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Antibiotics
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Drug Repositioning in Antimicrobial Therapy
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Drug Repositioning in Antimicrobial Therapy

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

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 25121

Special Issue Editor

Prof. Dr. Alessia Carocci

E-Mail Website
Guest Editor
Department of Pharmacy-Drug Science, University of Bari Aldo Moro, Bari, Italy
Interests: biological active compounds; antimicrobials; antiarrhythmics; anticancers; melatonergic drugs; voltage-gated sodium channel blockers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Finding new uses for existing drugs is the goal of a novel drug discovery strategy called drug repositioning, that has increased exponentially in the past decade.

The repurposing of drugs has been successfully applied in several therapeutic strategies to treat human diseases such as cancer, neurodegenerative disorders, neglected tropical diseases, and infections caused by resistant bacteria, to mention a few. This method has proved to be a valid option for the rapid discovery of drugs, since it is relatively cheap and presents minimum risks to patients due to the availability of pharmacological, safety, and toxicological data. It is now considered an interesting approach to overcome the drawbacks of conventional antibiotics. The global situation of antibiotic resistance and the reduction of investments in antibiotics research by the pharmaceutical industry underscore the need for specific cost-effective approaches in order to identify drugs for the treatment of many microbial infections. In this regard, drug repurposing has produced some encouraging results. Furthermore, combinations of drugs have been successfully used to treat multi-drug resistant bacteria thanks to their synergistic effect. Thus, the combination of repositioned drugs with natural compounds or essential oils is also an interesting approach for the rapid identification of new therapies to treat acute infections.

Prof. Alessia Carocci
Guest Editor

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Keywords

  • Drug repositioning
  • anti-infective agents
  • bacterial resistance
  • essential oils
  • chemotherapy

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Published Papers (7 papers)

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Research

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31 pages, 3229 KiB  
Article
Cheminformatics Bioprospection of Sunflower Seeds’ Oils against Quorum Sensing System of Pseudomonas aeruginosa
by Nosipho Wendy S’thebe, Jamiu Olaseni Aribisala and Saheed Sabiu
Antibiotics 2023, 12(3), 504; https://doi.org/10.3390/antibiotics12030504 - 2 Mar 2023
Cited by 7 | Viewed by 2493
Abstract
Clinically significant pathogens such as Pseudomonas aeruginosa evade the effects of antibiotics using quorum sensing (QS) systems, making antimicrobial resistance (AMR) a persistent and potentially fatal global health issue. Hence, QS has been identified as a novel therapeutic target for identifying novel drug [...] Read more.
Clinically significant pathogens such as Pseudomonas aeruginosa evade the effects of antibiotics using quorum sensing (QS) systems, making antimicrobial resistance (AMR) a persistent and potentially fatal global health issue. Hence, QS has been identified as a novel therapeutic target for identifying novel drug candidates against P. aeruginosa, and plant-derived products, including essential oils, have been demonstrated as effective QS modulators. This study assessed the antipathogenic efficacy of essential oils from two sunflower cultivars (AGSUN 5102 CLP and AGSUN 5106 CLP) against P. aeruginosa ATCC 27853 in vitro and in silico. At the sub-inhibitory concentrations, both AGSUN 5102 CLP (62.61%) and AGSUN 5106 CLP (59.23%) competed favorably with cinnamaldehyde (60.74%) and azithromycin (65.15%) in suppressing the expression of QS-controlled virulence phenotypes and biofilm formation in P. aeruginosa. A further probe into the mechanism of anti-QS action of the oils over a 100-ns simulation period against Las QS system revealed that phylloquinone (−66.42 ± 4.63 kcal/mol), linoleic acid (−53.14 ± 3.53 kcal/mol), and oleic acid (−52.02 ± 3.91 kcal/mol) had the best affinity and structural compactness as potential modulators of LasR compared to cinnamaldehyde (−16.95 ± 1.75 kcal/mol) and azithromycin (−32.08 ± 10.54 kcal/mol). These results suggest that the identified compounds, especially phylloquinone, could be a possible LasR modulator and may represent a novel therapeutic alternative against infections caused by P. aeruginosa. As a result, phylloquinone could be further studied as a QS modulator and perhaps find utility in developing new therapeutics. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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17 pages, 2118 KiB  
Article
The Assessment of Antimicrobial and Anti-Biofilm Activity of Essential Oils against Staphylococcus aureus Strains
by Caglar Ersanli, Athina Tzora, Ioannis Skoufos, Konstantina Fotou, Eleni Maloupa, Katerina Grigoriadou, Chrysoula (Chrysa) Voidarou and Dimitrios I. Zeugolis
Antibiotics 2023, 12(2), 384; https://doi.org/10.3390/antibiotics12020384 - 13 Feb 2023
Cited by 15 | Viewed by 3503
Abstract
The increase in antimicrobial resistance and tolerance over the years has become a serious public health problem, leading to the inevitable development of alternative antimicrobial agents as substitutes for industrial pharmaceutical antibiotics targeting humans and animals under the concept of one health. Essential [...] Read more.
The increase in antimicrobial resistance and tolerance over the years has become a serious public health problem, leading to the inevitable development of alternative antimicrobial agents as substitutes for industrial pharmaceutical antibiotics targeting humans and animals under the concept of one health. Essential oils (EOs) extracted from aromatic and pharmaceutical plants incorporate several bioactive compounds (phytochemicals) that positively affect human and animal health. Herein, this work aimed to examine a standardized chemical composition and screen the antimicrobial and anti-biofilm activity of Thymus sibthorpii, Origanum vulgare, Salvia fruticosa, and Crithmum maritimum EOs against three different Staphylococcus aureus strains by gold-standard disc diffusion, broth microdilution, and microtiter plate biofilm assays. Therefore, the evaluation of the above-mentioned EOs were considered as substitutes for antibiotics to combat the ever-mounting antimicrobial resistance problem. The observed bacterial growth inhibition varied significantly depending on the type and concentration of the antimicrobials. Thymus sibthorpii was determined as the strongest antimicrobial, with 0.091 mg/mL minimum inhibitory concentration (MIC) and a 14–33 mm diameter inhibition zone at 5% (v/v) concentration. All tested EOs indicated almost 95% inhibition of biofilm formation at their half MIC, while gentamicin sulfate did not show sufficient anti-biofilm activity. None of the methicillin-resistant strains showed resistance to the EOs compared to methicillin-sensitive strains. Thymus sibthorpii and Origanum vulgare could be potential alternatives as antimicrobial agents to overcome the problem of microbial resistance. The tested EOs might be incorporated into antimicrobial products as safe and potent antimicrobial and anti-biofilm agents. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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12 pages, 1724 KiB  
Article
Synergistic Action of Cinnamomum verum Essential Oil with Sertraline
by Alexia Barbarossa, Sabina Sblano, Antonio Rosato, Antonio Carrieri, Filomena Corbo, Maria Lisa Clodoveo, Giuseppe Fracchiolla and Alessia Carocci
Antibiotics 2022, 11(11), 1617; https://doi.org/10.3390/antibiotics11111617 - 13 Nov 2022
Cited by 8 | Viewed by 2410
Abstract
Cinnamomum verum L. essential oil (CEO), commonly known as Ceylon cinnamon or cinnamon tree, is regarded as one of the most employed essential oils in the field of aromatherapy. It is usually applied externally as astringent, antipruritic, rubefacient, and anti-septic agent. Furthermore, both [...] Read more.
Cinnamomum verum L. essential oil (CEO), commonly known as Ceylon cinnamon or cinnamon tree, is regarded as one of the most employed essential oils in the field of aromatherapy. It is usually applied externally as astringent, antipruritic, rubefacient, and anti-septic agent. Furthermore, both in vitro and in vivo research have demonstrated its numerous pharmacological effects, including the potentiality for treating neuralgia, myalgia, headache, and migraine. Several pieces of research also corroborated its significant antiviral and antimicrobial properties. Cinnamaldehyde, eugenol, caryophyllene, cinnamyl acetate, and cinnamic acid are the most representative compounds that are generally found in greater quantities in CEO and play a pivotal role in determining its pharmacological activities. Due to the global antibiotic resistance scenario and the dwindling amount of funding dedicated to developing new antibiotics, in recent years research has concentrated on exploring specific economic approaches against microbial infections. In this context, the purpose of this study was the investigation of the synergistic antibacterial activities of commercially available and chemically characterized CEO in combination with sertraline, a selective serotonin reuptake inhibitor (SSRI), whose repositioning as a non-antibiotic drug has been explored over the years with encouraging results. In vitro effects of the titled combination were assessed toward a wide panel of both Gram-positive and Gram-negative bacteria. The antimicrobial efficacy was investigated by using the checkerboard microdilution method. The interesting preliminary results obtained suggested a synergistic effect (fractional inhibitory index, FICI < 0.5) of sertraline in combination with CEO, leading to severe growth inhibition for all bacterial species under investigation. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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9 pages, 2696 KiB  
Article
In Vitro Antimicrobial Effectiveness Tests Using Garlic (Allium sativum) against Salmonella enterica Subspecies enterica Serovar Enteritidis
by Elena Circella, Gaia Casalino, Francesco D’Amico, Nicola Pugliese, Michela Maria Dimuccio, Antonio Camarda and Giancarlo Bozzo
Antibiotics 2022, 11(11), 1481; https://doi.org/10.3390/antibiotics11111481 - 26 Oct 2022
Cited by 5 | Viewed by 3464
Abstract
In recent years, there has been a more prudent use of drugs on livestock farms and alternative products have been considered, with a view of reducing the risk of the onset of antibiotic resistance. Salmonella enterica subsp. enterica serovar Enteritidis (S. Enteritidis) [...] Read more.
In recent years, there has been a more prudent use of drugs on livestock farms and alternative products have been considered, with a view of reducing the risk of the onset of antibiotic resistance. Salmonella enterica subsp. enterica serovar Enteritidis (S. Enteritidis) may cause disease in poultry, and it is also responsible for human food poisoning. The aim of this study was to evaluate the efficacy of garlic against S. Enteritidis and to define its Minimal Inhibitory Concentration (MIC)90 and MIC50 values. The study was carried out in vitro, testing 26 S. Enteritidis strains identified in laying hens from various farms in Southern Italy. A preliminary efficacy trial was carried out on two strains, S. Enteritidis and Escherichia coli, using a garlic concentration of 10 mg/mL (1%). Later, 26 strains of S. Enteritidis at 106 Colony Forming Unit (CFU) and 104 CFU were tested with different concentrations of garlic, ranging from 10 mg/mL to 1 mg/mL. Based on the results, intermediate concentrations of garlic, from 5 mg/mL to 4 mg/mL and 4 mg/mL to 3 mg/mL, were used to test 106 CFU and 104 CFU, respectively. The data were statistically analyzed. The MIC90 was 4.75 mg/mL for strains tested at 106 CFU and 4 mg/mL for strains tested at 104 CFU. The results highlight garlic’s potential to inhibit the growth of Salmonella enterica ser. Enteritidis in vitro. Efficacy was dependent on the microbial concentration used. In vivo efficacy trials will be crucial to confirm the efficacy of garlic against S. Enteritidis and to assess whether garlic can be used in poultry flocks to prevent the spread of the bacterium in the field. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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19 pages, 1461 KiB  
Article
Computational Drug Repurposing for Antituberculosis Therapy: Discovery of Multi-Strain Inhibitors
by Valeria V. Kleandrova, Marcus T. Scotti and Alejandro Speck-Planche
Antibiotics 2021, 10(8), 1005; https://doi.org/10.3390/antibiotics10081005 - 19 Aug 2021
Cited by 16 | Viewed by 3113
Abstract
Tuberculosis remains the most afflicting infectious disease known by humankind, with one quarter of the population estimated to have it in the latent state. Discovering antituberculosis drugs is a challenging, complex, expensive, and time-consuming task. To overcome the substantial costs and accelerate drug [...] Read more.
Tuberculosis remains the most afflicting infectious disease known by humankind, with one quarter of the population estimated to have it in the latent state. Discovering antituberculosis drugs is a challenging, complex, expensive, and time-consuming task. To overcome the substantial costs and accelerate drug discovery and development, drug repurposing has emerged as an attractive alternative to find new applications for “old” drugs and where computational approaches play an essential role by filtering the chemical space. This work reports the first multi-condition model based on quantitative structure–activity relationships and an ensemble of neural networks (mtc-QSAR-EL) for the virtual screening of potential antituberculosis agents able to act as multi-strain inhibitors. The mtc-QSAR-EL model exhibited an accuracy higher than 85%. A physicochemical and fragment-based structural interpretation of this model was provided, and a large dataset of agency-regulated chemicals was virtually screened, with the mtc-QSAR-EL model identifying already proven antituberculosis drugs while proposing chemicals with great potential to be experimentally repurposed as antituberculosis (multi-strain inhibitors) agents. Some of the most promising molecules identified by the mtc-QSAR-EL model as antituberculosis agents were also confirmed by another computational approach, supporting the capabilities of the mtc-QSAR-EL model as an efficient tool for computational drug repurposing. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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10 pages, 270 KiB  
Article
Synergistic Activity of New Diclofenac and Essential Oils Combinations against Different Candida spp.
by Antonio Rosato, Elisabetta Altini, Sabina Sblano, Lara Salvagno, Filippo Maggi, Giuliana de Michele, Alessia Carocci, Maria Lisa Clodoveo, Filomena Corbo and Giuseppe Fracchiolla
Antibiotics 2021, 10(6), 688; https://doi.org/10.3390/antibiotics10060688 - 8 Jun 2021
Cited by 13 | Viewed by 3298
Abstract
According to recent studies, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) have shown a good antimicrobial and antifungal activity. Their association with essential oils (EOs) could be useful for the treatment of infections caused by Candida spp. The aim of this studyis to evaluate the [...] Read more.
According to recent studies, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) have shown a good antimicrobial and antifungal activity. Their association with essential oils (EOs) could be useful for the treatment of infections caused by Candida spp. The aim of this studyis to evaluate the synergistic antifungal activity of new combinations between Diclofenac Sodium Salt (DSS), a widely used NSAID, with EOs of Mentha × piperita, Pelargonium graveolens and Melaleuca alternifolia. The in-vitro antifungal activity was determined on different Candida strains. The determination of the chemical composition of EOs was carried out by gaschromatography-massspectrometry (GC-MS). Susceptibility testing of planktonic cells was performed by using the broth microdilution assay and checkerboard methods. Minimum Inhibitory Concentrations (MIC) of DSS was in a range from 1.02 to 2.05 μg/mL reaching a MIC value of 0.05 μg/mL when combined with Pelargonium graveolens (FICI = 0.23–0.35) or Menthapiperita (FICI = 0.22–0.30) EOs. These preliminary results show thatthe combination of the EOs with DSS improves the antifungal activity on all the tested Candida strains. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)

Review

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18 pages, 345 KiB  
Review
Non-Antibiotic Drug Repositioning as an Alternative Antimicrobial Approach
by Alexia Barbarossa, Antonio Rosato, Filomena Corbo, Maria Lisa Clodoveo, Giuseppe Fracchiolla, Antonio Carrieri and Alessia Carocci
Antibiotics 2022, 11(6), 816; https://doi.org/10.3390/antibiotics11060816 - 17 Jun 2022
Cited by 29 | Viewed by 4509
Abstract
The worldwide scenario of antibiotic resistance and the falling number of funds for the development of novel antibiotics have led research efforts toward the study of specific cost-effective strategies aimed at discovering drugs against microbial infections. Among the potential options, drug repositioning, which [...] Read more.
The worldwide scenario of antibiotic resistance and the falling number of funds for the development of novel antibiotics have led research efforts toward the study of specific cost-effective strategies aimed at discovering drugs against microbial infections. Among the potential options, drug repositioning, which has already exhibited satisfactory results in other medical fields, came out as the most promising. It consists of finding new uses for previously approved medicines and, over the years, many “repurposed drugs” displayed some encouraging in vitro and in vivo results beyond their initial application. The principal theoretical justification for reusing already existing drugs is that they have known mechanisms of action and manageable side effects. Reuse of old drugs is now considered an interesting approach to overcome the drawbacks of conventional antibiotics. The purpose of this review is to offer the reader a panoramic view of the updated studies concerning the repositioning process of different classes of non-antibiotic drugs in the antimicrobial field. Several research works reported the ability of some non-steroidal anti-inflammatory drugs (NSAIDs), antidepressants, antipsychotics, and statins to counteract the growth of harmful microorganisms, demonstrating an interesting winning mode to fight infectious diseases caused by antimicrobial resistant bacteria. Full article
(This article belongs to the Special Issue Drug Repositioning in Antimicrobial Therapy)
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