Iron chelation has already been proposed to be a feasible strategy for cancer therapeutics in that reinforced iron demand is demonstrated in cancer cells, and quite a few iron chelators have been developed for this purpose. Desferrioxamine (DFO), an iron chelator approved by the U.S. Food and Drug Administration (FDA), has been extensively examined to remove extra iron. However, DFO has been found to harbor limited efficacies in combating cancer cells due to poor cellular permeability. In the current study, we synthesized the DFO derivative, named as desferrioxamine-caffeine dimer (DFCAF) by linking DFO to caffeine with high purity and excellent stability. Our data showed that DFCAF displayed greater cellular permeability to chelate intracellular iron in 4T1 breast cancer cells than DFO, posing more inhibition on cell growth and cellular motility/invasion. Importantly, DFCAF was uncovered to remarkably deplete cancer stem cells (CSCs), as characterized by the remarkable decrease of the CD44/CD24 and ALDH subpopulation. In parallel, DFCAF was also found to greatly reverse epithelial-mesenchymal transition (EMT), suggesting the potential application to restrain tumor progression and metastasis. Collectively, these data unveiled the improved efficacy to target cancer cells and to deplete CSCs, thus opening a new path for better cancer therapeutics through iron chelation.
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http://dx.doi.org/10.1016/j.jtemb.2019.01.004 | DOI Listing |
Chem Biodivers
January 2025
Guizhou Medical University, School of Pharmaceutical Sciences, University Town, Gui'an New District, 550025, Guiyang, CHINA.
An unrevealed dihydroflavone-monoterpene conjugate (1), two unrevealed kavalactones (2-3, including one with an uncommon side chain), and thirteen previously identified compounds (4-16) were extracted from Alpinia katsumadai Hayata. seeds. The two-dimension structures of the new compounds were authenticated utilizing HRESIMS as well as NMR spectral analysis, while their absolute chiral configurations were ascertained either by correlating the experimental and simulated values of electronic circular dichroism (ECD) patterns or conducting X-ray diffraction experiments.
View Article and Find Full Text PDFHeliyon
January 2025
Department of Medical Oncology, Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Guangdong Key Laboratory of Nasopharyngeal Carcinoma Diagnosis and Therapy, Guangdong Provincial Clinical Research Center for Cancer, Guangzhou, 510060, PR China.
Background: In several studies of head and neck squamous cell carcinoma (HNSC), the regulation of tumorigenesis and therapeutic sensitivity by pyroptosis has been observed. However, a systematic analysis of gasdermin family members (GSDMs, including GSDMA/B/C/D/E and PJVK), which are deterministic executors of pyroptosis, has not yet been reported in HNSC.
Methods: We performed comprehensive analyses of the expression profile, prognostic value, regulatory network, and immune infiltration modulation of GSDMs in HNSC on the basis of a computational approach and bioinformatic analysis of publicly available datasets.
Background And Aim: The high rate of tumor growth results in an increased need for amino acids. As solute carriers (SLC) transporters are capable of transporting different amino acids, cancer may develop as a result of these transporters' over-expression due to their complex formation with other biological molecules. Therefore, this review investigated the role of SLC transporters in the progression of cancer.
View Article and Find Full Text PDFVet Res Forum
November 2024
Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Docetaxel (DTX) is widely utilized in breast cancer treatment. However, cancer cell resistance has limited its anti-tumor efficacy. Some molecules called microRNAs (miRNAs), acting like fine-tuned switches, can influence how breast cancer develops and spreads.
View Article and Find Full Text PDFMol Ther Nucleic Acids
March 2025
Department of Medicine, Division of Hematology & Oncology, University of Virginia, Charlottesville, VA 22903, USA.
The CDKN2A gene, responsible for encoding the tumor suppressors p16(INK4A) and p14(ARF), is frequently inactivated in non-small cell lung cancer (NSCLC). Herein, an uncharacterized long non-coding RNA (lncRNA) (ENSG00000267053) on chromosome 19p13.12 was found to be overexpressed in NSCLC cells with an active, wild-type CDKN2A gene.
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