Abstract

Antibiotic resistance is currently one of the main threats to public health security. Biofilm formation is a resistance mechanism that is responsible for most human bacterial infections and requires new and effective therapeutic approaches, such as those provided by nanotechnology. In this work, the antibacterial effect of carbosilane metallodendrimers with different metals (copper(II) and ruthenium(II)), ligands (chloride and nitrate) and generations (generation 0, 1 and 2) has been studied using planktonic Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. Furthermore, the ability of the metallodendrimers to avoid the formation of S. aureus biofilms was also evaluated. The results showed a promising biocide activity in both types of planktonic bacteria, especially for first-generation dendrimers, which arises from the metal complexation to the dendrimer. Cu(II) metallodendrimers require lower concentration than Ru(II) counterpart to inhibit the production of S. aureus biofilms, but none produce hemolysis at the inhibitory concentrations and can be safely used as antibacterial agents. In particular, the first-generation Cu(II) metallodendrimer with nitrate ligands displayed the most promising properties to continue with further studies in both planktonic cells and biofilms.

Highlights

  • Escherichia coli and Staphylococcus aureus are representatives of Gram-negative and Gram-positive microbes, respectively

  • The metal complexes and metallodendrimers selected for this study exhibited cationic properties, according to the Z-potential measurements (Table 1)

  • The surface charge on the dendrimers increased from G0 to G2 according to the increase in the number of branches and the number of positive charges in the periphery

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Summary

Introduction

Escherichia coli and Staphylococcus aureus are representatives of Gram-negative and Gram-positive microbes, respectively. Biomolecules 2019, 9, 405 is facultative anaerobic, coagulase-positive, catalase-positive and oxidase-negative. It grows forming colonies in an optimum temperature range 30–40 ◦ C [2,3], and they can even grow in seawater and ferment glucose, lactose and maltose [1,4,5]. S. aureus is an opportunistic pathogen found in the normal human microbiota, at the skin of healthy individuals [6,7]. S. aureus infections can affect the skin, the bloodstream, bone tissues or the eyes, leading to life-threatening diseases like endocarditis, pneumonia, toxic shock syndrome or keratitis

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