New analogs of temporin-LK1 as inhibitors of multidrug-resistant (MDR) bacterial pathogens |
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| Authors: | Zafar Ali Shah Saba Farooq Syed Abid Ali Abdul Hameed M Iqbal Choudhary |
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| Institution: | 1. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan;2. Department of Chemistry, University of Swabi, Anbar, Pakistan;3. Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan;4. Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan;5. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia |
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| Abstract: | The peptide temporin-LK1 (1) was obtained from the skin secretion of frog Limnonectes kuhlii (Ranidae). It is a unique antimicrobial peptide with 17 residues, including four L-phenylalanines and single glycine. Mass spectrometry and Edmand degradation were used for the determination of sequence of amino acids in temporin-LK 1 (1), and confirmed by cDNA cloning. We report here the synthesis and structural studies of temporin-LK1 (1) and its analogs 2–4. Peptides 2–4 were prepared by substitution of achiral glycine residue of temporin-LK1 (1) with D-alanine, L-phenylglycine, and L-naphthylalanine, respectively. Peptides 1–4 were evaluated against multidrug-resistant (MDR) strains of Staphylococcus aureus and Pseudomonas aeruginosa. Analog 2 was found active against all MDR strains of S. aureus and P. aeruginosa at a much lower dose than the clinically used antibiotics. |
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| Keywords: | Antibacterial peptides MDR bacterial strains Pseudomonas aeruginosa Staphylococcus aureus temporin-LK1 |
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