4.5 Article

Discovery of potent antimicrobial peptide analogs of Ixosin-B

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 12, Pages 4185-4188

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.018

Keywords

Antimicrobial peptides; Ixosin-B; Antimicrobial activity; Hemolytic activity

Funding

  1. National Science Council [NSC98-2113-M-029-004, NSC99-2113-M-029-001]
  2. Taichung Veterans General Hospital, Taiwan, ROC [TCVGH-987808, TCVGH-997805]

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Antimicrobial peptides (AMPs) represent the first defense line against infection when organisms are infected by pathogens. These peptides are generally good targets for the development of antimicrobial agents. Peptide amide analogs of Ixosin-B, an antimicrobial peptide with amino acid sequence of QLKVDLWGTRSGIQPEQHSSGKSDVRRWRSRY, were designed, synthesized and examined for antimicrobial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Within the peptides synthesized, we discovered an 11-mer peptide, KRLRRVWRRWR-amide, which exhibited potent antimicrobial activity while very little hemolytic activity in human erythrocytes was observed even at high dose level (100 mu M). With further modifications, this peptide could be developed into a potent antimicrobial agent in the future. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

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