Publications Repository - Gdańsk University of Technology

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.

Authors

• Natalia Ptaszyńska,
• Katarzyna Olkiewicz,
• Joanna Okońska,
• Dr inż. Katarzyna Gucwa,
• Anna Łęgowska,
• Agata Gitlin-Domagalska,
• Dębowski Dawid,
• mgr Jan Jakub Lica link open in new tab ,
• Mateusz Heldt link open in new tab ,
• prof. dr hab. inż. Sławomir Milewski link open in new tab ,
• Tzi Ng,
• Krzysztof Rolka