Anti-microbial and Anti-biofilm activity of a novel Dibenzyl (benzo[d] thiazol-2-yl (hydroxy) methyl) phosphonate by inducing protease expression in Staphylococcus aureus

AbstractIn the present study a novel Dibenzyl (benzo[d]thiazol-2-yl(hydroxy)methyl) phosphonate (3b) derived from α-Hydroxyphosphonate exhibited anti-Staphylococcus aureus and anti-biofilm properties against penicillin, ampicillin and methicillin-resistant strains ofS. aureus. The compound3b showed Minimum inhibitory concentration (MIC90) at 160  ± 1 µg/ml and lethal dose (LD50) at 80  ± 1 µg/ml.S. aureus growing as planktonic culture shows a formation of aggregates which is the prerequisite for the formation of biofilms, the compound3b disrupted aggregates and cleared all the preformed planktonic biofilms and prevented their recurrence. The SDS-PAGE analysis of compound3b treatedS. aureus showed gradual lysis of total proteins. The zymogram analysis indicated overexpression of proteases which is the principle reason for lysis of total proteins ofS. aureus on incubation with compound3b. Further, the dot blot analysis indicated complete lysis of Protein-A in the culture filtrate of all the drug-resistant strains ofS. aureus a prominent virulence factor and biofilm forming protein. All these features exhibited by compound3b makes it as a potential therapeutic molecule in the treatment ofS. aureus infections.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research