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Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01

Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains a difficult task. Indeed, there is an urgent need for innovation in the design and development of a microbial inhibitor. Given that many promising antimi...

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Autores principales: Serafin, Pawel, Kowalczyk, Paweł, Mollica, Adriano, Stefanucci, Azzurra, Laskowska, Anna K., Zawadzka, Magdalena, Kramkowski, Karol, Kleczkowska, Patrycja
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10343207/
https://www.ncbi.nlm.nih.gov/pubmed/37446618
http://dx.doi.org/10.3390/molecules28134955
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author Serafin, Pawel
Kowalczyk, Paweł
Mollica, Adriano
Stefanucci, Azzurra
Laskowska, Anna K.
Zawadzka, Magdalena
Kramkowski, Karol
Kleczkowska, Patrycja
author_facet Serafin, Pawel
Kowalczyk, Paweł
Mollica, Adriano
Stefanucci, Azzurra
Laskowska, Anna K.
Zawadzka, Magdalena
Kramkowski, Karol
Kleczkowska, Patrycja
author_sort Serafin, Pawel
collection PubMed
description Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains a difficult task. Indeed, there is an urgent need for innovation in the design and development of a microbial inhibitor. Given that many promising antimicrobial peptides with excellent broad-spectrum antibacterial properties are secreted by some frog species (e.g., bombesins, opioids, temporins, etc.), our goal was to identify the antimicrobial properties of amphibian-derived dermorphin and ranatensin peptides, which were combined to produce a hybrid compound. This new chimera (named LENART01) was tested for its antimicrobial activity against E. coli strains K12 and R1–R4, which are characterized by differences in lipopolysaccharide (LPS) core oligosaccharide structure. The results showed that LENART01 had superior activity against the R2 and R4 strains compared with the effects of the clinically available antibiotics ciprofloxacin or bleomycin (MIC values). Importantly, the inhibitory effect was not concentration dependent; however, LENART01 showed a time- and dose-dependent hemolytic effect in hemolytic assays.
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spelling pubmed-103432072023-07-14 Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01 Serafin, Pawel Kowalczyk, Paweł Mollica, Adriano Stefanucci, Azzurra Laskowska, Anna K. Zawadzka, Magdalena Kramkowski, Karol Kleczkowska, Patrycja Molecules Article Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains a difficult task. Indeed, there is an urgent need for innovation in the design and development of a microbial inhibitor. Given that many promising antimicrobial peptides with excellent broad-spectrum antibacterial properties are secreted by some frog species (e.g., bombesins, opioids, temporins, etc.), our goal was to identify the antimicrobial properties of amphibian-derived dermorphin and ranatensin peptides, which were combined to produce a hybrid compound. This new chimera (named LENART01) was tested for its antimicrobial activity against E. coli strains K12 and R1–R4, which are characterized by differences in lipopolysaccharide (LPS) core oligosaccharide structure. The results showed that LENART01 had superior activity against the R2 and R4 strains compared with the effects of the clinically available antibiotics ciprofloxacin or bleomycin (MIC values). Importantly, the inhibitory effect was not concentration dependent; however, LENART01 showed a time- and dose-dependent hemolytic effect in hemolytic assays. MDPI 2023-06-23 /pmc/articles/PMC10343207/ /pubmed/37446618 http://dx.doi.org/10.3390/molecules28134955 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Serafin, Pawel
Kowalczyk, Paweł
Mollica, Adriano
Stefanucci, Azzurra
Laskowska, Anna K.
Zawadzka, Magdalena
Kramkowski, Karol
Kleczkowska, Patrycja
Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title_full Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title_fullStr Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title_full_unstemmed Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title_short Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
title_sort evaluation of antimicrobial activities against various e. coli strains of a novel hybrid peptide—lenart01
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10343207/
https://www.ncbi.nlm.nih.gov/pubmed/37446618
http://dx.doi.org/10.3390/molecules28134955
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