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https://www.readbyqxmd.com/read/29779181/tailoring-acyclovir-prodrugs-with-enhanced-antiviral-activity-rational-design-synthesis-human-plasma-stability-and-in-vitro-evaluation
#1
Radoslav L Chayrov, Evgenios K Stylos, Maria V Chatziathanasiadou, Kiril N Chuchkov, Aleksandra I Tencheva, Androniki D Kostagianni, Tsenka S Milkova, Assia L Angelova, Angel S Galabov, Stoyan A Shishkov, Daniel G Todorov, Andreas G Tzakos, Ivanka G Stankova
Bile acid prodrugs have served as a viable strategy for refining the pharmaceutical profile of parent drugs through utilizing bile acid transporters. A series of three ester prodrugs of the antiherpetic drug acyclovir (ACV) with the bile acids cholic, chenodeoxycholic and deoxycholic were synthesized and evaluated along with valacyclovir for their in vitro antiviral activity against herpes simplex viruses type 1 and type 2 (HSV-1, HSV-2). The in vitro antiviral activity of the three bile acid prodrugs was also evaluated against Epstein-Barr virus (EBV)...
May 19, 2018: Amino Acids
https://www.readbyqxmd.com/read/29778963/ph-dependent-silica-nanoparticle-dissolution-and-cargo-release
#2
Giorgia Giovaninni, Colin J Moore, Andrew J Hall, Hugh J Byrne, Vladimir Gubala
The dissolution of microporous silica nanoparticles (NP) in aqueous environments of different biologically relevant pH was studied in order to assess their potential as drug delivery vehicles. Silica NPs, loaded with fluorescein, were prepared using different organosilane precursors (tetraethoxysilane, ethyl triethoxysilane or a 1:1 molar ratio of both) and NP dissolution was evaluated in aqueous conditions at pH 4, pH 6 and pH 7.4. These conditions correspond to the acidity of the intracellular environment (late endosome, early endosome, cytosol respectively) and gastrointestinal tract ('fed' stomach, duodenum and jejunum respectively)...
May 16, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29778947/dissociable-contributions-of-dorsal-and-ventral-striatal-regions-on-a-rodent-cost-benefit-decision-making-task-requiring-cognitive-effort
#3
Mason M Silveira, Melanie Tremblay, Catharine A Winstanley
Cognitive effort is a ubiquitous process, yet surprisingly little is known about the brain mechanisms responsible for evaluating it. Here, we utilize the rat Cognitive Effort Task (rCET) to probe the striatum's role in deciding between options that vary in the amount of cognitive effort required for success. In the rCET, animals choose to perform either an easy trial, in which the attentional demand is low but the potential reward is small, or a difficult trial which is more attentionally demanding but can yield twice the sugar pellets...
April 24, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29778899/dopamine-loss-alters-the-hippocampus-nucleus-accumbens-synaptic-transmission-in-the-tg2576-mouse-model-of-alzheimer-s-disease
#4
Alberto Cordella, Paraskevi Krashia, Annalisa Nobili, Annabella Pignataro, Livia La Barbera, Maria Teresa Viscomi, Alessandro Valzania, Flavio Keller, Martine Ammassari-Teule, Nicola Biagio Mercuri, Nicola Berretta, Marcello D'Amelio
The functional loop involving the ventral tegmental area (VTA), dorsal hippocampus and nucleus accumbens (NAc) plays a pivotal role in the formation of spatial memory and persistent memory traces. In particular, the dopaminergic innervation from the VTA to the hippocampus is critical for hippocampal-related memory function and alterations in the midbrain dopaminergic system are frequently reported in Alzheimer's disease (AD), contributing to age-related decline in memory and non-cognitive functions. However, much less is known about the hippocampus-NAc connectivity in AD...
May 17, 2018: Neurobiology of Disease
https://www.readbyqxmd.com/read/29778183/high-genetic-diversity-of-extended-spectrum-%C3%AE-lactamases-producing-escherichia-coli-in-feces-of-horses
#5
Syndia Sadikalay, Yann Reynaud, Stéphanie Guyomard-Rabenirina, Mélanie Falord, Célia Ducat, Laetitia Fabre, Simon Le Hello, Antoine Talarmin, Séverine Ferdinand
Extended-spectrum beta-lactamases (ESBLs), especially those of the CTX-M type, represent a major public health problem throughout the world. Although the carriage of ESBL-producing Enterobacteriaceae (EPE) in feces of horses is now well recognized, little is known about the diversity of EPE after treatment of horses with antibiotics. We undertook this study to assess and follow the diversity of EP Escherichia coli isolated from horses after antibiotic treatment for an infection. Fecal samples from two horses treated and two that were untreated were tested for the presence of EPE on different days...
June 2018: Veterinary Microbiology
https://www.readbyqxmd.com/read/29778076/design-and-synthesis-of-core-shell-fe-3-o-4-ptmt-composite-magnetic-microspheres-for-adsorption-of-heavy-metals-from-high-salinity-wastewater
#6
Xin Huang, Jinyue Yang, Jingkang Wang, Jingtao Bi, Chuang Xie, Hongxun Hao
In this study, a novel magnetic nanoparticles (MNP) modified by an organodisulfide polymer (PTMT) was designed for adsorption of heavy metals (Hg(II), Pb(II) and Cd(II)) from simulated coal chemical high salinity wastewater. The MNP-PTMT nano-composite was synthesize and characterized by SEM, TEM, FTIR, BET, VSM, TGA and XRD. The results indicate that the wanted MNP-PTMT magnetic nanoparticles were successfully obtained by modification. Adsorption experiments were systematically carried out to evaluate the performance of the obtained nanoparticles and to build up the adsorption models...
May 10, 2018: Chemosphere
https://www.readbyqxmd.com/read/29777988/insight-into-structural-requirements-for-selective-and-or-dual-cxcr3-and-cxcr4-allosteric-modulators
#7
Anja Kolarič, Urban Švajger, Tihomir Tomašič, Regine Brox, Theresa Frank, Nikola Minovski, Nuska Tschammer, Marko Anderluh
Based on the previously published pyrazolopyridine-based hit compound for which negative allosteric modulation of both CXCR3 and CXCR4 receptors was disclosed, we designed, synthesized and biologically evaluated a set of novel, not only negative, but also positive allosteric modulators with preserved pyrazolopyridine core. Compound 9e is a dual negative modulator, inhibiting G protein activity of both receptors. For CXCR4 receptor para-substituted aromatic group of compounds distinguishes between negative and positive modulation...
May 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777879/standardizing-evaluation-process-necessary-for-achieving-sdgs-a-case-study-of-india
#8
Alok Srivastava
A set of 17 Sustainable Development Goals (SDGs) adopted by the United Nations General Assembly in September 2015 are to be implemented and achieved in every country from the year 2016 to 2030. In Indian context, all these goals are very relevant and critical, as India missed the target on many components of the Millennium Development Goals (MDGs). The author strongly feels that one of the key reasons was lack of an in-built robust system for measuring the progress and achievements of MDGs. Monitoring and Evaluation of programmes and schemes, aiming at different SDGs, in a robust and regular manner is therefore need of the hour...
May 9, 2018: Evaluation and Program Planning
https://www.readbyqxmd.com/read/29776930/modifying-the-lantibiotic-mutacin-1140-for-increased-yield-activity-and-stability
#9
Mengxin Geng, Leif Smith
Mutacin 1140 belongs to the epidermin family of type AI lantibiotics. This family has a broad spectrum of activity against Gram-positive bacteria. The binding of mutacin 1140 to lipid II leads to the inhibition of cell wall synthesis. Pharmacokinetic experiments on type AI lantibiotics are generally discouraging for clinical applications due to their short half-life. The unprotected dehydrated and protease susceptible residues outside of the lanthionine rings may play a role in their short half-life in physiological settings...
May 18, 2018: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/29776710/pharmacokinetics-pharmacodynamics-computer-decision-support-technologies-and-antimicrobial-stewardship-the-compass-and-rudder
#10
REVIEW
Robert C Owens, Catharine C Bulik, David R Andes
The first guidelines for conducting antimicrobial stewardship in the hospitalized setting were published in 2007. These guidelines recommend that stewardship programs employ the science of pharmacokinetics-pharmacodynamics (PK-PD) as well as adopting computerized decision support technologies when possible. The United States Food and Drug Administration have adopted PK-PD as a cornerstone in the evaluation of antimicrobial agents during clinical development. The core principles of PK-PD center around describing the relationship between drug exposure indexed to the susceptibility of the infecting bacterial pathogen and patient response...
April 13, 2018: Diagnostic Microbiology and Infectious Disease
https://www.readbyqxmd.com/read/29776646/international-consortium-of-vascular-registries-consensus-recommendations-for-peripheral-revascularisation-registry-data-collection
#11
Christian-Alexander Behrendt, Daniel Bertges, Nikolaj Eldrup, Adam W Beck, Kevin Mani, Maarit Venermo, Zoltán Szeberin, Gabor Menyhei, Ian Thomson, Georg Heller, Pius Wigger, Gudmundur Danielsson, Giuseppe Galzerano, Cristina Lopez, Martin Altreuther, Birgitta Sigvant, Henrik C Rieß, Art Sedrakyan, Barry Beiles, Martin Björck, Jonathan R Boyle, E Sebastian Debus, Jack Cronenwett
OBJECTIVE/BACKGROUND: To achieve consensus on the minimum core data set for evaluation of peripheral arterial revascularisation outcomes and enable collaboration among international registries. METHODS: A modified Delphi approach was used to achieve consensus among international vascular surgeons and registry members of the International Consortium of Vascular Registries (ICVR). Variables, including definitions, from registries covering open and endovascular surgery, representing 14 countries in ICVR, were collected and analysed to define a minimum core data set and to develop an optimum data set for registries...
May 15, 2018: European Journal of Vascular and Endovascular Surgery
https://www.readbyqxmd.com/read/29775949/design-and-synthesis-of-some-new-carboxamide-and-propanamide-derivatives-bearing-phenylpyridazine-as-a-core-ring-and-the-investigation-of-their-inhibitory-potential-on-in-vitro-acetylcholinesterase-and-butyrylcholinesterase
#12
Burcu Kilic, Hayrettin O Gulcan, Fatma Aksakal, Tugba Ercetin, Nihan Oruklu, E Umit Bagriacik, Deniz S Dogruer
A series of new carboxamide and propanamide derivatives bearing phenylpyridazine as a core ring were designed, synthesized and evaluated for their ability to inhibit both cholinesterase enzymes. In addition, a series of carboxamide and propanamide derivatives bearing biphenyl instead of phenylpyridazine were also synthesized to examine the inhibitory effect of pyridazine moiety on both cholinesterase enzymes. The inhibitory activity results revealed that compounds 5b, 5f, 5h, 5j, 5l pyridazine-3-carboxamide derivative, exhibited selective acetylcholinesterase (AChE) inhibition with IC50 values ranging from 0...
May 8, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29775509/exploring-the-growth-trajectory-of-cultural-competence-in-taiwanese-paediatric-nurses
#13
Chiu-I Chen, Mei-Chih Huang
AIM: The purpose of this study was to explore the evolution of cultural competence in Taiwanese paediatric nurses. BACKGROUND: Because transnational marriage has become a social phenomenon in Taiwan, the proportion of newborns of new immigrant mothers accounts for 8-10% of total births every year. Since family-centered care is the core value of paediatric nursing, it is necessary to teach caregivers how to take care of hospitalized children and perform related nursing care as well as to determine what difficulties nurses will encounter when they care for patients from diverse cultures and to find solutions for these problems...
May 18, 2018: Journal of Clinical Nursing
https://www.readbyqxmd.com/read/29775437/digital-microscopic-evaluation-of-vertical-marginal-discrepancies-of-cad-cam-fabricated-zirconia-cores
#14
Syed Rashid Habib
OBJECTIVE: The aim of this in vitro research study was to evaluate the vertical marginal discrepancies of zirconia (Zr) cores fabricated by five different computer-aided design and manufacturing (CAD/CAM) systems using a digital microscope. MATERIALS AND METHODS: A total of 60 specimens were prepared and randomly divided into five groups (n=12 each) using the following systems: Ceramill Motion 2 (CM, Amanngirrbach, Germany); Weiland (WI, Ivoclar Vivadent, USA); Cerec (CS, Sirona Dental, USA); Zirkonzahn (ZZ, Gmbh Bruneck, Italy) and Cad4dent (CD, Canada)...
May 18, 2018: Biomedizinische Technik. Biomedical Engineering
https://www.readbyqxmd.com/read/29775421/probability-of-heat-intolerance-standardized-interpretation-of-heat-tolerance-testing-results-versus-specialist-judgment
#15
Haggai Schermann, Erin Craig, Einat Yanovich, Itay Ketko, Gary Kalmanovich, Ran Yanovich
CONTEXT:   The heat-tolerance test (HTT) is a screening tool for secondary prevention of exertional heat illness by the Israel Defense Forces. To discern participant tolerance, recruits are exposed to intermediate environmental and exercise stresses, and their physiological responses, core temperature, and heart rate are monitored. When their physiological measures rise at a higher rate or exceed the upper levels of absolute values compared with other participants, heat intolerance (HI) is diagnosed...
April 2018: Journal of Athletic Training
https://www.readbyqxmd.com/read/29775078/effects-of-a-parent-implemented-developmental-reciprocity-treatment-program-for-children-with-autism-spectrum-disorder
#16
Grace W Gengoux, Salena Schapp, Sarah Burton, Christina M Ardel, Robin A Libove, Gina Baldi, Kari L Berquist, Jennifer M Phillips, Antonio Y Hardan
Developmental approaches to autism treatment aim to establish strong interpersonal relationships through joint play. These approaches have emerging empirical support; however, there is a need for further research documenting the procedures and demonstrating their effectiveness. This pilot study evaluated changes in parent behavior and child autism symptoms following a 12-week Developmental Reciprocity Treatment parent-training program. A total of 22 children with autism spectrum disorder between 2 and 6 years (mean age = 44...
May 1, 2018: Autism: the International Journal of Research and Practice
https://www.readbyqxmd.com/read/29774957/progress-and-challenges-in-consolidating-the-management-of-amazonian-protected-areas-and-indigenous-territories
#17
Raymond E Gullison, Jared Hardner
Achieving the effective management of all existing protected areas and indigenous territories in the Amazon Biome may be needed to avoid a deforestation "tipping point" beyond which regional climatic feedbacks and global climate change interact to catalyze irreversible drying and savannization of large portions of the biome. However, the time and money required to consolidate the effective management of all types of protected sites in the Amazon is still poorly understood. At present, protected areas and indigenous territories cover 45...
May 18, 2018: Conservation Biology: the Journal of the Society for Conservation Biology
https://www.readbyqxmd.com/read/29774926/an-anionic-shell-shields-a-cationic-core-allowing-for-uptake-and-release-of-polyelectrolytes-within-core-shell-responsive-microgels
#18
Arjan P H Gelissen, Andrea Scotti, Sarah K Turnhoff, Corinna Janssen, Aurel Radulescu, Andrij Pich, Andrey A Rudov, Igor I Potemkin, Walter Richtering
To realize carriers for drug delivery, cationic containers are required for anionic guests. Nevertheless, the toxicity of cationic carriers limits their practical use. In this study, we investigate a model system of polyampholyte N-isopropylacrylamide (NIPAM)-based microgels with a cationic core and an anionic shell to study whether the presence of a negative shell allows the cationic core to be shielded while still enabling the uptake and release of the anionic guest polyelectrolytes. These microgels are loaded with polystyrene sulfonate of different molecular weights to investigate the influence of their chain length on the uptake and release process...
May 18, 2018: Soft Matter
https://www.readbyqxmd.com/read/29774785/development-of-a-management-algorithm-for-the-diagnosis-of-cellular-fibroepithelial-lesions-from-core-needle-biopsies
#19
Jaehag Jung, Eunyoung Kang, Su Min Chae, Hyojin Kim, So Yeon Park, Bo La Yun, Sun Mi Kim, Mijung Jang, Sung-Won Kim, Eun-Kyu Kim
PURPOSE: Surgical excision is recommended for complete evaluation of cellular fibroepithelial lesions identified from core needle biopsy. The purpose of this study was to determine factors associated with phyllodes tumor among cellular fibroepithelial lesions from core biopsies and develop a scoring system to predict the risk of phyllodes tumor. METHODS: We retrospectively reviewed clinical data of 169 breast lesions that were diagnosed as cellular fibroepithelial lesions from core needle biopsy at the Seoul National University Bundang Hospital between March 2005 and January 2013...
May 1, 2018: International Journal of Surgical Pathology
https://www.readbyqxmd.com/read/29774599/deep-convolutional-neural-network-for-segmentation-of-knee-joint-anatomy
#20
Zhaoye Zhou, Gengyan Zhao, Richard Kijowski, Fang Liu
PURPOSE: To describe and evaluate a new segmentation method using deep convolutional neural network (CNN), 3D fully connected conditional random field (CRF), and 3D simplex deformable modeling to improve the efficiency and accuracy of knee joint tissue segmentation. METHODS: A segmentation pipeline was built by combining a semantic segmentation CNN, 3D fully connected CRF, and 3D simplex deformable modeling. A convolutional encoder-decoder network was designed as the core of the segmentation method to perform high resolution pixel-wise multi-class tissue classification for 12 different joint structures...
May 17, 2018: Magnetic Resonance in Medicine: Official Journal of the Society of Magnetic Resonance in Medicine
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