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A Nonbactericidal Zinc‐Complexing Ligand as a Biofilm Inhibitor: Structure‐Guided Contrasting Effects on Staphylococcus aureus Biofilm
Author(s) -
Kapoor Vidushi,
Rai Rajanikant,
Thiyagarajan Durairaj,
Mukherjee Sandipan,
Das Gopal,
Ramesh Aiyagari
Publication year - 2017
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201700139
Subject(s) - biofilm , staphylococcus aureus , zinc , chemistry , microbiology and biotechnology , ligand (biochemistry) , chelation , hela , adhesion , biochemistry , in vitro , bacteria , biology , receptor , organic chemistry , genetics
Zinc‐complexing ligands are prospective anti‐biofilm agents because of the pivotal role of zinc in the formation of Staphylococcus aureus biofilm. Accordingly, the potential of a thiosemicarbazone (compound C1) and a benzothiazole‐based ligand (compound C4) in the prevention of S. aureus biofilm formation was assessed. Compound C1 displayed a bimodal activity, hindering biofilm formation only at low concentrations and promoting biofilm growth at higher concentrations. In the case of C4, a dose‐dependent inhibition of S. aureus biofilm growth was observed. Atomic force microscopy analysis suggested that at higher concentrations C1 formed globular aggregates, which perhaps formed a substratum that favored adhesion of cells and biofilm formation. In the case of C4, zinc supplementation experiments validated zinc complexation as a plausible mechanism of inhibition of S. aureus biofilm. Interestingly, C4 was nontoxic to cultured HeLa cells and thus has promise as a therapeutic anti‐biofilm agent. The essential understanding of the structure‐driven implications of zinc‐complexing ligands acquired in this study might assist future screening regimes for identification of potent anti‐biofilm agents.