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Abstract
The big problem of antimicrobial resistance is that it requires great efforts in the design of improved drugs which can quickly reach their target of action. Studies of antibiotic uptake and interaction with their target it is a key factor in this important challenge. We investigated the accumulation of ozenoxacin (OZN), moxifloxacin (MOX), levofloxacin (LVX), and ciprofloxacin (CIP) into the bacterial cells of 5 species, including Staphylococcus aureus (SA4-149), Staphylococcus epidermidis (SEP7602), Streptococcus pyogenes (SPY165), Streptococcus agalactiae (SAG146), and Enterococcus faecium (EF897) previously characterized.The concentration of quinolone uptake was estimated by agar disc-diffusion bioassay. Furthermore, we determined the inhibitory concentrations 50 (IC50) of OZN, MOX, LVX, and CIP against type II topoisomerases from S. aureus.The accumulation of OZN inside the bacterial cell was superior in comparison to MOX, LVX, and CIP in all tested species. The accumulation of OZN inside the bacterial cell was superior in comparison to MOX, LVX, and CIP in all tested species. The rapid penetration of OZN into the cell was reflected during the first minute of exposure with antibiotic values between 190 and 447 ng/mg (dry weight) of bacteria in all strains. Moreover, OZN showed the greatest inhibitory activity among the quinolones tested for both DNA gyrase and topoisomerase IV isolated from S. aureus with IC50 values of 10 and 0.5 mg/L, respectively. OZN intracellular concentration was significantly higher than that of MOX, LVX and CIP. All of these features may explain the higher in vitro activity of OZN compared to the other tested quinolones.
Highlights
Introduction iationsA long list of compounds with antagonistic activity against bacteria have been described by various researchers worldwide [1]
We predominantly focused on the main pathogens associated with skin infections, such as S. aureus, S
The study of Cama et al, 2016 [39], comment that the presence of fluorine atom on the aromatic ring of some quinolones could be increase the lipophilicity and the permeability of antibiotic generating a greater accumulation inside the bacterial cell
Summary
Generally speaking, for Gram-positive bacteria the opposite is true, i.e., the higher the hydrophobicity, the greater the concentration accumulated [36] In this sense, OZN and MOX are the most strongly hydrowith other tested quinolones. MOX was accumulated in high concentrations in the first minute of exposure inside the bacterial cell of E. faecium and S. epidermidis in comparison with LEV and CIP (values between 168 and 312 ng/mg (dry weight) of bacteria, respectively). In the study of Piddock et al [38], there were exceptions to this principle related to molecular weight which leads to the idea that other factors could influence the accumulation rate In this sense, the study of Cama et al, 2016 [39], comment that the presence of fluorine atom on the aromatic ring of some quinolones could be increase the lipophilicity and the permeability of antibiotic generating a greater accumulation inside the bacterial cell. [23] (Figure 2), allowing for high accumulation values of OZN
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