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阳离子肽及其 Cu(II)和 Ni(II)配合物:配位和生物学特性。

Cationic Peptides and Their Cu(II) and Ni(II) Complexes: Coordination and Biological Characteristics.

机构信息

Department of Inorganic Chemistry, Wroclaw Medical University, Borowska 211A, 50-556 Wroclaw, Poland.

Department of Pharmacology, Wroclaw Medical University, Jana Mikulicza-Radeckiego 2, 50-345 Wroclaw, Poland.

出版信息

Int J Mol Sci. 2021 Nov 6;22(21):12028. doi: 10.3390/ijms222112028.

Abstract

Antimicrobial peptides are a promising group of compounds used for the treatment of infections. In some cases, metal ions are essential to activate these molecules. Examples of metalloantibiotics are, for instance, bleomycin and dermcidin. This study is focused on three new pseudopeptides with potential biological activity. The coordination behavior of all ligands with Cu(II) and Ni(II) ions has been examined. Various analytical methods such as potentiometric titration, UV-Vis and CD spectroscopies, and mass spectrometry were used. All compounds are convenient chelators for metal ion-binding. Two of the ligands tested have histidine residues. Surprisingly, imidazole nitrogen is not involved in the coordination of the metal ion. The -terminal amino group, Dab side chains, and amide nitrogen atoms of the peptide bonds coordinated Cu(II) and Ni(II) in all the complexes formed. The cytotoxicity of three pseudopeptides and their complexes was evaluated. Moreover, their other model allowed for assessing the attenuation of LPS-induced cytotoxicity and anti-inflammatory activities were also evaluated, the results of which revealed to be very promising.

摘要

抗菌肽是一类很有前途的化合物,可用于治疗感染。在某些情况下,金属离子对于激活这些分子是必不可少的。金属抗生素的例子有博来霉素和皮肤素。本研究集中于三种具有潜在生物学活性的新假肽。研究了所有配体与 Cu(II)和 Ni(II)离子的配位行为。使用了各种分析方法,如电位滴定、紫外可见和 CD 光谱以及质谱。所有化合物都是方便的金属离子结合螯合剂。测试的两种配体含有组氨酸残基。令人惊讶的是,咪唑氮不参与金属离子的配位。在所有形成的配合物中,-末端氨基、Dab 侧链和肽键的酰胺氮原子与 Cu(II)和 Ni(II)配位。评估了三种假肽及其配合物的细胞毒性。此外,还评估了它们的其他模式,以评估对 LPS 诱导的细胞毒性的抑制作用和抗炎活性,结果非常有前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0844/8584440/a6d772b4d135/ijms-22-12028-g001.jpg

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