Synthetic Antimicrobial Peptides. II. Antimicrobial and Hemolytic Activity of Cationic Peptides Containing Cysteine Residues with Free Sulfhydryl Groups
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The antimicrobial and hemolytic activities of R9F2С2 (P1ss), (KFF)3KС2 (P2ss), and (RAhaR)4AhaβAС2 (P3ss) (where Aha is 6-aminohexanoic acid and βA is beta-alanine) synthetic antimicrobial peptides (SAMP) with different amphipathic properties and containing the cysteine residues with free sulfhydryl groups were studied. The introduction of cysteine residues into the composition of SAMP was shown to increase their antimicrobial activity 3–7 times, while their hemolytic activity increased 2–12 times in relation to human erythrocytes for different peptides in different ways, which determined their different selectivity. The P1ss peptide with a linear type of amphipathicity showed the highest antimicrobial activity and high selectivity against the fungus Candida albicans and bacterium Staphylococcus aureus (MIC 0.5 μM; TI 52 μM). The P1ss peptide possessed not only greater antimicrobial activity against pathogenic fungus C. albicans in comparison to the P2ss peptide (MIC 3.9 μM) with the classical helical amphipathicity, but also more than three times lower hemolytic activity (MHC 26 and 8 μM, respectively). Therefore, TI for the P2ss peptide (TI 2.1) turned out to be more than 20 times lower than that for the P1ss peptide. Thus, the P1ss peptide is the most promising antimicrobial preparation among the studied SAMP.
Keywords:synthetic antimicrobial peptides amphiphilicity amphipathicity sulfhydryl group hemolytic activity selectivity Candida albicans Staphylococcus aureus
Microbial strains were obtained from the Collection of Extremophilic Microorganisms and Type Cultures.
This study was supported by the Program of Basic Scientific Research of State Academies of Sciences for years 2017–2020 (project nos. VI.62.1.4, 0309-2016-0004 and VI.55.1.1, 0309-2016-0002).
COMPLIANCE WITH ETHICAL STANDARDS
The work has no studies involving humans or animals as subjects of the study.
Conflict of Interests
Authors declare that they have no conflicts of interests.
Statement of Compliance with Standards of Research Involving Humans as Subjects
All procedures performed in studies involving human participants (during blood sampling to test the hemolytic activity of preparations) were in accordance with the ethical standards of the institutional and/or national research committee and with the 1964 Helsinki Declaration and its later amendments or comparable ethical standards. Informed consent was obtained from all individual participants involved in the study.
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