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Antibiotics
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Editorial Board Members’ Collection Series: New Strategies to Overcome Antibiotic...
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Editorial Board Members’ Collection Series: New Strategies to Overcome Antibiotic Resistance

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 31 March 2025 | Viewed by 3888

Special Issue Editors

Dr. Francesca Sisto

E-Mail Website
Guest Editor
Department of Biomedical, Surgical and Dental Sciences, University of Milan, 20133 Milan, Italy
Interests: study of the effects of drugs on the internalization process of Helicobacter pylori; molecular studies of resistance to antimicrobial agents; effect of new molecules against H. pylori in sessile and planktonic form; pathogenicity of H. pylori; antimicrobial susceptibility testing of H. pylori to new synthetized drugs.
Special Issues, Collections and Topics in MDPI journals
Dr. Simone Carradori

E-Mail Website
Guest Editor
Department of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, 66100 Chieti, Italy
Interests: natural compounds; medicinal chemistry; food chemistry; antioxidants; antimicrobials; anti-inflammatory; anticancer; extracion; bioactive compounds; nutrceutical; well-being; food supplement; functional food
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibiotic resistance is becoming a global public health issue due to the increasing morbidity, mortality, and healthcare costs attributed to resistant bacteria, as also reported in a recent publication by the World Health Organization. Non-rational antibiotic use, including overuse, abuse, misuse in terms of dose and duration, and use with the wrong indication, exacerbates the phenomenon. Furthermore, antibiotic resistance does not only concern human health, but it must be seen from a 'one health' perspective. Therefore, many approaches have to be considered. Despite the increasing failure of current antimicrobial therapy, no new antibiotics have been approved. Given that, multi drug-resistant bacteria have also been isolated. The aim of this Special Issue is to collect and analyze in-depth the approaches applied or proposed as alternatives (direct antibacterials or resistance modifiers) to traditional drugs. These strategies include combination therapy with natural and synthetic compounds, agents targeting enzymes or proteins responsible for antibacterial resistance (biofilm, Quorum Sensing, efflux pumps, virulence factors, and the content of bacterial extracellular vesicles), new bacterial targets, resistant bacteria, nanosystems, drug delivery systems, and physico-chemical methods (e.g., photodynamic therapy). Collectively, these strategies may holistically contribute to the treatment of multi-drug-resistant bacteria in clinical settings. Clinical and epidemiological studies, unravelling pharmacological potentials, are also welcome, as well as studies on the role of human gut microbiota modulation to limit or counteract the spread of these infections.

Dr. Francesca Sisto
Dr. Simone Carradori
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antibiotics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • antimicrobial resistance
  • biofilm
  • new targets
  • synthetic drugs
  • natural compounds
  • quorum sensing
  • in vivo models
  • checkerboard assay
  • resistance modifiers
  • probiotics

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Published Papers (3 papers)

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Research

16 pages, 1857 KiB  
Article
Bacteriocin-Producing Staphylococci and Mammaliicocci Strains for Agro-Food and Public Health Applications with Relevance of Micrococcin P1
by Rosa Fernández-Fernández, Carmen Lozano, Allelen Campaña-Burguet, Carmen González-Azcona, Tamara Álvarez-Gómez, Rocío Fernández-Pérez, Raquel Peña, Myriam Zarazaga, Jaime Carrasco and Carmen Torres
Antibiotics 2025, 14(1), 97; https://doi.org/10.3390/antibiotics14010097 - 16 Jan 2025
Viewed by 861
Abstract
Antimicrobial-producing strains and their bacteriocins hold great promise for the control of bacterial diseases, being an attractive alternative to antibiotics. Thus, the aim of this study was to evaluate the inhibitory activity of 15 bacteriocin-producing staphylococci and mammaliicocci (BP-S/M) strains and their pre-purified [...] Read more.
Antimicrobial-producing strains and their bacteriocins hold great promise for the control of bacterial diseases, being an attractive alternative to antibiotics. Thus, the aim of this study was to evaluate the inhibitory activity of 15 bacteriocin-producing staphylococci and mammaliicocci (BP-S/M) strains and their pre-purified extracts with butanol (BT) against a collection of 27 harmful or zoonotic strains (including Gram-positive/-negative bacteria and molds) with relevance in the public health and agro-food fields. These indicators (excluding Gram-negative strains) were grouped into seven categories based on their potential application areas: dairy livestock mastitis, avian pathogen zoonoses, swine zoonoses, food safety, aquaculture, wine making, and mushroom cultivation. In addition, cross-immunity assays between the BP-S/M strains were carried out to identify potential strain combinations to enhance their activity against pathogens. Finally, the hemolytic and gelatinase activities were tested in the BP-S/M strains. A strong inhibitory capacity of the BP-S/M strains was verified against relevant Gram-positive indicators, such as methicillin-resistant Staphylococcus aureus, Listeria monocytogenes, and Clostridium perfringens, among others, while no activity was detected against Gram-negative ones. Interestingly, several BT extracts inhibited the two mold indicators included in this study as representants of mushroom pathogens. The Micrococcin P1 producer Staphylococcus hominis C5835 (>60% of indicators were intensively inhibited by all the methods) can be proposed as a potential candidate for the control of bacterial diseases in the aforementioned categories alone or in combination with other BP-S/M strains (mainly with Staphylococcus warneri X2969). In this regard, five potential combinations of BP-S/M strains that enhanced their activity against specific pathogens were detected. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: New Strategies to Overcome Antibiotic Resistance)
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15 pages, 1743 KiB  
Article
Potent Antimicrobial Azoles: Synthesis, In Vitro and In Silico Study
by Zeynep Özdemir, Yaren Nur Zenni, Arzu Karakurt, Suat Sari, Selma Saraç, Mevlüt Akdağ, İrem Bozbey Merde, Didem Kart, Roberto Venanzoni, Giancarlo Angeles Flores, Paola Angelini, Muzammil Kabier, Bijo Mathew and Simone Carradori
Antibiotics 2024, 13(11), 1044; https://doi.org/10.3390/antibiotics13111044 - 4 Nov 2024
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Abstract
Background/Objectives: The increase in fungal infections, both systemic and invasive, is a major source of morbidity and mortality, particularly among immunocompromised people such as cancer patients and organ transplant recipients. Because of their strong therapeutic activity and excellent safety profiles, azole antifungals [...] Read more.
Background/Objectives: The increase in fungal infections, both systemic and invasive, is a major source of morbidity and mortality, particularly among immunocompromised people such as cancer patients and organ transplant recipients. Because of their strong therapeutic activity and excellent safety profiles, azole antifungals are currently the most extensively used systemic antifungal drugs. Antibacterial properties of various topical antifungals, such as oxiconazole, which features oxime ether functionality, were discovered, indicating an exciting prospect in antimicrobial chemotherapy. Methods: In this study, eleven new oxime ether derivatives with the azole scaffold (5a–k) were synthesized and tested for their antimicrobial effects using the microdilution method to obtain broad-spectrum hits. Results: Although the title compounds showed limited efficacy against Candida species, they proved highly effective against dermatophytes. Compounds 5c and 5h were the most potent derivatives against Trichophyton mentagrophytes and Arthroderma quadrifidum, with minimum inhibitory concentration (MIC) values lower than those of the reference drug, griseofulvin. The MIC of 5c and 5h were 0.491 μg/mL and 0.619 μg/mL against T. mentagrophytes (MIC of griseofulvin: 2.52 μg/mL). The compounds were also tested against Gram-positive and Gram-negative bacteria. Briefly, 5c was the most active against Escherichia coli and Bacillus subtilis, with MIC values much better than that of ciprofloxacin (MIC of 5c = 1.56 μg/mL and 1.23 μg/mL, MIC of ciprofloxacin = 31.49 and 125.99 μg/mL, respectively). Molecular docking suggested a good fit in the active site of fungal lanosterol 14α-demethylase (CYP51) and bacterial FtsZ (Filamenting temperature-sensitive mutant Z) protein. Conclusions: As a result, the title compounds emerged as promising entities with broad antifungal and antibacterial effects, highlighting the utility of oxime ether function in the azole scaffold. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: New Strategies to Overcome Antibiotic Resistance)
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17 pages, 679 KiB  
Article
Imidazoles and Quaternary Ammonium Compounds as Effective Therapies against (Multidrug-Resistant) Bacterial Wound Infections
by Lauren Van de Vliet, Thijs Vackier, Karin Thevissen, David Decoster and Hans P. Steenackers
Antibiotics 2024, 13(10), 949; https://doi.org/10.3390/antibiotics13100949 - 10 Oct 2024
Viewed by 1206
Abstract
Background/Objectives: The rise and spread of antimicrobial resistance complicates the treatment of bacterial wound pathogens, further increasing the need for newer, effective therapies. Azoles such as miconazole have shown promise as antibacterial compounds; however, they are currently only used as antifungals. Previous research [...] Read more.
Background/Objectives: The rise and spread of antimicrobial resistance complicates the treatment of bacterial wound pathogens, further increasing the need for newer, effective therapies. Azoles such as miconazole have shown promise as antibacterial compounds; however, they are currently only used as antifungals. Previous research has shown that combining azoles with quaternary ammonium compounds yields synergistic activity against fungal pathogens, but the effect on bacterial pathogens has not been studied yet. Methods: In this study, the focus was on finding active synergistic combinations of imidazoles and quaternary ammonium compounds against (multidrug-resistant) bacterial pathogens through checkerboard assays. Experimental evolution in liquid culture was used to evaluate the possible emergence of resistance against the most active synergistic combination. Results: Several promising synergistic combinations were identified against an array of Gram-positive pathogens: miconazole/domiphen bromide, ketoconazole/domiphen bromide, clotrimazole/domiphen bromide, fluconazole/domiphen bromide and miconazole/benzalkonium chloride. Especially, miconazole with domiphen bromide exhibits potential, as it has activity at a low concentration against a broad range of pathogens and shows an absence of strong resistance development over 11 cycles of evolution. Conclusions: This study provides valuable insight into the possible combinations of imidazoles and quaternary ammonium compounds that could be repurposed for (topical) wound treatment. Miconazole with domiphen bromide shows the highest application potential as a possible future wound therapy. However, further research is needed into the mode of action of these compounds and their efficacy and toxicity in vivo. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: New Strategies to Overcome Antibiotic Resistance)
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