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The antibacterial activity of polyoxometalates: structures, antibiotic effects and future perspectives.

ABSTRACT: Polyoxometalates (POMs) are, mostly anionic, metal oxide compounds that span a wide range of tunable physical and chemical features rendering them very interesting for biological purposes, an continuously emerging but little explored field. Due to their biological and biochemical effects, including antitumor, -viral and -bacterial properties, POMs and POM-based systems are considered as promising future metallodrugs. In this article, we focus on the antibacterial activity of POMs and their therapeutic potential in the battle against bacteria and their increasing resistance against pharmaceuticals. Recent advances in the synthesis of POMs are highlighted, with emphasis on the development and properties of biologically active POM-based hybrid and nanocomposite structures. By analysing the antibacterial activity and structure of POMs, putative mode of actions are provided, including potential targets for POM-protein interactions, and a structure-activity-relationship was established for a series of POMs against two bacteria, namely Helicobacter pylori and Streptococcus pneumoniae.

SUBMITTER: Bijelic A

PROVIDER: S-EPMC5804480 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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The antibacterial activity of polyoxometalates: structures, antibiotic effects and future perspectives.

Bijelic Aleksandar A Aureliano Manuel M Rompel Annette A

Chemical communications (Cambridge, England) 20180101 10

Polyoxometalates (POMs) are, mostly anionic, metal oxide compounds that span a wide range of tunable physical and chemical features rendering them very interesting for biological purposes, an continuously emerging but little explored field. Due to their biological and biochemical effects, including antitumor, -viral and -bacterial properties, POMs and POM-based systems are considered as promising future metallodrugs. In this article, we focus on the antibacterial activity of POMs and their thera ...[more]

PMID: 29355262

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Project description:ObjectivesMultidrug-resistant (MDR) Gram-negative bacterial infections have limited treatment options due to the impermeability of the outer membrane. New therapeutic strategies or agents are urgently needed, and combination therapies using existing antibiotics are a potentially effective means to treat these infections. In this study, we examined whether phentolamine can enhance the antibacterial activity of macrolide antibiotics against Gram-negative bacteria and investigated its mechanism of action.MethodsSynergistic effects between phentolamine and macrolide antibiotics were evaluated by checkerboard and time-kill assays and in vivo using a Galleria mellonella infection model. We utilized a combination of biochemical tests (outer membrane permeability, ATP synthesis, ΔpH gradient measurements, and EtBr accumulation assays) with scanning electron microscopy to clarify the mechanism of phentolamine enhancement of macrolide antibacterial activity against Escherichia coli.ResultsIn vitro tests of phentolamine combined with the macrolide antibiotics erythromycin, clarithromycin, and azithromycin indicated a synergistic action against E. coli test strains. The fractional concentration inhibitory indices (FICI) of 0.375 and 0.5 indicated a synergic effect that was consistent with kinetic time-kill assays. This synergy was also seen for Salmonella typhimurium, Klebsiella pneumoniae, and Actinobacter baumannii but not Pseudomonas aeruginosa. Similarly, a phentolamine/erythromycin combination displayed significant synergistic effects in vivo in the G. mellonella model. Phentolamine added singly to bacterial cells also resulted in direct outer membrane damage and was able to dissipate and uncouple membrane proton motive force from ATP synthesis that, resulted in enhanced cytoplasmic antibiotic accumulation via reduced efflux pump activity.ConclusionsPhentolamine potentiates macrolide antibiotic activity via reducing efflux pump activity and direct damage to the outer membrane leaflet of Gram-negative bacteria both in vitro and in vivo.

Dataset Information

The antibacterial activity of polyoxometalates: structures, antibiotic effects and future perspectives.

Publications

The antibacterial activity of polyoxometalates: structures, antibiotic effects and future perspectives.

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