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Updated: Sep 20, 2025
A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
α-Terthienyl induces prostate cancer cell death through inhibiting androgen receptor expression
Xia Gan1, Hailing Huang2, Jing Wen2
1Guangxi Zhuang Yao Medicine Center of Engineering and Technology, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China; Institute of Marine Drugs, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China.
Abstract:
Prostate cancer is a disease that often occurs in elderly men. Androgen receptor signaling pathway runs through the occurrence and development of prostate cancer. Thereby, targeting androgen receptor is a crucial strategy for the treatment of prostate cancer. α-Terthienyl, which has been used as photosensitive activator and insecticide, is a natural compound rich in marigold. In the present study, we found α- terthienyl could inhibit the cell viability of four prostate cancer cell lines, especially on LNCaP and 22Rv1 cells which endogenously express androgen receptor. Then we proved that it could inhibit the proliferation of prostate cancer cells and induce apoptosis of prostate cancer cells by plate clone formation assay and flow cytometry respectively. Furthermore, we found α-terthienyl could inhibit androgen receptor nuclear translocation, reduce androgen receptor expression, reduce the mRNA and protein expression of androgen receptor target genes (KLK3, TMPRSS2, PCA3) and nuclear proliferation antigen Ki67 and PCNA. In addition, it inhibited the expression and phosphorylation of Akt protein while increasing the expression of tumor suppressor p27. Besides, we constructed a mouse xenograft prostate cancer model and confirmed that α-terthienyl also inhibited the growth of prostate cancer in vivo. In conclusively, α-terthienyl played an anti-prostate cancer role by inhibiting both the expression of androgen receptor and the transduction of its signal pathway, suggesting that it is a promising natural small molecule for the treatment of prostate cancer.
Insights
Natural compound α-Terthienyl inhibits prostate cancer growth by targeting the androgen receptor signaling pathway. This marigold-derived molecule reduces cell viability, proliferation, and tumor growth, offering a promising new treatment strategy.
Area of Science:
- Oncology
- Natural Products Chemistry
- Molecular Biology
Background:
- Prostate cancer is a prevalent disease in elderly men.
- The androgen receptor (AR) signaling pathway is critical for prostate cancer development and progression.
- Targeting the AR pathway is a key therapeutic strategy for prostate cancer.
Purpose of the Study:
- To investigate the anti-cancer effects of α-Terthienyl, a natural compound from marigold.
- To determine the mechanism by which α-Terthienyl affects prostate cancer cells.
- To evaluate the efficacy of α-Terthienyl in a preclinical prostate cancer model.
Main Methods:
- Cell viability assays on four prostate cancer cell lines.
- Clonogenic assays and flow cytometry to assess proliferation and apoptosis.
- Western blotting and qRT-PCR to analyze AR signaling pathway components and proliferation markers.
- Mouse xenograft model to evaluate in vivo efficacy.
Main Results:
- α-Terthienyl inhibited viability and proliferation while inducing apoptosis in prostate cancer cells, particularly those expressing AR.
- It suppressed AR nuclear translocation, reduced AR and its target gene expression (KLK3, TMPRSS2, PCA3).
- In vivo studies confirmed α-Terthienyl inhibited tumor growth in a mouse xenograft model.
Conclusions:
- α-Terthienyl exhibits significant anti-prostate cancer activity by inhibiting AR signaling.
- It reduces AR expression and downstream signaling, impacting cell proliferation and survival.
- α-Terthienyl is a potential natural therapeutic agent for prostate cancer treatment.
