bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of endo‐ and exo‐N‐Protected 5‐Arylated 2‐Aminothiazoles through Direct Arylation: An Efficient Route to Cell Differentiation Accelerators
Authors: Dao‐Huy Toan , Waldner Birgit J. , Wimmer Laurin , Schnürch Michael , Mihovilovic Marko D. 
Published: June 2015

AbstractAn improved protocol for the direct arylation of N‐phenyl‐N‐benzyl(thiazol‐2‐yl)amine by using aryl bromides as aryl donors is reported. The procedure was compared with a previously reported protocol in which aryl iodides were used as arylating agents. The improved direct arylation protocol was applied to structurally isomeric and nonaromatic 3‐benzyl‐N‐phenylthiazol‐2(3H)‐imine. The two substrates for direct arylation were obtained from a common starting material, N‐phenyl(thiazol‐2‐yl)amine, which was regioselectively benzylated either on the exo‐cyclic or the endo‐cyclic nitrogen by using two sets of reaction conditions. For the arylation of the isomeric nonaromatic 3‐benzyl‐N‐phenylthiazol‐2(3H)‐imine, exclusive regioselectivity in the 5‐position could be achieved.
Synthesis of Chromen[4,3‐b]pyrrolidines by Intramolecular 1,3‐Dipolar Cycloadditions of Azomethine Ylides: An Experimental and Computational Assessment of the Origin of Stereocontrol
Authors: Costa Paulo R. R. , Sansano José M. , Cossío Unai , Barcellos Julio C. F. , Dias Ayres G. , Nájera Carmen , Arrieta Ana , de Cózar Abel , Cossío Fernando P. 
Published: June 2015

AbstractAzomethine ylides, generated from imine‐derived O‐cinnamyl or O‐crotonyl salicylaldeyde and α‐amino acids, undergo intramolecular 1,3‐dipolar cycloaddition, leading to chromene[4,3‐b]pyrrolidines. Two reaction conditions are used: (a) microwave‐assisted heating (200 W, 185 °C) of a neat mixture of reagents, and (b) conventional heating (170 °C) in PEG‐400 as solvent. In both cases, a mixture of two epimers at the α‐position of the nitrogen atom in the pyrrolidine nucleus was formed through the less energetic endo‐approach (B/C ring fusion). In many cases, the formation of the stereoisomer bearing a trans‐arrangement into the B/C ring fusion was observed in high proportions. Comprehensive computational and kinetic simulation studies are detailed. An analysis of the stability of transient 1,3‐dipoles, followed by an assessment of the intramolecular pathways and kinetics are also reported.
Machine learning on encephalographic activity may predict opioid analgesia
Authors: Gram M. , Graversen C. , Olesen A.E. , Drewes A.M. 
Published: June 2015

AbstractBackgroundOpioids are used for the treatment of pain. However, 30–50% of patients have insufficient effect to the opioid initially selected by the physician, and there is an urgent need for biomarkers to select responders to the most appropriate drug. Since opioids mediate their effect in the central nervous system, this study aimed to investigate if electroencephalography (EEG) during rest or pain before treatment could predict the analgesic response.MethodsEEG from 62 channels was recorded in volunteers during rest and tonic pain (cold pressor test). Morphine (30 mg) or placebo was then administered, and the pain test repeated 60 min after. Washout period between drugs was 7 days. Based on pain ratings, subjects were stratified into responders and non‐responders. Spectral analysis was performed on the EEG. Conventional statistics on group basis were used and, furthermore, the most discriminative EEG features were subjected to support vector machine classification to predict the response for the individual subjects.ResultsConventional statistics on the frequency bands revealed no differences between responders and non‐responders. On the individual basis, no differences between groups were found using resting EEG. However, EEG during cold pain was able to classify responders with an accuracy of 72% (p = 0.01) and the result was reproducible using baseline data from both study days.ConclusionsMachine learning based on EEG before treatment enabled separation between responders and non‐responders. This study represents the first step towards the prediction of opioid analgesia based on EEG features prior to drug administration, and advocates for the use of machine learning in future studies.
A Different Light on Normalization: Critical Theory and Responsive Evaluation Studying Social Justice in Participation Practices
Authors: Woelders Susan , Abma Tineke 
Published: June 2015

AbstractResponsive evaluation provides guidelines to include various stakeholders in dialogue. However, a substantial theory to understand power asymmetries and inequalities is lacking. The purpose of this article is to consider which theoretical framework for societal critique can be helpful to evaluate practices in relation to social justice. These questions will be addressed using fragments from a responsive evaluation study on the involvement of people with an intellectual disability in public policy. Our study shows that Foucault's framework on normalization was helpful. It revealed that the engagement and striving for equality and social justice can turn out to be disciplining itself.
Integrating Human Rights in Program Evaluation: Lessons From Law and Health Programs in Kenya
Authors: Gruskin Sofia , Waller Emily , Safreed‐Harmon Kelly , Ezer Tamar , Cohen Jonathan , Gathumbi Anne , Kameri‐Mbote Patricia 
Published: June 2015

AbstractMethods for assessing both the inclusion and impact of human rights within health program design and implementation are still nascent. We used human rights concepts and methods to evaluate the programs of three Kenyan nongovernmental organizations that integrate legal and health services as a means to empower key populations to better understand and claim their rights and improve their access to health care and justice. Drawing on evaluation experiences and results, this paper demonstrates that the systematic application of human rights principles and strategies can support the conceptualization of monitoring and evaluation objectives through logic model design, the identification and selection of appropriate evaluation measures, and the analysis of evaluation data. This evaluation represents an important step in moving human rights–related evaluation work beyond the mere conceptual and into the operational.
Promoting Social Justice Through a New Teacher Training Program for the Bedouin Population in the Negev: An Evaluation Case Study
Authors: Zamir Judith , Abu Jaber Saleem 
Published: June 2015

AbstractThis article presents the changes that took place in a new training model for student teachers in the Bedouin population as a result of joint work with the Evaluation Department and the Training Team of Kaye College for Education from the beginning of the program. The cooperation between the evaluation team and the program developers promoted equal opportunities for the Bedouin women teachers involved in the program. The joint project lasted for three years. Throughout this period, the evaluation department contributed to program development by means of developmental evaluation. The results show a higher quality of teacher training, including the enrichment of practicum at schools, the development of team and students’ social commitment and belonging, and the empowerment of women by improving their status at the professional and community level. The sense of independence and self‐confidence acquired by Bedouin women participating in the program constitutes a small and central step on the way toward social justice.
The Role of Evaluation in Affirmative Action–Type Programs
Authors: Zoabi Khawla , Awad Yaser 
Published: June 2015

AbstractThis article analyzes two cases of evaluation programs involving the Palestinian minority in Israel from the perspective of social justice and responsibility. The first focuses on the evaluation of a Pre‐Academic Preparatory Program (PAPP) of minority students in Sakhnin College. The second focuses on the evaluation of Equal Opportunities for Arab Minority Students at the Technion–Israel Institute of Technology. This article concludes that evaluation could be conceptualized as a promoter of social justice. The article suggests that the contribution of participatory–responsive evaluation is limited and maybe marginal. The article concludes that evaluation for social justice should be only a step in a longer process, which should feed into decision making afterward in order to change and improve policies and programs, as the case of PAPP suggests. Eventually, we conclude that evaluation played a role in promoting social justice in both systems.
Apatite fission‐track analysis of Cretaceous alkaline rocks of Ponta Grossa and Alto Paranaíba Arches, Brazil
Authors: Soares C. J. , Guedes S. , Jonckheere R. , Hadler J. C. , Passarella S. M. , Dias A. N. C. 
Published: June 2015

AbstractThis work presents fission‐track ages and thermal history modelling of apatite samples from two Brazilian alkaline formations: Alto Paranaíba and Ponta Grossa Arches. The apatite fission‐track ages obtained for Alto Paranaíba Arch agree with those determined by other radiometric dating methods presenting higher closure temperatures. The ages given by the fission‐track thermochronometer suggest that no strong tectonic event has occurred after Alto Paranaíba Formation during Upper Cretaceous. This event is also supported by thermal history modelling of this arch, which is characterized by fast cooling followed by residence at lower temperatures. On the other hand, apatite fission‐track ages from Ponta Grossa Arch are systematically lower than other radiometric ages, suggesting that at least one tectonic event occurred after Ponta Grossa Formation, around 130 Ma. Copyright © 2015 John Wiley & Sons, Ltd.
Cortical correlates of perceptual decision making during tactile spatial pattern discrimination
Authors: Li Hegner Yiwen , Lindner Axel , Braun Christoph 
Published: June 2015

AbstractPerceptual decision making involves a distributed cortical network including areas related to sensory feature extraction, decision formation, and finally signalling the decision through a motor response. Although these processing steps are supposed to occur in sequence, the seemingly instant mapping of a perceptual decision onto a motor response renders these processes almost indistinguishable. To dissociate cortical areas related to sensory decision making from areas that prepare the subsequent motor response, we performed functional magnetic resonance imaging during a tactile spatial pattern discrimination task with interleaved immediate and delayed response conditions. Decision difficulty was manipulated parametrically by adding spatial noise to the tactile patterns, resulting in a rise in decision time with increasing noise. We assumed that areas involved in making the decision should show a variation in their activation with decision time and irrespective of whether (immediate response condition) or not (delayed response condition) a motor response could be prepared in advance. To exhibit these putative decision areas, we used response time, as was obtained in the immediate response condition, as parametric predictor for the difficulty‐dependent variations of blood oxygenation level‐dependent (BOLD)‐activity in both response conditions. BOLD activations in right (contralateral) postcentral sulcus, right intraparietal sulcus (IPS) and bilateral anterior insula (aINS) reflected this parametric modulation in both response conditions, suggesting a role of these areas in tactile decisions independent of decision‐specific motor preparation. Furthermore, a multivariate pattern analysis performed on the BOLD responses in the delayed response condition for a single difficulty level independently validated IPS and aINS as decision‐related areas. Hum Brain Mapp 36:3339–3350, 2015. © 2015 Wiley Periodicals, Inc.
Brain tissue compartment density estimated using diffusion‐weighted MRI yields tissue parameters consistent with histology
Authors: Sepehrband Farshid , Clark Kristi A. , Ullmann Jeremy F.P. , Kurniawan Nyoman D. , Leanage Gayeshika , Reutens David C. , Yang Zhengyi 
Published: June 2015

AbstractWe examined whether quantitative density measures of cerebral tissue consistent with histology can be obtained from diffusion magnetic resonance imaging (MRI). By incorporating prior knowledge of myelin and cell membrane densities, absolute tissue density values were estimated from relative intracellular and intraneurite density values obtained from diffusion MRI. The NODDI (neurite orientation distribution and density imaging) technique, which can be applied clinically, was used. Myelin density estimates were compared with the results of electron and light microscopy in ex vivo mouse brain and with published density estimates in a healthy human brain. In ex vivo mouse brain, estimated myelin densities in different subregions of the mouse corpus callosum were almost identical to values obtained from electron microscopy (diffusion MRI: 42 ± 6%, 36 ± 4%, and 43 ± 5%; electron microscopy: 41 ± 10%, 36 ± 8%, and 44 ± 12% in genu, body and splenium, respectively). In the human brain, good agreement was observed between estimated fiber density measurements and previously reported values based on electron microscopy. Estimated density values were unaffected by crossing fibers. Hum Brain Mapp 36:3687–3702, 2015. © 2015 Wiley Periodicals, Inc.
Requirements Driven e‐SE
Authors: McCay Brian M. 
Published: June 2015

AbstractThis article discusses how custom system/software order request for quote (RFQ) responses are being supported via the Net by requirements driven e‐SE processes. These e‐SE processes couple traditional SE development point tool solutions with enterprise level collaborative product commerce (CPC) tool solutions to manage the custom system/software order RFQ bid process. This marriage of traditional SE and software development, application tool solutions with CPC solutions is coined “e‐Product Lifecycle Management (e‐PLM).”
Implementing on the Internet–Don't Take It Lightly
Authors: Mackey William , Bagg Thomas C. 
Published: June 2015

AbstractImplementing capabilities on the World Wide Web should never be taken lightly. A good systems engineer is able to examine such implementations from all points of view, including political, legal, security, access, technical deployment, and quality. This article summarizes the issues that were identified and evaluated in preparation for publishing the RECALL (Reusable Experience with Case‐Based Reasoning (CBR) for Automating Lessons Learned).
Fusion peptide P15‐CSP shows antibiofilm activity and pro‐osteogenic activity when deposited as a coating on hydrophilic but not hydrophobic surfaces
Authors: Li Xian , Contreras‐Garcia Angel , LoVetri Karen , Yakandawala Nandadeva , Wertheimer Michael R. , De Crescenzo Gregory , Hoemann Caroline D. 
Published: June 2015

AbstractIn the context of porous bone void filler for oral bone reconstruction, peptides that suppress microbial growth and promote osteoblast function could be used to enhance the performance of a porous bone void filler. We tested the hypothesis that P15‐CSP, a novel fusion peptide containing collagen‐mimetic osteogenic peptide P15, and competence‐stimulating peptide (CSP), a cationic antimicrobial peptide, has emerging properties not shared by P15 or CSP alone. Peptide‐coated surfaces were tested for antimicrobial activity toward Streptoccocus mutans, and their ability to promote human mesenchymal stem cell (MSC) attachment, spreading, metabolism, and osteogenesis. In the osteogenesis assay, peptides were coated on tissue culture plastic and on thin films generated by plasma‐enhanced chemical vapor deposition to have hydrophilic or hydrophobic character (water contact angles 63°, 42°, and 92°, respectively). S. mutans planktonic growth was specifically inhibited by CSP, whereas biofilm formation was inhibited by P15‐CSP. MSC adhesion and actin stress fiber formation was strongly enhanced by CSP, P15‐CSP, and fibronectin coatings and modestly enhanced by P15 versus uncoated surfaces. Metabolic assays revealed that CSP was slightly cytotoxic to MSCs. MSCs developed alkaline phosphatase activity on all surfaces, with or without peptide coatings, and consistently deposited the most biomineralized matrix on hydrophilic surfaces coated with P15‐CSP. Hydrophobic thin films completely suppressed MSC biomineralization, consistent with previous findings of suppressed osteogenesis on hydrophobic bioplastics. Collective data in this study provide new evidence that P15‐CSP has unique dual capacity to suppress biofilm formation, and to enhance osteogenic activity as a coating on hydrophilic surfaces. © 2015 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 103A: 3736–3746, 2015.
Rapid fabrication system for three‐dimensional tissues using cell sheet engineering and centrifugation
Authors: Hasegawa Akiyuki , Haraguchi Yuji , Shimizu Tatsuya , Okano Teruo 
Published: June 2015

AbstractThree‐dimensional (3D) tissues can be reconstructed by cell sheet technology, and various clinical researches using these constructed tissues have already been initiated to regenerate damaged tissues. While 3D tissues can be easily fabricated by layering cell sheets, the attachment period for cell adhesion between a cell sheet and a culture dish, or double‐layered cell sheets normally takes 20–30 min. This study proposed a more rapid fabrication system for bioengineered tissue using cell sheet technology and centrifugation. A C2C12 mouse myoblast sheet harvested from a temperature‐responsive culture dish will attach tightly to a culture dish or another cell sheet at 37°C after a 20 min‐incubation. However, the same cell sheet centrifuged (12–34 × g) for 3 min also attached tightly to a dish or another cell sheet at 37°C after only a 3 min‐incubation. The manipulation time was reduced by approximately two‐thirds by centrifugation. The rapid attachments were also cross‐sectionally confirmed by optical coherence tomography. These rapidly constructed cell sheet‐tissues using centrifugation showed active cell metabolism, cell viability, and very high production of vascular endothelial growth factor, like those prepared by the conventional method; indicating complete cell sheet‐attachment without any cell damage. This new system will be a powerful tool in the fields of cell sheet‐based tissue engineering and regenerative medicine, and accelerate the use of cell sheets in clinical applications. © 2015 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 103A: 3825–3833, 2015.
Energy Excess, Glucose Utilization, and Skeletal Remodeling: New Insights
Authors: Lecka-Czernik Beata , Rosen Clifford J 
Published: June 2015

Abstract

Skeletal complications have recently been recognized as another of the several comorbidities associated with diabetes. Clinical studies suggest that disordered glucose and lipid metabolism have a profound effect on bone. Diabetes-related changes in skeletal homeostasis result in a significant increased risk of fractures, although the pathophysiology may differ from postmenopausal osteoporosis. Efforts to understand the underlying mechanisms of diabetic bone disease have focused on the direct interaction of adipose tissue with skeletal remodeling and the potential influence of glucose utilization and energy uptake on these processes. One aspect that has emerged recently is the major role of the central nervous system in whole-body metabolism, bone turnover, adipose tissue remodeling, and beta cell secretion of insulin. Importantly, the skeleton contributes to the metabolic balance inherent in physiologic states. New animal models have provided the insights necessary to begin to dissect the effects of obesity and insulin resistance on the acquisition and maintenance of bone mass. In this Perspective, we focus on potential mechanisms that underlie the complex interactions between adipose tissue and skeletal turnover by focusing on the clinical evidence and on preclinical studies indicating that glucose intolerance may have a significant impact on the skeleton. In addition, we raise fundamental questions that need to be addressed in future studies to resolve the conundrum associated with glucose intolerance, obesity, and osteoporosis. © 2015 American Society for Bone and Mineral Research.
The Effect of GADD45a on Furazolidone‐Induced S‐Phase Cell‐Cycle Arrest in Human Hepatoma G2 Cells
Authors: Sun Yu , Tang Shusheng , Xiao Xilong 
Published: June 2015

ABSTRACTIn this study, overexpression of GADD45a induced by furazolidone in HepG2 cells could arouse S‐phase cell cycle arrest, suppress cell proliferation, and increase the activities of cyclin D1, cyclin D3, and cyclin‐dependent kinase 6 (CDK6). To the opposite, GADD45a knockdown cells by RNAi could reduce furazolidone‐induced S‐phase cell cycle arrest, increase the cell viability, decrease the activities of cyclin D1, cyclin D3, and CDK6; however, cyclin‐dependent kinase 4 (CDK4) showed no change. Moreover, data from our current studies show that cyclin D1, cyclin D3, and CDK6 are target genes functioning at the downstream of the GADD45a pathway induced by furazolidone. These results demonstrate that the GADD45a pathway is partially responsible for the furazolidone‐induced S‐phase cell cycle arrest. GADD45a influences furazolidone‐induced S‐phase cell cycle arrest in human hepatoma G2 cells via cyclin D1, cyclin D3, and CDK6, but not CDK4.
The Phytoalexin Resveratrol Ameliorates Ochratoxin A Toxicity in Human Embryonic Kidney (HEK293) Cells
Authors: Raghubeer Shanel , Nagiah Savania , Phulukdaree Alisa , Chuturgoon Anil 
Published: June 2015

ABSTRACTOchratoxin A (OTA) is a nephrotoxic mycotoxin produced by Aspergillus and Penicillium fungi. It contaminates human and animal food products, and chronic exposure is associated with renal fibrosis in humans (Balkan endemic nephropathy). Resveratrol, a phytoalexin, possesses anti‐cancer and antioxidant properties. We investigated the mechanism of cellular oxidative stress induced by OTA, and the effect of resveratrol in human embryonic kidney (HEK293) cells over 24 and 48 h. Cells were exposed to OTA [IC50 = 1.5 μM (24 h) and 9.4 μM (48 h) determined using MTT assay] and 25 μM resveratrol. Glutathione was quantified by luminometry and gene expression of Nrf2 and OGG1 was determined by qPCR. Protein expression of Nrf2, LonP1, SIRT3, and pSIRT1 was assessed by Western blot, DNA damage (comet assay), and intracellular reactive oxygen species (flow cytometry). At 24 h, resveratrol increased mRNA expression of the DNA repair enzyme, OGG1 (P < 0.05), whereas OTA and OTA+resveratrol significantly decreased OGG1 expression (P < 0.05). OGG1 expression increased during 48‐h exposure to resveratrol and OTA+resveratrol (P < 0.05). Comet tail lengths doubled in 48‐h OTA‐treated cells, whereas at both time periods, OTA+resveratrol yielded shorter comet tails (P < 0.0001). During 24‐ and 48‐h exposure, OTA, resveratrol, and OTA+resveratrol significantly decreased mRNA expression of Nrf2 (P < 0.05). Luminometry analysis of GSH revealed an increase by OTA+resveratrol for 24 and 48 h (P < 0.05 and P < 0.001, respectively). Western blot analysis showed decreased Nrf2 protein expression during 24‐h exposure, but increased Nrf2 expression during 48 h. LonP1 protein expression increased during 24‐h exposure to OTA (P < 0.05) and OTA+resveratrol (P < 0.0011) and during 48‐h exposure to resveratrol (P < 0.0005). J. Cell. Biochem. 116: 2947–2955, 2015. © 2015 Wiley Periodicals, Inc.