Natural and synthetic peptides with antifungal activity

Ciociola, Tecla; Giovati, Laura; Conti, Stefania; Magliani, Walter; Santinoli, Claudia; Polonelli, Luciano

doi:10.4155/fmc-2016-0035

Cited by 80 publications

(65 citation statements)

References 156 publications

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“…These modifications such as cyclization, backbone modification (eg, β‐peptides) or delivery modes (eg, liposomes, phosphate groups) aim to improve the stability and the half‐life of small peptides. Peptide‐based vaccine strategies against major fungal pathogens and the development of peptibodies are also considered. In this study, similar peptide‐based strategies were used to generate KK14 derivatives with enhanced abilities to inhibit the food contaminants, which are reportedly involved in invasive fungal diseases.…”

Section: Discussionmentioning

confidence: 99%

Antifungal activity of a de novo synthetic peptide and derivatives against fungal food contaminants

Thery

Shwaiki

O’Callaghan

et al. 2018

Journal of Peptide Science

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The development of novel solutions to fight microbial food contaminants rests upon two pillars, which are the development of resistant strains and consumers' desire for a reduced consumption of synthetic drugs. Natural antimicrobial peptides possess the qualities to overcome these issues. De novo synthesis of novel antifungal compounds is a major progress that has been facilitated by the identification of parameters involved in the antimicrobial activity. A 14-residue peptide named KK14, with the sequence KKFFRAWWAPRFLK-NH 2 , was designed and inhibited conidial germination and fungal growth of food contaminants within the range 6.25 to 50 μg/ml and 6.25 to 100 μg/ml, respectively. The study of three analogues of the peptide highlighted the role of some residues in the structural conformation of the peptide and its antifungal activity. The substitution of a Pro residue with Arg increased the helical content of the peptide not only its antifungal activity but also its cytotoxicity.The insertion of an unnatural bulky residue β-diphenylalanine or a full Denantiomerization overall increased the antifungal potency. The four peptides showed similar behaviour towards salt increase, heat treatment, and pH decrease. Interestingly, the Denantiomer remained the most active at high pH and after proteolytic digestion. The four peptides did not present haemolytic activity up to 200 μg/ml but had different behaviours of cytotoxicity. These differences could be crucial for potential application as pharmaceutical or food preservatives.

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Section: Discussionmentioning

confidence: 99%

Antifungal activity of a de novo synthetic peptide and derivatives against fungal food contaminants

Thery

Shwaiki

O’Callaghan

et al. 2018

Journal of Peptide Science

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“…The majority of natural cationic peptides are characterized by low biological activity or by high toxicity, and these peptides require modification in order to achieve high and broad-spectrum activity without toxicity (9). In addition, the potency of synthetic peptides is identical to that of natural peptides, and it is possible to produce large quantities of highly pure AMPs ready to be used in clinical applications (10). A 66-amino acid peptide was designed in the laboratory at the Department of Nanlou Pulmonology & National Clinical Research Center of Geriatrics Disease, Chinese People's Liberation Army General Hospital and derived from LCT-EF128 enterocin (11).…”

Section: Introductionmentioning

confidence: 99%

Effects of the antimicrobial peptide L12 against multidrug‑resistant Staphylococcus aureus

Dai

et al. 2019

Mol Med Report

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Methicillin-resistant Staphylococcus aureus (S. aureus; MRSA) is one of the most common bacterial pathogens and MRSA infections are characterized by high mortality rates. Antimicrobial peptides are considered one of the most promising drugs for the treatment of resistant strains of S. aureus. The present study aimed to examine the antimicrobial activity of L12 against numerous bacterial species using the broth microdilution method. Furthermore, the synergistic effect of L12 combined with various antibacterial drugs was tested, and its antibacterial mechanism was investigated by a checkerboard assay. The alterations in bacterial morphology were detected by electron microscopy, and biofilm formation and removal were tested by crystal violet staining. The present results suggested that L12 affected the growth of gram-positive strains, particularly S. aureus. Electron microscopy analysis suggested that L12 may target the cell membrane, and L12 increased the antibacterial activity of vancomycin and levofloxacin, exerting a synergistic effect. However, the minimal inhibitory concentrations (MICs) of L12 were not correlated with antibiotic resistance, the strains resistant to more antibiotics were not more resistant to L12. A sub-MIC of L12 was able to inhibit biofilm formation in a dose-dependent manner; however, concentrations of L12 ≤10 times the MIC were not sufficient to degrade previously formed biofilm. Collectively, the present study suggested that L12 may represent a novel potential therapeutic molecule for the treatment of S. aureus infections.

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“…Antimicrobial peptides (AMPs) constitute an important part of the innate defense toward pathogens and have been heralded as a new source of antifungal drugs . Several studies have been devoted to establishing the antifungal activities of natural AMPs, and the area was recently reviewed by van der Weerden and co‐workers .…”

Section: Introductionmentioning

confidence: 99%

“…5,6 Antimicrobial peptides (AMPs) constitute an important part of the innate defense toward pathogens 7 and have been heralded as a new source of antifungal drugs. [8][9][10] Several studies have been devoted to establishing the antifungal activities of natural AMPs, and the area was recently reviewed by van der Weerden and co-workers. 11 Lactoferrin/lactoferricin, 12,13 β-defensin 1, 14 the cathelicidins, 15,16 histatin, 17 halictins, 18 arenicin-1, 19 and the magainins 20 are examples of well-studied natural AMPs with powerful antifungal properties.…”

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confidence: 99%

Development and evaluation of cationic amphiphilic antimicrobial 2,5‐diketopiperazines

Labriere

Kondori

Caous

et al. 2018

Journal of Peptide Science

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Both pathogenic bacteria and fungi are developing resistance to common antimicrobial treatment at an alarming rate. To counteract this development, it is of essence to develop new classes of antimicrobial agents. One such class is antimicrobial peptides, most of which are derived from the innate immune system. In this study, a series of novel 2,5‐diketopiperazines were designed, synthesized, and evaluated for their antimicrobial abilities. The compounds were designed to probe the pharmacophore dictated for short linear mimics of antimicrobial cationic peptides, and as such, the compounds contain a range of cationic and hydrophobic functionalities. Several of the prepared compounds displayed high antimicrobial activities toward bacteria and also against human pathogenic fungi. Of particular interest was the high activity toward fungal strains with an inherent increased resistance toward conventional antifungal agents. The most effective compounds displayed inhibition of Candida glabrata and Candida krusei growth at concentrations between 4 and 8 μg/mL, which is comparable to commercial antifungal agents in use. Structure activity relationship studies revealed a similar dependence on cationic charge and the volume of the hydrophobic bulk as for linear cationic antimicrobial peptides. Finally, the hemolytic activity of selected compounds was evaluated, which revealed a potential to produce active compounds with attenuation of unwanted hemolysis. The findings highlight the potential of cyclic cationic amphiphilic peptidomimetics as a class of promising compounds for the treatment of infections caused by microorganisms with an increased resistance to conventional antimicrobial agents.

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Natural and synthetic peptides with antifungal activity

Cited by 80 publications

References 156 publications

Antifungal activity of a de novo synthetic peptide and derivatives against fungal food contaminants

Antifungal activity of a de novo synthetic peptide and derivatives against fungal food contaminants

Effects of the antimicrobial peptide L12 against multidrug‑resistant Staphylococcus aureus

Development and evaluation of cationic amphiphilic antimicrobial 2,5‐diketopiperazines

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