合成,抗癌活性和半三明治铁的分子对接 (II) 环丁烯复合体与马莱胺和素或酸连接物
Sujoy Das1, Marcelina Strachanowska2, Piotr Wadowski2
1Department of Organic Chemistry, University of Lodz, Faculty of Chemistry, Tamka 12, 91-403, Lodz, Poland.
Scientific reports
|March 7, 2024
概括
合成了五种新的铁 (II) 环二烯复合物,并对抗癌活性进行了评估. 综合体1和2b对癌细胞具有选择性细胞毒性,因此需要进一步研究它们的机制.
科学领域:
- 有机金属化学 有机金属化学
- 药用化学 医学化学
- 癌症生物学 癌症生物学
背景情况:
- 铁 (II) 复合物正在研究其潜在的治疗应用.
- 环乙复合物为药物设计提供独特的结构和电子特性.
- 开发选择性抗癌药物仍然是瘤学中的一个关键挑战.
研究的目的:
- 为了合成和表征新的铁 (II) 环丁烯复合物.
- 为了评估这些复合体对白血病和肺癌细胞系的体外抗癌活性.
- 研究有前途的化合物的基因毒性潜力和DNA相互作用.
主要方法:
- 五种铁 (II) 复合物的合成和全面光谱表征 (NMR,FT-IR,ESI-MS,UV-Vis,光,XRD,元素分析).
- 在体外细胞毒性测定中使用正常的外周血液单核细胞 (PBM),HL-60 (白血病) 细胞和A549 (非小细胞肺癌) 细胞.
- 评估DNA损伤,等离子体放松试验,DNA定位实验和分子对接研究.
主要成果:
- 所有合成的铁 (II) 复合物都对HL-60和A549癌细胞表现出细胞毒性,具有不同的选择性.
- 复合物3b的总体细胞毒性最高 (IC50值在5.80~19.16μM之间).
- 复合体2b对癌细胞具有选择性细胞毒性,并表现出具有基因毒性潜力.
- 分子对接表明,2a,2b,3b和3c复合体可以与不匹配的DNA结合.
- 铁 (II) 复合物没有诱导d-DNA中的DNA链断裂或插入DNA.
结论:
- 铁 (II) 复合物1和2b是选择性抗癌治疗的有希望的候选者.
- 需要进一步的研究来阐明它们观察到的抗癌活性背后的精确细胞机制.
- 氨酸和酸盐配体的设计显著影响这些铁 (II) 复合物的细胞毒性概况.
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