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Novel Antimicrobial Agents

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (20 February 2025) | Viewed by 7883

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Instituto de Investigação do Medicamento (iMed.ULisboa), Faculty of Pharmacy, Lisbon University, 1649-019 Lisbon, Portugal
Interests: the search for new compounds with anti-HIV activity and against respiratory viruses; the development of microbicide candidates to prevent HIV infection
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Dear Colleagues,

The need for novel antimicrobial agents is pressing due to the increasing prevalence of antimicrobial-resistant microorganisms. Antimicrobial resistance (AMR) is a major global health threat that has been exacerbated by the overuse and misuse of antimicrobials. AMR occurs when microorganisms evolve to become resistant to the drugs that are designed to kill them, leading to the development of so-called “superbugs” that are difficult or impossible to treat. These “superbugs” can cause severe infections and are a major concern for public health. To combat the growing problem of AMR, it is crucial to develop new antimicrobial agents that can effectively kill these resistant microorganisms. These novel agents could include new types of antibiotics, as well as antivirals, antifungals, and antiparasitics. In addition to developing these agents, it is also important to ensure that they are used responsibly in order to minimize the development of resistance. Overall, the need for novel antimicrobial agents is crucial for protecting public health and addressing the global threat of AMR. By investing in research and development of these agents, we can help to ensure that we have the tools necessary to effectively treat infectious diseases and keep communities healthy.

Dr. Inês Bártolo
Guest Editor

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Keywords

  • drug resistance
  • antimicrobial resistance (AMR)
  • drug-resistant bacteria
  • drug-resistant viruses
  • drug-resistant fungi
  • drug-resistant parasite
  • drug resistance biomolecular studies
  • mechanism of resistance
  • novel antimicrobial agents
  • treatment of infectious diseases

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Published Papers (5 papers)

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Research

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18 pages, 718 KiB  
Article
Investigation of the Possible Antibacterial Effects of Corticioid Fungi Against Different Bacterial Species
by Eugene Yurchenko, Małgorzata Krasowska, Małgorzata Kowczyk-Sadowy and Ewa Zapora
Int. J. Mol. Sci. 2025, 26(7), 3292; https://doi.org/10.3390/ijms26073292 - 2 Apr 2025
Viewed by 235
Abstract
Extracts from 58 species of corticioid fungi (phylum Basidiomycota), mainly belonging to the orders Hymenochaetales, Polyporales and Russulales, were tested for their inhibitory activity against five species of bacteria: Corynebacterium striatum, Haemophilus influenzae, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus [...] Read more.
Extracts from 58 species of corticioid fungi (phylum Basidiomycota), mainly belonging to the orders Hymenochaetales, Polyporales and Russulales, were tested for their inhibitory activity against five species of bacteria: Corynebacterium striatum, Haemophilus influenzae, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. Twenty-four of the species we analyzed in this study were tested for antibacterial activity for the first time. The fruiting bodies of the fungi were collected from dead wood in the forests of north-eastern Poland, and macerated in methanol. Dried extracts were redissolved in dimethyl sulfoxide and applied to broth cultures of the bacteria, which were then inoculated on agar plates. Noblesia crocea demonstrated moderate inhibitory activity against all five tested bacteria; Amylocorticium subincarnatum, Laxitextum bicolor, Peniophora laeta, P. rufomarginata, Phanerochaete sordida, and Xylobolus frustulatus inhibited four bacterial species. The extracts from 14 fungal species tested were moderately active against only two bacteria, P. aeruginosa and C. striatum; 17 species were active against C. striatum only. The full inhibition was observed with concentrations of extract 25 or 50 mg/mL. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents)
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11 pages, 6941 KiB  
Communication
Copper-Modified Cellulose Paper: A Comparative Study of How Antimicrobial Activity Is Affected by Particle Size and Testing Standards
by Sara Ramírez, Fabian Zúñiga, Alejandra Amenábar, Paulina Contreras, Viviana Benavides, Javiera Norambuena, Jessica Martínez and Nataly Silva
Int. J. Mol. Sci. 2025, 26(2), 480; https://doi.org/10.3390/ijms26020480 - 8 Jan 2025
Viewed by 672
Abstract
This study aims to provide evidence that when testing cellulose paper modified with copper particles (CuPs), the particle size and the analysis method influence the antimicrobial activity observed by this material. Commercial CuPs of nanometric size (2.7 nm, CuNPs) and micrometric size (2.5 [...] Read more.
This study aims to provide evidence that when testing cellulose paper modified with copper particles (CuPs), the particle size and the analysis method influence the antimicrobial activity observed by this material. Commercial CuPs of nanometric size (2.7 nm, CuNPs) and micrometric size (2.5 µm, CuMPs) were used to modify cellulose paper sheets. CuPs were incorporated during the pulp disintegration phase (stage 1) of the sheet formation process, according to the ISO 5269-1:2005 standard. Modified paper sheets retained 16% and 14% of CuNPs and CuMPs, respectively. Additionally, CuPs were distributed randomly on the fiber surfaces, often forming aggregates. Finally, the antimicrobial activity of the modified paper sheets was evaluated using ISO 20645:2004 and ISO 20743:2013. The results showed that the antimicrobial activity assessed using each standard method is conditioned by the mechanism of action of the CuPs and, therefore, by their size. It was concluded that ISO 20645:2004 is suitable for evaluating the antibacterial effect of paper/CuNPs, as nanoparticles diffuse from the paper and are released into the culture medium. In contrast, ISO 20743:2013 can be used for both CuNP- and CuMP-based paper, as it evaluates the antibacterial effect based on the direct interaction between the copper particle and the bacteria. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents)
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19 pages, 1163 KiB  
Article
Interaction between Enrofloxacin and Three Essential Oils (Cinnamon Bark, Clove Bud and Lavender Flower)—A Study on Multidrug-Resistant Escherichia coli Strains Isolated from 1-Day-Old Broiler Chickens
by Sławomir Zych, Michalina Adaszyńska-Skwirzyńska, Małgorzata Anna Szewczuk and Danuta Szczerbińska
Int. J. Mol. Sci. 2024, 25(10), 5220; https://doi.org/10.3390/ijms25105220 - 10 May 2024
Cited by 4 | Viewed by 1729
Abstract
Avian pathogenic Escherichia coli (APEC) causes a variety of infections outside the intestine. The treatment of these infections is becoming increasingly difficult due to the emergence of multi-drug resistant (MDR) strains, which can also be a direct or indirect threat to humans as [...] Read more.
Avian pathogenic Escherichia coli (APEC) causes a variety of infections outside the intestine. The treatment of these infections is becoming increasingly difficult due to the emergence of multi-drug resistant (MDR) strains, which can also be a direct or indirect threat to humans as consumers of poultry products. Therefore, alternative antimicrobial agents are being sought, which could be essential oils, either administered individually or in interaction with antibiotics. Sixteen field isolates of E. coli (originating from 1-day-old broilers) and the ATCC 25922 reference strain were tested. Commercial cinnamon bark, clove bud, lavender flower essential oils (EOs) and enrofloxacin were selected to assess the sensitivity of the selected E. coli strains to antimicrobial agents. The checkerboard method was used to estimate the individual minimum inhibitory concentration (MIC) for each antimicrobial agent as well as to determine the interactions between the selected essential oil and enrofloxacin. In the case of enrofloxacin, ten isolates were resistant at MIC ≥ 2 μg/mL, three were classified as intermediate (0.5–1 μg/mL) and three as sensitive at ≤0.25 μg/mL. Regardless of the sensitivity to enrofloxacin, the MIC for cinnamon EO was 0.25% v/v and for clove EO was 0.125% v/v. All MDR strains had MIC values for lavender EO of 1% v/v, while drug-sensitive isolates had MIC of 0.5% v/v. Synergism between enrofloxacin and EO was noted more frequently in lavender EO (82.35%), followed by cinnamon EO (64.7%), than in clove EO (47.1%). The remaining cases exhibited additive effects. Owing to synergy, the isolates became susceptible to enrofloxacin at an MIC of ≤8 µg/mL. A time–kill study supports these observations. Cinnamon and clove EOs required for up to 1 h and lavender EO for up to 4 h to completely kill a multidrug-resistant strain as well as the ATCC 25922 reference strain of E. coli. Through synergistic or additive effects, blends with a lower than MIC concentration of enrofloxacin mixed with a lower EO content required 6 ± 2 h to achieve a similar effect. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents)
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20 pages, 4084 KiB  
Article
Inhibitors of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase Decrease the Growth, Ergosterol Synthesis and Generation of petite Mutants in Candida glabrata and Candida albicans
by Dulce Andrade-Pavón, Eugenia Sánchez-Sandoval, Joaquín Tamariz, Jose Antonio Ibarra, César Hernández-Rodríguez and Lourdes Villa-Tanaca
Int. J. Mol. Sci. 2023, 24(23), 16868; https://doi.org/10.3390/ijms242316868 - 28 Nov 2023
Cited by 2 | Viewed by 1476
Abstract
Candida glabrata and Candida albicans, the most frequently isolated candidiasis species in the world, have developed mechanisms of resistance to treatment with azoles. Among the clinically used antifungal drugs are statins and other compounds that inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), resulting [...] Read more.
Candida glabrata and Candida albicans, the most frequently isolated candidiasis species in the world, have developed mechanisms of resistance to treatment with azoles. Among the clinically used antifungal drugs are statins and other compounds that inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), resulting in decreased growth and ergosterol levels in yeasts. Ergosterol is a key element for the formation of the yeast cell membrane. However, statins often cause DNA damage to yeast cells, facilitating mutation and drug resistance. The aim of the current contribution was to synthesize seven series of compounds as inhibitors of the HMGR enzyme of Candida ssp., and to evaluate their effect on cellular growth, ergosterol synthesis and generation of petite mutants of C. glabrata and C. albicans. Compared to the reference drugs (fluconazole and simvastatin), some HMGR inhibitors caused lower growth and ergosterol synthesis in the yeast species and generated fewer petite mutants. Moreover, heterologous expression was achieved in Pichia pastoris, and compounds 1a, 1b, 6g and 7a inhibited the activity of recombinant CgHMGR and showed better binding energy values than for α-asarone and simvastatin. Thus, we believe these are good candidates for future antifungal drug development. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents)
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Review

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18 pages, 4831 KiB  
Review
The Potential Role of Nitric Oxide as a Therapeutic Agent against SARS-CoV-2 Infection
by Shuqi Xiao, Zhiming Yuan and Yi Huang
Int. J. Mol. Sci. 2023, 24(24), 17162; https://doi.org/10.3390/ijms242417162 - 5 Dec 2023
Cited by 6 | Viewed by 2355
Abstract
The global coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become the greatest worldwide public health threat of this century, which may predispose multi-organ failure (especially the lung) and death despite numerous mild and moderate [...] Read more.
The global coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become the greatest worldwide public health threat of this century, which may predispose multi-organ failure (especially the lung) and death despite numerous mild and moderate symptoms. Recent studies have unraveled the molecular and clinical characteristics of the infectivity, pathogenicity, and immune evasion of SARS-CoV-2 and thus improved the development of many different therapeutic strategies to combat COVID-19, including treatment and prevention. Previous studies have indicated that nitric oxide (NO) is an antimicrobial and anti-inflammatory molecule with key roles in pulmonary vascular function in the context of viral infections and other pulmonary disease states. This review summarized the recent advances of the pathogenesis of SARS-CoV-2, and accordingly elaborated on the potential application of NO in the management of patients with COVID-19 through antiviral activities and anti-inflammatory properties, which mitigate the propagation of this disease. Although there are some limits of NO in the treatment of COVID-19, it might be a worthy candidate in the multiple stages of COVID-19 prevention or therapy. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents)
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