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151.
Tim Helbing Caterina Carraro Alexander Francke Dr. Alice Sosic Michele De Franco Prof. Dr. Valentina Gandin Prof. Dr. Richard Göttlich Prof. Dr. Barbara Gatto 《ChemMedChem》2020,15(21):2040-2051
In this study, we describe the synthesis and biological evaluation of a set of bis-3-chloropiperidines (B−CePs) containing rigid aromatic linker structures. A modification of the synthetic strategy also enabled the synthesis of a pilot tris-3-chloropiperidine (Tri-CeP) bearing three reactive meta-chloropiperidine moieties on the aromatic scaffold. A structure–reactivity relationship analysis of B−CePs suggests that the arrangement of the reactive units affects the DNA alkylating activity, while also revealing correlations between the electron density of the aromatic system and the reactivity with biologically relevant nucleophiles, both on isolated DNA and in cancer cells. Interestingly, all aromatic 3-chloropiperidines exhibited a marked cytotoxicity and tropism for 2D and 3D cultures of pancreatic cancer cells. Therefore, the new aromatic 3-chloropiperidines appear to be promising contenders for further development of mustard-based anticancer agents aimed at pancreatic cancers. 相似文献
152.
Luiz Pereira Olivier Podda Barbara Fayard Annabelle Laplace Franck Pigeonneau 《Journal of the American Ceramic Society》2020,103(4):2453-2462
This work aims to study the mechanisms of oxygen bubble formation coming from redox reaction of a polyvalent element incorporated in a glass melt. Borosilicate glass composition is selected for its use as a glass matrix for nuclear waste conditioning. Cerium is selected as a polyvalent element as it may be found in nuclear waste. The chosen material is characterized in terms of physical properties which influence bubble formation and growth. A postmortem optical microscope approach is used to observe bubbles in the investigated material after thermal treatment for varying temperatures (900°C-1100°C) and durations. To support the understanding of oxygen bubble formation, cerium speciation by X-ray absorption near-edge structure (XANES) and bubble gas composition are experimentally evaluated. In this article, we indicate how bubbles are formed in the investigated glass melt system. It is also demonstrated that the mechanisms that govern bubble evolution are fundamentally the same and that the plot's optimum points are strongly influenced by the temperature. These last statements are confirmed by considering some bubble features, such as bubble mean density and bubble mean diameter evolutions, and normalizing the experimental time using a characteristic residence time (tη) obtaining thereafter a dimensionless time, which is a function of the glass melt properties obtained by the physical characterizations. The impact of temperature and time on bubble formation is described. 相似文献
153.
Alessandra Dellaquila Gabriele Greco Elisabetta Campodoni Mauro Mazzocchi Barbara Mazzolai Anna Tampieri Nicola M. Pugno Monica Sandri 《应用聚合物科学杂志》2020,137(22):48739
Silks have been widely used as biomaterials due to their biocompatibility, biodegradability, and excellent mechanical properties. In the present work, native spider silk was used as organic template for controlled nucleation of hydroxyapatite (HA) nano-coating that can act as biomimetic interface. Different bio-inspired neutralization methods and process parameters were evaluated to optimize the silk functionalization. The morphology and chemical composition were investigated by scanning electron microscopy, energy-dispersive X-ray spectroscopy, Fourier transform infrared spectroscopy, and X-ray diffraction analysis and mechanical properties were studied through tensile tests. Results showed that the optimized protocol enabled a controlled and homogeneous nucleation of apatite nano-crystals while maintaining silk mechanical performances after mineralization. This study reports the optimization of a simple and effective bio-inspired nucleation process for precise nucleation of HA onto spider silk templates, suitable to develop high-performance hybrid interfaces for bone tissue engineering. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48739. 相似文献
154.
Cora Chmielowska Dorota Korsak Barbara Szmulkowska Alicja Krop Kinga Lipka Martyna Krupiska Dariusz Bartosik 《International journal of molecular sciences》2020,21(22)
Listeria monocytogenes is a pathogen responsible for severe cases of food poisoning. Listeria spp. strains occurring in soil and water environments may serve as a reservoir of resistance determinants for pathogenic L. monocytogenes strains. A large collection of Listeria spp. strains (155) isolated from natural, agricultural, and urban areas was screened for resistance to heavy metals and metalloids, and the presence of resistance determinants and extrachromosomal replicons. Of the tested strains, 35% were resistant to cadmium and 17% to arsenic. Sequence analysis of resistance plasmids isolated from strains of Listeria seeligeri and Listeria ivanovii, and the chromosome of L. seeligeri strain Sr73, identified a novel variant of the cadAC cadmium resistance efflux system, cadA6, that was functional in L. monocytogenes cells. The cadA6 cassette was detected in four Listeria species, including strains of L. monocytogenes, isolated from various countries and sources—environmental, food-associated, and clinical samples. This resistance cassette is harbored by four novel composite or non-composite transposons, which increases its potential for horizontal transmission. Since some cadAC cassettes may influence virulence and biofilm formation, it is important to monitor their presence in Listeria spp. strains inhabiting different environments. 相似文献
155.
Elzbieta Pawluczuk Marta ukaszewicz-Zajc Barbara Mroczko 《International journal of molecular sciences》2020,21(22)
Gastric cancer (GC) is the fifth most common cancer worldwide and the second leading cause of cancer-related death. GC is usually diagnosed at an advanced stage due to late presentation of symptoms. Therefore, there is a need for establishing more sensitive and specific markers useful in early detection of the disease when a cancer is asymptomatic to improve the diagnostic and clinical decision-making process. Some researchers suggest that chemokines and their specific receptors play an important role in GC initiation and progression via promotion of angiogenesis, tumor transformation, invasion, survival and metastasis as well as protection from host response and inter-cell communication. Chemokines are small proteins produced by various cells such as endothelial cells, fibroblasts, leukocytes, and epithelial and tumor cells. According to our knowledge, the significance of chemokines and their specific receptors in diagnosing GC and evaluating its progression has not been fully elucidated. The present article offers a review of current knowledge on general characteristics of chemokines, specific receptors and their role in GC pathogenesis as well as their potential usefulness as novel biomarkers for GC. 相似文献
156.
157.
Irene Vanni Simona Coco Anna Truini Marta Rusmini Maria Giovanna Dal Bello Angela Alama Barbara Banelli Marco Mora Erika Rijavec Giulia Barletta Carlo Genova Federica Biello Claudia Maggioni Francesco Grossi 《International journal of molecular sciences》2015,16(12):28765-28782
Next-generation sequencing (NGS) is a cost-effective technology capable of screening several genes simultaneously; however, its application in a clinical context requires an established workflow to acquire reliable sequencing results. Here, we report an optimized NGS workflow analyzing 22 lung cancer-related genes to sequence critical samples such as DNA from formalin-fixed paraffin-embedded (FFPE) blocks and circulating free DNA (cfDNA). Snap frozen and matched FFPE gDNA from 12 non-small cell lung cancer (NSCLC) patients, whose gDNA fragmentation status was previously evaluated using a multiplex PCR-based quality control, were successfully sequenced with Ion Torrent PGM™. The robust bioinformatic pipeline allowed us to correctly call both Single Nucleotide Variants (SNVs) and indels with a detection limit of 5%, achieving 100% specificity and 96% sensitivity. This workflow was also validated in 13 FFPE NSCLC biopsies. Furthermore, a specific protocol for low input gDNA capable of producing good sequencing data with high coverage, high uniformity, and a low error rate was also optimized. In conclusion, we demonstrate the feasibility of obtaining gDNA from FFPE samples suitable for NGS by performing appropriate quality controls. The optimized workflow, capable of screening low input gDNA, highlights NGS as a potential tool in the detection, disease monitoring, and treatment of NSCLC. 相似文献
158.
Influence of the Multivalency of Ultrashort Arg‐Trp‐Based Antimicrobial Peptides (AMP) on Their Antibacterial Activity 下载免费PDF全文
Barbara C. Hoffknecht Dennis J. Worm Sandra Bobersky Pascal Prochnow Prof. Dr. Julia E. Bandow Prof. Dr. Nils Metzler‐Nolte 《ChemMedChem》2015,10(9):1564-1569
Peptide dendrimers are a class of molecules of high interest in the search for new antibiotics. We used microwave‐assisted, copper(I)‐catalyzed alkyne–azide cycloaddition (CuAAC; “click” chemistry) for the simple and versatile synthesis of a new class of multivalent antimicrobial peptides (AMPs) containing solely arginine and tryptophan residues. To investigate the influence of multivalency on antibacterial activity, short solid‐phase‐ synthesized azide‐modified Arg‐Trp‐containing peptides were “clicked” to three different alkyne‐modified benzene scaffolds to access scaffolds with one, two, or three peptides. The antibacterial activity of 15 new AMPs was investigated by minimal inhibitory concentration (MIC) assays on five different bacterial strains, including a multidrug‐resistant Staphylococcus aureus (MRSA) strain. With ultrashort (2–3 residues) peptides, a clear synergistic effect of the trivalent display was observed, whereas this effect was not apparent with longer peptides. The best candidates showed activities in the low‐micromolar range against Gram‐positive MRSA. Surprisingly, the best activity against Gram‐negative Acinetobacter baumannii was observed with an ultrashort dipeptide on the trivalent scaffold (MIC: 7.5 μM ). The hemolytic activity was explored for the three most active peptides. At concentrations ten times the MIC values, <1 % hemolysis of red blood cells was observed. 相似文献
159.
Porosity effect on microstructure,mechanical, and fluid dynamic properties of Ti2AlC by direct foaming and gel‐casting 下载免费PDF全文
Marek Potoczek Anna Chmielarz Murilo D. de M. Innocentini Izabela C. P. da Silva Paolo Colombo Barbara Winiarska 《Journal of the American Ceramic Society》2018,101(12):5346-5357
In this study, Ti2AlC foams were fabricated by direct foaming and gel‐casting using agarose as gelling agent. Slurry viscosity, determined by the agarose content (at a fixed solids loading), as well as surfactant concentration and foaming time were the key parameters employed for controlling the foaming yield, and hence the foam porosity after sintering process. Fabricated foams having total porosity in the 62.5‐84.4 vol% range were systematically characterized to determine their pore size and morphology. The effect of the foam porosity on the room‐temperature compression strength and elastic modulus was also determined. Depending on the amount of porosity, the compression strength and Young's modulus were found to be in the range of 9‐91 MPa and 7‐52 GPa, respectively. Permeability to air flow at temperatures up to 700°C was investigated. Darcian (k1) and non‐Darcian (k2) permeability coefficients displayed values in the range 0.30‐93.44 × 10?11 m2 and 0.39‐345.54 × 10?7 m, respectively. The amount of porosity is therefore a very useful microstructural parameter for tuning the mechanical and fluid dynamic properties of Ti2AlC foams. 相似文献
160.
Penny M. Kris-Etherton Michael Lefevre Ronald P. Mensink Barbara Petersen Jennifer Fleming Brent D. Flickinger 《Lipids》2012,47(10):931-940
Because of efforts to decrease trans fatty acids (TFA) in the food supply, intake should be assessed in the population to establish a baseline TFA intake. The 1999?C2002 National Health and Nutrition Examination Survey (NHANES) was used to identify a benchmark for TFA intake. TFA was estimated by mean, median, and quintile of intake, TFA intake data were weighted using the NHANES 4-year sample weights. The main outcome measures included TFA intake in grams per day and percentage of energy in the top 25 food sources of TFA. Data are reported for 16,669 individuals ??3 years of age. Median TFA intake was 2.3?% of calories (5?g/day) with 0.9?C4.5?% of energy (1.5?C13.1?g/day) over different quintiles of intake. Mean TFA intake was 2.5?% of energy (6.1?g/day). The range of TFA intake in the fifth quintile was very large, i.e., 3.5?C12.5?% of energy or 8.8?C92.4?g/day. Increasing quintiles of TFA intake were associated with increases in total fat (26.7?C37.6?% of energy), saturated fat (7.6?C10.5?% of energy), and calories (for those >20?years of age: 2,416?C2,583 for men and 1,679?C1,886 for women). Major food sources of dietary TFA were cakes, cookies, pies, and pastries. Based on current dietary guidance to consume as little industrial TFA as possible, much progress is needed to attain this goal, including food industry efforts to remove TFA from the food supply and educating the public about making healthy food choices. 相似文献