在分子NF-κB依赖途径中,Ciminalum-4-thiazolidinone杂交物的作用
Dominika Szlachcikowska1, Anna Tabęcka-Łonczyńska1, Serhii Holota2,3
1Department of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland.
International journal of molecular sciences
|July 13, 2024
概括
两种新型的提阿索利丁衍生物,Les-45和Les-247,通过降低代谢活性和抑制癌症和健康细胞中与炎症相关的基因表达,显示出潜在的抗癌性质.
科学领域:
- 药用化学 医学化学
- 分子生物学分子生物学
- 细胞生物学 细胞生物学
背景情况:
- 具有 thiazolidinone 环的混合分子表现出抗癌和抗菌活性.
- 铁利丁衍生物正在研究它们的治疗潜力.
研究的目的:
- 评估两个4-thiazolidinone衍生物Les-45和Les-247的特性和作用机制.
- 研究它们对人类纤维细胞 (BJ) 和肺癌细胞 (A549) 的代谢活性,酶-3活性和基因/蛋白质表达的影响.
主要方法:
- 在24小时和48小时内,BJ和A549细胞暴露于不同度 (1nM到100μM) 的Les-45和Les-247中.
- 对代谢活性,卡斯巴-3活性和基因表达 (NRF2,β-actin,NF-κB) 的分析.
- 对NF-κB的蛋白质表达的评估和细胞骨重组的评估.
主要成果:
- 莱斯-45和莱斯-247都降低了BJ和A549细胞中的代谢活性,度为10-100μM.
- 在BJ细胞中观察到NRF2和β-actin的mRNA表达减少.
- 在BJ细胞中NF-κB基因和蛋白质表达的显著减少,表明抗炎作用.
结论:
- 莱斯-45和莱斯-247显示出细胞毒性作用和抗炎功能.
- 这些化合物干扰炎症通路 (NF-κB) 和抗氧化防御 (NRF2).
- 需要进一步的研究来了解它们对素/动氨酸细胞骨的影响.
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