Journal Description
Antibiotics
Antibiotics
is an international, peer-reviewed, open access journal on all aspects of antibiotics, published monthly online by MDPI.
- Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
- High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, PMC, Embase, CAPlus / SciFinder, and other databases.
- Journal Rank: JCR - Q1 (Pharmacology & Pharmacy) / CiteScore - Q1 (General Pharmacology, Toxicology and Pharmaceutics)
- Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 13.7 days after submission; acceptance to publication is undertaken in 2.5 days (median values for papers published in this journal in the second half of 2023).
- Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
Impact Factor:
4.8 (2022);
5-Year Impact Factor:
4.9 (2022)
Latest Articles
Emergence of High-Level Gentamicin Resistance in Streptococcus agalactiae Hypervirulent Serotype IV ST1010 (CC452) Strains by Acquisition of a Novel Integrative and Conjugative Element
Antibiotics 2024, 13(6), 491; https://doi.org/10.3390/antibiotics13060491 (registering DOI) - 26 May 2024
Abstract
Streptococcus agalactiae (group B streptococci, GBS) is responsible for severe infections in both neonates and adults. Currently, empiric antimicrobial therapy for sepsis and meningitis is the combined use of penicillin and gentamicin due to the enhanced bactericidal activity. However, high-level gentamicin resistance (HLGR)
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Streptococcus agalactiae (group B streptococci, GBS) is responsible for severe infections in both neonates and adults. Currently, empiric antimicrobial therapy for sepsis and meningitis is the combined use of penicillin and gentamicin due to the enhanced bactericidal activity. However, high-level gentamicin resistance (HLGR) abrogates the synergism. The rate of HLGR was investigated within a dataset of 433 GBS strains collected from cases of invasive disease in both adults and neonates as well as from pregnant carriers. GBS isolates (n = 20, 4.6%) presented with HLGR (gentamicin MIC breakpoint >1024 mg/L) that was differently diffused between strains from adults or neonates (5.2% vs. 2.8%). Notably, 70% of HLGR GBS strains (14 isolates) were serotype IV. Serotype IV HLGR-GBS isolates were susceptible to all antibiotics tested, exhibited the alpha-C/HvgA/PI-2b virulence string, and belonged to sequence type 1010 (clonal complex (CC) 452). The mobile element that harbored the HLGR aac(6′)-aph(2)″ gene is a novel integrative and conjugative element (ICE) about 45 kb long, derived from GBS 515 ICE tRNALys. The clonal expansion of this HLGR hypervirulent serotype IV GBS CC452 sublineage may pose a threat to the management of infections caused by this strain type.
Full article
(This article belongs to the Special Issue Sepsis Management and Antibiotic Therapy)
Open AccessReview
Relevance of the Adjuvant Effect between Cellular Homeostasis and Resistance to Antibiotics in Gram-Negative Bacteria with Pathogenic Capacity: A Study of Klebsiella pneumoniae
by
Mildred Azucena Rivera-Galindo, Félix Aguirre-Garrido, Ulises Garza-Ramos, José Geiser Villavicencio-Pulido, Francisco José Fernández Perrino and Marcos López-Pérez
Antibiotics 2024, 13(6), 490; https://doi.org/10.3390/antibiotics13060490 (registering DOI) - 26 May 2024
Abstract
Antibiotic resistance has become a global issue. The most significant risk is the acquisition of these mechanisms by pathogenic bacteria, which can have a severe clinical impact and pose a public health risk. This problem assumes that bacterial fitness is a constant phenomenon
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Antibiotic resistance has become a global issue. The most significant risk is the acquisition of these mechanisms by pathogenic bacteria, which can have a severe clinical impact and pose a public health risk. This problem assumes that bacterial fitness is a constant phenomenon and should be approached from an evolutionary perspective to develop the most appropriate and effective strategies to contain the emergence of strains with pathogenic potential. Resistance mechanisms can be understood as adaptive processes to stressful conditions. This review examines the relevance of homeostatic regulatory mechanisms in antimicrobial resistance mechanisms. We focus on the interactions in the cellular physiology of pathogenic bacteria, particularly Gram-negative bacteria, and specifically Klebsiella pneumoniae. From a clinical research perspective, understanding these interactions is crucial for comprehensively understanding the phenomenon of resistance and developing more effective drugs and treatments to limit or attenuate bacterial sepsis, since the most conserved adjuvant phenomena in bacterial physiology has turned out to be more optimized and, therefore, more susceptible to alterations due to pharmacological action.
Full article
(This article belongs to the Special Issue Antibiotics Use and Therapy in Gram-Negative Bacterial Infection)
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Open AccessArticle
The Effects of Different Antimicrobial Peptides (A-11 and AP19) on Isolated Bacteria from Fresh Boar Semen and Semen Quality during Storage at 18 °C
by
Krittika Keeratikunakorn, Panida Chanapiwat, Ratchaneewan Aunpad, Natharin Ngamwongsatit and Kampon Kaeoket
Antibiotics 2024, 13(6), 489; https://doi.org/10.3390/antibiotics13060489 - 24 May 2024
Abstract
Antibiotic resistance (AMR) is a major public health concern. Antimicrobial peptides (AMPs) could be an alternative to conventional antibiotics. The purpose of this research was to investigate the antimicrobial ability of the synthetic AMPs (i.e., A-11 and AP19) on the most frequently isolated
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Antibiotic resistance (AMR) is a major public health concern. Antimicrobial peptides (AMPs) could be an alternative to conventional antibiotics. The purpose of this research was to investigate the antimicrobial ability of the synthetic AMPs (i.e., A-11 and AP19) on the most frequently isolated bacteria in boar semen and their effect on extended boar semen quality during storage. We tested the antimicrobial effect of A-11 and AP19 at different concentrations and compared them with gentamicin for inhibiting the growth of E. coli, Pseudomonas aeruginosa and Proteus mirabilis that were isolated from fresh boar semen. In order to evaluate the effect of AMP on semen qualities on days 0, 1, 3, and 5 after storage at 18 °C, seven fresh boar semen samples were collected, diluted with semen extender with antibiotic (i.e., gentamicin at 200 µg/mL, positive control) or without (negative control), and semen extender contained only A-11 or AP19 at different concentrations (i.e., 62.50, 31.25, and 15.625 µg/mL). The total bacterial count was also measured at 0, 24, 36, 48, and 72 h after storage. Comparable to gentamicin, both A-11 and AP19 inhibited the growth of E. coli, Pseudomonas aeruginosa, and Proteus mirabilis at 62.50, 31.25, and 15.625 µg/mL, respectively. Comparing the total bacterial count at 0, 24, 36, 48 and 72 h after storage, the lowest total bacterial concentration was found in the positive control group (p < 0.05), and an inferior total bacterial concentration was found in the treatment groups than in the negative control. On day 1, there is a lower percentage of all sperm parameters in the AP19 group at a concentration of 62.50 µg/mL compared with the other groups. On day 3, the highest percentage of all sperm parameters was found in the positive control and A-11 at a concentration of 31.25 µg/mL compared with the other groups. The AP19 group at 62.5 µg/mL constantly yielded inferior sperm parameters. On day 5, only A-11 at a concentration of 15.625 µg/mL showed a total motility higher than 70%, which is comparable to the positive control. A-11 and AP19 showed antimicrobial activity against E. coli, Pseudomonas aeruginosa and Proteus mirabilis isolated from boar semen. Considering their effect on semen quality during storage, these antimicrobial peptides are an alternative to conventional antibiotics used in boar semen extenders. Nevertheless, the utilization of these particular antimicrobial peptides relied on the concentration and duration of storage.
Full article
(This article belongs to the Special Issue Antimicrobial Peptides: An Emerging Hope in the Era of New Infections and Resistance)
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Open AccessArticle
Antifungal Activity of Aniba canelilla (Kunth) Mez Essential Oil and Its Main Compound 1-Nitro-2-Phenylethane against Dermatophytes
by
Tainá Kreutz, Eliane Oliveira Salines Duarte, Priscilla Maciel Quatrin, Simone Braga Carneiro, Valdir F. Veiga-Junior, Alexandre Meneghello Fuentefria and Letícia S. Koester
Antibiotics 2024, 13(6), 488; https://doi.org/10.3390/antibiotics13060488 - 24 May 2024
Abstract
The essential oil of Aniba canelilla (Kunth) Mez (EOAC), an Amazon plant composed of a rare nitro compound, has shown scientific evidence of antifungal activity but is still unexplored against dermatophytes. The antifungal susceptibility of EOAC and its main compound, 1-nitro-2-phenylethane (NP), was
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The essential oil of Aniba canelilla (Kunth) Mez (EOAC), an Amazon plant composed of a rare nitro compound, has shown scientific evidence of antifungal activity but is still unexplored against dermatophytes. The antifungal susceptibility of EOAC and its main compound, 1-nitro-2-phenylethane (NP), was evaluated against dermatophytes (Trichophyton rubrum, T. mentagrophytes and Microsporum canis), evidencing antifungal activity with an inhibitory concentration lower than 256 μg/mL. The mechanism of action was also evaluated, and it is suggested that EOAC and NP have fungicidal action in the fungal membrane, since the antifungal activity occurs through a modification of the shape of the conidial structures of the fungus, showing the permeability of the intracellular content due to the visually observed plasmolysis and cytosolic extravasation through an osmotic process. These results suggest the essential oil and its main compound are promising plant-derived alternatives for treating ungual dermatophytosis.
Full article
(This article belongs to the Special Issue Exploring Antimicrobial Properties and Bioactive Compounds of Edible and Medicinal Plants)
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Open AccessReview
Antimicrobial Metabolites of Caucasian Medicinal Plants as Alternatives to Antibiotics
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Marta Fik-Jaskółka, Valentina Mittova, Catherine Motsonelidze, Malkhaz Vakhania, Caterina Vicidomini and Giovanni N. Roviello
Antibiotics 2024, 13(6), 487; https://doi.org/10.3390/antibiotics13060487 - 24 May 2024
Abstract
This review explores the potential of antimicrobial metabolites derived from Caucasian medicinal plants as alternatives to conventional antibiotics. With the rise of antibiotic resistance posing a global health threat, there is a pressing need to investigate alternative sources of antimicrobial agents. Caucasian medicinal
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This review explores the potential of antimicrobial metabolites derived from Caucasian medicinal plants as alternatives to conventional antibiotics. With the rise of antibiotic resistance posing a global health threat, there is a pressing need to investigate alternative sources of antimicrobial agents. Caucasian medicinal plants have traditionally been used for their therapeutic properties, and recent research has highlighted their potential as sources of antimicrobial compounds. Representatives of 15 families of Caucasian medicinal plant extracts (24 species) have been explored for their efficacy against these pathogens. The effect of these plants on Gram-positive and Gram-negative bacteria and fungi is discussed in this paper. By harnessing the bioactive metabolites present in these plants, this study aims to contribute to the development of new antimicrobial treatments that can effectively combat bacterial infections while minimizing the risk of resistance emergence. Herein we discuss the following classes of bioactive compounds exhibiting antimicrobial activity: phenolic compounds, flavonoids, tannins, terpenes, saponins, alkaloids, and sulfur-containing compounds of Allium species. The review discusses the pharmacological properties of selected Caucasian medicinal plants, the extraction and characterization of these antimicrobial metabolites, the mechanisms of action of antibacterial and antifungal plant compounds, and their potential applications in clinical settings. Additionally, challenges and future directions in the research of antimicrobial metabolites from Caucasian medicinal plants are addressed.
Full article
(This article belongs to the Special Issue Innovations in Antibacterial Agents: Combating Resistance, Improving Efficacy and Exploring New Mechanisms)
Open AccessArticle
Impact of Soil Fertilization with Pig Slurry on Antibiotic Residues and Resistance Genes: A Longitudinal Study
by
Luisa Massaccesi, Elisa Albini, Francesca Romana Massacci, Danilo Giusepponi, Fabiola Paoletti, Stefano Sdogati, Francesco Morena, Alberto Agnelli, Angelo Leccese, Chiara Francesca Magistrali and Roberta Galarini
Antibiotics 2024, 13(6), 486; https://doi.org/10.3390/antibiotics13060486 - 24 May 2024
Abstract
The impact of soil fertilization with animal manure on the spread and persistence of antibiotic resistance in the environment is far from being fully understood. To add knowledge about persistence and correlations between antibiotic residues and antibiotic resistance genes (ARGs) in fertilized soil,
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The impact of soil fertilization with animal manure on the spread and persistence of antibiotic resistance in the environment is far from being fully understood. To add knowledge about persistence and correlations between antibiotic residues and antibiotic resistance genes (ARGs) in fertilized soil, a longitudinal soil mesocosm study was conducted. Soil samples were collected from the mesocosms immediately before spreading and then afterward at fifteen time points during a 320-day observation period. Eight ARGs (ermB, sul1, tetA, tetG, tetM, cfr, fexA, and optrA) and the class 1 integron-integrase gene, intI1, were determined in both pig slurry and soil, as well as residues of 36 antibiotics. Soil chemical and biochemical parameters were also measured. Twelve antibiotics were detected in the slurry in the range of 3 µg kg−1–3605 µg kg−1, with doxycycline, lincomycin, and tiamulin being the most abundant, whereas ermB, sul1, and tetM were the predominant ARGs. Before spreading, neither antibiotic residues nor ARGs were detectable in the soil; afterwards, their concentrations mirrored those in the slurry, with a gradual decline over the duration of the experiment. After about three months, the effect of the amendment was almost over, and no further evolution was observed.
Full article
(This article belongs to the Special Issue Antimicrobial Resistance Monitoring in Food-Producing Animals)
Open AccessArticle
Spent Material Extractives from Hemp Hydrodistillation as an Underexplored Source of Antimicrobial Cannabinoids
by
Simon Vlad Luca, Krzysztof Wojtanowski, Izabela Korona-Głowniak, Krystyna Skalicka-Woźniak, Mirjana Minceva and Adriana Trifan
Antibiotics 2024, 13(6), 485; https://doi.org/10.3390/antibiotics13060485 - 24 May 2024
Abstract
Hemp (Cannabis sativa L.) has been used for millennia as a rich source of food and fibers, whereas hemp flowers have only recently gained an increased market interest due to the presence of cannabinoids and volatile terpenes. Currently, the hemp flower processing
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Hemp (Cannabis sativa L.) has been used for millennia as a rich source of food and fibers, whereas hemp flowers have only recently gained an increased market interest due to the presence of cannabinoids and volatile terpenes. Currently, the hemp flower processing industry predominantly focuses on either cannabinoid or terpene extraction. In an attempt to maximize the valorization of hemp flowers, the current study aimed to evaluate the phytochemical composition and antimicrobial properties of several extracts obtained from post-distillation by-products (e.g., spent material, residual distillation water) in comparison to the essential oil and total extract obtained from unprocessed hemp flowers. A terpene analysis of the essential oil revealed 14 monoterpenes and 35 sesquiterpenes. The cannabinoid profiling of extracts showed seven acidic precursors and 14 neutral derivatives, with cannabidiol (CBD) reaching the highest concentration (up to 16 wt.%) in the spent material extract. The antimicrobial assessment of hemp EO, cannabinoid-containing extracts, and single compounds (i.e., CBD, cannabigerol, cannabinol, and cannabichromene) against a panel of 20 microbial strains demonstrated significant inhibitory activities against Gram-positive bacteria, Helicobacter pylori, and Trichophyton species. In conclusion, this work suggests promising opportunities to use cannabinoid-rich materials from hemp flower processing in functional foods, cosmetics, and pharmaceuticals with antimicrobial properties.
Full article
(This article belongs to the Special Issue Plants, Lichens, Fungi, and Algae Extracts and Derivatives with Antimicrobial Properties for Nutrition and Health)
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Open AccessReview
Exploring the Link between Helicobacter pylori, Gastric Microbiota and Gastric Cancer
by
Costantino Sgamato, Alba Rocco, Debora Compare, Kateryna Priadko, Marco Romano and Gerardo Nardone
Antibiotics 2024, 13(6), 484; https://doi.org/10.3390/antibiotics13060484 - 24 May 2024
Abstract
Gastric cancer (GC) still represents one of the leading causes of cancer-related mortality and is a major public health issue worldwide. Understanding the etiopathogenetic mechanisms behind GC development holds immense potential to revolutionize patients’ treatment and prognosis. Within the complex web of genetic
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Gastric cancer (GC) still represents one of the leading causes of cancer-related mortality and is a major public health issue worldwide. Understanding the etiopathogenetic mechanisms behind GC development holds immense potential to revolutionize patients’ treatment and prognosis. Within the complex web of genetic predispositions and environmental factors, the connection between Helicobacter pylori (H. pylori) and gastric microbiota emerges as a focus of intense research investigation. According to the most recent hypotheses, H. pylori triggers inflammatory responses and molecular alterations in gastric mucosa, while non-Helicobacter microbiota modulates disease progression. In this review, we analyze the current state of the literature on the relationship between H. pylori and non-Helicobacter gastric microbiota in gastric carcinogenesis, highlighting the mechanisms by which microecological dysbiosis can contribute to the malignant transformation of the mucosa.
Full article
(This article belongs to the Special Issue Pathogenesis, Diagnosis and Treatment of H. pylori Infection)
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Open AccessArticle
CRISPR Interference-Mediated Silencing of the mmpL3 Gene in Mycobacterium smegmatis and Its Impact on Antimicrobial Susceptibility
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Yonita Yuliani, Azizah Fitriana Nurul Ilmi, Suthidee Petsong, Ajcharaporn Sawatpanich, Sunisa Chirakul, Tanittha Chatsuwan, Tanapat Palaga and Suwatchareeporn Rotcheewaphan
Antibiotics 2024, 13(6), 483; https://doi.org/10.3390/antibiotics13060483 - 24 May 2024
Abstract
Background: The discovery of novel therapeutic agents, especially those targeting mycobacterial membrane protein large 3 (mmpL3), has shown promise. In this study, the CRISPR interference-Streptococcus thermophilus nuclease-deactivated Cas9 (CRISPRi-dCas9Sth1) system was utilized to suppress mmpL3 expression in Mycobacterium
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Background: The discovery of novel therapeutic agents, especially those targeting mycobacterial membrane protein large 3 (mmpL3), has shown promise. In this study, the CRISPR interference-Streptococcus thermophilus nuclease-deactivated Cas9 (CRISPRi-dCas9Sth1) system was utilized to suppress mmpL3 expression in Mycobacterium smegmatis, and its impacts on susceptibility to antimicrobial agents were evaluated. Methods: The repression of the mmpL3 gene was confirmed by RT-qPCR. The essentiality, growth curve, viability, and antimicrobial susceptibility of the mmpL3 knockdown strain were investigated. Results: mmpL3 silencing was achieved by utilizing 0.5 and 1 ng/mL anhydrotetracycline (ATc), resulting in reductions in the expression of 60.4% and 74.4%, respectively. mmpL3 silencing led to a significant decrease in bacterial viability when combined with one-half of the minimal inhibitory concentrations (MICs) of rifampicin, rifabutin, ceftriaxone, or isoniazid, along with 0.1 or 0.5 ng/mL ATc (p < 0.05). However, no significant difference was observed for clarithromycin or amikacin. Conclusions: The downregulation of the mmpL3 gene in mycobacteria was achieved through the use of CRISPRi-dCas9Sth1, resulting in growth deficiencies and resensitization to certain antimicrobial agents. The impact was dependent upon the level of gene expression.
Full article
(This article belongs to the Section Antibiotic Therapy in Infectious Diseases)
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Open AccessArticle
Gum Arabic Increases Phagocytosis of Escherichia coli by Blood Leukocytes of Young and Old Healthy Volunteers
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Christin Freibrodt, Shima Baien, Maren von Köckritz-Blickwede, Nicole de Buhr, Roland Nau and Jana Seele
Antibiotics 2024, 13(6), 482; https://doi.org/10.3390/antibiotics13060482 - 24 May 2024
Abstract
Background: Gum arabic, a polysaccharide exudate from Acacia senegal (L.) Willdenow trees, has already been used by African native people in natural medicine. Methods: Using whole-blood samples from young (20–35 years) and older (>80 years) healthy volunteers (each group n = 10), the
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Background: Gum arabic, a polysaccharide exudate from Acacia senegal (L.) Willdenow trees, has already been used by African native people in natural medicine. Methods: Using whole-blood samples from young (20–35 years) and older (>80 years) healthy volunteers (each group n = 10), the effect of an aqueous solution of GA on phagocytosis of Escherichia coli was examined with a gentamicin protection assay. Whole-blood samples of each volunteer were stimulated with GA and as a control with CpG oligodeoxynucleotides (Toll-like receptor -9 agonists) for 2 h, then co-incubated with E. coli for 30 min and thereafter treated with gentamicin for up to 240 min to kill extracellular bacteria. Then, whole-blood cells were lysed with distilled water, and colony-forming units were counted by quantitative plating. Cytokine enzyme-linked immunosorbent assay for the detection of TNF-α and IL-6 was performed using the blood supernatant. Results: The GA concentration tested (20 mg/mL) did not affect the viability of eukaryotic cells. Phagocytosis of E. coli by whole-blood leukocytes derived from young (p = 0.008) and older (p = 0.004) healthy volunteers was increased by 120.8% (young) and 39.2% (old) after stimulation with GA. In contrast, CpG only stimulated the bacterial phagocytosis by cells derived from young volunteers (p = 0.004). Stimulation of whole blood with GA increased the intracellular killing of E. coli in young (p = 0.045) and older volunteers (p = 0.008) and induced a TNF-α release in whole blood collected from older volunteers but not from younger ones (p = 0.008). Conclusions: These data encourage the isolation of active compounds of GA and the initiation of clinical trials addressing the preventive effect of GA on bacterial infections.
Full article
(This article belongs to the Special Issue Natural Products and Bio-Nanomaterials: Novel Strategies to Overcome Antibiotic Resistance)
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Open AccessSystematic Review
Antibiotic-Resistant Bacteria Isolated from Street Foods: A Systematic Review
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Carmine Fusaro, Valentina Miranda-Madera, Nancy Serrano-Silva, Jaime E. Bernal, Karina Ríos-Montes, Francisco Erik González-Jiménez, Dennys Ojeda-Juárez and Yohanna Sarria-Guzmán
Antibiotics 2024, 13(6), 481; https://doi.org/10.3390/antibiotics13060481 - 23 May 2024
Abstract
Street food may be a vehicle of antibiotic-resistant bacteria (ARB) and antibiotic resistance genes (ARGs) to humans. Foods contaminated with ARB entail serious problems or challenges in the fields of medical care, animal husbandry, food industry, and public health worldwide. The objectives of
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Street food may be a vehicle of antibiotic-resistant bacteria (ARB) and antibiotic resistance genes (ARGs) to humans. Foods contaminated with ARB entail serious problems or challenges in the fields of medical care, animal husbandry, food industry, and public health worldwide. The objectives of this systematic review were to identify and evaluate scientific reports associated with ARB isolated from various street foods. “Preferred reporting items for systematic reviews and meta-analysis” (PRISMA) guidelines were followed. The bibliographic material covers a period from January 2015 to April 2024. Six electronic scientific databases were searched individually for full-text articles; only those papers that met the inclusion and exclusion criteria were selected. Seventeen papers were included in this systematic review. This study highlighted the wide distribution of ARB resistant to β-lactams and other antibiotics, posing significant health risks to consumers. High resistance levels were observed for antibiotics such as ampicillin, ceftriaxone, and tetracycline, while some antibiotics, such as ceftazidime, clavulanic acid, cefoperazone, cotrimoxazole, doxycycline, doripenem, fosfomycin, vancomycin, and piperacillin-tazobactam, demonstrated 100% susceptibility. The prevalence of ARB in street foods varied between 5.2% and 70.8% among different countries. The multiple resistance of various bacteria, including Escherichia coli, Staphylococcus, Salmonella, and Klebsiella, to multiple classes of antibiotics, as well as environmental factors contributing to the spread of antibiotic resistance (AR), emphasize the urgent need for comprehensive approaches and coordinated efforts to confront antimicrobial resistance (AMR) under the “One Health” paradigm.
Full article
(This article belongs to the Special Issue A One Health Approach to Antimicrobial Resistance)
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Open AccessArticle
Pharmacist-Led Antimicrobial Stewardship Programme in Two Tertiary Hospitals in Malawi
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Nelson Nyoloka, Charlotte Richards, William Mpute, Hope Michael Chadwala, Hanna Stambuli Kumwenda, Violet Mwangonde-Phiri, Aggrey Phiri, Ceri Phillips and Charlotte Makanga
Antibiotics 2024, 13(6), 480; https://doi.org/10.3390/antibiotics13060480 - 23 May 2024
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The ultimate goal of antimicrobial stewardship (AMS) programmes is to decrease the occurrence and spread of antimicrobial resistance (AMR). In response to this, a pharmacist partnership was established between Malawi and Wales (UK) with the aim of strengthening antimicrobial stewardship (AMS) activities in
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The ultimate goal of antimicrobial stewardship (AMS) programmes is to decrease the occurrence and spread of antimicrobial resistance (AMR). In response to this, a pharmacist partnership was established between Malawi and Wales (UK) with the aim of strengthening antimicrobial stewardship (AMS) activities in Malawi, with the initial project focusing on two tertiary referral hospitals. The Global Point Prevalence Survey (GPPS) was undertaken for the first time in Malawi at these sites and demonstrated a prescribing rate slightly lower than the African average, with ceftriaxone indicated for almost every bacterial infection. An educational intervention was also delivered, with a train-the-trainer approach upskilling pharmacists at the two sites, who then cascaded co-produced training sessions to an additional 120 multidisciplinary health professionals. A toolkit to support AMS at an individual patient level was also developed and disseminated to provide an ongoing reference to refer to. Both the trainings and toolkit were well received. Over the course of this project, significant progress has been made with the AMS programmes at the two sites, with local staff empowered to implement AMS activities. These interventions could be easily replicated and scaled and support the delivery of some of the AMS elements of the Malawi Ministry of Health National Action Plan for Antimicrobial Resistance.
Full article
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Open AccessArticle
Hybrid Caffeic Acid-Based DHFR Inhibitors as Novel Antimicrobial and Anticancer Agents
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Renu Sehrawat, Ritu Pasrija, Priyanka Rathee, Deepika Kumari, Anurag Khatkar, Esra Küpeli Akkol and Eduardo Sobarzo-Sánchez
Antibiotics 2024, 13(6), 479; https://doi.org/10.3390/antibiotics13060479 - 23 May 2024
Abstract
A novel series of 1,2,4-triazole analogues of caffeic acid was designed, synthesized, characterized, and assessed for their capacity to inhibit DHFR, as well as their anticancer and antimicrobial properties. A molecular docking analysis was conducted on DHFR, utilizing PDB IDs 1U72 and 2W9S,
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A novel series of 1,2,4-triazole analogues of caffeic acid was designed, synthesized, characterized, and assessed for their capacity to inhibit DHFR, as well as their anticancer and antimicrobial properties. A molecular docking analysis was conducted on DHFR, utilizing PDB IDs 1U72 and 2W9S, aiming to design anticancer and antimicrobial drugs, respectively. Among all the synthesized derivatives, compound CTh7 demonstrated the highest potency as a DHFR inhibitor, with an IC50 value of 0.15 μM. Additionally, it exhibited significant cytotoxic properties, with an IC50 value of 8.53 µM. The molecular docking analysis of the CTh7 compound revealed that it forms strong interactions with key residues of homo sapiens DHFR such as Glu30, Phe34, Tyr121, Ile16, Val115, and Phe31 within the target protein binding site and displayed excellent docking scores and binding energy (−9.9; −70.38 kcal/mol). Additionally, synthesized compounds were screened for antimicrobial properties, revealing significant antimicrobial potential against bacterial strains and moderate effects against fungal strains. Specifically, compound CTh3 exhibited notable antibacterial efficacy against Staphylococcus aureus (MIC = 5 µM). Similarly, compound CTh4 demonstrated significant antibacterial activity against both Escherichia coli and Pseudomonas aeruginosa, with MIC values of 5 µM for each. A docking analysis of the most active antimicrobial compound CTh3 revealed that it forms hydrogen bonds with Thr121 and Asn18, a π–cation bond with Phe92, and a salt bridge with the polar residue Asp27.
Full article
(This article belongs to the Special Issue Microbial Natural Products as a Source of Novel Antimicrobials)
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Open AccessArticle
Phytochemical Screening and Antibacterial Activity of Commercially Available Essential Oils Combinations with Conventional Antibiotics against Gram-Positive and Gram-Negative Bacteria
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Răzvan Neagu, Violeta Popovici, Lucia-Elena Ionescu, Viorel Ordeanu, Andrei Biță, Diana Mihaela Popescu, Emma Adriana Ozon and Cerasela Elena Gîrd
Antibiotics 2024, 13(6), 478; https://doi.org/10.3390/antibiotics13060478 - 23 May 2024
Abstract
The present study aims to evaluate the antibacterial activity of five commercially available essential oils (EOs), Lavender (LEO), Clove (CEO), Oregano (OEO), Eucalyptus (EEO), and Peppermint (PEO), against the most-known MDR Gram-positive and Gram-negative bacteria—Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922),
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The present study aims to evaluate the antibacterial activity of five commercially available essential oils (EOs), Lavender (LEO), Clove (CEO), Oregano (OEO), Eucalyptus (EEO), and Peppermint (PEO), against the most-known MDR Gram-positive and Gram-negative bacteria—Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), and Pseudomonas aeruginosa (ATCC 27853)—alone and in various combinations. Gas Chromatography–Mass Spectrometry (GC-MS) analysis established their complex compositions. Then, their antibacterial activity—expressed as the inhibition zone diameter (IZD) value (mm)—was investigated in vitro by the diffusimetric antibiogram method, using sterile cellulose discs with Ø 6 mm impregnated with 10 µL of sample and sterile borosilicate glass cylinders loaded with 100 µL; the minimum inhibitory concentration (MIC) value (µg/mL) for each EO was calculated from the IZD values (mm) measured after 24 h. The following EO combinations were evaluated: OEO+CEO, CEO+EEO, CEO+PEO, LEO+EEO, and EEO+PEO. Then, the influence of each dual combination on the activity of three conventional antibacterial drugs—Neomycin (NEO), Tetracycline (TET), and Bacitracin (BAC)—was investigated. The most active EOs against S. aureus and E. coli were LEO and OEO (IZD = 40 mm). They were followed by CEO and EEO (IZD = 20–27 mm); PEO exhibited the lowest antibacterial activity (IZD = 15–20 mm). EEO alone showed the highest inhibitory activity on P. aeruginosa (IZD = 25–35 mm). It was followed by CEO, LEO, and EEO (IZD = 7–11 mm), while PEO proved no antibacterial action against it (IZD = 0 mm). Only one synergic action was recorded (OEO+CEO against P. aeruginosa); EEO+PEO revealed partial synergism against S. aureus and CEO+PEO showed additive behavior against E. coli. Two triple associations with TET showed partial synergism against E. coli, and the other two (with NEO and TET) evidenced the same behavior against S. aureus; all contained EEO+PEO or CEO+PEO. Most combinations reported indifference. However, numerous cases involved antagonism between the constituents included in the double and triple combinations, and the EOs with the strongest antibacterial activities belonged to the highest antagonistic combinations. A consistent statistical analysis supported our results, showing that the EOs with moderate antibacterial activities could generate combinations with higher inhibitory effects based on synergistic or additive interactions.
Full article
(This article belongs to the Special Issue Plants, Lichens, Fungi, and Algae Extracts and Derivatives with Antimicrobial Properties for Nutrition and Health)
Open AccessArticle
The Impact of SARS-CoV-2 Pandemic on Antibiotic Prescriptions and Resistance in a University Hospital from Romania
by
Dana Carmen Zaha, Codrin Dan Nicolae Ilea, Florica Ramona Dorobanțu, Carmen Pantiș, Ovidiu Nicolae Pop, Dorina Gabriela Dascal, Cătălin Dorin Dorobanțu and Felicia Manole
Antibiotics 2024, 13(6), 477; https://doi.org/10.3390/antibiotics13060477 - 23 May 2024
Abstract
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This paper aimed to evaluate the effects of the COVID-19 pandemic on prescription rates and antibiotic resistance in a university hospital. A retrospective study was conducted on the medical records of patients admitted to the Bihor Emergency Clinical County Hospital in Romania in
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This paper aimed to evaluate the effects of the COVID-19 pandemic on prescription rates and antibiotic resistance in a university hospital. A retrospective study was conducted on the medical records of patients admitted to the Bihor Emergency Clinical County Hospital in Romania in 2019 (pre-pandemic) and 2021 (during the pandemic period). We evaluated the antibiotic consumption index (ACI) and susceptibility rates. The overall percentage of antibiotic prescribing increased in 2021, while the total number of patients decreased. Genito-urinary, digestive, respiratory infections, heart diseases and wounds were the most common conditions for antibiotic prescriptions, but the number of them decreased in 2021. There was a decrease in the proportion of antibiotics from the Watch and Reserve class and an increase in the proportion of antibiotics from the Access class. Antibiotic use has been reduced despite an increase in the number of patients, with a high consumption in the Watch group in the ICU wards. By contrast, surgical wards had the highest rate of antibiotic prescriptions, but a decrease in the number of patients. The patients who were administered antibiotics were hospitalized for diagnoses other than COVID-19. Almost all prescribed antibiotics displayed decreasing sensitivity rates. The number of isolated ESKAPE pathogens, except for Staphylococcus aureus methicillin-resistant strains, were increased. Strategies to control antibiotic prescriptions and the spread of resistant pathogens should be improved.
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Open AccessArticle
A New “Non-Traditional” Antibacterial Drug Fluorothiazinone—Clinical Research in Patients with Complicated Urinary Tract Infections
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Nailya A. Zigangirova, Nadezda L. Lubenec, Vladimir B. Beloborodov, Anna B. Sheremet, Stanislava A. Nelyubina, Nataliia E. Bondareva, Konstantin A. Zakharov, Sergey I. Luyksaar, Sergey A. Zolotov, Evgenia U. Levchenko, Svetlana V. Luyksaar, Ekaterina A. Koroleva, Elena D. Fedina, Yana V. Simakova, Dmitry Yu. Pushkar and Alexander L. Gintzburg
Antibiotics 2024, 13(6), 476; https://doi.org/10.3390/antibiotics13060476 - 22 May 2024
Abstract
In order to combat resistance, it is necessary to develop antimicrobial agents that act differently from conventional antibiotics. Fluorothiazinone, 300 mg tablet (The Gamaleya National Research Center), is an original antibacterial drug based on a new small molecule T3SS and flagellum inhibitor. A
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In order to combat resistance, it is necessary to develop antimicrobial agents that act differently from conventional antibiotics. Fluorothiazinone, 300 mg tablet (The Gamaleya National Research Center), is an original antibacterial drug based on a new small molecule T3SS and flagellum inhibitor. A total of 357 patients with complicated urinary tract infections (UTIs) were divided into two groups and given Fluorothiazinone 1200 mg/day or a placebo for 7 days to evaluate the efficacy and safety of the drug. Additionally, all patients were given Cefepime 2000 mg/day. Fluorothiazinone with Cefepime showed superiority over placebo/Cefepime based on the assessment of the proportion of patients with an overall outcome in the form of a cure after 21 days post-therapy (primary outcome), overall outcome in cure rates, clinical cure rates, and microbiological efficacy at the end of therapy and after 21 days post-therapy (secondary outcomes). In patients who received Fluorothiazinone, the rate of infection recurrences 53 and 83 days after the end of the therapy was lower by 18.9%, compared with patients who received placebo. Fluorothiazinone demonstrated a favorable safety profile with no serious unexpected adverse events reported. The results showed superiority of the therapy with Fluorothiazinone in combination with Cefepime compared with placebo/Cefepime in patients with cUTIs.
Full article
(This article belongs to the Special Issue Antimicrobial Drug Discovery: New Theories and New Therapies)
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Open AccessArticle
Triple-Antibiotic Combination Exerts Effective Activity against Mycobacterium avium subsp. hominissuis Biofilm and Airway Infection in an In Vivo Murine Model
by
Elliot M. Offman, Amy Leestemaker-Palmer, Reza Fathi, Bailey Keefe, Aida Bibliowicz, Gilead Raday and Luiz E. Bermudez
Antibiotics 2024, 13(6), 475; https://doi.org/10.3390/antibiotics13060475 - 22 May 2024
Abstract
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Objectives: Slow-growing nontuberculous mycobacteria (NTMs) are highly prevalent and routinely cause opportunistic intracellular infectious disease in immunocompromised hosts. Methods: The activity of the triple combination of antibiotics, clarithromycin (CLR), rifabutin (RFB), and clofazimine (CFZ), was evaluated and compared with the activity of single
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Objectives: Slow-growing nontuberculous mycobacteria (NTMs) are highly prevalent and routinely cause opportunistic intracellular infectious disease in immunocompromised hosts. Methods: The activity of the triple combination of antibiotics, clarithromycin (CLR), rifabutin (RFB), and clofazimine (CFZ), was evaluated and compared with the activity of single antibiotics as well as with double combinations in an in vitro biofilm assay and an in vivo murine model of Mycobacterium avium subsp. hominissuis (M. avium) lung infection. Results: Treatment of 1-week-old biofilms with the triple combination exerted the strongest effect of all (0.12 ± 0.5 × 107 CFU/mL) in reducing bacterial growth as compared to the untreated (5.20 ± 0.5 × 107/mL) or any other combination (≥0.75 ± 0.6 × 107/mL) by 7 days. The treatment of mice intranasally infected with M. avium with either CLR and CFZ or the triple combination provided the greatest reduction in CLR-sensitive M. avium bacterial counts in both the lung and spleen compared to any single antibiotic or remaining double combination by 4 weeks posttreatment. After 4 weeks of treatment with the triple combination, there were no resistant colonies detected in mice infected with a CLR-resistant strain. No clear relationships between treatment and spleen or lung organ weights were apparent after triple combination treatment. Conclusions: The biofilm assay data and mouse disease model efficacy results support the further investigation of the triple-antibiotic combination.
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Open AccessArticle
Linalool Reduces Virulence and Tolerance to Adverse Conditions of Listeria monocytogenes
by
Joel P. Dias, Fernanda C. Domingues and Susana Ferreira
Antibiotics 2024, 13(6), 474; https://doi.org/10.3390/antibiotics13060474 - 22 May 2024
Abstract
Listeria monocytogenes, a foodborne pathogen causing listeriosis, poses substantial societal, economic, and public health challenges due to its resistance, persistence, and biofilm formation in the food industry. Exploring subinhibitory concentrations of compounds to target virulence inhibition and increase susceptibility to adverse conditions
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Listeria monocytogenes, a foodborne pathogen causing listeriosis, poses substantial societal, economic, and public health challenges due to its resistance, persistence, and biofilm formation in the food industry. Exploring subinhibitory concentrations of compounds to target virulence inhibition and increase susceptibility to adverse conditions presents a promising strategy to mitigate its impact of L. monocytogenes and unveils new potential applications. Thus, this study aims to explore the effect of linalool on virulence factors of L. monocytogenes and potential use in the reduction in its tolerance to stressful conditions. This action was analysed considering the use of two sub-inhibitory concentrations of linalool, 0.312 and 0.625 mg/mL. We found that even with the lowest tested concentrations, a 65% inhibition of violacein production by Chromobacterium violaceum, 55% inhibition in biofilm formation by L. monocytogenes and 62% reduction on haemolysis caused by this bacterium were observed. In addition to its impact on virulence factors, linalool diminished the tolerance to osmotic stress (up to 4.3 log reduction after 24 h with 12% NaCl), as well as to high (up to 3.8 log reduction after 15 min at 55 °C) and low temperatures (up to 4.6 log reduction after 84 days with 12% NaCl at 4 °C). Thus, this study paves the way to further investigation into the potential utilization of linalool to mitigate the threat posed by L. monocytogenes in the field of food safety and public health.
Full article
(This article belongs to the Special Issue Exploring Antimicrobial Properties and Bioactive Compounds of Edible and Medicinal Plants)
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Open AccessArticle
Combinations of Cannabinoids with Silver Salts or Silver Nanoparticles for Synergistic Antibiotic Effects against Methicillin-Resistant Staphylococcus aureus
by
John Jackson, Ali Shademani, Manisha Dosanjh, Claudia Dietrich, Mark Pryjma, Dana M. Lambert and Charles J. Thompson
Antibiotics 2024, 13(6), 473; https://doi.org/10.3390/antibiotics13060473 - 22 May 2024
Abstract
Silver has been shown to improve the antibiotic effects of other drugs against both Gram- positive and -negative bacteria. In this study, we investigated the antibiotic potential of cannabidiol (CBD), cannabichromene (CBC) and cannabigerol (CBG) and their acidic counterparts (CBDA, CBCA, CBGA) against
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Silver has been shown to improve the antibiotic effects of other drugs against both Gram- positive and -negative bacteria. In this study, we investigated the antibiotic potential of cannabidiol (CBD), cannabichromene (CBC) and cannabigerol (CBG) and their acidic counterparts (CBDA, CBCA, CBGA) against Gram-positive bacteria and further explored the additive or synergistic effects of silver nitrate or silver nanoparticles using 96-well plate growth assays and viability (CFUs- colony-forming units). All six cannabinoids had strong antibiotic effects against MRSA with minimal inhibitory concentrations (MICs) of 2 mg/L for CBG, CBD and CBCA; 4 mg/L for CBGA; and 8 mg/L for CBC and CBDA. Using 96-well checkerboard assays, CBC, CBG and CBGA showed full or partial synergy with silver nitrate; CBC, CBDA and CBGA were fully synergistic with silver nanoparticles against MRSA. Using CFU assays, combinations of CBC, CBGA and CBG with either silver nitrate or silver nanoparticles, all at half or quarter MICs, demonstrated strong, time-dependent inhibition of bacterial growth (silver nitrate) and bactericidal effects (silver nanoparticles). These data will lead to further investigation into possible biomedical applications of specific cannabinoids in combination with silver salts or nanoparticles against drug-resistant Gram-positive bacteria.
Full article
(This article belongs to the Special Issue Silver and Gold Compounds as Antibiotics, 2nd Volume)
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Open AccessReview
Meropenem/Vaborbactam—A Mechanistic Review for Insight into Future Development of Combinational Therapies
by
Trae Hillyer and Woo Shik Shin
Antibiotics 2024, 13(6), 472; https://doi.org/10.3390/antibiotics13060472 - 21 May 2024
Abstract
Beta-lactam antibiotics have been a major climacteric in medicine for being the first bactericidal compound available for clinical use. They have continually been prescribed since their development in the 1940s, and their application has saved an immeasurable number of lives. With such immense
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Beta-lactam antibiotics have been a major climacteric in medicine for being the first bactericidal compound available for clinical use. They have continually been prescribed since their development in the 1940s, and their application has saved an immeasurable number of lives. With such immense use, the rise in antibiotic resistance has truncated the clinical efficacy of these compounds. Nevertheless, the synergism of combinational antibiotic therapy has allowed these drugs to burgeon once again. Here, the development of meropenem with vaborbactam—a recently FDA-approved beta-lactam combinational therapy—is reviewed in terms of structure rationale, activity gamut, pharmacodynamic/pharmacokinetic properties, and toxicity to provide insight into the future development of analogous therapies.
Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery, 2nd Volume)
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