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Updated: Mar 30, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Anti-androgenic effects of flavonols in prostate cancer
1Royal Liverpool University Hospital, Prescot Street, Liverpool, Merseyside, L7 8XP, UK.
Abstract:
Dietary-derived agents, such as the flavonoids, are of particular interest for prostate cancer (PCa) chemoprevention as they may offer a favourable safety and side-effect profile. An agent that demonstrates action on the androgen receptor (AR) axis may have value for preventing or treating castrate-resistant PCa. Four main flavonols - quercetin, myricetin, kaempferol, and fisetin - have been demonstrated in laboratory studies to have chemopreventive action in both castrate-resistant and castrate-sensitive PCa models. Mechanisms of flavonol action on the AR axis in PCa have been proposed to be inhibition of the 5α-reductase enzymes, direct androgen competition, suppression of the AR complex and transactivation by coregulators such as c-Jun, Sp1, and the PI3K/Akt pathway. It is, however, still unclear with current levels of evidence whether AR axis-mediated effects can fully account for the flavonols' chemopreventive action.
Insights
Flavonoids show promise for prostate cancer (PCa) chemoprevention. These compounds, including quercetin and fisetin, may target the androgen receptor (AR) axis, offering a safer approach for PCa treatment.
Area of Science:
- Oncology
- Nutritional Science
- Molecular Biology
Background:
- Dietary flavonoids are explored for prostate cancer (PCa) chemoprevention due to their safety.
- Agents targeting the androgen receptor (AR) axis are crucial for castrate-resistant PCa (CRPC).
Purpose of the Study:
- To review the chemopreventive potential of four major flavonols (quercetin, myricetin, kaempferol, fisetin) in PCa.
- To explore the mechanisms by which flavonols may act on the AR axis in PCa models.
Main Methods:
- Laboratory studies investigating flavonol efficacy in PCa models (castrate-sensitive and castrate-resistant).
- Analysis of proposed mechanisms of flavonol action on the AR axis.
Main Results:
- Four key flavonols demonstrated chemopreventive action in both PCa models.
- Proposed mechanisms include 5α-reductase inhibition, androgen competition, AR complex suppression, and coregulator modulation (c-Jun, Sp1, PI3K/Akt pathway).
Conclusions:
- Flavonols exhibit chemopreventive potential against PCa.
- While AR axis modulation is a proposed mechanism, further evidence is needed to confirm its full contribution to flavonol efficacy.
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