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

被引:2
作者
Baek, Suji [1 ]
Nah, Sanghee [2 ]
Park, Joo Yeon [1 ]
Lee, Sang Ju [3 ]
Kang, Yong Gil [1 ]
Kwon, Seung Hae [2 ]
Oh, Seung Jun [3 ]
Lee, Kang Pa [1 ]
Moon, Byung Seok [4 ]
机构
[1] UMUST R&D Corp, Res & Dev Ctr, Seoul 01411, South Korea
[2] Korea Basic Sci Inst, Seoul Ctr, Seoul 02841, South Korea
[3] Univ Ulsan, Coll Med, Asan Med Ctr, Dept Nucl Med, Seoul 05505, South Korea
[4] Ewha Womans Univ, Seoul Hosp, Dept Nucl Med, Coll Med, Seoul 07804, South Korea
基金
新加坡国家研究基金会;
关键词
Chalcone; Pancreatic cancer; Apoptosis; Lipid accumulation; Stimulated Raman scattering microscopy;
D O I
10.1016/j.bmc.2023.117458
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 & mu;M) 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.
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页数:8
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