Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2022 Sep;54(9):1327-1336.
doi: 10.1007/s00726-022-03189-7. Epub 2022 Jul 19.

Design and modification of frog skin peptide brevinin-1GHa with enhanced antimicrobial activity on Gram-positive bacterial strains

Şeyda Kara  1 , Cemil Kürekci  2 , Muharrem Akcan  3
Affiliations

Design and modification of frog skin peptide brevinin-1GHa with enhanced antimicrobial activity on Gram-positive bacterial strains

Şeyda Kara et al. Amino Acids. 2022 Sep.

Abstract

Naturally occurring frog skin peptides are one of largest sources of antimicrobial peptides that have many advantages including high potency, broad spectrum of targets and low susceptibility to multiple drug-resistance bacteria. However, they also have disadvantages such as hemolytic activity, low stability and high production costs. For these reasons, various strategies have been applied to overcome these drawbacks restricting their use in clinical trials. Previously reported brevinin-1GHa (BR-1GHa) is a 24 amino acid long antimicrobial peptide isolated from Hylarana guentheri with hemolytic activity. To enhance the antimicrobial activity of this peptide and to reduce its hemolytic activity, we designed five new temporin like analogues and examined their bioactivities. Temporins are another class of frog skin peptides without hemolytic activity and shorter than brevinins. When the antimicrobial activities of new analogues were examined against a panel of microorganisms, BR-1GHa-3, in which two alanine residues in the truncated version of BR-1GHa were replaced with leucine, exhibited significantly improved antimicrobial activity against Gram-positive bacterial strains (e.g., S. aureus ATCC 29213 and E. casseliflavus ATCC 700327) with lower hemolytic activity compared to the BR-1GHa peptide. Furthermore, BR-1GHa-4 analogue, in which Gly3 was replaced with Pro, did not show any hemolytic activity except for highest (128 µM) concentration tested and have a strong antimicrobial effect on Gram-positive bacteria (e.g., E. faecalis ATCC 51299 and B. cereus ATCC 13061).

Keywords: Antimicrobial activity; Frog skin peptides; Hemolytic activity; Solid-phase peptide synthesis; Structure–activity relationships.

PubMed Disclaimer

References

    1. Abbassi F, Oury B, Blasco T et al (2008) Isolation, characterization and molecular cloning of new temporins from the skin of the North African ranid Pelophylax saharica. Peptides 29:1526–1533. https://doi.org/10.1016/j.peptides.2008.05.008 - DOI - PubMed
    1. Abbassi F, Piesse C, Foulon T et al (2014) Effects of residue 5-point mutation and N-terminus hydrophobic residues on temporin-SHc physicochemical and biological properties. Mol Cell Biochem 394:91–99. https://doi.org/10.1007/s11010-014-2084-5 - DOI - PubMed
    1. Amiss AS, Henriques ST, Lawrence N (2021) Antimicrobial peptides provide wider coverage for targeting drug-resistant bacterial pathogens. Peptide Sci. https://doi.org/10.1002/pep2.24246 - DOI
    1. Avitabile C, Netti F, Orefice G et al (2013) Design, structural and functional characterization of a Temporin-1b analog active against Gram-negative bacteria. Biochim Biophys Acta Gen Subj 1830:3767–3775. https://doi.org/10.1016/j.bbagen.2013.01.026 - DOI
    1. Barbosa EA, Oliveira A, Plácido A et al (2018) Structure and function of a novel antioxidant peptide from the skin of tropical frogs. Free Radical Biol Med 115:68–79. https://doi.org/10.1016/j.freeradbiomed.2017.11.001 - DOI

LinkOut - more resources