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Open AccessArticle

Simplified Head-to-Tail Cyclic Polypeptides as Biomaterial-Associated Antimicrobials with Endotoxin Neutralizing and Anti-Inflammatory Capabilities

1
State Key Laboratory of Animal Nutrition, College of Animal Science and Technology, China Agricultural University, Beijing 100193, China
2
The Laboratory of Molecular Nutrition and Immunity, Institute of Animal Nutrition, Northeast Agricultural University, Harbin 150030, China
3
Heilongjiang Key Laboratory of Molecular Design and Preparation of Flame Retarded Materials, College of Science, Northeast Forestry University, Harbin 150040, China
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(23), 5904; https://doi.org/10.3390/ijms20235904
Received: 18 October 2019 / Revised: 15 November 2019 / Accepted: 20 November 2019 / Published: 25 November 2019
(This article belongs to the Section Molecular Pharmacology)
The therapeutic application of antimicrobial peptides (AMPs), a potential type of peptide-based biomaterial, is impeded by their poor antimicrobial activity and potential cytotoxicity as a lack of understanding of their structure–activity relationships. In order to comprehensively enhance the antibacterial and clinical application potency of AMPs, a rational approach was applied to design amphiphilic peptides, including head-to-tail cyclic, linear and D-proline antimicrobial peptides using the template (IR)nP(IR)nP (n = 1, 2 and 3). Results showed that these amphiphilic peptides demonstrated antimicrobial activity in a size-dependent manner and that cyclic peptide OIR3, which contained three repeating units (IR)3, had greater antimicrobial potency and cell selectivity than liner peptide IR3, DIR3 with D-Pro and gramicidin S (GS). Surface plasmon resonance and endotoxin neutralization assays indicated that OIR3 had significant endotoxin neutralization capabilities, which suggested that the effects of OIR3 were mediated by binding to lipopolysaccharides (LPS). Using fluorescence spectrometry and electron microscopy, we found that OIR3 strongly promoted membrane disruption and thereby induced cell lysis. In addition, an LPS-induced inflammation assay showed that OIR3 inhibited the pro-inflammatory factor TNF-α in RAW264.7 cells. OIR3 was able to reduce oxazolone-induced skin inflammation in allergic dermatitis mouse model via the inhibition of TNF-α, IL-1β and IL-6 mRNA expression. Collectively, the engineered head-to-tail cyclic peptide OIR3 was considerable potential candidate for use as a clinical therapeutic for the treatment of bacterial infections and skin inflammation. View Full-Text
Keywords: head-to-tail cyclic antimicrobial peptides; cell selectivity; membrane; bactericidal mechanism; skin inflammation head-to-tail cyclic antimicrobial peptides; cell selectivity; membrane; bactericidal mechanism; skin inflammation
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MDPI and ACS Style

Dong, N.; Wang, C.; Li, X.; Guo, Y.; Li, X. Simplified Head-to-Tail Cyclic Polypeptides as Biomaterial-Associated Antimicrobials with Endotoxin Neutralizing and Anti-Inflammatory Capabilities. Int. J. Mol. Sci. 2019, 20, 5904. https://doi.org/10.3390/ijms20235904

AMA Style

Dong N, Wang C, Li X, Guo Y, Li X. Simplified Head-to-Tail Cyclic Polypeptides as Biomaterial-Associated Antimicrobials with Endotoxin Neutralizing and Anti-Inflammatory Capabilities. International Journal of Molecular Sciences. 2019; 20(23):5904. https://doi.org/10.3390/ijms20235904

Chicago/Turabian Style

Dong, Na; Wang, Chensi; Li, Xinran; Guo, Yuming; Li, Xiaoli. 2019. "Simplified Head-to-Tail Cyclic Polypeptides as Biomaterial-Associated Antimicrobials with Endotoxin Neutralizing and Anti-Inflammatory Capabilities" Int. J. Mol. Sci. 20, no. 23: 5904. https://doi.org/10.3390/ijms20235904

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