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Title: Intracellular activity of a membrane-active glycopeptide antibiotic against meticillin-resistant Staphylococcus aureus infection
Authors: Yarlagadda, Venkateswarlu
Samaddar, Sandip
Haldar, Jayanta
Keywords: Infectious Diseases
Pharmacology & Pharmacy
Membrane-active antibiotic
Intracellular activity
Meticillin-resistant Staphylococcus aureus
Issue Date: 2016
Publisher: Elsevier Sci Ltd
Citation: Yarlagadda, V.; Samaddar, S.; Haldar, J., Intracellular activity of a membrane-active glycopeptide antibiotic against meticillin-resistant Staphylococcus aureus infection. Journal of Global Antimicrobial Resistance 2016, 5, 71-74
Journal of Global Antimicrobial Resistance
Abstract: Staphylococcus aureus is a facultative intracellular pathogen and there are limited options for the treatment of severe intracellular bacterial infections. The membrane-active glycopeptide antibiotic Van-QC(8) is a permanent positively charged lipophilic vancomycin analogue that demonstrates high activity against clinically relevant drug-resistant Gram-positive bacteria both in vitro and in vivo. In this study, the intracellular activity of Van-QC(8) was evaluated against meticillin-resistant S. aureus (MRSA) infection in RAW macrophages. Furthermore, the mechanism of intracellular uptake of Van-QC(8) was investigated. Van-QC(8) showed time-and concentration-dependent bactericidal activity against intracellular MRSA. Van-QC(8) displayed significantly higher intracellular activity compared with vancomycin and linezolid. Cellular uptake of Van-QC(8) was found to be through clathrin-dependent and independent and caveolin-dependent and -independent endocytic pathways. The findings of this study suggest that Van-QC(8) could be translated clinically for the treatment of intracellular infections due to MRSA. (C) 2016 International Society for Chemotherapy of Infection and Cancer. Published by Elsevier Ltd. All rights reserved.
Description: Restricted Access
ISSN: 2213-7165
Appears in Collections:Research Papers (Jayanta Haldar)

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