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1.
Dr. Daniela Carbone Dr. Barbara Parrino Dr. Stella Cascioferro Camilla Pecoraro Prof. Elisa Giovannetti Dr. Veronica Di Sarno Dr. Simona Musella Dr. Giulia Auriemma Prof. Girolamo Cirrincione Prof. Patrizia Diana 《ChemMedChem》2021,16(3):537-554
A new series of topsentin analogs, in which the central imidazole ring of the natural lead was replaced by a 1,2,4-oxadiazole moiety, was efficiently synthesized. All derivatives were pre-screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. The five most potent compounds were further investigated in various pancreatic ductal adenocarcinoma (PDAC) cell lines, including SUIT-2, Capan-1, and Panc-1 cells, eliciting EC50 values in the micromolar and sub-micromolar range, associated with significant reduction of cell migration. These remarkable results might be explained by the effects of these new topsentin analogues on epithelial-to-mesenchymal transition markers, including SNAIL-1/2 and metalloproteinase-9. Moreover, flow cytometric analysis after Annexin V-FITC and propidium iodide staining demonstrated that these derivatives enhanced apoptosis of PDAC cells. Keeping with these data, the PathScan intracellular signaling and ELISA array revealed cleavage of caspase-3 and PARP and a significant inhibition of GSK3β phosphorylation, suggesting this kinase as a potential downstream target of our novel compounds. This was further supported by a specific assay for the evaluation of GSK3β activity, showing IC50 values for the most active compounds against this enzyme in the micromolar range. 相似文献
2.
Policicchio Alfonso Putz Ana-Maria Conte Giuseppe Stelitano Sara Bonaventura Carlo Poselle Ianăşi Cătălin Almásy László Wacha András Horváth Zsolt Endre Agostino Raffaele G. 《Journal of Porous Materials》2021,28(4):1049-1058
Journal of Porous Materials - The present study reports a systematic analysis of morphology and hydrogen sorption capacity of mesoporous organic-inorganic silica prepared by varying the silica... 相似文献
3.
Alessandra Danza Amalia Conte Annamaria Cedola Inna Chisacova Matteo Alessandro Del Nobile 《International Journal of Food Science & Technology》2015,50(12):2688-2693
The best packaging conditions for rocket salad were assessed by subsequent experimental trials. In the first step, a preliminary screening of different packaging materials was performed and two micro‐perforated oriented polypropylene films with different micro‐hole diameters (90 and 110 μm) were selected as best packaging solutions. In the subsequent experimental step, modified headspace conditions were applied without any improvement on product quality. In the last step, the effects of an ethylene adsorbent were analysed. Rocket salad packaged in both films with the ethylene adsorbent recorded a shelf life of about 16 days, compared to the control samples that remained acceptable for 13 days. During storage, the microbial quality (mesophilic and psychrotrophic bacteria, pseudomonadaceae, lactic acid bacteria, yeasts, total coliforms and enterobacteriacae), the pH, the colour changes and the main sensory parameters were also monitored. 相似文献
4.
Mine Water and the Environment - Artisanal and small-scale mining (ASM) of gold has adversely affected the environment and human health for decades, mostly due to excessive use of mercury. With the... 相似文献
5.
C. S. Manso S. Thom E. Uhlmann C. L. F. de Assis E. G. del Conte 《The International Journal of Advanced Manufacturing Technology》2020,107(3):1179-1189
Micromilling allows for the high precision machining of different types of materials and thus promotes the manufacturing of micro-components for various te 相似文献
6.
Roberta D’Ambrosio Alessio Aghemo Raffaele De Francesco Maria Grazia Rumi Enrico Galmozzi Stella De Nicola Cristina Cheroni Paul J. Clark Guido Ronchi Pietro Lampertico Massimo Colombo 《International journal of molecular sciences》2014,15(5):7213-7224
The interleukin 28B (IL28B) rs12979860 polymorphism is associated with treatment outcome in hepatitis C virus (HCV) genotype 1 and 4 patients. Its association with the histological features of chronic hepatitis C and disease severity needs further clarifications. To assess the correlation between IL28B genotype, HCV genotype and liver biopsy findings in untreated patients.
Materials and Methods
Pre-treatment liver biopsies from 335 HCV Caucasian patients (59% males, age 50 years) enrolled in the MIST study were staged for fibrosis and inflammation according to the METAVIR and the Ishak scoring systems; steatosis was dichotomized as <5% or ≥5%. IL28B was typed by Taqman Single Nucleotide Polymorphism (SNP) genotyping assay. HCV genotype was 1 in 151 (45%), 2 in 99 (30%), 3 in 50 (15%) and 4 in 35 (10%) patients. IL28B genotype was CC in 117 (34%), CT in 166 (49%) and TT in 52 (15%). At univariate analysis, the IL28B CC genotype was associated with severe portal inflammation in HCV-1 patients (CC vs. CT/TT: 86% vs. 63%, p = 0.005), severe lobular inflammation in HCV-2 patients (CC vs. CT/TT: 44% vs. 23%, p = 0.03), and less fatty infiltration in HCV-1 patients (CC vs. CT/TT: 72% vs. 51%, p = 0.02). Despite the lack of any association between IL28B and fibrosis stage, in HCV-3 patients IL28B CC correlated with METAVIR F3–F4 (CC vs. CT/TT: 74% vs. 26%, p = 0.05). At multivariate analysis, the genotype CC remained associated with severe portal inflammation in HCV-1, only (Odds Ratio (OR): 95% Confidence Interval (CI): 3.24 (1.23–8.51)). IL28B genotype is associated with the histological features of chronic hepatitis C in a HCV genotype dependent manner, with CC genotype being independently associated with severe portal inflammation. 相似文献7.
8.
Simple sample preparation procedures involving sonication and solid phase extraction (SPE), followed by reversed-phase high performance liquid chromatography (HPLC) and spectrofluorometric detection, were used to analyse polycyclic aromatic hydrocarbons (PAHs) in soil and olives collected in areas contaminated with creosote-treated railway ties. Very high PAH contents (with amounts ranging from 114.7 to 2157.2 and from 167.3 to 3121.8 microg kg(-1) dry weight for total light PAHs and total heavy PAHs, respectively) were found in soil sampled up to 1 m from the source of contamination. The PAH load decreased rapidly with the distance from the railway ties. High amounts of light PAHs, up to 6359.9 microg kg(-1), were also found in oil extracted from olives collected in a rural area where old railway ties were stored. No appreciable transfer of heavy PAHs and benzo[a]pyrene was observed in oil samples. 相似文献
9.
The biodegradation of urea in river waters has been evaluated under laboratory conditions. Urea will degrade to ammonia at a rate depending on the bacterial state of the river water and on the water temperature. Under normal conditions no breakdown may be expected to occur at temperatures below 8°C for 14 days contact. In river waters with a high suspended solids content, simulating extreme winter river conditions, a maximum breakdown of 3–6 per cent daily of the original urea levels was found for temperatures not exceeding 8°C during the first 7 days contact. 相似文献
10.
León-Mejía G Espitia-Pérez L Hoyos-Giraldo LS Da Silva J Hartmann A Henriques JA Quintana M 《The Science of the total environment》2011,409(4):686-691
Coal mining is one of the most important causes of environmental pollution, as large quantities of coal dust particles are emitted. Colombia-South America has large natural coal reserves and “El Cerrejón” is the world's largest open-cast mine located in the northern department of Guajira. The aim of the present study was to evaluate genotoxic effects in a population exposed to coal residues from the open-cast mine “El Cerrejón”. 100 exposed workers and 100 non-exposed control individuals were included in this study. The exposed group was divided according to different mining area activities: (i). Transport of extracted coal, (ii). Equipment field maintenance, (iii). Coal stripping and, (iv). Coal embarking. Blood samples were taken to investigate biomarkers of genotoxicity, specifically, primary DNA damage as damage index (DI), tail length and% of tail DNA using the Comet assay (alkaline version) and chromosome damage as micronucleus (MN) frequency in lymphocytes. Both biomarkers showed statistically significantly higher values in the exposed group compared to the non-exposed control group. No difference was observed between the exposed groups executing different mining activities. These results indicate that exposure to coal mining residues may result in an increased genotoxic exposure in coal mining workers. We did not find a correlation between age, alcohol consumption and service time with the biomarkers of genotoxicity. Our results are the first data of genotoxic effects induced by coal mining exposure in Colombia, and thus, contribute to the exploration of test batteries use for monitoring of exposed populations and may stimulate designing control, hygiene and prevention strategies for occupational health risk assessment in developing countries. 相似文献