Abstract
To develop a novel cell-selective antimicrobial peptide with potent anti-inflammatory activity as well as high bacterial cell selectivity, we synthesized a Leu/Lys-rich model peptide, KLW-f (KWKKLLKKfLKLfKKLLK-NH2) containing two Phe-peptoid residues in its middle position. KLW-f exhibited high antimicrobial activity (the MIC range: 0.5∼ 2.0μM) against the tested six bacterial cells. In contrast, KLW-f was no cytotoxic to human red blood cells and HeLa and NIH-3T3 cells. KLW-f caused no or little dye leakage from EYPE/EYPG (7:3, w/w) vesicles (bacterial membranemimicking environments), indicating its bacterial-killing action is probably not due to permeabilization/disruption of bacterial cytoplasmic membranes. Furthermore, KLW-f induced a significant inhibition in LPS-stimulated NO production from mouse macrophage RAW264.7 cells at 10μg/ml. Taken together, our results suggest that KLW-f appear to have promising therapeutic potential for future development as a novel antisepsis agent as well as antimicrobial agent.
Keywords: antimicrobial peptide, KLW-f, Phe-peptoid residue (Nphe), cell selectivity, anti-inflammatory activity
Protein & Peptide Letters
Title: Antimicrobial and Anti-Inflammatory Activities of a Leu/Lys-Rich Antimicrobial Peptide with Phe-Peptoid Residues
Volume: 14 Issue: 10
Author(s): Yong Hai Nan, Ka Hyon Park, Young Jin Jeon, Yoonkyung Park, Il-Seon Park, Kyung-Soo Hahm and Song Yub Shin
Affiliation:
Keywords: antimicrobial peptide, KLW-f, Phe-peptoid residue (Nphe), cell selectivity, anti-inflammatory activity
Abstract: To develop a novel cell-selective antimicrobial peptide with potent anti-inflammatory activity as well as high bacterial cell selectivity, we synthesized a Leu/Lys-rich model peptide, KLW-f (KWKKLLKKfLKLfKKLLK-NH2) containing two Phe-peptoid residues in its middle position. KLW-f exhibited high antimicrobial activity (the MIC range: 0.5∼ 2.0μM) against the tested six bacterial cells. In contrast, KLW-f was no cytotoxic to human red blood cells and HeLa and NIH-3T3 cells. KLW-f caused no or little dye leakage from EYPE/EYPG (7:3, w/w) vesicles (bacterial membranemimicking environments), indicating its bacterial-killing action is probably not due to permeabilization/disruption of bacterial cytoplasmic membranes. Furthermore, KLW-f induced a significant inhibition in LPS-stimulated NO production from mouse macrophage RAW264.7 cells at 10μg/ml. Taken together, our results suggest that KLW-f appear to have promising therapeutic potential for future development as a novel antisepsis agent as well as antimicrobial agent.
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Cite this article as:
Nan Hai Yong, Park Hyon Ka, Jeon Jin Young, Park Yoonkyung, Park Il-Seon, Hahm Kyung-Soo and Shin Yub Song, Antimicrobial and Anti-Inflammatory Activities of a Leu/Lys-Rich Antimicrobial Peptide with Phe-Peptoid Residues, Protein & Peptide Letters 2007; 14 (10) . https://dx.doi.org/10.2174/092986607782541042
DOI https://dx.doi.org/10.2174/092986607782541042 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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