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Development, Bioactivity, and Application of New Antimicrobial Peptides

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 September 2024) | Viewed by 5686

Special Issue Editor


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Guest Editor
School of Pharmacy, Lanzhou University, Lanzhou 730000, China
Interests: antimicrobial

Special Issue Information

Dear Colleagues,

Antimicrobial peptides, also known as host defense peptides, are small-molecule active peptides that are important components of the natural immunity. They are widely present in biological organisms such as insects, animals, and microorganisms and exhibit strong, rapid, and broad-spectrum antimicrobial activity against a range of pathogens, including Gram-positive and Gram-negative bacteria, viruses, fungi, and parasites. Most antimicrobial peptides have both positive charge and hydrophobicity. They typically utilize electrostatic interactions between positive charge and anionic bacterial cell membranes to attract each other and use hydrophobicity to insert into the interior of bacterial cell membranes, disrupting their integrity and exerting antibacterial effects. Compared to antibiotics that act on a single and specific molecular target, antimicrobial peptides have multiple mechanisms of action, including membrane action, which can effectively combat drug-resistant bacteria without obvious resistance. In addition, the surface of bacterial cell membranes contains a large number of substances such as phospholipids and lipopolysaccharides, which are negatively charged, while mammalian cell membranes contain a large number of cholesterols and sphingolipids, which are electrically neutral. Therefore, the cationic antimicrobial peptides are more inclined to interact with bacteria. In addition, antimicrobial peptides have conformational characteristics and are prone to undergo conformational changes on bacterial cell membranes, but they are less likely to undergo conformational changes on host cell membranes, and thus, they are less likely to be toxic to host cells. Thus, antimicrobial peptides have laid a solid foundation for the development of new generation antimicrobial drugs.

Dr. Chao Zhong
Guest Editor

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Keywords

  • antimicrobial peptides
  • antimicrobial activity
  • bacterial resistance
  • antimicrobial drugs
  • bioactivity

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Published Papers (3 papers)

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Research

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29 pages, 3776 KiB  
Article
Antibacterial Properties of Peptide and Protein Fractions from Cornu aspersum Mucus
by Lyudmila Velkova, Aleksandar Dolashki, Ventsislava Petrova, Emiliya Pisareva, Dimitar Kaynarov, Momchil Kermedchiev, Maria Todorova and Pavlina Dolashka
Molecules 2024, 29(12), 2886; https://doi.org/10.3390/molecules29122886 - 18 Jun 2024
Cited by 2 | Viewed by 1734
Abstract
The discovery and investigation of new natural compounds with antimicrobial activity are new potential strategies to reduce the spread of antimicrobial resistance. The presented study reveals, for the first time, the promising antibacterial potential of two fractions from Cornu aspersum mucus with an [...] Read more.
The discovery and investigation of new natural compounds with antimicrobial activity are new potential strategies to reduce the spread of antimicrobial resistance. The presented study reveals, for the first time, the promising antibacterial potential of two fractions from Cornu aspersum mucus with an MW < 20 kDa and an MW > 20 kDa against five bacterial pathogens—Bacillus cereus 1085, Propionibacterium acnes 1897, Salmonella enterica 8691, Enterococcus faecalis 3915, and Enterococcus faecium 8754. Using de novo sequencing, 16 novel peptides with potential antibacterial activity were identified in a fraction with an MW < 20 kDa. Some bioactive compounds in a mucus fraction with an MW > 20 kDa were determined via a proteomic analysis on 12% sodium dodecyl sulfate–polyacrylamide gel electrophoresis (SDS–PAGE) and bioinformatics. High homology with proteins and glycoproteins was found, with potential antibacterial activity in mucus proteins named aspernin, hemocyanins, H-lectins, and L-amino acid oxidase-like protein, as well as mucins (mucin-5AC, mucin-5B, mucin-2, and mucin-17). We hypothesize that the synergy between the bioactive components determined in the composition of the fraction > 20 kDa are responsible for the high antibacterial activity against the tested pathogens in concentrations between 32 and 128 µg/mL, which is comparable to vancomycin, but without cytotoxic effects on model eukaryotic cells of Saccharomyces cerevisiae. Additionally, a positive effect, by reducing the levels of intracellular oxidative damage and increasing antioxidant capacity, on S. cerevisiae cells was found for both mucus extract fractions of C. aspersum. These findings may serve as a basis for further studies to develop a new antibacterial agent preventing the development of antibiotic resistance. Full article
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Review

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18 pages, 1027 KiB  
Review
Antimicrobial Potential of Scorpion-Venom-Derived Peptides
by Zhiqiang Xia, Lixia Xie, Bing Li, Xiangyun Lv, Hongzhou Zhang and Zhijian Cao
Molecules 2024, 29(21), 5080; https://doi.org/10.3390/molecules29215080 - 27 Oct 2024
Viewed by 1811
Abstract
The frequent and irrational use of antibiotics by humans has led to the escalating rise of antimicrobial resistance (AMR) with a high rate of morbidity-mortality worldwide, which poses a challenge to the development of effective treatments. A large number of host defense peptides [...] Read more.
The frequent and irrational use of antibiotics by humans has led to the escalating rise of antimicrobial resistance (AMR) with a high rate of morbidity-mortality worldwide, which poses a challenge to the development of effective treatments. A large number of host defense peptides from different organisms have gained interest due to their broad antibacterial spectrum, rapid action, and low target resistance, implying that these natural sources might be a new alternative to antimicrobial drugs. As important effectors of prey capture, defense against other animal attacks, and competitor deterrence, scorpion venoms have been developed as important candidate sources for modern drug development. With the rapid progress of bioanalytical and high throughput sequencing techniques, more and more scorpion-venom-derived peptides, including disulfide-bridged peptides (DBPs) and non-disulfide-bridged peptides (NDBPs), have been recently identified as having massive pharmacological activities in channelopathies, pathogen infections, and cancer treatments. In this review, we summarize the molecular diversity and corresponding structural classification of scorpion venom peptides with antibacterial, antifungal, and/or antiparasitic activity. We also aim to improve the understanding of the underlying mechanisms by which scorpion-venom-derived peptides exert these antimicrobial functions, and finally highlight their key aspects and prospects for antimicrobial therapeutic or pharmaceutical application. Full article
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18 pages, 1603 KiB  
Review
Colistin: Lights and Shadows of an Older Antibiotic
by Erica Diani, Gabriele Bianco, Milo Gatti, Davide Gibellini and Paolo Gaibani
Molecules 2024, 29(13), 2969; https://doi.org/10.3390/molecules29132969 - 21 Jun 2024
Cited by 2 | Viewed by 1776
Abstract
The emergence of antimicrobial resistance represents a serious threat to public health and for infections due to multidrug-resistant (MDR) microorganisms, representing one of the most important causes of death worldwide. The renewal of old antimicrobials, such as colistin, has been proposed as a [...] Read more.
The emergence of antimicrobial resistance represents a serious threat to public health and for infections due to multidrug-resistant (MDR) microorganisms, representing one of the most important causes of death worldwide. The renewal of old antimicrobials, such as colistin, has been proposed as a valuable therapeutic alternative to the emergence of the MDR microorganisms. Although colistin is well known to present several adverse toxic effects, its usage in clinical practice has been reconsidered due to its broad spectrum of activity against Gram-negative (GN) bacteria and its important role of “last resort” agent against MDR-GN. Despite the revolutionary perspective of treatment with this old antimicrobial molecule, many questions remain open regarding the emergence of novel phenotypic traits of resistance and the optimal usage of the colistin in clinical practice. In last years, several forward steps have been made in the understanding of the resistance determinants, clinical usage, and pharmacological dosage of this molecule; however, different points regarding the role of colistin in clinical practice and the optimal pharmacokinetic/pharmacodynamic targets are not yet well defined. In this review, we summarize the mode of action, the emerging resistance determinants, and its optimal administration in the treatment of infections that are difficult to treat due to MDR Gram-negative bacteria. Full article
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