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Abstract <p><b>Objective:</b> The synthesis and comparative screening of antifungal activity of de novo constructed histidine-containing synthetic antimicrobial peptides (SAMP) H10, H16, F2H16, and H16F2 was carried out in relation to the most common and active species of pathogenic and opportunistic fungi of the genus <i>Candida</i>. <b>Methods:</b> During the experiments, the studied strains were divided into two groups. The minimum inhibitory concentration (MIC) of the peptides was determined against strains of <i>C. albicans</i>, <i>C. glabrata</i>, <i>C. parapsilosis</i>, <i>C. tropicalis</i>, <i>C. auris,</i> and <i>C. lusitaniae</i>. <b>Results and Discussion:</b> The studied strains were stratified into a first, most aggressive group (average MIC &gt; 4 μmol) and a second, less aggressive group (MIC ≤ 4 μmol). Histidine-containing peptides were shown to exhibit selective activity against certain species of fungal cultures, depending on the number of His residues. Peptide H16 (16 His) showed increased activity against aggressive strains like <i>C. parapsilosis</i> (3759), <i>C. parapsilosis</i> (2555), and <i>C. auris</i> (9771) (MIC = 1.6, 3.1, and 3.1 μmol), which is more than 23, 6, and 16 times higher than the activity of the H10 peptide against the same cultures, respectively. Conversely, peptide H10 showed increased activity against highly aggressive strains such as <i>C. glabrata</i> (3097) and <i>C. glabrata</i> (2563) (MIC = 1.6 and 1.6 μmol), which was more than 11 and 7 times higher than the activity of peptide H16 against the same strains, respectively. Peptides H10 and H16, due to their low hydrophobicity, exhibit low hemolytic toxicity, and peptide H10 has practically zero hemolytic toxicity. It is particularly noteworthy that the efficacy of peptide H16 and its antifungal activity against <i>C. auris</i> (MIC = 1.6 μmol) was more than 30 times higher than the control antifungal peptide P113, and even 1.5 times higher than the efficacy of the most active known antifungal agent, Amphotericin B. <b>Conclusions:</b> Peptides H10 and H16, due to their high antifungal properties and low hemolytic toxicity, can be used as promising synthetic antifungal peptide drugs against a wide range of both pathogenic and opportunistic fungal cultures of the genus <i>Candida</i>. Peptide H10 can be successfully used against such an aggressive species as <i>C. glabrata</i>, while the H16 peptide is effective against <i>C. parapsilosis</i> and especially against <i>C. auris</i>. Peptides H10 and H16 can be represented as some of the most promising antifungal peptide drugs not only due to their high antifungal activity, low hemolytic toxicity, and high therapeutic significance, but also in terms of the cost-effectiveness of their synthesis, since they represent a homogeneous sequence consisting of only one histidine amino acid residue.</p>

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Synthetic Antimicrobial Peptides. VI. Antifungal Activity of Histidine-containing Peptides against Various Pathogenic and Opportunistic Species of Candida Fungi

  • 期刊论文

  • 发表日期：

    2026年6月3日

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  • N. V. Amirkhanov,
  • A. V. Bardasheva,
  • N. V. Tikunova,
  • V. N. Silnikov

摘要

Abstract

Objective: The synthesis and comparative screening of antifungal activity of de novo constructed histidine-containing synthetic antimicrobial peptides (SAMP) H10, H16, F2H16, and H16F2 was carried out in relation to the most common and active species of pathogenic and opportunistic fungi of the genus Candida. Methods: During the experiments, the studied strains were divided into two groups. The minimum inhibitory concentration (MIC) of the peptides was determined against strains of C. albicans, C. glabrata, C. parapsilosis, C. tropicalis, C. auris, and C. lusitaniae. Results and Discussion: The studied strains were stratified into a first, most aggressive group (average MIC > 4 μmol) and a second, less aggressive group (MIC ≤ 4 μmol). Histidine-containing peptides were shown to exhibit selective activity against certain species of fungal cultures, depending on the number of His residues. Peptide H16 (16 His) showed increased activity against aggressive strains like C. parapsilosis (3759), C. parapsilosis (2555), and C. auris (9771) (MIC = 1.6, 3.1, and 3.1 μmol), which is more than 23, 6, and 16 times higher than the activity of the H10 peptide against the same cultures, respectively. Conversely, peptide H10 showed increased activity against highly aggressive strains such as C. glabrata (3097) and C. glabrata (2563) (MIC = 1.6 and 1.6 μmol), which was more than 11 and 7 times higher than the activity of peptide H16 against the same strains, respectively. Peptides H10 and H16, due to their low hydrophobicity, exhibit low hemolytic toxicity, and peptide H10 has practically zero hemolytic toxicity. It is particularly noteworthy that the efficacy of peptide H16 and its antifungal activity against C. auris (MIC = 1.6 μmol) was more than 30 times higher than the control antifungal peptide P113, and even 1.5 times higher than the efficacy of the most active known antifungal agent, Amphotericin B. Conclusions: Peptides H10 and H16, due to their high antifungal properties and low hemolytic toxicity, can be used as promising synthetic antifungal peptide drugs against a wide range of both pathogenic and opportunistic fungal cultures of the genus Candida. Peptide H10 can be successfully used against such an aggressive species as C. glabrata, while the H16 peptide is effective against C. parapsilosis and especially against C. auris. Peptides H10 and H16 can be represented as some of the most promising antifungal peptide drugs not only due to their high antifungal activity, low hemolytic toxicity, and high therapeutic significance, but also in terms of the cost-effectiveness of their synthesis, since they represent a homogeneous sequence consisting of only one histidine amino acid residue.