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Antibiotics
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Novel Approaches to Enhance the Discovery and Efficacy of Antibiotics...
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Novel Approaches to Enhance the Discovery and Efficacy of Antibiotics and Antifungals

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (28 February 2022) | Viewed by 6922

Special Issue Editor

Dr. Sumant Puri

E-Mail Website
Guest Editor
Oral Microbiome Research Laboratory, Department of Oral Health Sciences, Kornberg School of Dentistry, Temple University, Philadelphia, PA, USA
Interests: oropharyngeal candidiasis; iron; mucosal immunity; neutrophils; mycobiome; bacteria-fungi cross-kingdom interaction

Special Issue Information

Dear Colleagues,

Antimicrobial resistance (AMR) among bacterial and fungal pathogens presents an uphill battle for clinicians treating infectious diseases. WHO has declared AMR a serious global health threat and has recently underscored that the existing pipeline of antibiotics falls short in addressing AMR. Multidrug-resistant bacteria, especially among the Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp. (ESKAPE) group, as well as the recently discovered fungal species of Candida (Candida auris) that is resistant to most known antifungals, particularly highlight this problem. Thus, novel approaches to address AMR are warranted. This Special Issue welcomes all submissions related to unique strategies to counteract AMR, with a special focus on the following areas:

  • Discovery and identification of novel antimicrobials or applications of antimicrobial peptides or naturally-derived bioactives;
  • Fresh high throughput screens of existing drug and compound libraries to identify novel antimicrobial uses for existing molecules;
  • Modulation of host factors (such as iron levels) that can alter antimicrobial sensitivities to existing antimicrobials during infection;
  • Identifying and repurposing existing FDA-approved drugs with antimicrobial potential;
  • Synergistic approaches between different antimicrobials or non-antimicrobial drugs that can enhance the microbicidal potential of existing antibiotics and antifungals;
  • Use of novel, cost- and time-efficient infection models such as Galleria mellonella, Drosophila melanogaster, and Caenorhabditis elegans for screening antimicrobials against pathogens

Dr. Sumant Puri
Guest Editor

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 peptides
  • naturally-derived bioactives
  • antimicrobial drug-screening
  • host factors in antimicrobial resistance
  • drug-repurposing
  • synergy
  • infection models for antimicrobial screening

Published Papers (3 papers)

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Research

20 pages, 38372 KiB  
Article
The Synthesis of Triazolium Salts as Antifungal Agents: A Biological and In Silico Evaluation
by Serghei Pogrebnoi, Oleg Radul, Eugenia Stingaci, Lucian Lupascu, Vladimir Valica, Livia Uncu, Anastasia Smetanscaia, Anthi Petrou, Ana Ćirić, Jasmina Glamočlija, Marina Soković, Athina Geronikaki and Fliur Z. Macaev
Antibiotics 2022, 11(5), 588; https://doi.org/10.3390/antibiotics11050588 - 27 Apr 2022
Cited by 2 | Viewed by 1694
Abstract
The control of fungal pathogens is increasingly difficult due to the limited number of effective drugs available for antifungal therapy. In addition, both humans and fungi are eukaryotic organisms; antifungal drugs may have significant toxicity due to the inhibition of related human targets. [...] Read more.
The control of fungal pathogens is increasingly difficult due to the limited number of effective drugs available for antifungal therapy. In addition, both humans and fungi are eukaryotic organisms; antifungal drugs may have significant toxicity due to the inhibition of related human targets. Furthermore, another problem is increased incidents of fungal resistance to azoles, such as fluconazole, ketoconazole, voriconazole, etc. Thus, the interest in developing new azoles with an extended spectrum of activity still attracts the interest of the scientific community. Herein, we report the synthesis of a series of triazolium salts, an evaluation of their antifungal activity, and docking studies. Ketoconazole and bifonazole were used as reference drugs. All compounds showed good antifungal activity with MIC/MFC in the range of 0.0003 to 0.2/0.0006–0.4 mg/mL. Compound 19 exhibited the best activity among all tested with MIC/MFC in the range of 0.009 to 0.037 mg/mL and 0.0125–0.05 mg/mL, respectively. All compounds appeared to be more potent than both reference drugs. The docking studies are in accordance with experimental results. Full article
(This article belongs to the Special Issue Novel Approaches to Enhance the Discovery and Efficacy of Antibiotics and Antifungals)
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12 pages, 787 KiB  
Article
Synthesis, Characterization and Biological Evaluation of Novel Benzamidine Derivatives: Newer Antibiotics for Periodontitis Treatment
by Mohammad Auwal Sa’ad, Ramasamy Kavitha, Shivkanya Fuloria, Neeraj Kumar Fuloria, Manickam Ravichandran and Pattabhiraman Lalitha
Antibiotics 2022, 11(2), 207; https://doi.org/10.3390/antibiotics11020207 - 07 Feb 2022
Cited by 11 | Viewed by 2153
Abstract
Periodontal disease (PD) is complex polymicrobial disease which destroys tooth-supporting tissue. Although various synthetic inhibitors of periodontitis-triggering pathogens have been recognized, their undesirable side effects limit their application. Hence, the present study intended to perform the synthesis, characterization, antimicrobial evaluation, and cytotoxicity analysis [...] Read more.
Periodontal disease (PD) is complex polymicrobial disease which destroys tooth-supporting tissue. Although various synthetic inhibitors of periodontitis-triggering pathogens have been recognized, their undesirable side effects limit their application. Hence, the present study intended to perform the synthesis, characterization, antimicrobial evaluation, and cytotoxicity analysis of novel benzamidine analogues (NBA). This study involved the synthesis of novel imino bases of benzamidine (4a–c), by reacting different aromatic aldehydes with 2-(4-carbamimidoylphenoxy) acetohydrazide (3), which was synthesized by the hydrazination of ethyl 2-(4-carbamimidoylphenoxy) acetate (2), the derivative of 4-hydroxybenzene carboximidamide (1). This was followed by characterization using FTIR, 1H, 13C NMR and mass spectrometry. All synthesized compounds were further tested for antimicrobial potential against PD-triggering pathogens by the micro broth dilution method. The cytotoxicity analysis of the NBA against HEK 293 cells was conducted using an MTT assay. The present study resulted in a successful synthesis of NBA and elucidated their structures. The synthesized NBA exhibited significant antimicrobial activity values between 31.25 and 125 µg/mL against tested pathogens. All NBA exhibited weak cytotoxicity against HEK 293 cells at 7.81 µg, equally to chlorhexidine at 0.2%. The significant antimicrobial activity of NBA against PD-triggering pathogens supports their potential application in periodontitis treatment. Full article
(This article belongs to the Special Issue Novel Approaches to Enhance the Discovery and Efficacy of Antibiotics and Antifungals)
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13 pages, 3679 KiB  
Article
Antifungal Mechanism of Vip3Aa, a Vegetative Insecticidal Protein, against Pathogenic Fungal Strains
by Seong-Cheol Park, Jin-Young Kim, Jong-Kook Lee, Hye Song Lim, Hyosuk Son, Su-Hyang Yoo, Seong-Eun Mun, Mi-Kyeong Jang and Jung Ro Lee
Antibiotics 2021, 10(12), 1558; https://doi.org/10.3390/antibiotics10121558 - 20 Dec 2021
Cited by 1 | Viewed by 2316
Abstract
Discovering new antifungal agents is difficult, since, unlike bacteria, mammalian and fungal cells are both eukaryotes. An efficient strategy is to consider new antimicrobial proteins that have variety of action mechanisms. In this study, a cDNA encoding Bacillus thuringiensis Vip3Aa protein, a vegetative [...] Read more.
Discovering new antifungal agents is difficult, since, unlike bacteria, mammalian and fungal cells are both eukaryotes. An efficient strategy is to consider new antimicrobial proteins that have variety of action mechanisms. In this study, a cDNA encoding Bacillus thuringiensis Vip3Aa protein, a vegetative insecticidal protein, was obtained at the vegetative growth stage; its antifungal activity and mechanism were evaluated using a bacterially expressed recombinant Vip3Aa protein. The Vip3Aa protein demonstrated various concentration- and time-dependent antifungal activities, with inhibitory concentrations against yeast and filamentous fungi ranging from 62.5 to 125 µg/mL and 250 to 500 µg/mL, respectively. The uptake of propidium iodide and cellular distributions of rhodamine-labeled Vip3Aa into fungal cells indicate that its growth inhibition mechanism involves its penetration within cells and subsequent intracellular damage. Furthermore, we discovered that the death of Candida albicans cells was caused by the induction of apoptosis via the generation of mitochondrial reactive oxygen species and binding to nucleic acids. The presence of significantly enlarged Vip3Aa-treated fungal cells indicates that this protein causes intracellular damage. Our findings suggest that Vip3Aa protein has potential applications in the development of natural antimicrobial agents. Full article
(This article belongs to the Special Issue Novel Approaches to Enhance the Discovery and Efficacy of Antibiotics and Antifungals)
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