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Antiproliferative and antibacterial properties of biocompatible copper(II) complexes bearing chelating N,N-heterocycle ligands and potential mechanisms of action
Biometals ( IF 4.1 ) Pub Date : 2021-08-05 , DOI: 10.1007/s10534-021-00334-9
Rodica Olar 1 , Mihaela Badea 1 , Mihaela Bacalum 2 , Mina Răileanu 2, 3 , Lavinia L Ruţă 4 , Ileana C Farcaşanu 4 , Arpad Mihai Rostas 5 , Ioana Dorina Vlaicu 5 , Marcela Popa 6 , Mariana Carmen Chifiriuc 6, 7
Affiliation  

In an attempt to propose new applications for the biomedical field, complexes with mixed ligands {[Cu(bpy)22OClO3)]ClO4}n (1) and [Cu(phen)2(OH2)](ClO4)2 (2) (bpy: 2,2′-biyridine; phen and 1,10-phenantroline) were evaluated for their antibacterial and cytotoxicicity features and for the elucidation of some of the mechanisms involved. Complex (2) proved to be a very potent antibacterial agent, exhibing MIC and MBEC values 2 to 54 times lower than those obtained for complex (1) against both susceptible or resistant Gram-positive and Gram-negative strains, in planktonic or biofilm growth state. In exchange, complex (1) exhibited selective cytotoxicity against melanoma tumor cells (B16), proving a promising potential for developing novel anticancer drugs. The possible mechanisms of both antimicrobial and antitumor activity of the copper(II) complexes is their DNA intercalative ability coupled with ROS generation. The obtained results recommend the two complexes for further development as multipurpose copper-containing drugs.



中文翻译:

具有螯合 N,N-杂环配体的生物相容性铜 (II) 配合物的抗增殖和抗菌特性及其潜在作用机制

为了在生物医学领域提出新的应用,与混合配体 {[Cu(bpy) 22 OClO 3 )]ClO 4 }n ( 1 ) 和 [Cu(phen) 2 (OH 2 )](评估了ClO 4 ) 2 ( 2 ) (bpy: 2,2'-biyridine; phen 和 1,10-phenantroline) 的抗菌和细胞毒性特征,并阐明了一些相关机制。复合物 ( 2 ) 被证明是一种非常有效的抗菌剂,其 MIC 和 MBEC 值比复合物 ( 1 ) 低 2 到 54 倍) 针对浮游或生物膜生长状态的易感或耐药革兰氏阳性和革兰氏阴性菌株。作为交换,复合物 ( 1 ) 对黑色素瘤细胞 (B16) 表现出选择性细胞毒性,证明了开发新型抗癌药物的潜力。铜 (II) 复合物的抗菌和抗肿瘤活性的可能机制是它们的 DNA 嵌入能力与 ROS 的产生相结合。所得结果推荐这两种配合物进一步开发为多用途含铜药物。

更新日期:2021-08-10
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