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Effect of Net Charge on DNA-Binding, Protein-Binding and Anticancer Properties of Copper(I) Phosphine-Diimine Complexes
Journal of Inorganic and Organometallic Polymers and Materials ( IF 4 ) Pub Date : 2021-07-07 , DOI: 10.1007/s10904-021-02063-5
Sammar Alsaedi 1 , Bandar A. Babgi 1 , Mostafa A. Hussien 1, 2 , Magda H. Abdellatif 3 , Abdul-Hamid Emwas 4 , Mariusz Jaremko 5 , Mark G. Humphrey 6
Affiliation  

The syntheses of [Cu(PPh3)2(L)]NO3 and [Cu(PPh3)2(L-SO3Na)]NO3 were achieved through the reaction of Cu(PPh3)2NO3 and equimolar amount of the ligands (L = 5,6-diphenyl-3-[2-pyridyl]-1,2,4-triazine; LSO3Na = 5,6-diphenyl-3-[2-pyridyl]-1,2,4-triazine-4,4′-disulfonic acid disodium salt). The complexes were characterized by NMR and IR spectroscopy and mass spectrometry. The compounds exhibit similar absorption and emission spectra, suggesting a similar electronic structure. Ct-DNA binding studies show the strong influence of the net charge as Cu-L (positively charged) is able to bind to ct-DNA while Cu-LSO3Na (negatively charged) is not. The net charge of the complexes affects the thermodynamic and kinetic binding parameters toward human serum albumin. HSA-binding of the complexes was further investigated by molecular docking, revealing different binding sites on the HSA protein as a function of the net charge. The different anticancer activities of the complexes towards ovcar-3 and hope-62 cancer cell lines are suggestive of a role for the overall charge of the complexes. Interaction with the DNA is not the major mechanism for this class of complexes. The overall net charge of the pharmacophore (anticancer agent) should be a key consideration in the design of anticancer metal complexes.



中文翻译:

净电荷对铜 (I) 膦-二亚胺配合物的 DNA 结合、蛋白质结合和抗癌特性的影响

[Cu(PPh 3 ) 2 (L)]NO 3和[Cu(PPh 3 ) 2 (L-SO 3 Na)]NO 3的合成是通过Cu(PPh 3 ) 2 NO 3和等摩尔的反应实现的。配体的量(L = 5,6-diphenyl-3-[2-pyridyl]-1,2,4-triazine; LSO 3Na = 5,6-二苯基-3-[2-吡啶基]-1,2,4-三嗪-4,4'-二磺酸二钠盐)。通过NMR和IR光谱以及质谱对配合物进行表征。这些化合物表现出相似的吸收和发射光谱,表明具有相似的电子结构。Ct-DNA 结合研究表明净电荷的强烈影响,因为 Cu-L(带正电荷)能够与 ct-DNA 结合,而 Cu-LSO 3Na(带负电)不是。复合物的净电荷影响对人血清白蛋白的热力学和动力学结合参数。通过分子对接进一步研究了复合物的 HSA 结合,揭示了作为净电荷函数的 HSA 蛋白上的不同结合位点。复合物对 ovcar-3 和希望-62 癌细胞系的不同抗癌活性暗示了复合物的整体电荷的作用。与 DNA 的相互作用不是此类复合物的主要机制。药效团(抗癌剂)的总净电荷应该是设计抗癌金属配合物的关键考虑因素。

更新日期:2021-07-08
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