Abstract:
:Pseudomonas aeruginosa is particularly difficult to treat because it possesses a variety of resistance mechanisms and because it often forms biofilms. Antimicrobial peptides represent promising candidates for future templates of antibiotic-resistant bacterial infections due to their unique mechanism of antimicrobial action. In this study, we first found that the antimicrobial peptide Feleucin-K3 has potent antimicrobial activity against not only the standard strain of P. aeruginosa but also against the multidrug-resistant strains isolated from clinics. Then, the structure-activity relationship of the peptide was investigated using alanine and D-amino acid scanning. Among the analogs synthesized, FK-1D showed much more potent antimicrobial activity, superior stability, and very low toxicity, and it was able to permeabilize bacterial membranes. Furthermore, it exhibited significant anti-biofilm activity. More importantly, FK-1D showed excellent antimicrobial activity in vivo, especially against clinical multidrug-resistant bacteria, in contrast to ceftazidime. Our results suggested that FK-1D could be subjected to fixed-point modification in the first and fourth sites to further optimize its medicinal properties and potential as a lead compound for the treatment of infections caused by multidrug-resistant P. aeruginosa and the associated biofilms.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Xie J,Li Y,Li J,Yan Z,Wang D,Guo X,Zhang J,Zhang B,Mou L,Yang W,Jiang Xdoi
10.1007/s00726-018-2625-4subject
Has Abstractpub_date
2018-10-01 00:00:00pages
1471-1483issue
10eissn
0939-4451issn
1438-2199pii
10.1007/s00726-018-2625-4journal_volume
50pub_type
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