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Water Research Dec 2023Two-dimensional materials are widely used in membrane separation, but the loose distribution and severe expansion between graphene oxide (GO) nanosheets limit its...
Two-dimensional materials are widely used in membrane separation, but the loose distribution and severe expansion between graphene oxide (GO) nanosheets limit its application. Here, we introduce a two-dimensional MOF material into the GO membrane to enhance its water permeance and separation performance. The MOF/GO composite membrane was prepared by vacuum filtration. The MOF and GO nanosheets were tightly stacked through the π-π effect, and the shortened transmission path and enhanced pore structure greatly improved the water permeance of the composite membrane. The MOF/GO membrane exhibited a high water permeance of 56.94 L m h bar. The rejection rates of methylene blue and was as methyl orange dyes were as high as 99.79% and 99.11%, respectively. At increased dye concentration, the rejection rate of methylene blue was still maintained greater than 99%. Dye rejection after 18 h of continuous operation remains above 90%. This work provides new ideas for improving membrane separation materials. The combination of two-dimensional heterogeneous materials can result in synergistic advantages for the development of composite membranes with high water permeance and high rejection rate.
Topics: Methylene Blue; Coloring Agents; Filtration; Water
PubMed: 37976627
DOI: 10.1016/j.watres.2023.120693 -
Current Drug Discovery Technologies Sep 2023This research work aimed to design and synthesize some new molecules of phenothiazine. The work's emphasis was on forming new phenothiazines in two series,...
AIM
This research work aimed to design and synthesize some new molecules of phenothiazine. The work's emphasis was on forming new phenothiazines in two series, 1-(10H-phenothiazin-10-yl)-2-((4-(1-(phenylimino)ethyl)phenyl)amino)ethan-1-one derivatives (4a-4j) and 1-(4-((2-oxo-2-(10H-phenothiazin-10-yl)ethyl)amino)phenyl)-3-phenylprop-2-en-1-one derivatives (P1-P5).
METHODS
Chloroacetylation of phenothiazine was done to afford 2-chloro-1-(10H-phenothiazin-10-yl)ethan-1-one, which was further reacted with 4-amino acetophenone to produce 2-((4-acetylphenyl)amino)-1-(10H-phenothiazin-10-yl)ethan-1-one. Then, it was treated with substituted anilines and substituted benzaldehydes to produce the final derivatives 4a-4j and P1-P5, respectively.
RESULTS
All 15 derivatives (4a-4j and P1-P5) were characterized by evaluating their Rf value, melting point, solubility, IR spectroscopy, and 1HNMR spectroscopy. Molecular docking was performed by using AutoDock Vina v.1.2.0 (The Scripps Research Institute, La Jolla, CA, USA) docking software, and the anxiolytic activity of the derivatives was assessed by using the elevated plus maze model.
CONCLUSION
The designed scheme was executed in the departmental laboratory. The chemical structure of the compounds was confirmed on the basis of TLC, IR, and 1HNMR analyses. The docking study revealed a good docking score of the compounds. The Log P value of the compounds indicated their good penetration into CNS. The compounds were also screened for anxiolytic activity. Among them, compounds 4f, 4h, and P3 showed maximum activity as anti-anxiolytic agents.
PubMed: 37723630
DOI: 10.2174/1570163820666230918100218 -
Molecules (Basel, Switzerland) May 2020This mini-review summarizes the syntheses and functionalizations of dithieno[1,4]thiazines and bis[1]benzothieno[1,4]thiazines, both electron density-enriched congeners... (Review)
Review
This mini-review summarizes the syntheses and functionalizations of dithieno[1,4]thiazines and bis[1]benzothieno[1,4]thiazines, both electron density-enriched congeners of phenothiazines with remarkable electronic properties. Diversity-oriented, straightforward, and efficient syntheses, including versatile one-pot processes, have been developed for the anellated 1,4-thiazines as well as various functionalization for the expansion of the π-systems. Thereby, syntheses of different regioisomers depending on the (benzo)thieno-thiazine anellation are discussed, which exert a deep impact on the electronic properties. The tunable photophysical and electrochemical properties of dithieno[1,4]thiazines and bis[1]benzothieno[1,4]thiazines outscore phenothiazines on many points and promise an enormous potential in molecular electronics and applications beyond.
Topics: Electrons; Heterocyclic Compounds; Organometallic Compounds; Phenothiazines; Protein Isoforms; Thiazines
PubMed: 32392728
DOI: 10.3390/molecules25092180 -
Spectrochimica Acta. Part A, Molecular... Nov 2021Bifunctional fluorescent probes with dual-emission response attract extensive attention. A novel fluorescent probe FP, a hybrid of fluoran and phenothiazine, has been...
Bifunctional fluorescent probes with dual-emission response attract extensive attention. A novel fluorescent probe FP, a hybrid of fluoran and phenothiazine, has been designed and synthesized for selective sensing of Fe and ClO with dual-emission changes, which involes mechanisms of Fe-promoted spirolactone ring opening and ClO-induced oxidation of phenothiazine moiety, respectively. In addition, the detection limits for Fe and ClO were estimated to be 49.1 and 35.9 nM, respectively. Significantly, FP can be employed as an tracer for the detection of Fe ions within living HeLa cells by fluorescence imaging.
Topics: Fluoresceins; Fluorescent Dyes; HeLa Cells; Humans; Hypochlorous Acid; Ions; Optical Imaging; Phenothiazines
PubMed: 34146825
DOI: 10.1016/j.saa.2021.120061 -
Journal of Veterinary Emergency and... Nov 2021To determine the effects of time after sampling on CO-oximetry measurements of equine blood samples and the effects of adding ascorbic acid (AscAc) and methylene blue...
OBJECTIVES
To determine the effects of time after sampling on CO-oximetry measurements of equine blood samples and the effects of adding ascorbic acid (AscAc) and methylene blue (MetBlue) to samples with methemoglobinemia.
DESIGN
Experimental study.
SETTING
University teaching hospital.
ANIMALS
Thirty healthy adult horses assigned to 5 groups.
INTERVENTIONS
Repeated CO-oximetry determinations were performed on venous (n = 6) and arterial blood samples (n = 7) stored at 0°C for 48 hours. Methemoglobinemia was induced in vitro in 17 additional blood samples. Six were used as untreated controls, 6 had AscAc added, and 5 had MetBlue added. Total hemoglobin, oxyhemoglobin, carboxyhemoglobin, methemoglobin (MetHb), and oxygen saturation of hemoglobin (SO ) were measured.
MEASUREMENTS AND MAIN RESULTS
Oxyhemoglobin and SO increased from 69.8% ± 10.2% and 90% ± 3% to 82.8% ± 7.9% and 99% ± 3%, respectively, after 8 hours in venous blood (mean ± SD, P < 0.001). There was an effect of treatment (P = 0.032) and of time (interaction P = 0.003) on MetHb% in methemoglobinemic samples. The difference in absolute MetHb% from time 0 was as follows: 7.0% (interquartile range [IQR] = 21.2), -0.2% (IQR = 3.5), and -4.4% (IQR = 5.2) at 48 hours in control, AscAc, and MetBlue groups, respectively (P < 0.05). There was no effect of time on MetHb% in the AscAc group (23% [IQR = 52.6] at time 0 to 23.2% [IQR = 56.9] after 48 h).
CONCLUSIONS
Storage of blood in ice water to determine O Hb and SO using a CO-oximeter should not exceed 4 hours. Measurement of MetHb% could be delayed by up to 48 hours if AscAc is added to the sample. MetBlue significantly decreased MetHb% over time. The limitations of this study include the fact that the antioxidant effects of AscAc and MetBlue were evaluated in vitro and not in vivo. Further studies are needed to evaluate different storage temperatures and syringe types.
Topics: Animals; Antioxidants; Ascorbic Acid; Horses; Methylene Blue; Oximetry; Oxygen Saturation
PubMed: 34427385
DOI: 10.1111/vec.13089 -
Communications Biology Mar 2022Bacterial persister cells are temporarily tolerant to bactericidal antibiotics but are not necessarily dormant and may exhibit physiological activities leading to cell...
Bacterial persister cells are temporarily tolerant to bactericidal antibiotics but are not necessarily dormant and may exhibit physiological activities leading to cell damage. Based on the link between fluoroquinolone-mediated SOS responses and persister cell recovery, we screened chemicals that target fluoroquinolone persisters. Metabolic inhibitors (e.g., phenothiazines) combined with ofloxacin (OFX) perturbed persister levels in metabolically active cell populations. When metabolically stimulated, intrinsically tolerant stationary phase cells also became OFX-sensitive in the presence of phenothiazines. The effects of phenothiazines on cell metabolism and physiology are highly pleiotropic: at sublethal concentrations, phenothiazines reduce cellular metabolic, transcriptional, and translational activities; impair cell repair and recovery mechanisms; transiently perturb membrane integrity; and disrupt proton motive force by dissipating the proton concentration gradient across the cell membrane. Screening a subset of mutant strains lacking membrane-bound proteins revealed the pleiotropic effects of phenothiazines potentially rely on their ability to inhibit a wide range of critical metabolic proteins. Altogether, our study further highlights the complex roles of metabolism in persister cell formation, survival and recovery, and suggests metabolic inhibitors such as phenothiazines can be selectively detrimental to persister cells.
Topics: Anti-Bacterial Agents; Escherichia coli; Fluoroquinolones; Gram-Negative Bacteria; Phenothiazines
PubMed: 35264714
DOI: 10.1038/s42003-022-03172-8 -
PloS One 2021The rapid evolution of antibiotic resistance in Clostridioides difficile and the consequent effects on prevention and treatment of C. difficile infections (CDIs) are...
The rapid evolution of antibiotic resistance in Clostridioides difficile and the consequent effects on prevention and treatment of C. difficile infections (CDIs) are matters of concern for public health. Thioridazine, a compound belonging to the phenothiazine group, has previous shown antimicrobial activity against C. difficile. The purpose of this present study was to investigate the potential of a novel phenothiazine derivative, JBC 1847, as an oral antimicrobial for treatment of intestinal pathogens and CDIs. The minimal inhibition concentration and the minimum bactericidal concentration of JBC 1847 against C. difficile ATCC 43255 were determined 4 μg/mL and high tolerance after oral administration in mice was observed (up to 100 mg/kg bodyweight). Pharmacokinetic modeling was conducted in silico using GastroPlusTM, predicting low (< 10%) systemic uptake after oral exposure and corresponding low Cmax in plasma. Impact on the intestinal bacterial composition after four days of treatment was determined by 16s rRNA MiSeq sequencing and revealed only minor impact on the microbiota in non-clinically affected mice, and there was no difference between colony-forming unit (CFU)/gram fecal material between JBC 1847 and placebo treated mice. The cytotoxicity of the compound was assessed in Caco-2 cell-line assays, in which indication of toxicity was not observed in concentrations up to seven times the minimal bactericidal concentration. In conclusion, the novel phenothiazine derivative demonstrated high antimicrobial activity against C. difficile, had low predicted gastrointestinal absorption, low intestinal (in vitro) cytotoxicity, and only induced minor changes of the healthy microbiota, altogether supporting that JBC 1847 could represent a novel antimicrobial candidate. The clinical importance hereof calls for future experimental studies in CDI models.
Topics: Administration, Oral; Animals; Caco-2 Cells; Clostridioides difficile; Clostridium Infections; Feces; Gastrointestinal Microbiome; Humans; Mice; Phenothiazines; RNA, Ribosomal, 16S
PubMed: 34597343
DOI: 10.1371/journal.pone.0258207 -
ACS Applied Bio Materials Oct 2023A formate (HCOO) bioanode was developed by utilizing a phenothiazine-based electropolymerized layer deposited on sucrose-derived carbon. The electrode modified with...
A formate (HCOO) bioanode was developed by utilizing a phenothiazine-based electropolymerized layer deposited on sucrose-derived carbon. The electrode modified with NAD-dependent formate dehydrogenase and the electropolymerized layer synergistically catalyzed the oxidation of the coenzyme (NADH) and fuel (HCOO) to achieve efficient electron transfer. Further, the replacement of carbon nanotubes with water-dispersible sucrose-derived carbon used as the electrode base allowed the fabrication of a surfactant-free bioanode delivering a maximum current density of 1.96 mA cm in the fuel solution. Finally, a separator- and surfactant-free HCOO/O biofuel cell featuring the above bioanode and a gas-diffusion biocathode modified with bilirubin oxidase and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) was fabricated, delivering a maximum power density of 70 μW cm (at 0.24 V) and an open-circuit voltage of 0.59 V. Thus, this study demonstrates the potential of formic acid as a fuel and possibilities for the application of carbon materials in bioanodes.
Topics: Surface-Active Agents; Bioelectric Energy Sources; Nanotubes, Carbon; Formates; Phenothiazines; Sucrose
PubMed: 37750824
DOI: 10.1021/acsabm.3c00502 -
Lasers in Medical Science Jul 2022Low-level laser therapy (LLLT) and methylene blue (MB) were proved to have neuroprotective effects. In this study, we evaluated the preventive effects of LLLT and MB...
Low-level laser therapy (LLLT) and methylene blue (MB) were proved to have neuroprotective effects. In this study, we evaluated the preventive effects of LLLT and MB alone and in combination to examine their efficacy against sleep deprivation (SD)-induced cognitive impairment. Sixty Balb/c male mice were randomly divided into five groups as follows: wide platform (WP), SD, LLLT, MB, LMB (treatment with both LLLT and MB). Daily MB (0.5 mg/kg) was injected for ten consecutive days. An 810-nm, 10-Hz pulsed laser was used in LLLT every other day. We used the T-maze test, social interaction test (SIT), and shuttle box to assess learning and memory and PSD-95, GAP-43, and synaptophysin (SYN) markers to examine synaptic proteins levels in the hippocampus. Our results showed that SD decreased alternation rate in the T-maze test, sociability and social novelty in SIT, and memory index in the shuttle box. Single treatments were not able to reverse these in most of the behavioral parameters. However, behavioral tests showed a significant difference between combined therapy and the SD group. The levels of synaptic plasticity markers were also significantly reduced after SD. There was a significant difference between the MB group and SD animals in GAP-43 and SYN biomarkers. Combination treatment with LLLT and MB also increased GAP-43, PSD-95, and SYN compared to the SD group. We found that the combined use of LLLT and MB pretreatment is more effective in protecting SD-induced cognitive impairment, which may be imparted via modulation of synaptic proteins.
Topics: Animals; GAP-43 Protein; Hippocampus; Low-Level Light Therapy; Male; Methylene Blue; Mice; Mice, Inbred BALB C; Sleep
PubMed: 35059872
DOI: 10.1007/s10103-021-03497-6 -
Journal of Experimental & Clinical... Jan 2020Glioblastoma multiforme is a CNS cancer characterized by diffuse infiltrative growth, aggressive clinical behavior and very poor prognosis. The state-of-art clinical...
BACKGROUND
Glioblastoma multiforme is a CNS cancer characterized by diffuse infiltrative growth, aggressive clinical behavior and very poor prognosis. The state-of-art clinical approach to this disease consists of surgical resection followed by radiotherapy plus concurrent and adjuvant chemotherapy with temozolomide. Tumor recurrence occurs in virtually all cases, therefore, despite any treatment, the median survival is very low (14.6 months), which makes the approach to these patients a challenging clinical issue.
MAIN BODY
The escalating costs and times required for new medications to reach the bedside make repurposing or repositioning of old drugs, when scientific bases allow their use in other pathologies, an appealing strategy. Here, we analyze a number of literature data concerning the antipsychotic chlorpromazine, the founder of the phenothiazines class of drugs, a medication widely used in the clinics for approximately 60 years. The drug exerts its effects on psychiatric patients by interfering with the dopamine receptor D, although more recent pharmacodynamics studies ascribe chlorpromazine a series of biological effects on cancer cells, all converging in hindering also glioblastoma survival capabilities.
SHORT CONCLUSIONS
On these bases, and assisted by the information on the well-established chlorpromazine toxicity and dosage in humans, we designed a Phase II clinical trial involving the combination of chlorpromazine with the standard treatment, temozolomide, in the adjuvant phase of the therapeutic protocol. Patients displaying hypo-methylation of the MGMT gene, and thus intrinsically resistant to temozolomide, will be enrolled. The endpoints of this study are the analysis of toxicity and clinical activity, as evaluated in terms of Progression-Free Survival, of the association of chlorpromazine with the first-line treatment for this very serious form of cancer.
Topics: Brain Neoplasms; Chlorpromazine; Drug Repositioning; Female; Glioblastoma; Humans; Male
PubMed: 32005270
DOI: 10.1186/s13046-020-1534-z