82 research outputs found

    SYNTHESIS AND EVALUATION OF ETHYL (4-(N-(THIAZOL-2-YL) SULFAMOYL) PHENYL)CARBAMATE (TSPC) AS A CORROSION INHIBITOR FOR MILD STEEL IN 0.1M HCL

    Get PDF
    Laboratory synthesized ethyl (4-(N-(thiazol-2-yl)sulfamoyl)phenyl)carbamate (TSPC), characterized by 1H NMR spectroscopy, was evaluated as corrosion inhibitor of mild steel in 0.1M HCl using electrochemical techniques. Open circuit potential, potentiodynamic polarization and impedance spectroscopy were used to evaluate the inhibition efficiency of (TSPC) at various concentrations. The obtained electrochemical data indicated that (TSPC) acts as moderate corrosion inhibitor for mild steel in acidic media. It is found that the inhibition efficiency increases with the concentration of the inhibitor till 400ppm. The adsorption isotherm involving physisorption of (TSPC) at room temperature and the experimental data complied to the Langmuir adsorption isotherms and the negative values of the Gibb’s free energy of adsorption obtained suggested that inhibitor molecules have been spontaneously adsorbed onto the mild steel surface

    Synthesis and Evaluation of Antibacterial and Antifungal Activities of 1,3-Disubstituted-4-thioxoimidazolidin-2-one Derivatives

    Get PDF
    1,3-Disubstituted-4-thioxoimidazolidin-2-one derivatives with various substituents at N1 and N3 were synthesized with high yields and excellent purity by the reaction of various N-arylcyanothioformamide derivatives with isocyanate derivatives. The activity of these products as antibacterial and antifungal agents was studied to through some light on structural activity relationship. Some of synthesized compounds showed significant antibacterial and antifungal activities. Most of the imidazole derivatives possess significant antifungal activity aginst S. cerevisiae (MIC 1–10 µg mL–1). As comparision with ketoconazole, most of the imidazole derivatives showed activity ranging from 50 % less activity to fourfold activity. This work is licensed under a Creative Commons Attribution 4.0 International License

    CHEMICAL PROFILE OF TWO JASMINUM SAMBAC L. (AIT) CULTIVARS CULTIVATED IN EGYPT–THEIR MEDIATED SILVER NANOPARTICLES SYNTHESIS AND SELECTIVE CYTOTOXICITY

    Get PDF
    Objective: Evaluation of two Jasminum sambac L. (Ait) cultivars; Arabian Nights (JSA) and Grand Duke of Tuscany (JSG) ethanolic leaves extracts as reducing agents for the green synthesis of silver nanoparticles (AgNPs) and evaluation of their cytotoxicity against MCF-7 breast cancer and 5637 bladder cancer cell lines and chemical profiling of the two cultivars. Methods: The synthesis of silver nanoparticles (AgNPs) by the two cultivars and characterization of AgNPs by ultraviolet (UV)–visible spectroscopy, Transmission electron microscopy (TEM) and Fourier Transform Infrared Spectroscopy (FTIR). Additionally, the use of The high-performance liquid chromatography coupled with photodiode array-mass-mass-spectroscopy (HPLC-PDA-MS/MS) for chemical profiling of both cultivars and evaluation of total leaves extracts and corresponding nanoparticles towards MCF-7 and 5637 cell lines compared to aneuploidy immortal keratinocyte (Ha Cat) normal cells by neutral cell assay. Results: The green synthesized AgNPs (of an average size range of 8.83 and 11.24 nm for JSA and JSG, respectively) exhibited cytotoxicity against MCF-7 and 5637 cell lines. The IC50 was determined for each total extract JSA (15.29±2.16 μg/ml) and JSG (20.28±1.20 μg/ml) and corresponding AgNPs 17.32±2.22 μg/ml and 6.32±1.01μg/ml for JSA and JSG, respectively. The IC50 of JSA and JSG against 5637 bladder cancer cell line were 13.76±1.11 μg/ml and 50.69±3.75 μg/ml, while the corresponding AgNPs showed IC50 of 5.54±0.88 μg/ml and 27.89±2.84 μg/ml, respectively. The HPLC-PDA-MS/MS allowed the identification of 59 compounds; 10 simple phenols, 17 flavonoids; quercetin and kaempferol glycosides, 2 lignans, and 30 secoiridoids; oleuropein, molihauside, and sambacoside. Conclusion: This study proved that JSA is an excellent source for the synthesis of AgNPs with optimum characters and enhanced activities toward MCF-7 and 5637 cell lines in correlation to identified compounds

    Applying an internal transcribed spacer as a single molecular marker to differentiate between Tetraselmis and Chlorella species

    Get PDF
    In the realm of applied phycology, algal physiology, and biochemistry publications, the absence of proper identification and documentation of microalgae is a common concern. This poses a significant challenge for non-specialists who struggle to identify numerous eukaryotic microalgae. However, a promising solution lies in employing an appropriate DNA barcoding technique and establishing comprehensive databases of reference sequences. To address this issue, we conducted a study focusing on the molecular characterization and strain identification of Tetraselmis and Chlorella species, utilizing the internal transcribed spacer (ITS) barcode approach. By analyzing the full nuclear ITS region through the Sanger sequencing approach, we obtained ITS barcodes that were subsequently compared with other ITS sequences of various Tetraselmis and Chlorella species. To ensure the reliability of our identification procedure, we conducted a meticulous comparison of the DNA alignment, constructed a phylogenetic tree, and determined the percentage of identical nucleotides. The findings of our study reveal the significant value of the ITS genomic region as a tool for distinguishing and identifying morphologically similar chlorophyta. Moreover, our results demonstrate that both the ITS1 and ITS2 regions are capable of effectively discriminating isolates from one another; however, ITS2 is preferred due to its greater intraspecific variation. These results underscore the indispensability of employing ITS barcoding in microalgae identification, highlighting the limitations of relying solely on morphological characterization

    Neuroprotective effect of ranolazine improves behavioral discrepancies in a rat model of scopolamine-induced dementia

    Get PDF
    BackgroundRanolazine (Rn), an antianginal agent, acts in the central nervous system and has been used as a potential treatment agent for pain and epileptic disorders. Alzheimer’s disease (AD) is one of the most prevalent neurodegenerative diseases and the leading factor in dementia in the elderly.AimWe examined the impact of Rn on scopolamine (Sco)-induced dementia in rats.MethodsThirty-two albino male rats were divided into four groups: control, Rn, Sco, and Rn + Sco.ResultsA significant decrease in the escape latency in the Morris water maze test after pre-treatment with Rn explained better learning and memory in rats. Additionally, Rn significantly upregulated the activities of the antioxidant enzymes in the treated group compared to the Sco group but substantially reduced acetylcholinesterase activity levels in the hippocampus. Moreover, Rn dramatically reduced interleukin-1 β (IL-1β) and IL-6 and upregulated the gene expression of brain-derived neurotrophic factor (BDNF). Furthermore, in the Sco group, the hippocampal tissue’s immunohistochemical reaction of Tau and glial factor activating protein (GFAP) was significantly increased in addition to the upregulation of the Caspase-3 gene expression, which was markedly improved by pre-treatment with Rn. The majority of pyramidal neurons had large vesicular nuclei with prominent nucleoli and appeared to be more or less normal, reflecting the all-beneficial effects of Rn when the hippocampal tissue was examined under a microscope.ConclusionOur findings indicated that Rn, through its antioxidative, anti-inflammatory, and anti-apoptotic effects, as well as the control of the expression of GFAP, BDNF, and Tau proteins, has a novel neuroprotective impact against scopolamine-induced dementia in rats

    PepFect 14, a novel cell-penetrating peptide for oligonucleotide delivery in solution and as solid formulation

    Get PDF
    Numerous human genetic diseases are caused by mutations that give rise to aberrant alternative splicing. Recently, several of these debilitating disorders have been shown to be amenable for splice-correcting oligonucleotides (SCOs) that modify splicing patterns and restore the phenotype in experimental models. However, translational approaches are required to transform SCOs into usable drug products. In this study, we present a new cell-penetrating peptide, PepFect14 (PF14), which efficiently delivers SCOs to different cell models including HeLa pLuc705 and mdx mouse myotubes; a cell culture model of Duchenne’s muscular dystrophy (DMD). Non-covalent PF14-SCO nanocomplexes induce splice-correction at rates higher than the commercially available lipid-based vector Lipofectamine™ 2000 (LF2000) and remain active in the presence of serum. Furthermore, we demonstrate the feasibility of incorporating this delivery system into solid formulations that could be suitable for several therapeutic applications. Solid dispersion technique is utilized and the formed solid formulations are as active as the freshly prepared nanocomplexes in solution even when stored at an elevated temperatures for several weeks. In contrast, LF2000 drastically loses activity after being subjected to same procedure. This shows that using PF14 is a very promising translational approach for the delivery of SCOs in different pharmaceutical forms

    Optimizing anti-gene oligonucleotide ‘Zorro-LNA’ for improved strand invasion into duplex DNA

    Get PDF
    Zorro-LNA (Zorro) is a newly developed, oligonucleotide (ON)-based, Z-shaped construct with the potential of specific binding to each strand of duplex DNA. The first-generation Zorros are formed by two hybridized LNA/DNA mixmers (2-ON Zorros) and was hypothesized to strand invade. We have now established a method, which conclusively demonstrates that an LNA ON can strand invade into duplex DNA. To make Zorros smaller in size and easier to design, we synthesized 3′–5′–5′–3′ single-stranded Zorro-LNA (ssZorro) by using both 3′- and 5′-phosphoramidites. With ssZorro, a significantly greater extent and rate of double-strand invasion (DSI) was obtained than with conventional 2-ON Zorros. Introducing hydrophilic PEG-linkers connecting the two strands did not significantly change the rate or extent of DSI as compared to ssZorro with a nucleotide-based linker, while the longest alkyl-chain linker tested (36 carbons) resulted in a very slow DSI. The shortest alkyl-chain linker (3 carbons) did not reduce the extent of DSI of ssZorro, but significantly decreased the DSI rate. Collectively, ssZorro is smaller in size, easier to design and more efficient than conventional 2-ON Zorro in inducing DSI. Analysis of the chemical composition of the linker suggests that it could be of importance for future therapeutic considerations

    Antimicrobial resistance among migrants in Europe: a systematic review and meta-analysis

    Get PDF
    BACKGROUND: Rates of antimicrobial resistance (AMR) are rising globally and there is concern that increased migration is contributing to the burden of antibiotic resistance in Europe. However, the effect of migration on the burden of AMR in Europe has not yet been comprehensively examined. Therefore, we did a systematic review and meta-analysis to identify and synthesise data for AMR carriage or infection in migrants to Europe to examine differences in patterns of AMR across migrant groups and in different settings. METHODS: For this systematic review and meta-analysis, we searched MEDLINE, Embase, PubMed, and Scopus with no language restrictions from Jan 1, 2000, to Jan 18, 2017, for primary data from observational studies reporting antibacterial resistance in common bacterial pathogens among migrants to 21 European Union-15 and European Economic Area countries. To be eligible for inclusion, studies had to report data on carriage or infection with laboratory-confirmed antibiotic-resistant organisms in migrant populations. We extracted data from eligible studies and assessed quality using piloted, standardised forms. We did not examine drug resistance in tuberculosis and excluded articles solely reporting on this parameter. We also excluded articles in which migrant status was determined by ethnicity, country of birth of participants' parents, or was not defined, and articles in which data were not disaggregated by migrant status. Outcomes were carriage of or infection with antibiotic-resistant organisms. We used random-effects models to calculate the pooled prevalence of each outcome. The study protocol is registered with PROSPERO, number CRD42016043681. FINDINGS: We identified 2274 articles, of which 23 observational studies reporting on antibiotic resistance in 2319 migrants were included. The pooled prevalence of any AMR carriage or AMR infection in migrants was 25·4% (95% CI 19·1-31·8; I2 =98%), including meticillin-resistant Staphylococcus aureus (7·8%, 4·8-10·7; I2 =92%) and antibiotic-resistant Gram-negative bacteria (27·2%, 17·6-36·8; I2 =94%). The pooled prevalence of any AMR carriage or infection was higher in refugees and asylum seekers (33·0%, 18·3-47·6; I2 =98%) than in other migrant groups (6·6%, 1·8-11·3; I2 =92%). The pooled prevalence of antibiotic-resistant organisms was slightly higher in high-migrant community settings (33·1%, 11·1-55·1; I2 =96%) than in migrants in hospitals (24·3%, 16·1-32·6; I2 =98%). We did not find evidence of high rates of transmission of AMR from migrant to host populations. INTERPRETATION: Migrants are exposed to conditions favouring the emergence of drug resistance during transit and in host countries in Europe. Increased antibiotic resistance among refugees and asylum seekers and in high-migrant community settings (such as refugee camps and detention facilities) highlights the need for improved living conditions, access to health care, and initiatives to facilitate detection of and appropriate high-quality treatment for antibiotic-resistant infections during transit and in host countries. Protocols for the prevention and control of infection and for antibiotic surveillance need to be integrated in all aspects of health care, which should be accessible for all migrant groups, and should target determinants of AMR before, during, and after migration. FUNDING: UK National Institute for Health Research Imperial Biomedical Research Centre, Imperial College Healthcare Charity, the Wellcome Trust, and UK National Institute for Health Research Health Protection Research Unit in Healthcare-associated Infections and Antimictobial Resistance at Imperial College London

    Design of a peptide-based vector, PepFect6, for efficient delivery of siRNA in cell culture and systemically in vivo

    Get PDF
    While small interfering RNAs (siRNAs) have been rapidly appreciated to silence genes, efficient and non-toxic vectors for primary cells and for systemic in vivo delivery are lacking. Several siRNA-delivery vehicles, including cell-penetrating peptides (CPPs), have been developed but their utility is often restricted by entrapment following endocytosis. Hence, developing CPPs that promote endosomal escape is a prerequisite for successful siRNA implementation. We here present a novel CPP, PepFect 6 (PF6), comprising the previously reported stearyl-TP10 peptide, having pH titratable trifluoromethylquinoline moieties covalently incorporated to facilitate endosomal release. Stable PF6/siRNA nanoparticles enter entire cell populations and rapidly promote endosomal escape, resulting in robust RNAi responses in various cell types (including primary cells), with minimal associated transcriptomic or proteomic changes. Furthermore, PF6-mediated delivery is independent of cell confluence and, in most cases, not significantly hampered by serum proteins. Finally, these nanoparticles promote strong RNAi responses in different organs following systemic delivery in mice without any associated toxicity. Strikingly, similar knockdown in liver is achieved by PF6/siRNA nanoparticles and siRNA injected by hydrodynamic infusion, a golden standard technique for liver transfection. These results imply that the peptide, in addition to having utility for RNAi screens in vitro, displays therapeutic potential
    corecore