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Bioactivity and Bactericidal Mechanism of Histidine-Rich β-Hairpin Peptide Against Gram-Negative Bacteria

Laboratory of Molecular Nutrition and Immunity. The Institute of Animal Nutrition, Northeast Agricultural University, Harbin 150030, China
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(16), 3954;
Received: 11 July 2019 / Revised: 6 August 2019 / Accepted: 13 August 2019 / Published: 14 August 2019
(This article belongs to the Section Molecular Microbiology)
PDF [4634 KB, uploaded 14 August 2019]


Antibacterial peptides (APMs) are a new type of antibacterial substance. The relationship between their structure and function remains indistinct; in particular, there is a lack of a definitive and fixed template for designing new antimicrobial peptides. Previous studies have shown that porcine Protegrin-1 (PG-1) exhibits considerable antimicrobial activity and cytotoxicity. In this study, to reduce cytotoxicity and increase cell selectivity, we designed histidine-rich peptides based on the sequence template RR(XY)2XDPGX(YX)2RR-NH2, where X represents I, W, V, and F. The results showed that the peptides form more β-hairpin structures in a lipid-rich environment that mimics cell membranes. Among them, the antimicrobial peptide HV2 showed strong antibacterial activity against Gram-negative strains and almost no toxicity to normal cells. The results of our analysis of its antibacterial mechanism showed that peptide HV2 acts on the bacterial cell membrane to increase its permeability, resulting in cell membrane disruption and death. Furthermore, peptide HV2 inhibited bacterial movement in a concentration-dependent manner and had a more robust anti-inflammatory effect by inhibiting the production of TNF-α. In summary, peptide HV2 exhibits high bactericidal activity and cell selectivity, making it a promising candidate for future use as an antibiotic. View Full-Text
Keywords: β-hairpin antimicrobial peptides; histidine; biological activity; bactericidal mechanism β-hairpin antimicrobial peptides; histidine; biological activity; bactericidal mechanism

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Dong, N.; Wang, C.; Zhang, T.; Zhang, L.; Xue, C.; Feng, X.; Bi, C.; Shan, A. Bioactivity and Bactericidal Mechanism of Histidine-Rich β-Hairpin Peptide Against Gram-Negative Bacteria. Int. J. Mol. Sci. 2019, 20, 3954.

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