Ngece Kwanele, Khwaza Vuyolwethu, Paca Athandwa M, Aderibigbe Blessing A
Department of Chemical and Earth Sciences, University of Fort Hare, Alice 5700, Eastern Cape, South Africa.
Antibiotics (Basel). 2025 May 16;14(5):516. doi: 10.3390/antibiotics14050516.
The alarming increase in antimicrobial resistance has intensified the search for novel therapeutic agents capable of combating resistant microbial strains. Copper complexes have emerged as promising antimicrobial agents due to their intrinsic redox activity, ability to disrupt microbial membranes, and interactions with vital biomolecules such as DNA and proteins. This review critically evaluates the antimicrobial potential of copper complexes reported between 2018 and 2025, emphasizing their structural diversity, mechanisms of action, and biological performance against a wide range of bacterial and fungal pathogens. Key findings reveal that Schiff base copper complexes, amino acid derivatives, heterocyclic ligands, and mixed-ligand systems exhibit potent antimicrobial activities, often surpassing standard antibiotics. Mechanistically, copper complexes induce reactive oxygen species (ROS) generation, inhibit enzyme function, cause DNA cleavage, and compromise cell membrane integrity. Furthermore, structure-activity relationship (SAR) analyses indicate that ligand type, coordination geometry, and lipophilicity significantly influence antimicrobial efficacy. Overall, the reviewed studies support the development of copper-based compounds as viable candidates for antimicrobial drug development. This review also identifies current challenges and gaps in knowledge, such as limited in vivo studies and toxicity assessments, which must be addressed to advance these compounds toward clinical application.
抗菌耐药性的惊人增长加剧了对能够对抗耐药微生物菌株的新型治疗剂的寻找。铜配合物因其固有的氧化还原活性、破坏微生物膜的能力以及与DNA和蛋白质等重要生物分子的相互作用,已成为有前景的抗菌剂。本综述批判性地评估了2018年至2025年间报道的铜配合物的抗菌潜力,强调了它们的结构多样性、作用机制以及对多种细菌和真菌病原体的生物学性能。主要发现表明,席夫碱铜配合物、氨基酸衍生物、杂环配体和混合配体系统表现出强大的抗菌活性,常常超过标准抗生素。从机制上讲,铜配合物诱导活性氧(ROS)生成、抑制酶功能、导致DNA裂解并损害细胞膜完整性。此外,构效关系(SAR)分析表明,配体类型、配位几何结构和亲脂性显著影响抗菌效果。总体而言,综述研究支持将铜基化合物开发为抗菌药物开发的可行候选物。本综述还确定了当前知识方面的挑战和差距,例如体内研究和毒性评估有限,必须解决这些问题才能推动这些化合物走向临床应用。