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胺基替代的异环胺基Cu (I) 和Ag (I) 复合物作为有效的抗癌和抗菌剂,向大肠杆菌细菌的周围质

Despoina Varna¹, George D Geromichalos¹, Panagiotis Dalezis²

¹Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124, Thessaloniki, Greece.

European journal of medicinal chemistry

|August 15, 2024

概括

新的铜 (Cu) 和银 (Ag) 金属复合体显示出对抗癌症和细菌的双重活性. 含有银的复合物1有效抑制细菌生长和癌细胞增殖,诱导细胞亡并与DNA相互作用.

科学领域:

协调化学协调化学
药用无机化学药用无机化学
材料科学材料科学材料科学

背景情况:

具有双重抗癌和抗菌活性的金属复合物对于治疗复杂疾病至关重要.
研究替代剂对11组 (Cu,Ag) d10金属复合物的生物活性的影响至关重要.

研究的目的:

合成和表征新的铜 (I) 和银 (I) 复合物,其中含有双NH2替代的异环胺联体 (dap2SH).
评估这些金属复合物的体外抗菌和抗癌特性.
探索它们生物活性背后的机制,包括细胞吸收,DNA相互作用和抗氧化能力.

主要方法:

单核Cu (I) 和Ag (I) 复合物的合成:[AgCl (dap2SH) (PPh3) ] (1),[CuBr (dap2SH) (PPh3) ] (2),[CuBr (dap2SH) (xantphos) ] (3),[Ag (dap2S) (xantphos) ] (4),和[Cu (dap2S) (xantphos) ] (5).
物理化学表征:单晶X射线衍射,FTIR,NMR,UV-Vis和光谱学.
在体外生物活性测定:抗菌 (阳性和阴性菌株),抗癌 (A549,MCF7,PC3细胞系),细胞吸收,亡诱导 (流细胞计),DNA相互作用 (CT DNA间隙),自由基清理和分子对接.

主要成果:

综合体1-3显示显著抑制了格拉姆阳性和格拉姆阴性细菌生长.
综合体1对A549,MCF7和PC3癌细胞系表现出高的抗增殖作用,诱导A549细胞的亡.
细胞吸收研究显示,对复合体1的大肠杆菌周等离子体中的Ag (I) 积累.
复合物1被插入CTDNA,所有复合物都表现出中等至高的自由基清除能力.

结论:

合成的Cu (I) 和Ag (I) 复合物表现出有前途的双重抗菌和抗癌活性.
连接物设计和金属选择显著影响这些复合物的生物活性概况.
复合物1,一种银复合物,显示出作为一种化合物的潜力,用于开发针对细菌感染和癌症的新疗法剂.

关键词:

AcrABZ-TolC多种药物排放输送胺基替代的异环基亚胺基.具有抗菌活性,具有抗菌活性.它具有抗癌活性.生物分布分析分析铜 (I) 和银 (I) 复合物.

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