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Citation
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HERO ID
7563212
Reference Type
Journal Article
Title
Indolicidin analogs with broad-spectrum antimicrobial activity and low hemolytic activity
Author(s)
Smirnova, MP; Kolodkin, NI; Kolobov, AA; Afonin, VG; Afonina, IV; Stefanenko, LI; Shpen', VM; Shamova, OV; Kolobov, AA; ,
Year
2020
Is Peer Reviewed?
1
Journal
Peptides
ISSN:
0196-9781
Publisher
ELSEVIER SCIENCE INC
Location
NEW YORK
Volume
132
Page Numbers
170356
Language
English
PMID
32593681
DOI
10.1016/j.peptides.2020.170356
Web of Science Id
WOS:000569761900003
URL
https://linkinghub.elsevier.com/retrieve/pii/S0196978120301054
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Abstract
To create a broad-spectrum peptide biocide, we synthesized 45 analogs of antimicrobial peptide indolicidin (H-Ile-Leu-Pro-Trp-Lys-Trp-Pro-Trp-Trp-Pro-Trp-Arg-Arg-NH2). Among them the peptides H-Ile-Leu-Pro-(2-Me)Phe-Lys-(2-Me)Phe-Pro-(2-Me)Phe-(2-Me)Phe-Pro-(2-Me)Phe-Arg-Arg-NH2 and HN2-(CH2)10-Ile-Leu-Pro-D-Phe-Lys-D-Phe-Pro-D-Phe-D-Phe-Pro-D-Phe-Arg-Arg-NH2 have the broadest spectrum of antimicrobial activity and the lowest hemolytic activity. They are active against all 11 tested strains of Gram-positive bacteria, Gram-negative bacteria and fungi with MIC50 from 0.9 to 6.1 μg/ml (0.5 to 3.2 μM), being up to 3 times more active than indolicidin, and are at least 1.8 times less hemolytically active than indolicidin (reached the detection limit). These peptides are patented and could be used for further drug development as antimicrobials.
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