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Although is known to have anti-inflammatory, anti-obesity, and anti-oxidant properties, the underlying apoptotic mechanism of extract has never been elucidated in prostate cancer. In this paper, the apoptotic mechanism of a water extract from the dried root of (WAM) was investigated in prostate cancer cells in association with heat shock protein 27 (HSP27)/androgen receptor (AR) signaling. WAM increased cytotoxicity and the sub-G1 population, cleaved poly (ADP-ribose) polymerase (PARP) and cysteine aspartyl-specific protease 3 (caspase 3), and attenuated the expression of B-cell lymphoma 2 (Bcl-2) in LNCaP cells after 24 h of exposure. Consistently, WAM significantly increased the number of terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL)-positive LNCaP cells. WAM decreased the phosphorylation of HSP27 on Ser82 and inhibited the expression of the AR and prostate-specific antigen (PSA), along with reducing the nuclear translocation of p-HSP27 and the AR via the disturbed binding of p-HSP27 with the AR in LNCaP cells. WAM consistently inhibited the expression of the AR and PSA in dihydrotestosterone (DHT)-treated LNCaP cells. WAM also suppressed AR stability, both in the presence and absence of cycloheximide, in LNCaP cells. Taken together, these findings provide evidence that WAM induces apoptosis via the inhibition of HSP27/AR signaling in prostate cancer cells and is a potent anticancer candidate for prostate cancer treatment.
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http://dx.doi.org/10.3390/ijms25052799 | DOI Listing |
J Med Chem
September 2025
State Key Laboratory of Advanced Drug Delivery and Release Systems, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
Resistance-conferring mutations in the androgen receptor (AR) ligand-binding pocket (LBP) compromise the effectiveness of clinically approved orthosteric AR antagonists. Targeting the dimerization interface pocket (DIP) of AR presents a promising therapeutic approach. In this study, we report the design and optimization of -(thiazol-2-yl) furanamide derivatives as novel AR DIP antagonists, among which was the most promising candidate.
View Article and Find Full Text PDFTurk J Biol
May 2025
Department of Veterinary Medicine, Susurluk Agriculture and Forestry Vocational School, Bandırma Onyedi Eylül University, Balıkesir, Turkiye.
Background/aim: A number of carbonic anhydrase (CA) family proteins have been implicated in cancer. They contribute to the hypoxic microenvironment. CAVII is often downregulated in colorectal carcinoma and it has been associated with increased tumor size, node metastasis, and adverse clinical outcomes.
View Article and Find Full Text PDFMed Oncol
September 2025
Department of Medical Physiology, School of Biomedical Sciences, College of Health Sciences, Makerere University, Kampala, Uganda.
This study investigates the cytotoxic effects of R. tridentata extracts on prostate cancer cells, providing insight into its potential therapeutic benefits and scientific validation for its traditional use in cancer treatment. The cytotoxicity of R.
View Article and Find Full Text PDFJ Proteome Res
September 2025
Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah 27272, United Arab Emirates.
Prostate cancer (PCa) remains a major global health concern, ranking among the most prevalent cancer in men worldwide. Despite the availability of various therapeutic options, the clinical efficacy of current anti-PCa agents is often compromised by drug resistance and adverse effects. DNA minor groove binders offer a potential therapeutic alternative, owing to their selective mechanism of action and favorable safety profiles.
View Article and Find Full Text PDFMolecules
August 2025
Veterans Affairs-Northern California Health System, Mather, CA 95655, USA.
However, in many cases, patients experience biochemical recurrence (BCR), heralded by rising prostate specific antigen (PSA) levels in the serum. Our goal was to identify metabolic pathways that are disrupted in BCR to determine potential targets of therapy. We conducted metabolomic analysis in prostate tissue from the tumors of 74 patients who underwent prostatectomy as treatment for localized PCa and correlated levels of metabolites with clinical and non-clinical factors.
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