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Antibiotics
Special Issues
New Insights into Antimicrobial Discovery
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New Insights into Antimicrobial Discovery

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

Deadline for manuscript submissions: 30 September 2024 | Viewed by 7806

Special Issue Editors

Dr. Veronica Folliero

E-Mail Website
Guest Editor
Department of Experimental Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy
Interests: peptides; antimicrobials
Special Issues, Collections and Topics in MDPI journals
Dr. Gianluigi Franci

E-Mail Website
Guest Editor
Dipartimento di Medicina, Chirurgia e Odontoiatria “Scuola Medica Salernitana”/DIPMED, Baronissi, Italy
Interests: peptides; microbial membranes; microbial drugs
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibiotics have revolutionized modern medicine, making it possible to treat otherwise deadly bacterial infections. Misuse of antibiotics has allowed the selection of resistant strains that do not respond to conventional treatments. Antibiotic resistance is a leading cause of morbidity and mortality, causing millions of deaths worldwide each year. To this end, the scientific community is conducting continuous research to discover new antibacterial agents with alternative mechanisms of action and pharmacological targets. This Special Issue covers all aspects of antimicrobial discovery, including nanomaterials, natural and synthetic compounds, repurposed drugs, and modifications of existing drugs for the treatment of multidrug-resistant infections. We invite researchers to contribute with original research and review articles.

Dr. Veronica Folliero
Dr. Gianluigi Franci
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 discovery
  • multidrug resistance
  • infectious agents
  • chemotherapy

Published Papers (5 papers)

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Research

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16 pages, 2605 KiB  
Article
Antimicrobial Activity and Molecular Docking Studies of the Biotransformation of Diterpene Acanthoic Acid Using the Fungus Xylaria sp.
by Andrey Moacir do Rosario Marinho, Claudia Maria S. C. de Oliveira, João Victor Silva-Silva, Samara C. Anchieta de Jesus, José Edson S. Siqueira, Luana C. de Oliveira, Jéssica Fernandes Auzier, Liviane N. Soares, Maria Lúcia Belém Pinheiro, Sebastião C. Silva, Lívia S. Medeiros, Emmanoel V. Costa and Patrícia S. Barbosa Marinho
Antibiotics 2023, 12(8), 1331; https://doi.org/10.3390/antibiotics12081331 - 18 Aug 2023
Cited by 1 | Viewed by 1374
Abstract
Biotransformations are reactions mediated by microorganisms, such as fungi. These bioreactions have high chemo- and stereoselectivity on organic substrates and can be applied in the search for new bioactive compounds. In this study, acanthoic acid (AA) was biotransformed using the fungus Xylaria sp., [...] Read more.
Biotransformations are reactions mediated by microorganisms, such as fungi. These bioreactions have high chemo- and stereoselectivity on organic substrates and can be applied in the search for new bioactive compounds. In this study, acanthoic acid (AA) was biotransformed using the fungus Xylaria sp., giving the novel compound 3β,7β-dihydroxyacanthoic acid (S1). Both the AA and the product S1 were tested against Gram-positive and Gram-negative bacteria. To identify and validate possible biological targets as enzymes or proteins involved in the activity observed in vitro, we used the molecular docking method. Hydroxylation at the C-3 and C-7 positions of the biotransformation product enhanced its activity against Escherichia coli as well as its binding affinity and interactions with superoxide dismutase 1 (SOD1; PDB ID 4A7G). Based on our results, the SOD1 enzyme was suggested to be a possible target for the antioxidant activity of product S1. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Discovery)
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21 pages, 3546 KiB  
Article
Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents
by Alexander Zubenko, Victor Kartsev, Anthi Petrou, Athina Geronikaki, Marija Ivanov, Jasmina Glamočlija, Marina Soković, Lyudmila Divaeva, Anatolii Morkovnik and Alexander Klimenko
Antibiotics 2022, 11(11), 1654; https://doi.org/10.3390/antibiotics11111654 - 18 Nov 2022
Cited by 2 | Viewed by 1531
Abstract
In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound [...] Read more.
In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound 2j was found to be the most potent (MIC/MBC at 0.23–0.94 mg/mL and 0.47–1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06–0.47 and 0.11–0.94 mg/mL respectively) with 2d being the most active one. The docking studies revealed that inhibition of E. coli MurB and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Discovery)
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8 pages, 1573 KiB  
Article
Andrographolide and 4-Phenylbutyric Acid Administration Increase the Expression of Antimicrobial Peptides Beta-Defensin-1 and Cathelicidin and Reduce Mortality in Murine Sepsis
by Albert Bolatchiev, Vladimir Baturin and Elizaveta Bolatchieva
Antibiotics 2022, 11(11), 1629; https://doi.org/10.3390/antibiotics11111629 - 15 Nov 2022
Cited by 1 | Viewed by 1349
Abstract
Antibiotic resistance is a global threat and requires the search for new treatment strategies. Natural antimicrobial peptides (AMPs) have pronounced antibacterial, antiviral, antifungal, and antitumor activity. AMPs’ clinical use is complicated by the high synthesis costs and rapid proteolytic degradation. The search for [...] Read more.
Antibiotic resistance is a global threat and requires the search for new treatment strategies. Natural antimicrobial peptides (AMPs) have pronounced antibacterial, antiviral, antifungal, and antitumor activity. AMPs’ clinical use is complicated by the high synthesis costs and rapid proteolytic degradation. The search for small molecules, inducers of endogenous AMP expression, could become a new approach. Here, we investigated for the first time the effect of seven small molecules (andrographolide, levofloxacin, azithromycin, montelukast, 4-phenylbutyric acid, rosuvastatin and valsartan) on AMP (beta-defensin-1, hBD-1 and cathelicidin, LL-37) serum levels in rats. In control groups, the level of hBD-1 was 295.0 (292.9–315.4) pg/mL, and for LL-37, it was 223.8 (213.3–233.6) pg/mL. Andrographolide (ANDR) and 4-phenylbutyric acid (4-PHBA) administration significantly enhanced the level of both AMPs. The hBD-1 level was 581.5 (476.3–607.7) pg/mL for ANDR and 436.9 (399.0–531.6) pg/mL for 4-PHBA. The LL-37 level was 415.4 (376.2–453.8) pg/mL for ANDR and 398.9 (355.7–410.1) pg/mL for 4-PHBA. Moreover, we have shown that these compounds reduce mortality in a murine model of sepsis caused by a carbapenem-resistant Klebsiella aerogenes isolate. From our point of view, these small molecules are promising candidates for further study as potent AMP inducers. The data obtained allow the development of new strategies to combat antibiotic resistance and infectious diseases. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Discovery)
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19 pages, 3979 KiB  
Article
Novel Polyhydroquinoline-Hydrazide-Linked Schiff’s Base Derivatives: Multistep Synthesis, Antimicrobial, and Calcium-Channel-Blocking Activities
by Zainab, Haitao Yu, Najeeb Ur Rehman, Mumtaz Ali, Aftab Alam, Abdul Latif, Nazish Shahab, Irfan Amir Khan, Abdul Jabbar Shah, Momin Khan, Ahmed Al-Ghafri, Ahmed Al-Harrasi and Manzoor Ahmad
Antibiotics 2022, 11(11), 1568; https://doi.org/10.3390/antibiotics11111568 - 07 Nov 2022
Cited by 15 | Viewed by 1340
Abstract
Polyhydroquinoline (PHQ) are the unsymmetrical Hantzsch derivatives of 1,4-dihydropyridines with several biological applications. In this work, twenty-five (3–27) new Schiff’s base derivatives of polyhydroquinoline hydrazide were synthesized in excellent to good yields by a multi-component reaction. The structures of [...] Read more.
Polyhydroquinoline (PHQ) are the unsymmetrical Hantzsch derivatives of 1,4-dihydropyridines with several biological applications. In this work, twenty-five (3–27) new Schiff’s base derivatives of polyhydroquinoline hydrazide were synthesized in excellent to good yields by a multi-component reaction. The structures of the synthesized products (1–27) were deduced with the help of spectroscopic techniques, such as 1H-, 13C -NMR, and HR-ESI-MS. The synthesized products (1–27) were tested for their antibacterial and in vitro calcium -channel-blocking (CCB) potentials using the agar-well diffusion method, and isolated rat aortic ring preparations, respectively. Among the series, sixteen compounds were found to inhibit the growth of Escherichia coli and Enterococcus faecalis. Among them, compound 17 was observed to be the most potent one at a dose 2 µg/mL, with an 18 mm zone of inhibition against both bacteria when it was compared with the standard drug amoxicillin. Eight compounds showed CCB activity of variable potency; in particular, compound 27 was more potent, with an EC50 value of 0.7 (0.3–1.1) µg/mL, indicating their CCB effect. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Discovery)
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Review

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26 pages, 1311 KiB  
Review
Nanoparticles and Their Antibacterial Application in Endodontics
by Nicoletta Capuano, Alessandra Amato, Federica Dell’Annunziata, Francesco Giordano, Veronica Folliero, Federica Di Spirito, Pragati Rajendra More, Anna De Filippis, Stefano Martina, Massimo Amato, Massimiliano Galdiero, Alfredo Iandolo and Gianluigi Franci
Antibiotics 2023, 12(12), 1690; https://doi.org/10.3390/antibiotics12121690 - 01 Dec 2023
Viewed by 1459
Abstract
Root canal treatment represents a significant challenge as current cleaning and disinfection methodologies fail to remove persistent bacterial biofilms within the intricate anatomical structures. Recently, the field of nanotechnology has emerged as a promising frontier with numerous biomedical applications. Among the most notable [...] Read more.
Root canal treatment represents a significant challenge as current cleaning and disinfection methodologies fail to remove persistent bacterial biofilms within the intricate anatomical structures. Recently, the field of nanotechnology has emerged as a promising frontier with numerous biomedical applications. Among the most notable contributions of nanotechnology are nanoparticles, which possess antimicrobial, antifungal, and antiviral properties. Nanoparticles cause the destructuring of bacterial walls, increasing the permeability of the cell membrane, stimulating the generation of reactive oxygen species, and interrupting the replication of deoxyribonucleic acid through the controlled release of ions. Thus, they could revolutionize endodontics, obtaining superior results and guaranteeing a promising short- and long-term prognosis. Therefore, chitosan, silver, graphene, poly(lactic) co-glycolic acid, bioactive glass, mesoporous calcium silicate, hydroxyapatite, zirconia, glucose oxidase magnetic, copper, and zinc oxide nanoparticles in endodontic therapy have been investigated in the present review. The diversified antimicrobial mechanisms of action, the numerous applications, and the high degree of clinical safety could encourage the scientific community to adopt nanoparticles as potential drugs for the treatment of endodontic diseases, overcoming the limitations related to antibiotic resistance and eradication of the biofilm. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Discovery)
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Title: Repurposing the antibacterial activity of chemioterapeutic drug Teniposide against Staphiloccocus epidermidis nosocomial infection
Authors: Veronica Folliero
Affiliation: Department of Experimental Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy
Abstract: Drug repurposing is attracting considerable interest due to reduced costs and development times. The present study reports the antibacterial activity of the antitumor drug teniposide, against Staphylococcus epidermidis (S. epidermidis), the main causative agent of nosocomial and transplant-related infections. The cytotoxicity was evaluated by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay and a hemolysis assay, on immortalized human keratinocyte cells (HaCaT) and human erythrocytes, respectively. After 20 h of drug exposure, the 50% cytotoxic and hemolytic concentrations (CC50 and EC50) were 25.24 and 57.30 μg/mL, respectively. The antibacterial potential was determined via disc diffusion, broth microdilution, LIVE/DEAD, time killing methods, scanning electron microscope (SEM) and fluorescence microscope observations, against S. epidermidis ATCC 12228 and 10 clinical isolates. The drug induced a growth inhibitory area of 22 mm and the 90% Minimum Inhibitory Concentration (MIC90) was 6.25 μg/mL, exhibiting bactericidal action. The treatment resulted in deformities in the cell morphology and revealed damage to the cell membrane, resulting in alterations of the selective permeability of the cell membrane. The drug action on biofilm biomass was investigated using crystal violet (CV) and MTT tests. Teniposide affected biofilm viability in a dose-dependent manner by inducing matrix inhibition of 41% at a concentration of 3.12 μg/mL. Overall, this study could promote the teniposide reuses as a therapeutic agent to counteract S. epidermidis infections.

Title: Magnetic nanoparticles: synthesis, characterization, and antibacterial potential
Authors: Veronica Folliero
Affiliation: Department of Experimental Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy
Abstract: Multidrug-resistant (MDR) bacteria are becoming a serious threat to global health requiring immediate action. The rapid emergence of resistant strains and the limited development of new antibacterial agents limit the therapeutic options available to tackle antibiotic-resistant infections. Therefore, the scientific community conducts ongoing research to identify new antibacterial agents with innovative modes of action and alternative drug targets. In this scenario the antimicrobial properties of different nanomaterials have been studied including those of magnetic nanoparticles (MNPs). MNs are a class of nanoparticles, characterized by a central magnetic core and coating which provides specific properties and functions. These nanostructures have attracted considerable attention due to their simple synthesis, low toxicity, biocompatibility, high functionalization capacity, directed and broad-spectrum antibacterial activity. To deploy the development of NMs with next generation antibacterial potential is essential to know the recent evidence on synthesis, characterization techniques, antibacterial activity, and related mechanisms of action. This review highlights recent progress in synthetic methods, characterization, and antibacterial potentials and antibiofilm on the most bacterial pathogens that arouse greater concern in hospital and community setting.

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