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生物重要咪唑部分在 Fe(III)和 Mn(II)配合物的抗菌和抗癌活性中的作用。

Role of biologically important imidazole moiety on the antimicrobial and anticancer activity of Fe(III) and Mn(II) complexes.

机构信息

Functional Inorganic Materials Lab (FIML), Department of Chemistry, Aligarh Muslim University, Aligarh, Uttar Pradesh, India.

Interdisciplinary Biotechnology Unit, Aligarh Muslim University, Aligarh, Uttar Pradesh, India.

出版信息

J Biomol Struct Dyn. 2021 Jul;39(11):4037-4050. doi: 10.1080/07391102.2020.1776156. Epub 2020 Jun 25.

Abstract

Currently, most pathogens influencing a number of epidemics outline a notable warning to human health. It has pushed researchers to design new antimicrobial drugs using transition metals that are studied in proceeding fewer years for their antimicrobial properties. Henceforth, in this work, two mononuclear complexes [Imz-H][Fe(pda)]⋅1⋅3HO () and [Mn(Imz)]⋅2Cl⋅2HO () [Imz = imidazole and Hpda = 2,6 pyridine dicarboxylic acid] are isolated and characterized systematically by various spectral and single-crystal XRD studies. The antimicrobial activity of the present hexadentate complexes of Fe(III) and Mn(II) against Gram-positive as well as Gram-negative bacteria is also assessed. Augmented activity against standard isolates of with a minimum inhibitory concentration (MIC) is observed. Similar activity was also observed toward , and . and have excellent bactericidal activity, and no resistant mutant for was seen. The compound also unveiled antibiofilm activity and was capable to disrupt significantly the pre-formed biofilms and this property was confirmed by XTT assay experiment. The MTT assay data indicate that and can be used as anticancer agents toward the RAW 64.7 (human macrophage/monocyte) cell line. Further, the molecular docking study reveals that the role of imidazole is very important in the biological activity of these complexes. Moreover, our results suggest that and with its effective anti-microbial, anti-biofilm and cytotoxicity activity can be used to treat bacterial and fungal infections and could be appraised clinically for further applications.Communicated by Ramaswamy H. Sarma.

摘要

目前,影响许多流行病的大多数病原体对人类健康构成了显著威胁。这促使研究人员设计新的抗菌药物,使用在过去几年中研究较少的过渡金属来发挥其抗菌特性。因此,在这项工作中,分离并系统地通过各种光谱和单晶 XRD 研究了两个单核配合物[Imz-H][Fe(pda)]⋅1⋅3HO()和[Mn(Imz)]⋅2Cl⋅2HO()[Imz = 咪唑和 Hpda = 2,6 吡啶二甲酸]。还评估了本研究的六配位 Fe(III)和 Mn(II)配合物对革兰氏阳性菌和革兰氏阴性菌的抗菌活性。观察到对标准分离株的活性增强,最小抑菌浓度(MIC)。对、和也观察到类似的活性。和对具有极好的杀菌活性,且未观察到对的耐药突变体。该化合物还表现出抗生物膜活性,并能够显著破坏已形成的生物膜,这一特性通过 XTT 测定实验得到证实。MTT 测定数据表明,和可作为 RAW 64.7(人巨噬细胞/单核细胞)细胞系的抗癌剂。此外,分子对接研究表明,咪唑在这些配合物的生物活性中起着非常重要的作用。此外,我们的结果表明,和具有有效的抗菌、抗生物膜和细胞毒性活性,可用于治疗细菌和真菌感染,并可在临床上进一步评估其应用。由 Ramaswamy H. Sarma 传达。

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