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Polymer-antimicrobial peptide constructs with tailored drug-release behavior
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SYSNO ASEP 0567633 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Polymer-antimicrobial peptide constructs with tailored drug-release behavior Author(s) Pola, Robert (UMCH-V) RID, ORCID
Vícha, Matěj (UMCH-V)
Trousil, Jiří (UMCH-V) RID, ORCID
Grosmanová, Eliška (UMCH-V) RID
Pechar, Michal (UMCH-V) RID, ORCID
Rumlerová, Anna (UMCH-V)
Studenovský, Martin (UMCH-V) RID, ORCID
Kučerová, E. (CZ)
Ulbrich, P. (CZ)
Vokatá, B. (CZ)
Etrych, Tomáš (UMCH-V) RID, ORCIDArticle number 406 Source Title Pharmaceutics. - : MDPI
Roč. 15, č. 2 (2023)Number of pages 16 s. Language eng - English Country CH - Switzerland Keywords antimicrobial peptides ; HPMA copolymers ; bacteria Subject RIV CD - Macromolecular Chemistry OECD category Polymer science R&D Projects GA20-04790S GA ČR - Czech Science Foundation (CSF) Method of publishing Open access Institutional support UMCH-V - RVO:61389013 UT WOS 000940898800001 EID SCOPUS 85149117262 DOI 10.3390/pharmaceutics15020406 Annotation Microbial resistance is one of the main problems of modern medicine. Recently, antimicrobial peptides have been recognized as a novel approach to overcome the microbial resistance issue, nevertheless, their low stability, toxicity, and potential immunogenic response in biological systems have limited their clinical application. Herein, we present the design, synthesis, and preliminary biological evaluation of polymer-antibacterial peptide constructs. The antimicrobial GKWMKLLKKILK-NH2 oligopeptide (PEP) derived from halictine, honey bee venom, was bound to a polymer carrier via various biodegradable spacers employing the pH-sensitive or enzymatically-driven release and reactivation of the PEP’s antimicrobial activity. The antibacterial properties of the polymer-PEP constructs were assessed by a determination of the minimum inhibitory concentrations, followed by fluorescence and transmission electron microscopy. The PEP exerted antibacterial activity against both, gram-positive and negative bacteria, via disruption of the bacterial cell wall mechanism. Importantly, PEP partly retained its antibacterial efficacy against Staphylococcus epidermidis, Escherichia coli, and Acinetobacter baumanii even though it was bound to the polymer carrier. Indeed, to observe antibacterial activity similar to the free PEP, the peptide has to be released from the polymer carrier in response to a pH decrease. Enzymatically-driven release and reactivation of the PEP antimicrobial activity were recognized as less effective when compared to the pH-sensitive release of PEP. Workplace Institute of Macromolecular Chemistry Contact Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358 Year of Publishing 2024 Electronic address https://www.mdpi.com/1999-4923/15/2/406
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