 mRNA was not affected in androgen-independent (22Rv1) or androgen-dependent (LNCaP) cells. Proliferation of both cell lines was significantly inhibited by 100 and 1,000 nM concentrations in similar manner and Berberine increased Annexin V staining, suggesting an apoptotic event.
Conclusions: Berberine inhibits proliferation of prostatic cell lines at pharmacologically reachable concentrations but with no apparent link to androgen receptor-driven target gene expression.