Abstract
Multi-drug resistant Staphylococcus aureus (MDRSA) remains a great challenge despite a decade of research on antimicrobial compounds against their infections. In the present study, various acyclic amines and diamines were chemically synthesized and tested for their antimicrobial as well as antibiofilm activity against MDRSA. Among all the synthesized compounds, an acyclic diamine, (2,2′-((butane-1,4-diylbis(azanediyl)bis(methylene))diphenol) designated as ADM 3, showed better antimicrobial activity (minimum inhibitory concentration at 50 μg/mL) and antibiofilm activity (MBIC50 at 5 μg/mL). In addition, ADM 3 was capable of reducing the virulence factors expression (anti-virulence). Confocal laser scanning microscope analysis of the in vitro tested urinary catheters showed biofilm reduction as well as bacterial killing by ADM 3. On the whole, our data suggest that acyclic diamines, especially ADM 3 can be a potent lead for the further studies in alternative therapeutic approaches.
Highlights
Staphylococcus aureus, a Gram-positive, facultative anaerobic cocci bacterium, is one of the most notorious pathogen, causing infections in humans
Various factors associated with S. aureus such as virulence gene expressions, cell to cell signaling mechanism, inactivation of antibiotics, alteration in target sites, efflux pumps, and biofilm formation have led to the emergence of multi-drug resistant S. aureus (MDRSA) (Dinges et al, 2000; Becker et al, 2003; Zhu et al, 2008; Arya et al, 2011; Qayyum et al, 2016)
Planktonic microbes attach to a particular substratum and produce an anchoring polymer called as an extracellular polysaccharide (EPS) which leads to the formation of the multicellular microbial community known as biofilm (Flemming et al, 2007)
Summary
Staphylococcus aureus, a Gram-positive, facultative anaerobic cocci bacterium, is one of the most notorious pathogen, causing infections in humans. Their abilities to evade the host immune defense mechanism and resistance to the first and second generation antibiotics has made the pathogen a subject of interest in the scientific community (Fedtke et al, 2004). Various factors associated with S. aureus such as virulence gene expressions, cell to cell signaling mechanism, inactivation of antibiotics, alteration in target sites, efflux pumps, and biofilm formation have led to the emergence of multi-drug resistant S. aureus (MDRSA) (Dinges et al, 2000; Becker et al, 2003; Zhu et al, 2008; Arya et al, 2011; Qayyum et al, 2016). The altered metabolic activity of the cells that are associated with biofilm formation have high rates of EPS production, activation of specific genes associated with biofilm formation and virulence, reduction in the growth rate than their planktonic
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