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A novel chalcone derivative exerts anticancer effects by promoting apoptotic cell death of human pancreatic cancer cells

Title
A novel chalcone derivative exerts anticancer effects by promoting apoptotic cell death of human pancreatic cancer cells
Authors
BaekSujiNahSangheeParkJoo YeonLeeSang JuKangYong GilKwonSeung HaeOhSeung JunKang PaMoonByung Seok
Ewha Authors
문병석
SCOPUS Author ID
문병석scopusscopus
Issue Date
2023
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
Bioorganic and Medicinal Chemistry vol. 93
Keywords
ApoptosisChalconeLipid accumulationPancreatic cancerStimulated Raman scattering microscopy
Publisher
Elsevier Ltd
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Aggressive pancreatic cancer is typically treated using chemotherapeutics to reduce the tumor pre-operatively and prevent metastasis post-operatively, as well as surgical approaches. In the present study, we synthesized a hydroxyl group-introduced chalcone derivative (1, IC50 = 32.1 μM) and investigated its potential as an anticancer drug candidate by evaluating its apoptosis-promoting effects on BXPC-3 cancer cells. The viability of BXPC-3 cells treated with 1 was measured using the water-soluble tetrazolium 1 reagent. BXPC-3 cells induced by 1 were stained with diverse probes or antibodies, such as ethidium homodimer-1, Hoechst, anti-Ki67, and MitoTracker. Protein expression was measured using an immunoblotting assay, and mRNA expression was determined using real-time polymerase chain reaction. Apoptotic molecular features, such as lipid accumulation and protein degradation, were monitored directly using stimulated Raman scattering microspectroscopy. Through incubation time- and concentration-dependent studies of 1, we found that it significantly reduced the proliferation and increased the number of apoptotic BXPC-3 cells. Compound 1 induced mitochondrial dysfunction, phosphorylation of p38, and caspase 3 cleavage. These results indicate that 1 is a potential therapeutic agent for pancreatic cancer, providing valuable insights into the development of new anticancer drug candidates. © 2023 Elsevier Ltd
DOI
10.1016/j.bmc.2023.117458
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의료원 > 의료원 > Journal papers
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