Cryochemical modification, activity, and toxicity of dioxidine

Vernaya, O. I.; Шабатин, В. П.; Шабатина, Т. И.; Khvatov, D. I.; Semenov, A. M.; Yudina, T. P.; Danilov, V.S.

doi:10.1134/s0036024417020339

Cited by 12 publications

(5 citation statements)

References 11 publications

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“…The drug substance particles were micronized, and silver or copper nanoparticles were incorporated into the dioxidine particles during cryogenic synthesis procedure. FTIR spectra of the systems obtained were similar to cryomodified form of dioxidine obtained via cryogenic freeze drying method [16,21,22]. The band corresponding to the vibrations of quinoxaline ring was at 1510 cm −1 ; the bands corresponding to the vibrations of the C-H bonds of the benzene rings were registered at 975, 1130, and 1160 cm −1 ; the band of C-O-H vibrations was observed at 1288 cm −1 .…”

Section: Resultsmentioning

confidence: 66%

“…X-ray diffraction patterns and the set of interplanar spacings (d, Å) and their intensities (I rel , %) corresponded to the cryomodified form of dioxidine [21,22] The UV-visible spectra of aqueous solutions of Ag/dioxidine and Cu/dioxidine composites also were corresponded to dioxidine. An intense absorption band at 250 nm, attributed to the π → π* electron transition of the carbon atoms of the aromatic system, was observed in UV spectra, along with a band at 375 nm characterized by low intensity and attributed to the n → π* transition.…”

Section: Resultsmentioning

confidence: 98%

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Metal Nanoparticle Containing Nanocomposites of Drug Substances and Their Potential Biomedical Applications

et al. 2019

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New hybrid nanosystems containing the antibacterial substances dioxidine or gentamicin sulfate with bioactive metal (Ag, Cu) nanoparticles have been obtained by a cryogenic freeze-drying method and incorporate further the nanocomposites thus obtained into the cryogenically structured biopolymeric matrices based on gelatin, calcium alginate, and chitosan. FTIR, UV-visible, and NMR spectroscopy, TEM and SEM microscopy data show that the resulting systems consist of wide-porous polymer sponges (pore diameters, 10–200 μm) that contain antibacterial drugs and silver (2–30 nm) or copper (1–5 nm) nanoparticles. The investigation showed that these systems ensure a gradual release of dioxidine (from 40 min up to 3 days), depending on the nature of the matrix and its microstructure. The higher activity of hybrid composites based on nanometals and dioxidine or incorporated into cryostructured biopolymer matrices against the bacterial strains of Escherichia coli 52, Staphylococcus aureus 144 is demonstrated as compared to the individual components in the same matrices.

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Section: Resultsmentioning

confidence: 66%

Section: Resultsmentioning

confidence: 98%

Metal Nanoparticle Containing Nanocomposites of Drug Substances and Their Potential Biomedical Applications

et al. 2019

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“…Ag NPs hold promises with their strong bactericidal potential against the emerging MDRs (Geilich et al, 2015). The particle size and surface properties of Ag NPs can be tailored through various methods such as spark discharging (Abd El-Aal et al, 2018), electrochemical reduction (Zhang et al, 2002), laser ablation (Boutinguiza et al, 2015), cryochemical synthesis (Vernaya et al, 2017) and green synthesis (Wypij et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of bactericidal effects of silver hydrosol nanotherapeutics against Enterococcus faecium 1449 drug resistant biofilms

Limayem

Mehta

Kondos

et al. 2023

Front. Cell. Infect. Microbiol.

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IntroductionSilver (Ag) nanoparticles (NPs) are well documented for their broad-spectrum bactericidal effects. This study aimed to test the effect of bioactive Ag-hydrosol NPs on drug-resistant E. faecium 1449 strain and explore the use of artificial intelligence (AI) for automated detection of the bacteria.MethodsThe formation of E. faecium 1449 biofilms in the absence and presence of Ag-hydrosol NPs at different concentrations ranging from 12.4 mg/L to 123 mg/L was evaluated using a 3-dimentional culture system. The biofilm reduction was evaluated using the confocal microscopy in addition to the Transmission Electronic Microscopy (TEM) visualization and spectrofluorimetric quantification using a Biotek Synergy Neo2 microplate reader. The cytotoxicity of the NPs was evaluated in human nasal epithelial cells using the MTT assay. The AI technique based on Fast Regional Convolutional Neural Network architecture was used for the automated detection of the bacteria.ResultsTreatment with Ag-hydrosol NPs at concentrations ranging from 12.4 mg/L to 123 mg/L resulted in 78.09% to 95.20% of biofilm reduction. No statistically significant difference in biofilm reduction was found among different batches of Ag-hydrosol NPs. Quantitative concentration-response relationship analysis indicated that Ag-hydrosol NPs exhibited a relative high anti-biofilm activity and low cytotoxicity with an average EC50 and TC50 values of 0.0333 and 6.55 mg/L, respectively, yielding an average therapeutic index value of 197. The AI-assisted TEM image analysis allowed automated detection of E. faecium 1449 with 97% ~ 99% accuracy.DiscussionConclusively, the bioactive Ag-hydrosol NP is a promising nanotherapeutic agent against drug-resistant pathogens. The AI-assisted TEM image analysis was developed with the potential to assess its treatment effect.

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“…Carbadox (CARB, Figure 1, 1) is an approved veterinary antibacterial agent used in the United States as a feed additive for the control and prevention of swine dysentery, helminthiasis and enteritis [5,9]. 2,3-Bis(hydroxymethyl)quinoxaline 1,4-dioxide (dioxidine, DIOX, 2, Figure 1) is another derivative of quinoxaline 1,4-dioxide, which has found an application in the medical practice as effective antibacterial drug with a broad spectrum of antimicrobial activity [10]. Moreover, some quinoxaline 1,4-dioxides have demonstrated promising anti-yeast activity on Candida albicans, C. glabrata, C. krusei, Saccharomyces cerevisiae and the clinically important C. parapsilosis [11].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Novel 2-Acyl-3-trifluoromethylquinoxaline 1,4-Dioxides as Potential Antimicrobial Agents

et al. 2022

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The emergence of drug resistance in pathogens leads to a loss of effectiveness of antimicrobials and complicates the treatment of bacterial infections. Quinoxaline 1,4-dioxides represent a prospective scaffold for search of new compounds with improved chemotherapeutic characteristics. Novel 2-acyl-3-trifluoromethylquinoxaline 1,4-dioxides with alteration of substituents at position 2 and 6 were synthesized via nucleophilic substitution with piperazine moiety and evaluated against a broad panel of bacteria and fungi by measuring their minimal inhibitory concentrations. Their mode of action was assessed by whole-genomic sequencing of spontaneous drug-resistant Mycobacterium smegmatis mutants, followed by comparative genomic analysis, and on an original pDualrep2 system. Most of the 2-acyl-3-trifluoromethylquinoxaline 1,4-dioxides showed high antibacterial properties against Gram-positive strains, including mycobacteria, and the introduction of a halogen atom in the position 6 of the quinoxaline ring further increased their activity, with 13c being the most active compound. The mode of action studies confirmed the DNA-damaging nature of the obtained quinoxaline 1,4-dioxides, while drug-resistance may be provided by mutations in redox homeostasis genes, encoding enzymes potentially involved in the activation of the compounds. This study extends views about the antimicrobial and antifungal activities of the quinoxaline 1,4-dioxides and can potentially lead to the discovery of new antibacterial drugs.

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Cryochemical modification, activity, and toxicity of dioxidine

Cited by 12 publications

References 11 publications

Metal Nanoparticle Containing Nanocomposites of Drug Substances and Their Potential Biomedical Applications

Metal Nanoparticle Containing Nanocomposites of Drug Substances and Their Potential Biomedical Applications

Evaluation of bactericidal effects of silver hydrosol nanotherapeutics against Enterococcus faecium 1449 drug resistant biofilms

Synthesis and Characterization of Novel 2-Acyl-3-trifluoromethylquinoxaline 1,4-Dioxides as Potential Antimicrobial Agents

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