Kakkar, Himanshu and Chaudhary, Nalini and Mehta, Devashish and Saini, Varsha and Maheshwari, Shallu and Singh, Jitender and Walia, Preeti and Bajaj, Avinash (2022) N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections. Molecules, 27 (11). p. 3501. ISSN 1420-3049

Text N-methyl Benzimidazole Tethered Cholic Acid Amphiphiles Can Eradicate S. aureus-Mediated Biofilms and Wound Infections.pdf - Published Version Restricted to Registered users only Download (1971Kb) | Request a copy

Abstract

Infections associated with Gram-positive bacteria like S. aureus pose a major threat as these bacteria can develop resistance and thereby limit the applications of antibiotics. Therefore, there is a need for new antibacterials to mitigate these infections. Bacterial membranes present an attractive therapeutic target as these membranes are anionic in nature and have a low chance of developing modifications in their physicochemical features. Antimicrobial peptides (AMPs) can disrupt the microbial membranes via electrostatic interactions, but the poor stability of AMPs halts their clinical translation. Here, we present the synthesis of eight N-methyl benzimidazole substituted cholic acid amphiphiles as antibacterial agents. We screened these novel heterocyclic cholic acid amphiphiles against different pathogens. Among the series, CABI-6 outperformed the other amphiphiles in terms of bactericidal activity against S. aureus. The membrane disruptive property of CABI-6 using a fluorescence-based assay has also been investigated, and it was inferred that CABI-6 can enhance the production of reactive oxygen species. We further demonstrated that CABI-6 can clear the pre-formed biofilms and can mitigate wound infection in murine models. View Full-Text Keywords: S. aureus; membrane targeting amphiphiles; cholic acid; antimicrobial resistance

Item Type:	Article
Subjects:	Bioengineering & Devices Biochemical and Biophysical Sciences
Depositing User:	RCB Library
Date Deposited:	21 Jun 2022 06:25
Last Modified:	21 Jun 2022 06:25
URI:	http://rcb.sciencecentral.in/id/eprint/713

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