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Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay
Published on: June 7, 2020
Down-regulation of androgen-receptor and PSA by phytochemicals
Sophie Chen1, Jian Gao, H Dorota Halicka
1Department of Medicine, New York Medical College, Valhalla, NY 10595, USA. s.chen@opcart-lab.org
Abstract:
The androgen receptor (AR) signaling pathway continues to be active in hormone resistant prostate cancer (HRPC) and can inappropriately activate transcription. Consequently the AR is a therapeutic target for HRPC. We reported that PC-SPES is active against HRPC, partly due to its actions in down-regulating AR protein expression and modulating cell cycle. Further investigation has identified five active anticancer compounds. This study describes the effects of three of these compounds (oridonin, isoliquiritigenin and wogonin) on cell proliferation, cell apoptosis, cell cycle parameters, AR and PSA protein expression. In each case, these compounds have independent activities which may partly contribute to the biological activity of PC-SPES.
Insights
Three compounds from PC-SPES, including oridonin, isoliquiritigenin, and wogonin, show anticancer activity by affecting cell proliferation, apoptosis, and androgen receptor (AR) signaling in hormone-resistant prostate cancer.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Androgen receptor (AR) signaling remains active in hormone-resistant prostate cancer (HRPC), driving aberrant transcription.
- AR is a key therapeutic target in HRPC.
- PC-SPES has demonstrated activity against HRPC, partly by down-regulating AR protein and modulating the cell cycle.
Purpose of the Study:
- To investigate the effects of three specific compounds (oridonin, isoliquiritigenin, and wogonin) identified from PC-SPES.
- To evaluate their impact on cell proliferation, apoptosis, cell cycle, and AR/PSA protein expression in HRPC.
Main Methods:
- Cell proliferation assays.
- Apoptosis assays.
- Cell cycle analysis.
- Western blot analysis for AR and PSA protein expression.
Main Results:
- Oridonin, isoliquiritigenin, and wogonin each demonstrated independent anticancer effects.
- These compounds influenced cell proliferation and apoptosis.
- Modulation of cell cycle parameters was observed.
- Effects on androgen receptor (AR) and prostate-specific antigen (PSA) protein expression were noted.
Conclusions:
- Oridonin, isoliquiritigenin, and wogonin possess distinct biological activities relevant to HRPC treatment.
- These individual compound activities may contribute to the overall efficacy of PC-SPES.
- Further research into these compounds could yield novel therapeutic strategies for HRPC.
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