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

Author:

Serafin Pawel1,Kowalczyk Paweł2ORCID,Mollica Adriano3ORCID,Stefanucci Azzurra3ORCID,Laskowska Anna K.4,Zawadzka Magdalena15ORCID,Kramkowski Karol6,Kleczkowska Patrycja17ORCID

Affiliation:

1. Military Institute of Hygiene and Epidemiology, 01-163 Warsaw, Poland

2. Department of Animal Nutrition, The Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciences, 05-110 Jabłonna, Poland

3. Department of Pharmacy, University “G. d’Annunzio” of Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy

4. Centre for Preclinical Research and Technology (CePT), Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland

5. Department of Epidemiology and Public Health Lodz, Medical University of Lodz, 90-419 Lodz, Poland

6. Department of Physical Chemistry, Medical University of Bialystok, 15-089 Białystok, Poland

7. Maria Sklodowska-Curie Medical Academy in Warsaw, 03-411 Warsaw, Poland

Abstract

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.

Funder

National Science Center

Medical University of Białystok

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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