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Published on: November 19, 2019
Quercetin inhibits the expression and function of the androgen receptor in LNCaP prostate cancer cells
1Department of Urology and Biochemistry and Molecular Biology, Mayo Graduate School, Mayo Foundation, Rochester, MN 55905, USA.
Abstract:
The androgen receptor (AR) is involved in the development and progression of prostate cancer. In order to find new compounds that may present novel mechanisms to attenuate the function of AR, we investigated the effect of a natural flavonoid chemical, quercetin, on androgen action in an androgen-responsive LNCaP prostate cancer cell line. Western blot analysis showed that AR protein expression was inhibited by quercetin in a dose-dependent manner. To demonstrate that the repression effects on AR expression can actually reduce its function, we found that quercetin inhibited the secretion of the prostate-specific, androgen-regulated tumor markers, PSA and hK2. The mRNA levels of androgen-regulated genes such as PSA, NKX3.1 as well as ornithine decarboxylase (ODC) were down-regulated by quercetin. Transient transfections further showed that quercetin inhibited AR-mediated PSA expression at the transcription level. Finally, it was demonstrated that quercetin could repress the expression of the AR gene at the transcription level. Our result suggests that quercetin can attenuate the function of AR by repressing its expression and has the potential to become a chemopreventive and/or chemotherapeutic agent for prostate cancer.
Insights
Quercetin, a natural flavonoid, inhibits prostate cancer growth by reducing androgen receptor (AR) expression and function. This suggests quercetin
Area of Science:
- Oncology
- Molecular Biology
- Natural Products Chemistry
Background:
- Androgen receptor (AR) signaling is crucial for prostate cancer development and progression.
- Novel therapeutic strategies targeting AR are needed to combat prostate cancer.
Purpose of the Study:
- To investigate the effect of quercetin, a natural flavonoid, on androgen action in prostate cancer.
- To determine if quercetin can attenuate androgen receptor (AR) function and expression.
Main Methods:
- Western blot analysis to assess AR protein levels.
- Measurement of prostate-specific antigen (PSA) and hK2 secretion.
- Quantitative real-time PCR to analyze mRNA levels of androgen-regulated genes.
- Transient transfection assays to evaluate transcriptional activity.
Main Results:
- Quercetin significantly inhibited AR protein expression in a dose-dependent manner.
- Quercetin reduced the secretion of androgen-regulated tumor markers PSA and hK2.
- Quercetin down-regulated mRNA levels of AR-regulated genes, including PSA, NKX3.1, and ODC.
- Quercetin repressed AR-mediated PSA expression and AR gene transcription.
Conclusions:
- Quercetin attenuates androgen receptor (AR) function by repressing its expression at both protein and transcriptional levels.
- Quercetin demonstrates potential as a chemopreventive and/or chemotherapeutic agent for prostate cancer.
