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https://www.readbyqxmd.com/read/28434186/new-thiourea-and-1-3-thiazolidin-4-one-derivatives-effective-on-the-hiv-1-virus
#1
Anna Bielenica, Giuseppina Sanna, Silvia Madeddu, Marta Struga, Michał Jóźwiak, Anna E Kozioł, Aleksandra Sawczenko, Ilona B Materek, Alessandra Serra, Gabriele Giliberti
Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. As part of our continuing effort to develop new active compounds, we report the synthesis and the evaluation of new fifteen thiourea derivatives with 1,3-benzothiazol-2-yl moiety, among them a group of biologically active (1-7) also underwent cyclisation to 1,3-thiazolidin-4-ones. Molecular structure of four compounds (4, 13, 15 and 3a) was determined by an X-ray crystallography. We here report the evaluation of their cytotoxicity against human leukaemia/lymphoma- and solid tumour-derived cell lines and of their antiviral activity against HIV-1 and representatives of ssRNA and dsDNA viruses...
April 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28433955/5-6-7-8-tetrahydro-2-2-phenylethyl-chromones-from-artificial-agarwood-of-aquilaria-sinensis-and-their-inhibitory-activity-against-acetylcholinesterase
#2
Ge Liao, Wen-Li Mei, Fan-Dong Kong, Wei Li, Jing-Zhe Yuan, Hao-Fu Dai
Thirteen previously undescribed 5,6,7,8-tetrahydro-2-(2-phenylethyl)chromones named tetrahydrochromone A-M, together with nine known ones, were isolated from artificial agarwood (induced by holing) originating from Aquilaria sinensis (Lour.) Gilg. The structures of these compounds were unambiguously determined based on extensive NMR spectroscopic analyses, and the absolute configuration was resolved by CD analyses, X-ray crystallographic, chemical and Mosher's method. Tetrahydrochromone A, B, K-M, and Oxidoagarochromone An exhibited inhibitory activity against AChE with the percentage inhibition range from 17...
April 20, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28433873/ph-dependent-synthesis-of-two-isomeric-dinuclear-cerium-ii-complexes-structures-dna-interactions-cytotoxic-activity-and-apoptotic-study
#3
En-Jun Gao, Jun-Qi Su, Hai-Tao Jin, Si-Jia Liu, Fu-Chen Zhao, Yang Meng, Xiao-Yu Ma, Jing Ge, Ya-Guang Sun, Wanzhong Zhang, Ming-Chang Zhu
Two isomeric dinuclear Cerium(II) complexes 1 and 2, formulated as Ce2(phen)2(NO3)2(L)4 [L=phenylacetic acid, phen=1,10-phenanthroline] was synthesized under solvothermal conditions at different pH values. The two complexes were characterized by elemental analysis, IR and single crystal X-ray diffraction. Complexes 1 and 2 were studied the binding with DNA and against cytotoxic activity. Fluorescence analysis indicated that the two complexes can bind to DNA. The changes with different gradient concentration of DNA added into the complexes in absorption spectra show a strongπ-stacking interaction between the complexes and DNA base pairs...
April 11, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28433872/biosynthesis-of-silver-nanoparticles-by-using-camellia-japonica-leaf-extract-for-the-electrocatalytic-reduction-of-nitrobenzene-and-photocatalytic-degradation-of-eosin-y
#4
R Karthik, Mani Govindasamy, Shen-Ming Chen, Yi-Hui Cheng, P Muthukrishnan, S Padmavathy, A Elangovan
In the present study, sphere-like silver nanoparticles (Ag-NPs) were synthesized by using Camellia japonica leaf extract and its remediation industrial pollutants such as nitrobenzene and Eosin-Y (EY). As-prepared sphere-like Ag-NPs were characterized by various analytical and spectroscopic methods such as UV-visible spectroscopy, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), High-resolution transmission electron microscopy (HR-TEM), Energy dispersive X-ray spectra (EDX), and the chemical constituents of the leaf extract were also analyzed by using Gas chromatography and Mass Spectroscopy (GC-MS)...
March 28, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28433858/reduced-graphene-oxide-chitosan-aptamer-interface-as-new-platform-for-ultrasensitive-detection-of-human-epidermal-growth-factor-receptor-2
#5
Arezoo Tabasi, Abdollah Noorbakhsh, Ensiyeh Sharifi
The present work describes an ultrasensitive electrochemical aptamer-based assay for detection of human epidermal growth factor receptor 2 protein (HER2) cancer biomarker as a model analyte. Results show that the reduced graphene oxide-chitosan (rGO-Chit) film as a suitable electrode material possesses great favorable properties including high homogeneity, good stability, large surface area and high fraction of amine groups as aptamer binding sites. Various steps of aptasensor fabrication were characterized using microscopic, energy-dispersive X-ray spectroscopy (EDAX), Fourier transform infrared (FTIR) spectroscopy and electrochemical techniques...
April 18, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28433734/prospective-association-of-fetal-liver-blood-flow-at-30-weeks-gestation-with-newborn-adiposity
#6
Satoru Ikenoue, Feizal Waffarn, Masanao Ohashi, Kaeko Sumiyoshi, Chigusa Ikenoue, Claudia Buss, Daniel L Gillen, Hyagriv N Simhan, Sonja Entringer, Pathik D Wadhwa
BACKGROUND: The production of variation in adipose tissue accretion represents a key fetal adaptation to energy substrate availability during gestation. Because umbilical venous blood transports nutrient substrate from the maternal to the fetal compartment, and the fetal liver is the primary organ where nutrient inter-conversion occurs, it has been proposed that variations in the relative distribution of umbilical venous blood flow shunting either through ductus venosus or perfusing the fetal liver represents a mechanism underlying this adaptation...
April 19, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28433709/pulmonary-pathobiology-induced-by-zinc-oxide-nanoparticles-in-mice-a-24-hour-and-28-day-follow-up-study
#7
Hsiao-Chi Chuang, Kai-Jen Chuang, Jen-Kun Chen, His-En Hua, Yen-Ling Shen, Wei-Neng Liao, Chii-Hong Lee, Chih-Hong Pan, Kuan-Yuan Chen, Kang-Yun Lee, Ta-Chih Hsiao, Tsun-Jen Cheng
Inhaled zinc oxide nanoparticles (ZnONPs) have high deposition rates in the alveolar region of the lungs; however, the adverse health effects of ZnONPs on the respiratory system are unclear. Herein, pathobiological responses of the respiratory system of mice that received intratracheal administration of ZnONPs were investigated by a combination of molecular and imaging (SPECT and CT) approaches. Also, normal BEAS-2B and adenocarcinoma A549 cells were used to confirm the results in mice. First, female BALB/c mice were administrated a series of doses of 20-nm ZnONPs and were compared to the phosphate-buffered saline control for 24-h and 28-day follow-up observations...
April 19, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28433539/rationally-designed-pi3k%C3%AE-mutants-to-mimic-atr-and-their-use-to-understand-binding-specificity-of-atr-inhibitors
#8
Yipin Lu, Mark Knapp, Kenneth Crawford, Robert Warne, Robert Elling, Kelly Yan, Michael Doyle, Gwynn Pardee, Li Zhang, Sylvia Ma, Mulugeta Mamo, Elizabeth Ornelas, Yue Pan, Dirksen Bussiere, Johanna Jansen, Isabel Zaror, Albert Lai, Paul Barsanti, Janet Sim
ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response and is an attractive anticancer drug target. Several potent and selective inhibitors of ATR have been reported showing significant antitumor efficacy, with most advanced ones entering clinical trials. However, due to the absence of an experimental ATR structure, the determinants contributing to ATR inhibitors' potency and specificity are not well understood. Here we present the mutations in the ATP-binding site of PI3Kα to progressively transform the pocket to mimic that of ATR...
April 19, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28433496/a-novel-storage-system-for-cryoem-samples
#9
Giovanna Scapin, Winifred Prosise, Michael K Wismer, Corey Strickland
We present here a new CryoEM grid boxes storage system designed to simplify sample labeling, tracking and retrieval. The system is based on the crystal pucks widely used by the x-ray crystallographic community for storage and shipping of crystals. This system is suitable for any cryoEM laboratory, but especially for large facilities that will need accurate tracking of large numbers of samples coming from different sources.
April 19, 2017: Journal of Structural Biology
https://www.readbyqxmd.com/read/28433450/a-retrospective-cohort-study-of-concomitant-ipsilateral-extra-capsular-and-intra-capsular-fractures-of-the-proximal-femur-are-they-casual-findings-or-an-undervalued-reality
#10
Miquel Videla-Cés, José-Miguel Sales-Pérez, Joan Girós-Torres, Rubén Sánchez-Navés, Sebastián Videla
BACKGROUND: Fractures of the proximal femur constitute a major public health problem, with an annual incidence in Spain of 7.6 cases per 1000 inhabitants over 65 years of age. Hip fractures are frequent in elderly patients, related to osteoporosis and with low energy trauma, which means that they can be considered a geriatric syndrome. Simultaneous ipsilateral extra- and intra-articular hip fractures are considered as very rare are, and generally speaking, classified as extra- or intra-capsular fractures...
April 13, 2017: Injury
https://www.readbyqxmd.com/read/28433178/preparation-and-characterization-of-biodegradable-nanocomposites-derived-from-carboxymethyl-cellulose-and-hydroxyapatite
#11
K Azzaoui, E Mejdoubi, A Lamhamdi, S Jodeh, O Hamed, M Berrabah, S Jerdioui, R Salghi, N Akartasse, A Errich, Á Ríos, M Zougagh
Development of a cost-effective technology for extraction and quantification of carcinogenic and toxic organic materials which are widely used in the industry are critical to humans. Membrane technology received much attention and has already been widely used in this area. In this work, we offer a newly developed bio-based nanocomposite membrane for removal of bisphenol-A (BPA) from water. Three natural components hydroxyapatite (HAp), carboxymethyl cellulose and lysine as a diluent were used for making the bio-based membrane...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28433164/characterization-and-application-of-cellulose-acetate-synthesized-from-sugarcane-bagasse
#12
R G Candido, G G Godoy, Adilson R Gonçalves
The synthesis and application of cellulose acetate (CA) from sugarcane bagasse were investigated. Firstly, cellulose was extracted by a sequential treatment with H2SO4 (10% v/v), NaOH (5% w/v), EDTA (0.5% w/V), and H2O2 (5% v/v), and characterized by X-ray diffraction (DRX). After the acetylation of the extracted cellulose, CA was characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermogravimetry analysis (TGA), and was applied in the membrane production...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28433157/enhanced-mechanical-properties-of-chitosan-nanodiamond-composites-by-improving-interphase-using-thermal-oxidation-of-nanodiamond
#13
Zahra Delavar, Akbar Shojaei
Polymer composite films based on chitosan (CS) and nanodimaond (ND) were prepared using solution casting method. ND with variable contents of carboxylic functional group was prepared using thermal oxidation at temperature of 420°C under air atmosphere at various durations of 1.5 and 4.5h. The interfacial interaction between NDs and CS and morphological evolution of CS in presence of NDs were investigated by Fourier transform infrared (FTIR), differential scanning calorimeter (DSC) and X-ray diffraction (XRD) analyses...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28433154/non-immunogenic-porous-and-antibacterial-chitosan-and-antheraea-mylitta-silk-sericin-hydrogels-as-potential-dermal-substitute
#14
Sunaina Sapru, Ananta K Ghosh, Subhas C Kundu
Limitation of existing grafts including restricted donor site, risks of immune reactions, infectious diseases and high cost alarms the growing need of natural, cost effective and functional graft as the dermal substitute. We fabricate stable (>6 weeks) and porous (57.23-75.22μm) yet flexible (in variable pH) matrices using Antheraea mylitta sericin crosslinked with well known biocompatible polysaccharide chitosan by natural crosslinker (genipin) without using any harsh chemical. The fabricated matrices are characterized in terms of chemical modifications (Fourier transform infrared spectroscopy), crystallinity (X-ray diffraction), swelling, degradability and thermal stability...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28433015/probing-the-effects-of-surface-hydrophobicity-and-tether-orientation-on-antibody-antigen-binding
#15
Derek B Bush, Thomas A Knotts
Antibody microarrays have the potential to revolutionize molecular detection for many applications, but their current use is limited by poor reliability, and efforts to change this have not yielded fruitful results. One difficulty which limits the rational engineering of next-generation devices is that little is known, at the molecular level, about the antibody-antigen binding process near solid surfaces. Atomic-level structural information is scant because typical experimental techniques (X-ray crystallography and NMR) cannot be used to image proteins bound to surfaces...
April 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28432999/effect-of-intra-oral-aging-on-t%C3%A2-m-phase-transformation-microstructure-and-mechanical-properties-of-y-tzp-dental-ceramics
#16
Luciana Meireles Miragaya, Renato Bastos Guimarães, Rodrigo Othávio de Assunção E Souza, Glauco Dos Santos Botelho, José Guilherme Antunes Guimarães, Eduardo Moreira da Silva
The aim of the present study was to evaluate the influence of intra-oral aging on the tetragonal-to-monoclinic (t→m) phase transformation of two Y-TZP dental ceramics - Lava Frame (Frame) and Lava Plus (Plus) - and determine the impact of this response on their microstructures and mechanical properties: flexural strength, Young's modulus, microhardness and fracture toughness. Standardized ceramic specimens were analyzed by X-ray diffraction (XRD), scanning electron microscopy (SEM) and atomic force microscopy (AFM)...
April 13, 2017: Journal of the Mechanical Behavior of Biomedical Materials
https://www.readbyqxmd.com/read/28432820/the-impact-of-small-motion-on-the-visualization-of-coronary-vessels-and-lesions-in-cardiac-ct-a-simulation-study
#17
Francisco Contijoch, J Webster Stayman, Elliot R McVeigh
PURPOSE: Coronary x-ray computed tomography angiography (CCTA) is used to non-invasively assess coronary artery geometry and has, combined with computational modeling, demonstrated the potential to identify physiologically significant lesions. These measurements require robust and accurate coronary imaging and delineation of vessels in the presence of small motion. This simulation study characterizes the impact of small, uncorrected vessel drifts during data acquisition on the assessment of vessel intensity, diameter, and shape...
April 22, 2017: Medical Physics
https://www.readbyqxmd.com/read/28432764/small-molecular-anion-recognition-by-a-shape-responsive-bowl-type-dodecavanadate
#18
Sho Kuwajima, Yuji Kikukawa, Yoshihito Hayashi
A dodecavanadate, [V₁₂O₃₂]⁴¯, is an inorganic bowl-type host with a cavity entrance with a diameter of 4.4 Å in the optimized structure. The linear, bent, and trigonal planar anions, are tested as a guest anion and the formation of host-guest complexes, [V₁₂O₃₂(X)]⁵¯ (X = CN¯, OCN¯, NO₂¯, NO₃¯, HCO₂¯, and CH₃CO₂¯) were confirmed by X-ray crystallographic analyses and ⁵¹V NMR study. The degree of the distortion of the bowl from a regular bowl to an oval bowl depends on the shape of the guest anion, after host-guest complex formation...
April 22, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#19
Abdelmoumin Zoghbi, Tianjiao Geng, Bo Wang
Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-β-cyclodextrin (HPβCD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HPβCD inclusion complex (KD)...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28432574/a-critical-appraisal-of-the-quality-of-adult-dual-energy-x-ray-absorptiometry-guidelines-in-osteoporosis-using-the-agree-ii-tool-an-euroaim-initiative
#20
Carmelo Messina, Bianca Bignotti, Alberto Bazzocchi, Catherine M Phan, Alberto Tagliafico, Giuseppe Guglielmi, Francesco Sardanelli, Luca Maria Sconfienza
OBJECTIVES: Dual energy X-ray absorptiometry (DXA) is the most widely used technique to measure bone mineral density (BMD). Appropriate and accurate use of DXA is of great importance, and several guidelines have been developed in the last years. Our aim was to evaluate the quality of published guidelines on DXA for adults. METHODS: Between June and July 2016 we conducted an online search for DXA guidelines, which were evaluated by four independent readers blinded to each other using the AGREE II instrument...
April 21, 2017: Insights Into Imaging
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