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以2-(1-乙基苄基)吡啶为配体的金(III)配合物作为有前景的抗菌和抗肿瘤药物

Gold(III) Complexes with 2-(1-Ethylbenzyl)pyridine as Promising Antimicrobial and Antitumor Agents.

作者信息

Zucca Antonio, Canu Bruna, Pilo Maria I, Stoccoro Sergio, Senzacqua Giacomo, Fais Sara, Pichiri Giuseppina, Scano Alessandra

机构信息

Department of Chemical, Physical, Mathematical and Natural Sciences, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.

Consorzio Interuniversitario Reattività Chimica e Catalisi (CIRCC), 70126 Bari, Italy.

出版信息

Molecules. 2025 Apr 4;30(7):1611. doi: 10.3390/molecules30071611.

Abstract

Antimicrobial resistance (AMR) is one of the most urgent public health problems worldwide; multidrug resistance (MDR) is also of concern. In an effort to find new classes of antibiotics, recent studies have found that coordination compounds of noble metals show promising biological effects both in vitro and in vivo, deserving attention as a new class of possible antimicrobial agents. Metal ions in biological systems can essentially have two roles: structural or functional. In the former, the metal ion serves to stabilize structures, especially proteins, while in the latter, the metal is involved in bio-site reactivity (essentially in metallo-enzymes). Two new complexes with 2-(1-ethyl-benzyl)pyridine (py), one monodentate adduct and one cyclometalated ([Au(py)Cl] and [Au(py-H)Cl], respectively), have been synthesized, characterized, and tested against Gram-positive and Gram-negative bacteria, as well as yeasts, revealing promising antibacterial and antibiofilm properties. The two complexes have been thoroughly characterized by means of 1D and 2D NMR spectroscopy, as well as by cyclic voltammetry, conductivity measurements, FT-IR, and elemental analysis. The study showed that the two derivatives are structurally and chemically different, with the cyclometalated complex being chemically and electrochemically more stable. Antimicrobial assays demonstrated that solutions of the monodentate adduct and of the cyclometalated complex have inhibitory and antibiofilm effects against the pathogenic bacteria . , . , . , and . but were unable to reveal a fungicidal effect on . . A preliminary study was conducted to assess the anti-cancer activity of the compounds, and treatments with the gold compounds also resulted in a significant reduction in the metabolic activity of HT29 colon cancer cells.

摘要

抗菌耐药性(AMR)是全球最紧迫的公共卫生问题之一;多重耐药性(MDR)也备受关注。为了寻找新型抗生素,最近的研究发现贵金属配位化合物在体外和体内均显示出有前景的生物学效应,作为一类新型的潜在抗菌剂值得关注。生物系统中的金属离子基本上有两种作用:结构作用或功能作用。在前一种情况下,金属离子用于稳定结构,尤其是蛋白质,而在后一种情况下,金属参与生物位点反应(主要是在金属酶中)。已经合成、表征了两种与2-(1-乙基苄基)吡啶(py)形成的新配合物,一种是单齿加合物,另一种是环金属化配合物(分别为[Au(py)Cl]和[Au(py-H)Cl]),并对革兰氏阳性菌、革兰氏阴性菌以及酵母进行了测试,结果显示出有前景的抗菌和抗生物膜特性。这两种配合物已通过一维和二维核磁共振光谱、循环伏安法、电导率测量、傅里叶变换红外光谱和元素分析进行了全面表征。研究表明,这两种衍生物在结构和化学性质上有所不同,环金属化配合物在化学和电化学方面更稳定。抗菌试验表明,单齿加合物和环金属化配合物的溶液对病原菌……有抑制和抗生物膜作用,但未能显示出对……的杀菌作用。进行了一项初步研究以评估这些化合物的抗癌活性,用金化合物处理也导致HT29结肠癌细胞的代谢活性显著降低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52d2/11990560/94e5bb16b3a3/molecules-30-01611-ch001.jpg

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