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Antibacterial Activity of Drug-Resistant Strains

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

Deadline for manuscript submissions: closed (25 December 2023) | Viewed by 12508

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Special Issue Editors

Dr. Rosa Sessa

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Guest Editor

Department of Public Health and Infectious Diseases, “Sapienza” University, 00185 Rome, Italy
Interests: identification of host defence factors towards C. trachomatis genital infection; study of C. trachomatis role in the pathogenesis of male infertility; study of chlamydia-host cell interaction; identification of new anti-chlamydial drugs; study of the etiopathogenic role Chlamydia pneumoniae in the chronic inflammatory diseases
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Dr. Simone Filardo

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Guest Editor

Department of Public Health and Infectious Diseases, “Sapienza” University, 00185 Rome, Italy
Interests: human microbiota; bioinformatic analysis; host-pathogen interactions; identification of novel antimicrobial molecules; study of C. trachomatis pathogenesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibacterial resistance is one of the greatest threats to human health, resulting in an increased number of deaths due to once curable infectious diseases. Indeed, the emergence of drug-resistant bacteria has been prioritized by the World Health Organization as one of the top ten public health problem worldwide. Over the years, the widespread misuse and overuse of antibiotics in the human, animal and environmental domains, has led to the global rapid spread of multi-drug resistant pathogens, beginning with the emergence of methicillin-resistant Staphylococcus aureus. The following appearance of extended-spectrum beta-lactamase (ESBL)-producing Enterobacteriaceae all over the globe, including some Escherichia coli strains and the ESKAPE pathogens, has further limited the treatment options at our disposal. In addition, other emerging bacterial pathogens, like intracellular bacteria, are acquiring increasing resistance to standard treatments, hence the needs for novel molecules. The aim of this Special Issue is to encourage original articles tackling this current issue, including the antibacterial activity of novel compounds as well as the molecular mechanisms underlying the antibiotic resistance for the discovery of new promising targets.

Dr. Rosa Sessa
Dr. Simone Filardo
Guest Editors

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Keywords

antibacterial activity
novel antimicrobial agents
drug-resistant strains
molecular mechanisms
emerging drug-resistant pathogens
genetic determinants
impact of MDR pathogens on human health
molecular methods for the diagnosis of antibiotic-resistance

Published Papers (9 papers)

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Editorial

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4 pages, 169 KiB

Open AccessEditorial

Editorial for the Special Issue “Antibacterial Activity of Drug-Resistant Strains”

by Marisa Di Pietro, Simone Filardo and Rosa Sessa

Int. J. Mol. Sci. 2024, 25(3), 1878; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms25031878 - 04 Feb 2024

Viewed by 627

Abstract

Antimicrobial resistance is an urgent global public health threat, as approximately 700,000 deaths annually can be attributed to antibiotic-resistant bacterial infections, and this figure is expected to reach 10 million deaths/year by 2050, a number that greatly exceeds the number of deaths resulting [...] Read more.

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

Research

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9 pages, 759 KiB

Open AccessCommunication

Pharmacokinetic and Pharmacodynamic Analysis of the Oxacephem Antibiotic Flomoxef against Extended-Spectrum β-Lactamase-Producing Enterobacterales from Dogs

by Mizuki Kusumoto, Makoto Jitsuiki, Tomoki Motegi and Kazuki Harada

Int. J. Mol. Sci. 2024, 25(2), 1105; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms25021105 - 16 Jan 2024

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Abstract

Flomoxef (FMX) may be a potential alternative to carbapenems for dogs infected with Enterobacterales-producing extended-spectrum β-lactamase (ESBL-E). However, the appropriate dosage of FMX in dogs with ESBL-E infections has yet to be established. This study was carried out to establish appropriate treatment regimens for FMX against ESBL-E infections in dogs using a pharmacokinetics–pharmacodynamics (PK–PD) approach. Five dogs were intravenously administered at a bolus dose of FMX (40 mg/kg body weight). Serum concentrations of FMX were calculated with high-performance liquid chromatography-tandem mass spectrometry, and then applied to determine PK indices based on a non-compartmental model. The cumulative fraction of response (CFR) was estimated based on the dissemination of minimum inhibitory concentrations among wild-type ESBL-E from companion animals. From the results, the dosage regimens of 40 mg/kg every 6 and 8 h were estimated to attain a CFR of >90% for wild-type isolates of ESBL-producing Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis for dogs. By contrast, all regimens had a CFR of <80% for ESBL-producing Enterobacter cloacae. Our results indicated that dosage regimens of 40 mg/kg FMX every 6 and 8 h can be a non-carbapenem treatment for canine infections of ESBL-producing Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis, but not for those of ESBL-producing Enterobacter cloacae. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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10 pages, 809 KiB

Open AccessArticle

Evaluation of Biological Equivalence for Generic Tulathromycin Injections in Cattle

by JeongWoo Kang, HyunYoung Chae, SungHoon Jeong, Rokeya Pervin and Md Akil Hossain

Int. J. Mol. Sci. 2023, 24(22), 16262; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms242216262 - 13 Nov 2023

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Abstract

The recent expiration of patents for the antibiotic tulathromycin has led to a significant increase in the number of generic tulathromycin products (GTPs) available. This study aims to evaluate the bioequivalence of four GTPs, which experienced a rapid increase in market share. The bioequivalence was evaluated by performing pharmacokinetic assessments. The four selected GTPs (Tulaject, Tulagen, Toulashot, and T-raxxin) were compared with the reference product, Draxxin. A dose of 2.5 mg/kg.bw/day was administered via subcutaneous injection, and blood samples were collected 460 times from 20 Holstein cattle. Plasma concentrations of tulathromycin were measured over time using LC-MS/MS analysis. Bioequivalence was evaluated using a statistical program for pharmacokinetic parameters, including the area under the concentration time curve (AUC) and the maximum plasma concentration (C_max). The bioequivalence was considered proven if the difference between the test and reference products was within 20% for both AUC and C_max. The results showed that the confidence interval (CI, 90%) for both AUC and C_max values was within the 80~120% range, demonstrating the bioequivalence of the four GTPs compared to Draxxin. This study provides evidence for the bioequivalence of the selected GTPs, contributing to their validation for use as effective antibiotics. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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13 pages, 4418 KiB

Open AccessArticle

Whole-Genome Sequencing-Based Profiling of Antimicrobial Resistance Genes and Core-Genome Multilocus Sequence Typing of Campylobacter jejuni from Different Sources in Lithuania

by Jurgita Aksomaitiene, Aleksandr Novoslavskij and Mindaugas Malakauskas

Int. J. Mol. Sci. 2023, 24(21), 16017; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms242116017 - 06 Nov 2023

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Abstract

Campylobacter jejuni is known as one of the main causative agents of gastroenteritis in humans worldwide, and the rise of antimicrobial resistance (AMR) in Campylobacter is a growing public health challenge of special concern. Whole-genome sequencing (WGS) was used to characterize genetic determinants of AMR in 53 C. jejuni isolates from dairy cattle, broiler products, wild birds, and humans in Lithuania. The WGS-based study revealed 26 C. jejuni AMR markers that conferred resistance to various antimicrobials. Genetic markers associated with resistance to beta-lactamases, tetracycline, and aminoglycosides were found in 79.3%, 28.3%, and 9.4% of C. jejuni isolates, respectively. Additionally, genetic markers associated with multidrug resistance (MDR) were found in 90.6% of C. jejuni isolates. The WGS data analysis revealed that a common mutation in the quinolone resistance-determining region (QRDR) was R285K (854G > A) at 86.8%, followed by A312T (934G > A) at 83% and T86I (257C > T) at 71.7%. The phenotypic resistance analysis performed with the agar dilution method revealed that ciprofloxacin (CIP) (90.6%), ceftriaxone (CRO) (67.9%), and tetracycline (TET) (45.3%) were the predominant AMR patterns. MDR was detected in 41.5% (22/53) of the isolates tested. Fifty-seven virulence genes were identified in all C. jejuni isolates; most of these genes were associated with motility (n = 28) and chemotaxis (n = 10). Additionally, all C. jejuni isolates harbored virulence genes related to adhesion, invasion, LOS, LPS, CPS, transportation, and CDT. In total, 16 sequence types (STs) and 11 clonal complexes (CC) were identified based on core-genome MLST (cgMLST) analysis. The data analysis revealed distinct diversity depending on phenotypic and genotypic antimicrobial resistance of C. jejuni. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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17 pages, 3805 KiB

Open AccessArticle

Hydroquinine Inhibits the Growth of Multidrug-Resistant Pseudomonas aeruginosa via the Suppression of the Arginine Deiminase Pathway Genes

by Sattaporn Weawsiangsang, Nontaporn Rattanachak, Touchkanin Jongjitvimol, Theerasak Jaifoo, Pensri Charoensit, Jarupa Viyoch, Sukunya Ross, Gareth M. Ross, Robert A. Baldock and Jirapas Jongjitwimol

Int. J. Mol. Sci. 2023, 24(18), 13914; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms241813914 - 10 Sep 2023

Cited by 1 | Viewed by 1800

Abstract

Hydroquinine has antimicrobial potential with demonstrated activity against several bacteria, including multidrug-resistant (MDR) P. aeruginosa reference strains. Despite this, there is limited evidence confirming the antibacterial activity of hydroquinine against clinical isolates and the underlying mechanism of action. Here, we aimed to investigate the antibacterial effect of hydroquinine in clinical P. aeruginosa strains using phenotypic antimicrobial susceptibility testing and synergistic testing. In addition, we examined the potential inhibitory mechanisms against MDR P. aeruginosa isolates using informatic-driven molecular docking analysis in combination with RT-qPCR. We uncovered that hydroquinine inhibits and kills clinical P. aeruginosa at 2.50 mg/mL (MIC) and 5.00 mg/mL (MBC), respectively. Hydroquinine also showed partial synergistic effects with ceftazidime against clinical MDR P. aeruginosa strains. Using SwissDock, we identified potential interactions between arginine deiminase (ADI)-pathway-related proteins and hydroquinine. Furthermore, using RT-qPCR, we found that hydroquinine directly affects the mRNA expression of arc operon. We demonstrated that the ADI-related genes, including the arginine/ornithine antiporter (arcD) and the three enzymes (arginine deiminase (arcA), ornithine transcarbamylase (arcB), and carbamate kinase (arcC)), were significantly downregulated at a half MIC of hydroquinine. This study is the first report that the ADI-related proteins are potential molecular targets for the inhibitory effect of hydroquinine against clinically isolated MDR P. aeruginosa strains. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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15 pages, 5065 KiB

Open AccessArticle

Extra Virgin Olive Oil-Based Formulations: A “Green” Strategy against Chlamydia trachomatis

by Marisa Di Pietro, Simone Filardo, Roberto Mattioli, Giuseppina Bozzuto, Agnese Molinari, Luciana Mosca and Rosa Sessa

Int. J. Mol. Sci. 2023, 24(16), 12701; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms241612701 - 11 Aug 2023

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Abstract

In recent decades, antibiotic misuse has emerged as an important risk factor for the appearance of multi-drug-resistant bacteria, and, recently, antimicrobial resistance has also been described in Chlamydia trachomatis as the leading cause of bacterial sexually transmitted diseases worldwide. Herein, we investigated, for the first time, the antibacterial activity against C. trachomatis of a polyphenolic extract of extra virgin olive oil (EVOO), alongside purified oleocanthal and oleacein, two of its main components, in natural deep eutectic solvent (NaDES), a biocompatible solvent. The anti-chlamydial activity of olive-oil polyphenols (OOPs) was tested in the different phases of chlamydial developmental cycle by using an in vitro infection model. Transmission and scanning electron microscopy analysis were performed for investigating potential alterations of adhesion and invasion, as well as morphology, of chlamydial elementary bodies (EBs) to host cells. The main result of our study is the anti-bacterial activity of OOPs towards C. trachomatis EBs down to a total polyphenol concentration of 1.7 μg/mL, as shown by a statistically significant decrease (93.53%) of the total number of chlamydial-inclusion-forming units (p < 0.0001). Transmission and scanning electron microscopy analysis supported its anti-chlamydial effect, suggesting that OOP might damage the chlamydial outer layers, impairing their structural integrity and hindering EB capability to infect the host cell. In conclusion, OOPs may represent an interesting alternative therapeutic option toward C. trachomatis, although further studies are necessary for exploring its clinical applications. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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20 pages, 5282 KiB

Open AccessArticle

Detection of Antibiotic Resistance in Feline-Origin ESBL Escherichia coli from Different Areas of China and the Resistance Elimination of Garlic Oil to Cefquinome on ESBL E. coli

by Yin-Chao Tong, Peng-Cheng Li, Yang Yang, Qing-Yi Lin, Jin-Tong Liu, Yi-Nuo Gao, Yi-Ning Zhang, Shuo Jin, Su-Zhu Qing, Fu-Shan Xing, Yun-Peng Fan, Ying-Qiu Liu, Wei-Ling Wang, Wei-Min Zhang and Wu-Ren Ma

Int. J. Mol. Sci. 2023, 24(11), 9627; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24119627 - 01 Jun 2023

Cited by 1 | Viewed by 1584

Abstract

The development of drug-resistance in the opportunistic pathogen Escherichia coli has become a global public health concern. Due to the share of similar flora between pets and their owners, the detection of pet-origin antibiotic-resistant E. coli is necessary. This study aimed to detect the prevalence of feline-origin ESBL E. coli in China and to explore the resistance elimination effect of garlic oil to cefquinome on ESBL E. coli. Cat fecal samples were collected from animal hospitals. The E. coli isolates were separated and purified by indicator media and polymerase chain reaction (PCR). ESBL genes were detected by PCR and Sanger sequencing. The MICs were determined. The synergistic effect of garlic oil and cefquinome against ESBL E. coli was investigated by checkerboard assays, time-kill and growth curves, drug-resistance curves, PI and NPN staining, and a scanning electronic microscope. A total of 80 E. coli strains were isolated from 101 fecal samples. The rate of ESBL E. coli was 52.5% (42/80). The prevailing ESBL genotypes in China were CTX-M-1, CTX-M-14, and TEM-116. In ESBL E. coli, garlic oil increased the susceptibility to cefquinome with FICIs from 0.2 to 0.7 and enhanced the killing effect of cefquinome with membrane destruction. Resistance to cefquinome decreased with treatment of garlic oil after 15 generations. Our study indicates that ESBL E. coli has been detected in cats kept as pets. The sensitivity of ESBL E. coli to cefquinome was enhanced by garlic oil, indicating that garlic oil may be a potential antibiotic enhancer. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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Review

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Open AccessReview

Research Progress of Benzothiazole and Benzoxazole Derivatives in the Discovery of Agricultural Chemicals

by Yue Zou, Yong Zhang, Xing Liu, Hongyi Song, Qingfeng Cai, Sheng Wang, Chongfen Yi and Jixiang Chen

Int. J. Mol. Sci. 2023, 24(13), 10807; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms241310807 - 28 Jun 2023

Cited by 6 | Viewed by 1580

Abstract

Benzoxazole and benzothiazole have a broad spectrum of agricultural biological activities, such as antibacterial, antiviral, and herbicidal activities, which are important fused heterocyclic scaffold structures in agrochemical discovery. In recent years, great progress has been made in the research of benzoxazoles and benzothiazoles, especially in the development of herbicides and insecticides. With the widespread use of benzoxazoles and benzothiazoles, there may be more new products containing benzoxazoles and benzothiazoles in the future. We systematically reviewed the application of benzoxazoles and benzothiazoles in discovering new agrochemicals in the past two decades and summarized the antibacterial, fungicidal, antiviral, herbicidal, and insecticidal activities of the active compounds. We also discussed the structural–activity relationship and mechanism of the active compounds. This work aims to provide inspiration and ideas for the discovery of new agrochemicals based on benzoxazole and benzothiazole. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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44 pages, 1086 KiB

Open AccessReview

Current State of Knowledge Regarding WHO High Priority Pathogens—Resistance Mechanisms and Proposed Solutions through Candidates Such as Essential Oils: A Systematic Review

by Mirabela Romanescu, Camelia Oprean, Adelina Lombrea, Bianca Badescu, Ana Teodor, George D. Constantin, Minodora Andor, Roxana Folescu, Delia Muntean, Corina Danciu, Olivia Dalleur, Stefan Laurentiu Batrina, Octavian Cretu and Valentina Oana Buda

Int. J. Mol. Sci. 2023, 24(11), 9727; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24119727 - 04 Jun 2023

Cited by 8 | Viewed by 2366

Abstract

Combating antimicrobial resistance (AMR) is among the 10 global health issues identified by the World Health Organization (WHO) in 2021. While AMR is a naturally occurring process, the inappropriate use of antibiotics in different settings and legislative gaps has led to its rapid progression. As a result, AMR has grown into a serious global menace that impacts not only humans but also animals and, ultimately, the entire environment. Thus, effective prophylactic measures, as well as more potent and non-toxic antimicrobial agents, are pressingly needed. The antimicrobial activity of essential oils (EOs) is supported by consistent research in the field. Although EOs have been used for centuries, they are newcomers when it comes to managing infections in clinical settings; it is mainly because methodological settings are largely non-overlapping and there are insufficient data regarding EOs’ in vivo activity and toxicity. This review considers the concept of AMR and its main determinants, the modality by which the issue has been globally addressed and the potential of EOs as alternative or auxiliary therapy. The focus is shifted towards the pathogenesis, mechanism of resistance and activity of several EOs against the six high priority pathogens listed by WHO in 2017, for which new therapeutic solutions are pressingly required. Full article

(This article belongs to the Special Issue Antibacterial Activity of Drug-Resistant Strains)

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