Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity - Publication - Bridge of Knowledge

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Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity

Abstract

Eight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and oneof the three antimicrobials — ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) — were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the “click chemistry” method. This novel approach is reported here for the first time. Unlike their components, CIP- and LVX-based conjugates exerted activity against Candida yeast. Similarly to the constituent peptides, synthesized conjugates showed activity against Gram-positive bacteria, especially S. epidermidis. The most active were the conjugates containing CIP linked to the peptide by the redox-sensitive disulfide bridge. Our results show a significant role of a linker between antimicrobial agent and a peptide. This was also confirmed by the lack of synergistic effects on the antimicrobial activity of the constituent compounds. Moreover, cytotoxicity assays revealed that the proposed conjugates cause a comparatively low cytotoxic effect in reference to antibiotics widely used in therapies. Therefore, they can be deliberated as attractive leading structures for the development of drugs.

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Category:
Articles
Type:
artykuł w czasopiśmie wyróżnionym w JCR
Published in:
PEPTIDES pages 1 - 13,
ISSN: 0196-9781
Language:
English
Publication year:
2019
Bibliographic description:
Ptaszyńska N., Olkiewicz K., Okońska J., Gucwa K., Łęgowska A., Gitlin-Domagalska A., Dawid D., Lica J. J., Heldt M., Milewski S., Ng T., Rolka K.: Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity// PEPTIDES. -, (2019), s.1-13
DOI:
Digital Object Identifier (open in new tab) 10.1016/j.peptides.2019.04.006
Sources of funding:
  • Grant NCN UMO-2016/21/B/ST5/00101
Verified by:
Gdańsk University of Technology

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