化复合物与替代的4'-phenyl-2',2':6',2′′-terpyridine连接物:合成,表征,抗扩散活性和生物分子相互作用
Benwei Wang1, Dameng Sun1, Sihan Wang1
1School of Chemistry and Chemical Engineering, Guangxi University, Nanning, 530004, Guangxi, People's Republic of China.
概括
新的 (II) 复合物显示出强大的抗癌活性,性能优于. 复合体3和7对食道癌细胞表现出强烈的抑制,而其他复合体则表现出选择性. 这些化合物与DNA和蛋白质相互作用,表明治疗潜力.
科学领域:
- 协调化学 协调化学
- 药用化学 医学化学
- 生物物理化学 生物物理化学
背景情况:
- 尼克尔 (II) 复合物与特皮里丁连接物被研究出它们的生物活性.
- 开发具有提高疗效和选择性的新型抗癌药物是研究的一个关键领域.
- 了解金属复合体与生物点 (如DNA和蛋白质) 的相互作用,对于药物设计至关重要.
研究的目的:
- 为了合成和表征新的Ni (II) 类三明治式协调化合物.
- 评估这些复合体对人类癌症细胞系的抗扩散潜力.
- 研究作用机制,包括与DNA和牛血清蛋白 (BSA) 的相互作用.
主要方法:
- 使用二化和替代的二连接物合成Ni (II) 复合物.
- 通过元素分析,FT-IR,ESI-MS,UV-Vis和X射线衍射进行结构性表征.
- 使用A549,Eca-109,Bel-7402和HL-7702细胞系进行体外抗增殖试验.
- 生物物理研究包括紫外线定位和循环二极化 (CD) 光谱学.
- 分子对接模拟用于预测DNA,DNA-Topo I和BSA的结合模式.
主要成果:
- 合成的Ni(II) 复合物对测试的癌症细胞系产生了显著的抑制作用,超过了思丁.
- 复合物3 (甲氧基) 和7 () 对Eca-109细胞系 (IC50值分别为0.223μM和0.335μM) 显示出强烈的活性.
- 复合体4和6表现出细胞选择性,复合体6在受控度下显示癌细胞抑制和正常细胞最小毒性之间的平衡.
- 实验和对接研究表明,这些复合物通过间隙与CT-DNA结合,并在裂变部位与DNA-Topo I相互作用.
- 关于BSA的结合性研究表明,BSA通过结合到有效部位来促进这些复合物的作用.
结论:
- 新的Ni (II) 复合物具有有前途的抗癌特性,有可能用于治疗.
- 观察到的抗增殖活性与它们与DNA和DNA-Topo I. 相互作用的能力有关.
- 对这些复合物的进一步研究可能会导致开发新的化疗剂.
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