bluuebunny/crossref_metadata_2025_split huggingface dataset:
Urea derivatives carrying a thiophenylthiazole moiety: Design, synthesis, and evaluation of antitubercular and InhA inhibitory activities
Authors: Keleş Atıcı Rüveyde , Doğan Şengül Dilem , Gündüz Miyase Gözde , Krishna Vagolu Siva , Chebaiki Melina , Homberset Håvard , Lherbet Christian , Mourey Lionel , Tønjum Tone 
Published: June 2022

AbstractThe recent emergence of drug‐resistant strains of Mycobacterium tuberculosis (Mtb) has complicated and significantly slowed efforts to eradicate and/or reduce the worldwide incidence of life‐threatening acute and chronic cases of tuberculosis. To overcome this setback, researchers have increased the intensity of their work to identify new small‐molecule compounds that are expected to remain efficacious antimicrobials against Mtb. Here, we describe our effort to apply the principles of molecular hybridization to synthesize 16 compounds carrying thiophene and thiazole rings beside the core urea functionality (TTU1–TTU16). Following extensive structural characterization, the obtained compounds were initially evaluated for their antimycobacterial activity against Mtb H37Rv. Subsequently, three derivatives standing out with their anti‐Mtb activity profiles and low cytotoxicity (TTU5, TTU6, and TTU12) were tested on isoniazid‐resistant clinical isolates carrying katG and inhA mutations. Additionally, due to their pharmacophore similarities to the well‐known InhA inhibitors, the molecules were screened for their enoyl acyl carrier protein reductase (InhA) inhibitory potentials. Molecular docking studies were performed to support the experimental enzyme inhibition data. Finally, drug‐likeness of the selected compounds was established by theoretical calculations of physicochemical descriptors.
Hemostasis using a covered self‐expandable metal stent for pseudoaneurysm bleeding from the perihilar bile duct
Authors: Ishii Yu , Nakayama Akihiro , Kikuchi Kazuo , Nakatani Kei , Konda Kenichi , Mori Daichi , Nishihara Shigetoshi , Oikawa Shu , Nomoto Tomohiro , Usami Tomono , Noguchi Toshihiro , Mitsui Yuta , Yoshida Hitoshi 
Published: June 2022

AbstractAlthough there are many reports of hemostasis with covered self‐expandable metal stent (CSEMS) for bleeding from the papilla of Vater and the intrapapillary and distal bile duct, there are rare reports of its use for hemostasis in the perihilar bile duct. We report the case of a patient undergoing supportive care for perihilar cholangiocarcinoma with acute cholecystitis after side‐by‐side placement of uncovered SEMS for perihilar bile duct obstruction. Percutaneous transhepatic gallbladder aspiration was performed upon admission, and hematemesis occurred the next day. Since computed tomography scanning showed a pseudoaneurysm in the right uncovered SEMS, hemostasis by interventional radiology (IVR) was performed thrice for massive bleeding; however, hemostasis could not be achieved. When endoscopic retrograde cholangiopancreatography was performed for scrutiny and treatment of melena and increased hepatobiliary enzyme, the endoscopic visual field could not be secured by bleeding, and changes in hemodynamics were observed; thus, IVR was required, but it was difficult to perform. Since bleeding from the right bile duct was expected, hemostasis was performed using CSEMS. This is the first report of hemostasis performed by placing a covered SEMS for bleeding from a pseudoaneurysm of the intrahepatic bile duct.
A flexible extended generalized Pareto distribution for tail estimation
Authors: Gamet Philémon , Jalbert Jonathan 
Published: June 2022

AbstractFor both financial and environmental applications, tail distributions often correspond to extreme risks and an accurate modeling is mandatory. The peaks‐over‐threshold model is a classic way to model the exceedances over a high threshold with the generalized Pareto distribution. However, for some applications, the choice of a high threshold is challenging and the asymptotic conditions for using this model are not always satisfied. The class of extended generalized Pareto models can be used in this case. However, the existing extended model have either infinite or null density at the threshold, which is not consistent with tail modeling. In the present article, we propose new extensions of the generalized Pareto distribution for which the density at the threshold is positive and finite. The proposed extensions provide better estimate of the upper tail index for low thresholds than existing models. They are also appropriate for high thresholds because in that case, the extended models simplify to the generalize Pareto model. The performance and flexibility of the models are illustrated with the modeling of temperature exceeding a low threshold and non‐zero precipitations recorded in Montreal. For non‐zero precipitation, the very low threshold of 0 is used.
Analysis of PDC cutter cutting‐broken conglomerate based on the discrete element method
Authors: Liu Xiaoao , Zou Deyong , Chen Yahui , Huang Yong , Wang Qing 
Published: June 2022

AbstractIt is well known that the magnitude of impact load is one main reason for polycrystalline diamond compact (PDC) cutter failure rapidly when drilling conglomerate formation. However, there are many factors affecting the magnitude of impact load. To assess and mitigate these impacts, the discrete element model of PDC cutting‐broken conglomerate has been established, and the influence law of cementation strength difference (CSD), gravel diameter, and cutting velocity on impact load and gravel fragmentation in the process of cutting broken conglomerate is performed. What is more, the laboratory experiment of rock cutting by different shaped PDC cutters under different CSD and gravel diameters has also been conducted, and the correctness of numerical simulation results is verified by laboratory experiment. Meanwhile, the cutting depth and impact load of different shape PDC cutters under different CSD and gravel diameters have been analyzed. First, the simulation results show that the stripping mode of gravel mainly occurs when the CSD is large, and the corresponding axial and tangential impact load (mean axial peak cutting force [MAPCF]/mean tangential peak cutting force [MTPCF]) is relatively small. As the decrease of CSD, the gravel will be directly broken and the magnitude of the MAPCF/MTPCF will gradually increase, and the probability of impact damage to the cutting cutter will incrementally increase. In addition, larger gravel diameter and cutting velocity will lead to larger MAPCF/MTPCF, and the mode of gravel fragmentation changes gradually from being stripped to being directly broken with the increase of gravel diameter. Second, the laboratory experiment results not only verify the correctness of the simulation results but also find that ridged diamond element cutter has the smallest impact load and the largest cutting depth under different CSD and gravel diameters. This paper can provide a theoretical foundation for the optimization of drilling parameters and PDC bit design in drilling conglomerate formation.
Chronic and Acute Effects of Imidacloprid on a Simulated BEEHAVE Honeybee Colony
Authors: Reiner Dominik , Spangenberg Matthias C. , Grimm Volker , Groeneveld Jürgen , Wiegand Kerstin 
Published: June 2022

Abstract
Honeybees (Apis mellifera) are important pollinators for wild plants as well as for crops, but honeybee performance is threatened by several stressors including varroa mites, gaps in foraging supply, and pesticides. The consequences of bee colony longtime exposure to multiple stressors are not well understood. The vast number of possible stressor combinations and necessary study duration require research comprising field, laboratory, and simulation experiments. We simulated long-term exposure of a honeybee colony to the insecticide imidacloprid and to varroa mites carrying the deformed wing virus in landscapes with different temporal gaps in resource availability as single stressors and in combinations. Furthermore, we put a strong emphasis on chronic lethal, acute sublethal, and acute lethal effects of imidacloprid on honeybees. We have chosen conservative published values to parameterize our model (e.g., highest reported imidacloprid contamination). As expected, combinations of stressors had a stronger negative effect on bee performance than each single stressor alone, and effect sizes were larger after 3 years of exposure than after the first year. Imidacloprid-caused reduction in bee performance was almost exclusively due to chronic lethal effects because the thresholds for acute effects were rarely met in simulations. In addition, honeybee colony extinctions were observed by the last day of the first year but more pronounced on the last days of the second and third simulation year. In conclusion, our study highlights the need for more long-term studies on chronic lethal effects of pesticides on honeybees. Environ Toxicol Chem 2022;41:2318–2327. © 2022 The Authors. Environmental Toxicology and Chemistry published by Wiley Periodicals LLC on behalf of SETAC.
The focus on foods for special medical purposes and food supplements in age‐related disorders
Authors: Ullah Hammad , Khan Ayesha , Daglia Maria 
Published: June 2022

AbstractThe number of people over 60 years of age is increasing worldwide, representing a population of one billion in 2019, which is predicted to nearly double by 2050. In old age, people are more prone to the development of chronic disorders, mainly due to altered body responses to intracellular and extracellular stresses, where overactive oxidative stress and inflammatory processes initiate and stimulate degenerative processes in the body, resulting in metabolic diseases, loss of muscle strength, bone and joint disorders, neurodegenerative disorders, cardiovascular pathologies, and carcinogenesis. Moreover, treatment of patients of advanced age is more complex, due to the simultaneous involvement of multiple disease mechanisms, and the nonlinear association between disease risk factors and their disease endpoints. Most people in their old age are receiving treatment with two or more pharmacological drugs for the management of old age ailments, but on other hand, this increases the occurrence of adverse events in this population, attributed to their pharmacokinetic and pharmacodynamic alterations. One of the better approaches is primary prevention that may postpone the onset of morbidity with an improvement in general quality of life. The use of food supplements by old aged subjects is proportionally increasing for this purpose. This short commentary is focused on the basis of the use of foods for special medical purposes, and food supplements in the prevention of age‐related disorders.
The importance of scientific data and historical heritage of the geophysical and astronomical observatory of coimbra university for the study of geophysical sciences
Authors: Gomes Ana , Ramos Anabela , Figueiredo Fernando , Ribeiro Paulo 
Published: June 2022

AbstractThe Geophysical and Astronomical Observatory of the University of Coimbra (OGAUC) was officially created in 2013 after merging of two historical institutions: the Astronomical Observatory and the Geophysical Institute. As a result of almost 200 years of observations and research in astronomy and geophysical sciences, the OGAUC possesses a unique and valuable collection of long‐term observational and instrumental records. These data have an indispensable value in current geophysical and climatic studies, being among the most complete and significant in Portugal and the world. The OGAUC's data collections are complemented by a vast technical‐scientific production such as reports, research memoranda, articles, books, and instruments. This archive is largely not inventoried and poorly studied (particularly concerning meteorological, geomagnetic, and seismological data). This paper highlights the importance of the OGAUC's extensive data collection and discusses the difficulties and barriers related to its inventorying, preservation, and dissemination to the scientific community, policymakers, stakeholders, and the general public.
Abnormal functional connectivities patterns of multidomain cognitive impairments in pontine stroke patients
Authors: Wang Yingying , Wang Caihong , Wei Ying , Miao Peifang , Liu Jingchun , Wu Luobing , Li Zhen , Li Xin , Wang Kaiyu , Cheng Jingliang 
Published: June 2022

AbstractCognitive dysfunction in patients with infratentorial stroke has been paid little attention. Brainstem stroke may disrupt network connectivity across the whole brain and affect multidomain cognition, but the details of this process remain unclear. The study aimed to investigate the effects of stroke‐induced pontine injury on whole‐brain network connectivity and cognitive function. We included 47 patients with pontine stroke and 56 healthy comparisons (HC), who underwent cognitive tests and functional magnetic resonance imaging (fMRI). Seven meaningful brain networks were identified using independent component analysis (ICA). Patients with pontine stroke had decreased intra‐network functional connectivities (FCs) in the primary perceptual and higher cognitive control networks, including sensorimotor network (SMN), visual network (VIS), default mode network (DMN), and salience network (SAN), as well as decreased inter‐network FCs in the primary perceptual (VIS‐SMN) and higher cognitive control networks (bilateral frontoparietal networks, rFPN‐lFPN). While the FCs between the primary perceptual and higher cognitive control networks (VIS‐DMN, VIS‐rFPN, VIS‐lFPN) were increased. Furthermore, the alterations in these FCs correlated with patients' cognitive measurements. These findings suggested that the infratentorial stroke can induce dysfunctional connectivity in both primary perceptual and higher cognitive control networks at the whole‐brain level, which may be attributable to the neural substrates of multidomain cognitive deficits in these patients.
Experimental suppression of transcranial magnetic stimulation‐electroencephalography sensory potentials
Authors: Ross Jessica M. , Sarkar Manjima , Keller Corey J. 
Published: June 2022

AbstractThe sensory experience of transcranial magnetic stimulation (TMS) evokes cortical responses measured in electroencephalography (EEG) that confound interpretation of TMS‐evoked potentials (TEPs). Methods for sensory masking have been proposed to minimize sensory contributions to the TEP, but the most effective combination for suprathreshold TMS to dorsolateral prefrontal cortex (dlPFC) is unknown. We applied sensory suppression techniques and quantified electrophysiology and perception from suprathreshold dlPFC TMS to identify the best combination to minimize the sensory TEP. In 21 healthy adults, we applied single pulse TMS at 120% resting motor threshold (rMT) to the left dlPFC and compared EEG vertex N100‐P200 and perception. Conditions included three protocols: No masking (no auditory masking, no foam, and jittered interstimulus interval [ISI]), Standard masking (auditory noise, foam, and jittered ISI), and our ATTENUATE protocol (auditory noise, foam, over‐the‐ear protection, and unjittered ISI). ATTENUATE reduced vertex N100‐P200 by 56%, “click” loudness perception by 50%, and scalp sensation by 36%. We show that sensory prediction, induced with predictable ISI, has a suppressive effect on vertex N100‐P200, and that combining standard suppression protocols with sensory prediction provides the best N100‐P200 suppression. ATTENUATE was more effective than Standard masking, which only reduced vertex N100‐P200 by 22%, loudness by 27%, and scalp sensation by 24%. We introduce a sensory suppression protocol superior to Standard masking and demonstrate that using an unjittered ISI can contribute to minimizing sensory confounds. ATTENUATE provides superior sensory suppression to increase TEP signal‐to‐noise and contributes to a growing understanding of TMS‐EEG sensory neuroscience.
Applying AcciMap and STAMP to the analysis of human error in complex manual assembly
Authors: Torres Yaniel , Nadeau Sylvie , Landau Kurt 
Published: June 2022

AbstractIn sectors such as aerospace manufacturing, human errors in the assembly of complex products can negatively impact quality, productivity, and safety. Until now, the analysis of assembly errors has focused more on the immediate human‐system interface and less on broader organizational factors. This article presents a case study‐based analysis of assembly errors in the aeronautical industry using the systemic methods AcciMap and Systems‐Theoretic Accident Model and Processes (STAMP). We seek to provide the company with elements to build a quality improvement strategy that considers human factors and ergonomics from a systemic perspective. The data and information necessary to conduct the analysis came from a project carried out at an aerospace manufacturing facility over a period of 12 months. The team had direct and recurrent access to primary data sources and communication with various stakeholders. A total of 31 influencing factors were identified with AcciMap at different levels within the manufacturing system. STAMP made it possible to model the sociotechnical control structure of the assembly process and identify several control flaws leading to hazards. The analysis shows that systemic methods require a high level of understanding of the manufacturing system and access to relatively high amounts of data and information. Therefore, direct contact with the field and stakeholders is crucial. Training quality specialists on systemic methods could support its use and help to close the gap between theory and practice. Globally, the field of quality in manufacturing could benefit from using systemic methods when deemed necessary.
Effectiveness of a digital telemonitoring platform for cancer care of older patients: The ConnectElderlyPatientToDoctor study
Authors: Rivière Clémentine , Brureau Laurent , Parnot Charles , Becherirat Selma , Duverger Claire , Picchi Hugo , Le Roy Audrey , Vuagnat Perrine , Schernberg Antoine , Vanquaethem Hélène , Helissey Carole 
Published: June 2022

AbstractWhile telemedicine has been shown to improve the quality of care for cancer patients, it remains underused for older patients (OP), partly due to the assumption that OPs are unabled or unwilling to use digital tools. However, more than 50% of new cancers are diagnosed in people over 70. The ConnectElderlyPatientToDoctor study aimed to evaluate the OP compliance with the use of the digital telemonitoring platform Cureety in oncology. All cancer patients followed at the Military Hospital Bégin were eligible for the study. Patients were invited to respond to a symptomatology questionnaire personalized to their pathology and treatment. An algorithm evaluated the health status of the patient based on the reported adverse events. The population was divided into two groups, OP and younger patients (YP), based on a cut‐off at 70 years. The primary endpoint was to assess the compliance of OPs with the use of the digital oncology platform Cureety, compared to YP. From July 2020 to September 2021, a total of 117 patients were included in our study. We found that 66% of the patients were compliant, with no difference between the two groups (71.2% of YP, 61.7% of OP, P = .29). In OPs, progression free survival (PFS) ratio at 6‐months was 64.6% in the tolerant patients vs 23.4% in the nontolerant patients (HR = 0.1980, 95% CI = 0.04431‐0.8845, P = .0339). The median PFS was 23.3 months in the tolerant group vs 3.3 months in the nontolerant group (P = .0339). The data of overall survival are immature. OPs had a clear benefit from using this platform, similar to what was observed for YP. Patients felt less isolated and felt that they benefited from personalized care with early ambulatory medical care of adverse events. We also found that the health indicators collected with the platform in the first month of treatment are predictive of the progression of the disease. This solution makes it possible to streamline and improve the care pathway of OP.
Evaluation of histopathological response to neoadjuvant therapy in rectal cancer using slide‐free, stain‐free multimodal multiphoton microscopy
Authors: Cui Yancheng , Zhong Qinghua , Sun Dawei , Chen Yan , Jiang Zhe , Yang Xiaodong , Shen Zhanlong , Sun Yunhua , Yin Mujun , Liang Bin , Zhu Xin , Guo Xuefeng , Ye Yingjiang 
Published: June 2022

AbstractNeoadjuvant therapy has become a standard treatment for patients with locally advanced rectal cancer to achieve better prognostic outcomes. The response to treatment has been shown to correlate closely with the prognosis. However, current evaluation systems only provide coarse assessment on limited information, due to the lack of accurate and reproducible approach for quantitation of different types of responses. In this study, a novel stain‐free, slide‐free multimodal multiphoton microscopy imaging technique was applied to image rectal cancer tissues after neoadjuvant therapies with high resolution and contrast. Qualitative and quantitative evaluation of tumor, stromal, and inflammatory responses were demonstrated which are consistent with current tumor regression grading system using American Joint Committee on Cancer criteria, showing the great potential of such approach to build a more informative grading system for accurate and standardizable assessment of neoadjuvant therapy in rectal cancer.
Adventitia‐derived extracellular matrix hydrogel enhances contractility of human vasa vasorum‐derived pericytes via α2β1 integrin and TGFβ receptor
Authors: Wintruba Kaitlyn L. , Hill Jennifer C. , Richards Tara D. , Lee Yoojin C. , Kaczorowski David J. , Sultan Ibrahim , Badylak Stephen F. , Billaud Marie , Gleason Thomas G. , Phillippi Julie A. 
Published: June 2022

AbstractPericytes are essential components of small blood vessels and are found in human aortic vasa vasorum. Prior work uncovered lower vasa vasorum density and decreased levels of pro‐angiogenic growth factors in adventitial specimens of human ascending thoracic aortic aneurysm. We hypothesized that adventitial extracellular matrix (ECM) from normal aorta promotes pericyte function by increasing pericyte contractile function through mechanisms deficient in ECM derived from aneurysmal aortic adventitia. ECM biomaterials were prepared as lyophilized particulates from decellularized adventitial specimens of human and porcine aorta. Immortalized human aortic adventitia‐derived pericytes were cultured within Type I collagen gels in the presence or absence of human or porcine adventitial ECMs. Cell contractility index was quantified by measuring the gel area immediately following gelation and after 48 h of culture. Normal human and porcine adventitial ECM increased contractility of pericytes when compared with pericytes cultured in absence of adventitial ECM. In contrast, aneurysm‐derived human adventitial ECM failed to promote pericyte contractility. Pharmacological inhibition of TGFβR1 and antibody blockade of α2β1 integrin independently decreased porcine adventitial ECM‐induced pericyte contractility. By increasing pericyte contractility, adventitial ECM may improve microvascular function and thus represents a candidate biomaterial for less invasive and preventative treatment of human ascending aortic disease.