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Keywords = fluoroquinolones toxicity

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19 pages, 5275 KiB  
Article
Ciprofloxacin Exerts Anti-Tumor Effects In Vivo Through cGAS-STING Activation and Modulates Tumor Microenvironment
by Jian-Syun Chen, Chih-Wen Chi, Cheng-Ta Lai, Shu-Hua Wu, Hui-Ru Shieh, Jiin-Cherng Yen and Yu-Jen Chen
Cells 2025, 14(13), 1010; https://doi.org/10.3390/cells14131010 - 2 Jul 2025
Viewed by 539
Abstract
Immunotherapy targeting the immune functions of the tumor microenvironment (TME) is beneficial for colorectal cancer; however, the response rate is poor. Ciprofloxacin is a fluoroquinolone-class antibiotic that is used to treat bacterial infections. The purpose of this study is to assess the mechanism [...] Read more.
Immunotherapy targeting the immune functions of the tumor microenvironment (TME) is beneficial for colorectal cancer; however, the response rate is poor. Ciprofloxacin is a fluoroquinolone-class antibiotic that is used to treat bacterial infections. The purpose of this study is to assess the mechanism of ciprofloxacin that enhances anti-PD1 in colorectal cancer. We found that ciprofloxacin induced cytosolic DNA, including single-stranded and double-stranded DNA, formation in mouse CT26 colorectal adenocarcinoma cells. Molecules in DNA-sensing signaling such as cGAS, STING, and IFNβ mRNA and protein expression were elicited after ciprofloxacin treatment in CT26 cells. STING siRNA abrogated the cGAS-STING pathway activation by ciprofloxacin. In vivo, ciprofloxacin exhibited a synergistic effect with anti-PD1 to suppress tumor growth in a CT26 syngeneic animal model without biological toxicity. The examination of TME revealed that ciprofloxacin, alone and in combination therapy, induced M1 and red pulp macrophage production in the spleen. In tumors, M1 and M2 macrophage levels were increased by ciprofloxacin, and CD8+ T cell granzyme B expression was increased after combination therapy. STING showed the highest expression in tumor specimens after combination treatment. Ciprofloxacin may enhance the anti-PD1 efficacy and modulate the TME through the cGAS-STING pathway. Full article
(This article belongs to the Special Issue Cellular Mechanisms of Anti-Cancer Therapies)
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28 pages, 3054 KiB  
Review
Impact of Antibacterial Agents in Horticulture: Risks to Non-Target Organisms and Sustainable Alternatives
by Mirza Abid Mehmood, Muhammad Mazhar Iqbal, Muhammad Ashfaq, Nighat Raza, Jianguang Wang, Abdul Hafeez, Samah Bashir Kayani and Qurban Ali
Horticulturae 2025, 11(7), 753; https://doi.org/10.3390/horticulturae11070753 - 1 Jul 2025
Viewed by 708
Abstract
The global population is rising at an alarming rate and is projected to reach 10 billion by 2050, necessitating a substantial increase in food production. However, the overuse of chemical pesticides, including antibacterial agents and synthetic fertilizers, poses a major threat to sustainable [...] Read more.
The global population is rising at an alarming rate and is projected to reach 10 billion by 2050, necessitating a substantial increase in food production. However, the overuse of chemical pesticides, including antibacterial agents and synthetic fertilizers, poses a major threat to sustainable agriculture. This review examines the ecological and health impacts of antibacterial agents (e.g., streptomycin, oxytetracycline, etc.) in horticultural crops, focusing on their effects on non-target organisms such as beneficial microbes involved in plant growth promotion and resistance development. Certain agents (e.g., triclosan, sulfonamides, and fluoroquinolones) leach into water systems, degrading water quality, while others leave toxic residues in crops, leading to human health risks like dysbiosis and antibiotic resistance. To mitigate these hazards, sustainable alternatives such as integrated plant disease management (IPDM) and biotechnological solutions are essential. Advances in genetic engineering including resistance-conferring genes like EFR1/EFR2 (Arabidopsis), Bs2 (pepper), and Pto (tomato) help combat pathogens such as Ralstonia solanacearum and Xanthomonas campestris. Additionally, CRISPR-Cas9 enables precise genome editing to enhance inherent disease resistance in crops. Emerging strategies like biological control, plant-growth-promoting rhizobacteria (PGPRs), and nanotechnology further reduce dependency on chemical antibacterial agents. This review highlights the urgent need for sustainable disease management to safeguard ecosystem and human health while ensuring food security. Full article
(This article belongs to the Special Issue New Insights into Stress Tolerance of Horticultural Crops)
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22 pages, 680 KiB  
Review
Fluoroquinolones for Dermatologists: A Practical Guide to Clinical Use and Risk Management
by Samer Wahood, Omar Alani, Iyla Draw, Lara Shqair, David Wang, Christopher G. Bunick, Giovanni Damiani, Jonathan D. Ho, Sabine Obagi, Hossein Akbarialiabad, Fabrizio Galimberti, Mahmoud Ghannoum and Ayman Grada
Pharmaceuticals 2025, 18(6), 800; https://doi.org/10.3390/ph18060800 - 26 May 2025
Viewed by 1647
Abstract
Background: Fluoroquinolones, available in topical and oral formulations, are used to manage bacterial skin and soft tissue infections, including Pseudomonas aeruginosa, atypical mycobacteria, and select multidrug-resistant Gram-negative organisms. Their excellent tissue penetration, bactericidal activity, and convenient dosing make them effective for certain [...] Read more.
Background: Fluoroquinolones, available in topical and oral formulations, are used to manage bacterial skin and soft tissue infections, including Pseudomonas aeruginosa, atypical mycobacteria, and select multidrug-resistant Gram-negative organisms. Their excellent tissue penetration, bactericidal activity, and convenient dosing make them effective for certain skin and soft tissue infections. However, their use is limited by potential safety concerns, including tendinopathy (odds ratio up to 9.1 in corticosteroid users), QT interval prolongation with risk of torsades de pointes, phototoxicity, and rising antimicrobial resistance. Methods: A literature search of PubMed, Scopus, and Web of Science was conducted for articles from January 1985 to April 2025 with the search terms (quinolone OR fluoroquinolone) AND (dermatology OR “skin and soft tissue infection” OR “skin structure infection”). Abstracts and presentations were excluded. A Google search used the same terms for articles from government regulatory agencies. Results: This review provides practical guidance on the clinical use of topical and oral fluoroquinolones in dermatology. Delafloxacin demonstrated over 90% cure rates in trials for complicated skin infections. However, serious safety concerns remain, including a ninefold increase in tendinopathy risk among older adults on corticosteroids and corrected QT intervals exceeding 500 milliseconds in high-risk patients. Phototoxicity varies, with agents like sparfloxacin linked to heightened ultraviolet sensitivity. Resistance to ciprofloxacin exceeds 20 percent in Escherichia coli and P. aeruginosa in some populations. Culture-based prescribing, shorter treatment courses, and preference for topical treatments can reduce risk and preserve efficacy. Conclusions: Fluoroquinolones remain clinically useful in dermatology when prescribed selectively. Their appropriate use requires careful attention to patient risk factors along with their evolving resistance patterns and ongoing stewardship efforts. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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27 pages, 2510 KiB  
Article
Norfloxacin Oxidative Degradation and Toxicity in Aqueous Media: Reciprocal Effects of Acidity Evolution on Metal Cations and Clay Catalyst Dispersion
by Roumaissa Djidja, David Dewez and Abdelkrim Azzouz
Int. J. Mol. Sci. 2025, 26(9), 4347; https://doi.org/10.3390/ijms26094347 - 2 May 2025
Viewed by 714
Abstract
The ozonation of norfloxacin (NOF), a widely used fluoroquinolone antibiotic, in the presence of Na+, Fe2+, Cu2+, Ni2+, and Co2+ cations and their montmorillonite-supported counterparts was investigated. The NOF degradation and the toxicity of [...] Read more.
The ozonation of norfloxacin (NOF), a widely used fluoroquinolone antibiotic, in the presence of Na+, Fe2+, Cu2+, Ni2+, and Co2+ cations and their montmorillonite-supported counterparts was investigated. The NOF degradation and the toxicity of the ozonized mixtures towards an aquatic organism (Lemna minor) were evaluated in terms of changes in its frond number, chlorophyll content, photosynthesis efficacy, and production of reactive oxygen species (ROS). The evolution over time of the NOF degradation grade and the toxicity were discussed in terms of i. the observed changes in the interactions of the cation and clay catalyst with NOF molecules; ii. the pH decay, during ozonation. Ion-exchange and Lewis acid–base interactions appear to govern NOF adsorption and clay catalyst dispersion in correlation with the progressive formation of acidic species in the aqueous media. These findings reveal promising prospects for tailoring optimum oxidative water treatments with minimum toxicity and for predicting their environmental impacts on aquatic media. Full article
(This article belongs to the Section Materials Science)
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16 pages, 3371 KiB  
Article
A Prospective Randomized Pilot Study on the Efficacy of a Dietary Supplementation Regimen of Vitamin E and Selenium for the Prevention of Fluoroquinolone-Induced Tendinopathy
by Oana-Maria Mișcă, Liviu-Coriolan Mișcă, Bogdan Huzum, Andreea-Adriana Neamţu, Simona Cerbu, Daniel-Raul Chioibaș, Petrișor Zorin Crăiniceanu and Andrei Gheorghe Marius Motoc
Pharmaceuticals 2025, 18(4), 575; https://doi.org/10.3390/ph18040575 - 15 Apr 2025
Viewed by 992
Abstract
Background: Fluoroquinolone-induced tendinopathy is a clinically significant adverse effect associated with this class of antibiotics, particularly affecting the Achilles tendon. Despite its growing recognition, the precise pathophysiological mechanisms remain incompletely understood, with hypotheses referencing increased matrix metalloproteinase activity, collagen degradation, and oxidative [...] Read more.
Background: Fluoroquinolone-induced tendinopathy is a clinically significant adverse effect associated with this class of antibiotics, particularly affecting the Achilles tendon. Despite its growing recognition, the precise pathophysiological mechanisms remain incompletely understood, with hypotheses referencing increased matrix metalloproteinase activity, collagen degradation, and oxidative stress. Methods: This prospective randomized pilot study evaluates the potential protective effectiveness of vitamin E and selenium supplementation in mitigating fluoroquinolone-induced tendinopathy. The study was conducted on 25 patients receiving 500 mg/day levofloxacin antibiotherapy, randomly divided into a control group and an experimental group—vitamin E (400 IU/day) and selenium (200 µg/day), oral supplementation for 28 days. Clinical assessment of the pain level through the VAS score and of functionality through the VISA-A score was performed, alongside ultrasound imaging of the Achilles tendon. To assess potential toxicity and ensure adherence to the supplementation protocol, serial biochemical analyses of serum vitamin E and selenium were performed at predetermined intervals. Results: A significant improvement was observed in pain scores (p = 0.0120) and functional outcomes (p = 0.0340) when comparing the control and experimental groups at the three-month follow-up. Ultrasound analysis revealed reduced tendon thickness and neovascularization, supporting structural recovery. Although the incidence of tendinopathy was lower in the interventional group (13.3% vs. 40%), statistical significance was not reached, possibly due to the small sample size. Conclusions: These findings suggest that antioxidant supplementation with vitamin E and selenium may provide a protective effect against fluoroquinolone-induced tendinopathy, warranting further investigation in larger randomized clinical trials. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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16 pages, 6838 KiB  
Article
The Acute Toxicity and Cardiotoxic Effects of Levofloxacin on Zebrafish (Danio rerio)
by Yixiao Wu, Wenjing Yu, Zhenyan Song, Jiawei He, Ze Li, Qi Chen, Shiwei Wang, Ping Li and Shaowu Cheng
Toxics 2025, 13(2), 122; https://doi.org/10.3390/toxics13020122 - 5 Feb 2025
Cited by 2 | Viewed by 1732
Abstract
Emerging contaminants refer to chemical substances that have not been widely regulated but possess the potential to cause adverse effects on both the environment and human health. Antibiotics, as emerging contaminants, pose significant threats to ecosystems and human health due to their widespread [...] Read more.
Emerging contaminants refer to chemical substances that have not been widely regulated but possess the potential to cause adverse effects on both the environment and human health. Antibiotics, as emerging contaminants, pose significant threats to ecosystems and human health due to their widespread use and persistence in the environment. Levofloxacin, a broad-spectrum fluoroquinolone antibiotic, is commonly employed in the treatment of bacterial infections, and has been frequently detected in environmental matrices and freshwater systems. In this study, we assessed the effects of levofloxacin on hatchability, mortality rates, malformations, behavioral changes, and cardiac development in zebrafish embryos by exposing them to varying concentrations of levofloxacin (0, 0.5, 1, 2, 4, and 8 mM). Our results demonstrate that levofloxacin exposure significantly impaired the growth and development of zebrafish larvae, particularly at higher concentrations. Notable effects included reduced body length, abnormal yolk sac and swim bladder development, pericardial edema, prolonged distances between the sinus venosus and arteriolar bulb (SV-BA), and disruptions in heart rate. Quantitative PCR analysis further revealed that levofloxacin exposure significantly upregulated the expression of key cardiac development genes in zebrafish larvae, including nppa, myh6, cacna1ab, myl7, gata4, nkx2.5, tbx2b, and tbx5b. These findings indicate that levofloxacin exposure exerts significant toxic effects on both embryonic and larval growth as well as heart development and gene expression in zebrafish. This study provides critical insights into the potential ecological risks posed by levofloxacin along with other antibiotics while laying a foundation for further investigation into their toxicological mechanisms. Full article
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31 pages, 3989 KiB  
Review
Fluoroquinolones and Biofilm: A Narrative Review
by Nicholas Geremia, Federico Giovagnorio, Agnese Colpani, Andrea De Vito, Alexandru Botan, Giacomo Stroffolini, Dan-Alexandru Toc, Verena Zerbato, Luigi Principe, Giordano Madeddu, Roberto Luzzati, Saverio Giuseppe Parisi and Stefano Di Bella
Pharmaceuticals 2024, 17(12), 1673; https://doi.org/10.3390/ph17121673 - 11 Dec 2024
Cited by 11 | Viewed by 5470
Abstract
Background: Biofilm-associated infections frequently span multiple body sites and represent a significant clinical challenge, often requiring a multidisciplinary approach involving surgery and antimicrobial therapy. These infections are commonly healthcare-associated and frequently related to internal or external medical devices. The formation of biofilms [...] Read more.
Background: Biofilm-associated infections frequently span multiple body sites and represent a significant clinical challenge, often requiring a multidisciplinary approach involving surgery and antimicrobial therapy. These infections are commonly healthcare-associated and frequently related to internal or external medical devices. The formation of biofilms complicates treatment, as they create environments that are difficult for most antimicrobial agents to penetrate. Fluoroquinolones play a critical role in the eradication of biofilm-related infections. Numerous studies have investigated the synergistic potential of combining fluoroquinolones with other chemical agents to augment their efficacy while minimizing potential toxicity. Comparative research suggests that the antibiofilm activity of fluoroquinolones is superior to that of beta-lactams and glycopeptides. However, their activity remains less effective than that of minocycline and fosfomycin. Noteworthy combinations include fluoroquinolones with fosfomycin and aminoglycosides for enhanced activity against Gram-negative organisms and fluoroquinolones with minocycline and rifampin for more effective treatment of Gram-positive infections. Despite the limitations of fluoroquinolones due to the intrinsic characteristics of this antibiotic, they remain fundamental in this setting thanks to their bioavailability and synergisms with other drugs. Methods: A comprehensive literature search was conducted using online databases (PubMed/MEDLINE/Google Scholar) and books written by experts in microbiology and infectious diseases to identify relevant studies on fluoroquinolones and biofilm. Results: This review critically assesses the role of fluoroquinolones in managing biofilm-associated infections in various clinical settings while also exploring the potential benefits of combination therapy with these antibiotics. Conclusions: The literature predominantly consists of in vitro studies, with limited in vivo investigations. Although real world data are scarce, they are in accordance with fluoroquinolones’ effectiveness in managing early biofilm-associated infections. Also, future perspectives of newer treatment options to be placed alongside fluoroquinolones are discussed. This review underscores the role of fluoroquinolones in the setting of biofilm-associated infections, providing a comprehensive guide for physicians regarding the best use of this class of antibiotics while highlighting the existing critical issues. Full article
(This article belongs to the Special Issue Fluoroquinolones)
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23 pages, 3203 KiB  
Article
Ultrasensitive Lateral Flow Immunoassay of Fluoroquinolone Antibiotic Gatifloxacin Using Au@Ag Nanoparticles as a Signal-Enhancing Label
by Olga D. Hendrickson, Nadezhda A. Byzova, Vasily G. Panferov, Elena A. Zvereva, Shen Xing, Anatoly V. Zherdev, Juewen Liu, Hongtao Lei and Boris B. Dzantiev
Biosensors 2024, 14(12), 598; https://doi.org/10.3390/bios14120598 - 6 Dec 2024
Cited by 3 | Viewed by 1486
Abstract
Gatifloxacin (GAT), an antibiotic belonging to the fluoroquinolone (FQ) class, is a toxicant that may contaminate food products. In this study, a method of ultrasensitive immunochromatographic detection of GAT was developed for the first time. An indirect format of the lateral flow immunoassay [...] Read more.
Gatifloxacin (GAT), an antibiotic belonging to the fluoroquinolone (FQ) class, is a toxicant that may contaminate food products. In this study, a method of ultrasensitive immunochromatographic detection of GAT was developed for the first time. An indirect format of the lateral flow immunoassay (LFIA) was performed. GAT-specific monoclonal antibodies and labeled anti-species antibodies were used in the LFIA. Bimetallic core@shell Au@Ag nanoparticles (Au@Ag NPs) were synthesized as a new label. Peroxidase-mimic properties of Au@Ag NPs allowed for the catalytic enhancement of the signal on test strips, increasing the assay sensitivity. A mechanism of Au@Ag NPs-mediated catalysis was deduced. Signal amplification was achieved through the oxidative etching of Au@Ag NPs by hydrogen peroxide. This resulted in the formation of gold nanoparticles and Ag+ ions, which catalyzed the oxidation of the peroxidase substrate. Such “chemical enhancement” allowed for reaching the instrumental limit of detection (LOD, calculated by Three Sigma approach) and cutoff of 0.8 and 20 pg/mL, respectively. The enhanced assay procedure can be completed in 21 min. The enhanced LFIA was tested for GAT detection in raw meat samples, and the recoveries from meat were 78.1–114.8%. This method can be recommended as a promising instrument for the sensitive detection of various toxicants. Full article
(This article belongs to the Special Issue Nanoparticle-Based Biosensors for Detection)
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19 pages, 5566 KiB  
Article
High Performance of Ciprofloxacin Removal Using Heterostructure Material Based on the Combination of CeO2 and Palygorskite Fibrous Clay
by Vanessa N. S. Campos, Josefa D. J. P. Santos, Rebecca J. P. Araújo, Pedro H. S. Lopes, Marco A. S. Garcia, Alex Rojas, Mayara M. Teixeira, Cícero W. B. Bezerra and Ana C. S. Alcântara
Minerals 2024, 14(8), 792; https://doi.org/10.3390/min14080792 - 31 Jul 2024
Cited by 2 | Viewed by 1548
Abstract
Ciprofloxacin, a second-generation fluoroquinolone, is widely used in human and veterinary medicine. However, it is known for its environmental persistence and ability to promote bacterial resistance, causing genotoxic impacts and chronic toxicity in various aquatic life forms. Adsorption is an effective technique for [...] Read more.
Ciprofloxacin, a second-generation fluoroquinolone, is widely used in human and veterinary medicine. However, it is known for its environmental persistence and ability to promote bacterial resistance, causing genotoxic impacts and chronic toxicity in various aquatic life forms. Adsorption is an effective technique for water treatment, removing multiple organic molecules, even in minimal concentrations. Hybrid materials based on fibrous clay minerals, such as palygorskite, are promising for environmental remediation, significantly when modified with oxides to improve their adsorption properties. This work prepared and characterized a CeO2/palygorskite hybrid material using various physicochemical techniques (XRD, FTIR, BET, SEM), which indicated the formation of the heterostructure material with interesting textural properties. This CeO2/palygorskite was evaluated as an adsorbent of the antibiotic drug ciprofloxacin. The influence of pH (3, 7, and 9) and ciprofloxacin concentration (6, 8, 10, and 14 ppm) on adsorption were studied, using pseudo-first- and pseudo-second-order kinetic models. The pseudo-second-order model showed the best fit (R2 > 0.99) and the lowest squared error (SSE), indicating chemisorption. The Langmuir, Freundlich, and Temkin isotherms were applied to the experimental data, where the Langmuir model had the best fit, indicating monolayer adsorption with a maximum capacity of 15 mg·g−1. Post-adsorption characterization by FTIR confirmed the structural stability of the material, highlighting its promising application in environmental remediation due to its high concentration of adsorbents. Full article
(This article belongs to the Special Issue Applications of Clay-Based Materials)
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36 pages, 1996 KiB  
Review
A Review on Fluoroquinolones’ Toxicity to Freshwater Organisms and a Risk Assessment
by Marianna Pauletto and Marco De Liguoro
J. Xenobiot. 2024, 14(2), 717-752; https://doi.org/10.3390/jox14020042 - 4 Jun 2024
Cited by 4 | Viewed by 2702
Abstract
Fluoroquinolones (FQs) have achieved significant success in both human and veterinary medicine. However, regulatory authorities have recommended limiting their use, firstly because they can have disabling side effects; secondly, because of the need to limit the spread of antibiotic resistance. This review addresses [...] Read more.
Fluoroquinolones (FQs) have achieved significant success in both human and veterinary medicine. However, regulatory authorities have recommended limiting their use, firstly because they can have disabling side effects; secondly, because of the need to limit the spread of antibiotic resistance. This review addresses another concerning consequence of the excessive use of FQs: the freshwater environments contamination and the impact on non-target organisms. Here, an overview of the highest concentrations found in Europe, Asia, and the USA is provided, the sensitivity of various taxa is presented through a comparison of the lowest EC50s from about a hundred acute toxicity tests, and primary mechanisms of FQ toxicity are described. A risk assessment is conducted based on the estimation of the Predicted No Effect Concentration (PNEC). This is calculated traditionally and, in a more contemporary manner, by constructing a normalized Species Sensitivity Distribution curve. The lowest individual HC5 (6.52 µg L−1) was obtained for levofloxacin, followed by ciprofloxacin (7.51 µg L−1), sarafloxacin and clinafloxacin (12.23 µg L−1), and ofloxacin (17.12 µg L−1). By comparing the calculated PNEC with detected concentrations, it is evident that the risk cannot be denied: the potential impact of FQs on freshwater ecosystems is a further reason to minimize their use. Full article
(This article belongs to the Special Issue Environmental Toxicology and Animal Health)
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11 pages, 765 KiB  
Review
Drugs Associated with Adverse Effects in Vulnerable Groups of Patients
by Claudia Simona Ștefan, Aurel Nechita, Oana-Maria Dragostin, Ana Fulga, Elena-Lăcrămioara Lisă, Rodica Vatcu, Ionut Dragostin, Cristian Velicescu and Iuliu Fulga
Clin. Pract. 2024, 14(3), 1010-1020; https://doi.org/10.3390/clinpract14030080 - 31 May 2024
Cited by 1 | Viewed by 1523
Abstract
In recent years, a series of recommendations have been issued regarding the administration of drugs because of awareness of the serious side effects associated with certain classes of drugs, especially in vulnerable patients. Taking into account the obligation of the continuous improvement of [...] Read more.
In recent years, a series of recommendations have been issued regarding the administration of drugs because of awareness of the serious side effects associated with certain classes of drugs, especially in vulnerable patients. Taking into account the obligation of the continuous improvement of professionals in the medical fields and the fact that we are in the midst of a “malpractice accusations pandemic”, through this work, we propose to carry out a “radiography” of the scientific literature regarding adverse effects that may occur as a result of the interaction of drugs with the physiopathological particularities of patients. The literature reports various cases regarding different classes of drugs administration associated with adverse effects in the elderly people, such as fluoroquinolones, which can cause torsade de pointes or tendinopathy, or diuretics, which can cause hypokalemia followed by torsade de pointes and cardiorespiratory arrest. Also, children are more prone to the development of adverse reactions due to their physiological particularities, while for pregnant women, some drugs can interfere with the normal development of the fetus, and for psychiatric patients, the use of neuroleptics can cause agranulocytosis. Considering the physiopathological particularities of each patient, the drug doses must be adjusted or even completely removed from the treatment scheme, thus requiring the mandatory active participation both of clinician pharmacists and specialists in the activity of medical-pharmaceutical analysis laboratories within the structure of hospitals. Full article
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10 pages, 700 KiB  
Article
Evaluation of the Antibacterial Activity of Isatin against Campylobacter jejuni and Campylobacter coli Strains
by Claudia B. Barroso, Liliane M. Seki, Wagner T. C. Esteves, Michele C. Nascimento and Aurea Echevarria
Appl. Microbiol. 2024, 4(1), 486-495; https://doi.org/10.3390/applmicrobiol4010034 - 8 Mar 2024
Cited by 1 | Viewed by 2015
Abstract
Antibiotic resistance, particularly against fluoroquinolones and macrolides, has emerged globally among thermophilic Campylobacters (Campylobacter jejuni and Campylobacter coli), giving rise to concerns about the efficacy of antibiotic treatment of these bacteria. Thus, developing new antibacterials with excellent activity is important. Isatin [...] Read more.
Antibiotic resistance, particularly against fluoroquinolones and macrolides, has emerged globally among thermophilic Campylobacters (Campylobacter jejuni and Campylobacter coli), giving rise to concerns about the efficacy of antibiotic treatment of these bacteria. Thus, developing new antibacterials with excellent activity is important. Isatin (IST) and its derivatives have exhibited promising antibacterial activities in several pathogenic bacteria. However, its activity against Campylobacter is unknown. Therefore, this study was conducted to evaluate the antibacterial activity of isatin against 29-Campylobacter strains (C. jejuni-17 and C. coli-12) and investigate the effects at the cellular level. The minimal inhibitory concentrations (MICs) of isatin were between <1.0 and 16.0 µg/mL in Campylobacter strains. Most strains presented with MIC = 8.0 µg/mL (76%). The minimal bactericidal concentration (MBC) was determined to be 16.0 µg/mL for 72% of the Campylobacter strains tested. The 50% inhibitory concentration (IC50) value for isatin was 125.63 µg/mL on the MRC-5 normal cell line, suggesting that isatin can be considered a safe substance in terms of cytotoxicity. In this study, we demonstrated the potential of isatin based on its low toxicity and effectiveness in vitro against antibiotic-resistant Campylobacter strains, which indicates that this compound could be an attractive candidate for future use in multidrug-resistant Campylobacter treatment. Full article
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23 pages, 3719 KiB  
Article
Identification and Mechanistic Analysis of Toxic Degradation Products in the Advanced Oxidation Pathways of Fluoroquinolone Antibiotics
by Shuhai Sun, Zhonghe Wang, Qikun Pu, Xinao Li, Yuhan Cui, Hao Yang and Yu Li
Toxics 2024, 12(3), 203; https://doi.org/10.3390/toxics12030203 - 6 Mar 2024
Cited by 5 | Viewed by 2535
Abstract
The degradation of fluoroquinolones (FQs) via advanced oxidation processes (AOPs) is a promising avenue, yet the complete mineralization of certain FQ molecules remains elusive, raising concerns about the formation of toxic by-products. This study delineates five primary AOP degradation pathways for 16 commercially [...] Read more.
The degradation of fluoroquinolones (FQs) via advanced oxidation processes (AOPs) is a promising avenue, yet the complete mineralization of certain FQ molecules remains elusive, raising concerns about the formation of toxic by-products. This study delineates five primary AOP degradation pathways for 16 commercially available FQ molecules, inferred from existing literature. Density functional theory (DFT) was employed to calculate the bond dissociation energies within these pathways to elucidate the correlation between bond strength and molecular architecture. Subsequently, Comparative Molecular Similarity Index Analysis (CoMSIA) models were constructed for various degradation reactions, including piperazine ring cleavage, defluorination, hydroxylation, and piperazine ring hydroxylation. Three-dimensional contour maps generated from these models provide a deeper understanding of the interplay between FQ molecular structure and bond dissociation energy. Furthermore, toxicity predictions for 16 FQ molecules and their advanced oxidation intermediates, conducted using VEGA 1.2.3 software, indicate that degradation products from pathways P2 and P5 pose a heightened health risk relative to their parent compounds. Furthermore, the application of the Multwfn program to compute the Fukui function for FQ molecules discerns the disparity in degradation propensities, highlighting that N atoms with higher f0 values can augment the likelihood of piperazine ring cleavage. HOMO-LUMO distribution diagrams further confirm that methoxy substitution at the 1-position leads to a dilution of HOMOs on the piperazine ring and an increased energy gap for free radical reactions, diminishing the reactivity with hydroxyl radicals. This study elucidates the pivotal role of structural characteristics in FQ antibiotics for their degradation efficiency within AOPs and unveils the underlying mechanisms of bond dissociation energy disparities. The toxicity parameter predictions for FQ molecules and their intermediates offer unique perspectives and theoretical underpinnings for mitigating the use of high-risk FQs and for devising targeted degradation strategies to circumvent the generation of toxic intermediates in AOPs through molecular structure optimization. Full article
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12 pages, 645 KiB  
Article
Wastewater Characterization: Chemical Oxygen Demand or Total Organic Carbon Content Measurement?
by László Wojnárovits, Renáta Homlok, Krisztina Kovács, Anna Tegze and Ezsébet Takács
Molecules 2024, 29(2), 405; https://doi.org/10.3390/molecules29020405 - 14 Jan 2024
Cited by 17 | Viewed by 5137
Abstract
The long time (2 h) required for measurement, expensive chemicals (Ag2SO4), and toxic reagents (K2Cr2O7, HgSO4) limit the application of the standard method for measuring the oxygen equivalent of organic content [...] Read more.
The long time (2 h) required for measurement, expensive chemicals (Ag2SO4), and toxic reagents (K2Cr2O7, HgSO4) limit the application of the standard method for measuring the oxygen equivalent of organic content in wastewater (chemical oxygen demand, COD). In recent years, the COD has increasingly been replaced by the total organic carbon (TOC) parameter. Since the limit values of the pollution levels are usually given in terms of the COD, efforts are being made to find the correlation between these parameters. Several papers have published correlation analyses of COD and TOC for industrial and municipal wastewater, but the relationship has not been discussed for individual chemicals. Here, this relationship was investigated using 70 contaminants (laboratory chemicals, pharmaceuticals, and pesticides). The calculated COD values, in most cases, agreed, within ~10%, with the experimental ones; for tetracyclines and some chloroaromatic molecules, the measured values were 20–50% lower than the calculated values. The COD/TOC ratios were between 2 and 3: for macrolides, they were ~3; for fluoroquinolones and tetracyclines, they were ~2. The molecular structure dependence of the ratio necessitates the establishing of the correlation on an individual basis. In advanced oxidation processes (AOPs), the ratio changes during degradation, limiting the application of TOC instead of COD. Full article
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22 pages, 1379 KiB  
Review
Occurrence, Bioaccumulation, Metabolism and Ecotoxicity of Fluoroquinolones in the Aquatic Environment: A Review
by Mengnan Shen, Yi Hu, Ke Zhao, Chenyang Li, Binshuo Liu, Ming Li, Chen Lyu, Lei Sun and Shuang Zhong
Toxics 2023, 11(12), 966; https://doi.org/10.3390/toxics11120966 - 29 Nov 2023
Cited by 27 | Viewed by 4114
Abstract
In recent years, there has been growing concern about antibiotic contamination in water bodies, particularly the widespread presence of fluoroquinolones (FQs), which pose a serious threat to ecosystems due to their extensive use and the phenomenon of “pseudo-persistence”. This article provides a comprehensive [...] Read more.
In recent years, there has been growing concern about antibiotic contamination in water bodies, particularly the widespread presence of fluoroquinolones (FQs), which pose a serious threat to ecosystems due to their extensive use and the phenomenon of “pseudo-persistence”. This article provides a comprehensive review of the literature on FQs in water bodies, summarizing and analyzing contamination levels of FQs in global surface water over the past three years, as well as the bioaccumulation and metabolism patterns of FQs in aquatic organisms, their ecological toxicity, and the influencing factors. The results show that FQs contamination is widespread in surface water across the surveyed 32 countries, with ciprofloxacin and norfloxacin being the most heavy contaminants. Furthermore, contamination levels are generally higher in developing and developed countries. It has been observed that compound types, species, and environmental factors influence the bioaccumulation, metabolism, and toxicity of FQs in aquatic organisms. FQs tend to accumulate more in organisms with higher lipid content, and toxicity experiments have shown that FQs exhibit the highest toxicity to bacteria and the weakest toxicity to mollusk. This article summarizes and analyzes the current research status and shortcomings of FQs, providing guidance and theoretical support for future research directions. Full article
(This article belongs to the Special Issue Innovative Strategies to Decompose Pollutants)
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