2. Academic Validation
  3. A novel Rhein derivative AQ-NC inhibits prostate cancer by suppressing the PI3K/AKT pathway

A novel Rhein derivative AQ-NC inhibits prostate cancer by suppressing the PI3K/AKT pathway

  • Biochem Biophys Res Commun. 2025 Sep 30:786:152718. doi: 10.1016/j.bbrc.2025.152718.
Tingting Yang 1,  Mulan Li 2,  Limei Yang 1,  Mingyu Ji 1,  Zhihong Zhou 1,  Yerong Liu 1,  Dong Ran 3,  Wei Tian 4,  Peilin Yang 5
Affiliations

Affiliations

  • 1 Guangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning, 530004, China.
  • 2 The First Affiliated Hospital of Guangxi Medical University, Nanning, China.
  • 3 Department of Medicine Laboratory, The Eighth People's Hospital of Nanning, Nanning, 530003, Guangxi, China. Electronic address: 375904072@qq.com.
  • 4 Guangxi International Zhuang Medicine Hospital, Nanning, 530201, China. Electronic address: tianweicpu@163.com.
  • 5 Guangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning, 530004, China; Guangxi Key Laboratory of Pharmaceutical Precision Detection and Screening, Key Laboratory of Micro-Nanoscale Bioanalysis and Drug Screening of Guangxi Education Department, State Key Laboratory of Targeting Oncology, Pharmaceutical College, Guangxi Medical University, Nanning, China; Key Laboratory of Basic Research on Regional Diseases (Guangxi Medical University), Education Department of Guangxi Zhuang Autonomous Region, China; Key Laboratory of Prevention and Control of Highly Prevalent Diseases (Guangxi Medical University), Education Department of Guangxi Zhuang Autonomous Region, China. Electronic address: yangpeilin@gxu.edu.cn.
PMID: 41045575 DOI: 10.1016/j.bbrc.2025.152718
Abstract

Objective: This research endeavors to explore the anti-prostate Cancer (PCa) activity and potential molecular mechanisms of the newly synthesized Rhein derivative AQ-NC.

Methods: The CCK-8 test was employed to evaluate the anti-PCa activity of AQ-NC and its lead compound, Rhein. The EdU assay was utilized to assess how AQ-NC impacts the proliferation of PCa cells. The scratch and Transwell assays were carried out to detect the influence of AQ-NC on the migratory capacity of DU-145 and C4-2 cells. Western blot analysis was used to measure the expression of proteins associated with migration. Flow cytometry was applied to detect the effect of AQ-NC on Apoptosis in DU-145 and C4-2 cells. Additionally, the expression levels of apoptosis-associated proteins were assessed using Western blot. Mechanistically, potential signaling pathways were predicted by molecular docking and the expression of relevant proteins were verified using Western Blot.

Results: AQ-NC demonstrated significantly superior cellular activity to Rhein, as determined by the CCK-8 assay. Observations of cell morphology and EdU assays further demonstrated that AQ-NC could suppress the proliferation of PCa cells. Scratch and Transwell assays revealed that AQ-NC effectively hindered the migration of PCa cells. Flow cytometry and Western blot analyses indicated that AQ-NC could trigger Apoptosis in PCa cells. Additionally, molecular docking and Western blot results indicated that AQ-NC could suppress the expression of proteins related to p-EGFR, p-PI3K, and p-AKT.

Conclusion: AQ-NC inhibits the proliferation and migration of PCa cells and induces Apoptosis, potentially through the inhibition of the PI3K/Akt signaling pathway.

Keywords

PI3K/AKT pathway; Prostate cancer; Rhein derivatives.

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