bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis, Characterization, and Inhibition Study of Novel Substituted Phenylureido Sulfaguanidine Derivatives as α‐Glycosidase and Cholinesterase Inhibitors
Authors: Akocak Suleyman , Taslimi Parham , Lolak Nebih , Işık Mesut , Durgun Mustafa , Budak Yakup , Türkeş Cüneyt , Gülçin İlhami , Beydemir Şükrü 
Published: February 2021

AbstractA series of six N‐carbamimidoyl‐4‐(3‐substituted phenylureido)benzenesulfonamide derivatives were synthesized by reaction of sulfaguanidine with aromatic isocyanates. In vitro and in silico inhibitory effects of the novel ureido‐substituted sulfaguanidine derivatives were investigated by spectrophotometric methods for α‐glycosidase (α‐GLY), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes associated with diabetes mellitus (DM) and Alzheimer's disease (AD). N‐Carbamimidoyl‐4‐{[(3,4‐dichlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide (2f) showed AChE and BChE inhibitory effects, with KI values of 515.98±45.03 nM and 598.47±59.18 nM, respectively, while N‐carbamimidoyl‐4‐{[(3‐chlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide (2e) showed strong α‐GLY inhibitory effect, with KI values of 103.94±13.06 nM. The antidiabetic effects of the novel synthesized compounds are higher than their anti‐Alzheimer's effects, because the inhibition effect of the compounds on the α‐GLY with diabetic enzyme is greater than the effect on esterase enzymes. Indeed, inhibition of the metabolic enzymes is important for the treatment of DM and AD.
RACK1 mediates the advanced glycation end product‐induced degradation of HIF‐1α in nucleus pulposus cells via competing with HSP90 for HIF‐1α binding
Authors: Xu Yi‐Chang , Gu Yong , Yang Jia‐Ying , Xi Kun , Tang Jin‐Cheng , Bian Jiang , Cai Feng , Chen Liang 
Published: February 2021

AbstractHyperglycemia can drive advanced glycation end product (AGE) accumulation and associated nucleus pulposus cell (NPC) dysfunction, but the basis for this activity has not been elucidated. Hypoxia‐inducible factor‐1α (HIF‐1α) is subject to cell‐type‐specific AGE‐mediated regulation. In the current study, we assessed the mechanistic relationship between AGE accumulation and HIF‐1α degradation in NPCs. Immunohistochemical staining of degenerated nucleus pulposus (NP) samples was used to assess AGE levels. AGE impact on NPC survival and glycolysis‐related gene expression was assessed via 3‐(4,5)‐dimethylthiazol(‐z‐y1)‐3,5‐di‐phenyltetrazolium bromide assay and quantitative reverse‐transcription polymerase chain reaction (qRT‐PCR), while HIF‐1α expression in NPCs following AGE treatment was monitored via Western blot analysis and qRT‐PCR. Additionally, a luciferase reporter assay was used to monitor HIF‐1α transcriptional activity. The importance of the receptor for activated C‐kinase 1 (RACK1) as a mediator of HIF‐1α degradation was evaluated through gain‐ and loss‐of‐function experiments. Competitive binding of RACK1 and HSP90 to HIF‐1α was evaluated via immunoprecipitation. Increased AGE accumulation was evident in NP samples from diabetic patients, and AGE treatment resulted in reduced HIF‐1α protein levels in NPCs that coincided with reduced HIF‐1α transcriptional activity. AGE treatment impaired the stability of HIF‐1α, leading to its RACK1‐mediated proteasomal degradation in a manner independent of the canonical PHD‐mediated degradation pathway. Additionally, RACK1 competed with HSP90 for HIF‐1α binding following AGE treatment. AGE treatment of NPCs leads to HIF‐1α protein degradation. RACK1 competes with HSP90 for HIF‐1α binding following AGE treatment, resulting in posttranslational HIF‐1α degradation. These results suggest that AGE is an intervertebral disc degeneration risk factor, and highlight potential avenues for the treatment or prevention of this disease.
Tumor suppressive microRNA‐485‐5p targets PRRX1 in human skin melanoma cells, regulating epithelial–mesenchymal transition and apoptosis
Authors: Wu Xiaolin , Bao Haiying 
Published: February 2021

AbstractMelanoma is one of the most aggressive skin cancers. Existing evidence has reported the aberrant expression of microRNAs (miRNAs) in melanoma, but their putative targets and underlying downstream effects remain to be further understood. Herein, we explored the suppressive role of miR‐485‐5p in melanoma progression. Initial bioinformatics analyses showed that the PRRX1 gene was differentially expressed in melanoma, while miR‐485‐5p was predicted to be a potential regulatory miRNA binding to PRRX1 mRNA. We confirmed that PRRX1 was upregulated, while miR‐485‐5p was downregulated in human melanoma samples compared with adjacent normal skin tissues. We then showed that PRRX1 was a target gene of miR‐485‐5p by dual‐luciferase reporter gene assay. Moreover, a reduction in the expression of PRRX1 and downregulation of important proteins of the transforming growth factor‐beta (TGFβ) signaling pathway was observed after miR‐485‐5p overexpression. Furthermore, miR‐485‐5p overexpression or PRRX1 knockdown suppressed epithelial–mesenchymal transition, cell viability, migration, and invasion, and promoted cell apoptosis in melanoma cells. Our study demonstrates the tumor‐suppressive functions of miR‐485‐5p in the development of human melanoma, providing a potential target for therapy.
Recurrent coronavirus diseases 19 (COVID‐19): A different presentation from the first episode
Authors: Shoar Saeed , Khavandi Siamak , Tabibzadeh Elsa , Khavandi Soheila , Naderan Mohammad , Shoar Nasrin 
Published: February 2021

AbstractA 31‐year‐old Caucasian male developed reinfection with

SARS‐CoV‐2, 2 ½ months after an initial episode of ICU admission for

respiratory support due to COVID‐19. The second episode was in the form of malaise,

aphthous gingival ulcer, and desquamating palmar lesion.
Direct Amination of Biomass‐based Furfuryl Alcohol and 5‐(Aminomethyl)‐2‐furanmethanol with NH3 over Hydrotalcite‐derived Nickel Catalysts via the Hydrogen‐borrowing Strategy
Authors: Zhou Kuo , Xie Ruihong , Xiao Meiting , Guo Darun , Cai Zhuodi , Kang Shimin , Xu Yongjun , Wei Jinjia 
Published: February 2021

AbstractA series of hydrotalcite‐derived nickel catalysts were synthesized and employed for the direct amination of biomass‐based furfuryl alcohol with NH3 via the hydrogen borrowing strategy. The effects of the Ni/Al molar ratio and calcination temperature of the NiAl hydrotalcite‐like precursors on the performance of the NixAl‐CT catalyst were investigated. The systematic characterization showed that the synergistic catalysis of the metal and acid‐base sites was of vital importance for the amination of alcohols. In particular, the Ni2Al‐600 catalyst with high amount of Ni0 sites (1.26 mmol g−1) and suitable density of acid‐base sites (0.71 mmol g−1 and 1.10 mmol g−1, respectively) exhibited the best dehydrogenation capability and therefore excellent catalytic activity. An 84.1 % yield of furfurylamine with complete conversion of furfuryl alcohol was obtained under the reaction conditions of 180 °C and 0.4 MPa NH3 in 36 h. The presence of Ni3N in the spent catalyst, confirmed by XRD, TEM and XPS characterizations, was demonstrated to be responsible for the deactivation of the NixAl‐CT catalyst. In addition, the Ni2Al‐600 catalyst exhibited satisfactory performance toward another important biomass‐related transformation of 5‐(aminomethyl)‐2‐furanmethanol to 2,5‐bis(aminomethyl)furan, with a yield of 70.5 %.
Pore Formation Mechanism and Sorption Studies Using Activated Carbon from Gleditsia triacanthos
Authors: Mathangi J. B. , Kalavathy M. Helen , Miranda Lima Rose 
Published: February 2021

AbstractLignocellulosic biomass (LB) is a good choice to be utilized as a substitute for activated carbon (AC) production. The main objective is to increase pore volume, porosity, and specific surface area (SSA) of activated Gleditsia triacanthos (AGT) and determine the relevant mechanism behind pore formation. Morphological, physical, and chemical characteristics were studied to evaluate the potential of AGT for Ni2+ removal. Ni2+ removal was carried out for different operating conditions such as contact time, pH, and initial Ni2+ concentration. Kinetics and equilibrium studies demonstrated that the mechanism for Ni2+ removal is chemical sorption.
Spatially Resolved Electron Transport through Anode‐Respiring Geobacter sulfurreducens Biofilms: Controls and Constraints
Authors: He Xiaojia , Chadwick Grayson , Jiménez Otero Fernanda , Orphan Victoria , Meile Christof 
Published: February 2021

AbstractMicrobial fuel cells (MFCs) with Geobacter sulfurreducens have been shown to produce high current densities; however, electron transport in G. sulfurreducens biofilms is not fully understood. Here, we utilize a spatially resolved numerical model describing this electron transfer to constrain mechanisms and controls on metabolic activity. Our model reproduces the metabolic activity profile obtained using nanoSIMS under positive (+0.24 V SHE) and negative (−0.1 V SHE) anode potentials. The simulations indicate that the distribution of the electric potential and pH both control cellular metabolism. Model simulations reproducing the experimentally determined activity patterns also support the presence of two activity modes in G. sulfurreducens biofilms, with a shift from a redox mid‐potential of −0.07 V SHE to −0.15 V SHE. Our model provides valuable insights into the fundamental mechanisms of electron transfer at Micron‐scale in conductive biofilms which can inform MFCs designs that maximize current production by minimizing the impact of inhibitory factors.
Generation of circular dichroism from superposed porphyrin films
Authors: Takechi Hideaki , Watarai Hitoshi 
Published: February 2021

AbstractCircular dichroism (CD) was observed from the superposed porphyrin deposited glass plates, which were prepared by the vapor deposition of achiral porphyrin molecules and oriented to one direction by rubbing parallel to the surface of plate. The CD spectra depended on the twisted angle between the plates and the number of plates superposed. The observed CD spectra agreed with the simulated ones by the Mueller matrices superposition calculation using the observed linear dichroism spectra and linear birefringence spectra of each plate.
Joint direct and transposed sparse matrix‐vector multiplication for multithreaded CPUs
Authors: Kozický Claudio , Šimeček Ivan 
Published: February 2021

AbstractRepeatedly performing sparse matrix‐vector multiplication (SpMV) followed by transposed sparse matrix‐vector multiplication (SpMTV) with the same matrix is a part of several algorithms, for example, the Lanczos biorthogonalization algorithm and the biconjugate gradient method. Such algorithms can benefit from combining parallel SpMV and SpMTV into a single operation we call joint direct and transposed sparse matrix‐vector multiplication (SpMMTV). In this article, we present a parallel SpMMTV algorithm for shared‐memory CPUs. The algorithm uses a sparse matrix format that divides the stored matrix into sparse matrix blocks and compresses the row and column indices of the matrix. This sparse matrix format can be also used for SpMV, SpMTV, and similar sparse matrix‐vector operations. We expand upon existing research by suggesting new variants of the parallel SpMMTV algorithm and by extending the algorithm to efficiently support symmetric matrices. We compare the performance of the presented parallel SpMMTV algorithm with alternative approaches, which use state‐of‐the‐art sparse matrix formats and libraries, using sparse matrices from real‐world applications. The performance results indicate that the median performance of our proposed parallel SpMMTV algorithm is up to 45% higher than of the alternative approaches.
General practitioners’ attitude toward early and pre‐dementia diagnosis of AD in five European countries—A MOPEAD project survey
Authors: Sannemann Lena , Müller Theresa , Waterink Lisa , Zwan Marissa , Wimo Anders , Stomrud Erik , Pinó Susana , Arrufat Jordi , Rodríguez‐Gomez Octavio , Benaque Alba , Bon Jaka , Ferreira Daniel , Johansson Gunilla , Dron Amanda , Dumas Annette , Georges Jean , Kramberger Milica G , Visser Pieter Jelle , Winblad Bengt , Campo Laura , Boada Mercè , Jessen Frank ,   MOPEAD consortium
Published: February 2021

AbstractIntroductionGeneral practitioners (GPs) play a key role in early identification of dementia, yet diagnosis is often missed or delayed in primary care. As part of the multinational Models of Patient Engagement for Alzheimer's Disease project, we assess GPs’ attitude toward early and pre‐dementia diagnosis of AD and explore barriers to early diagnosis.MethodsOur survey covered general attitude toward early diagnosis, diagnostic procedures, resources, and opinion on present and future treatment options across five European countries.ResultsIn total 343 GPs completed the survey; 74% of GPs indicated that an early diagnosis is valuable. There were country‐specific differences in GPs’ perceptions of reimbursement and time available for the patient. If a drug were available to slow down the progression of AD, 59% of the GPs would change their implementation of early diagnosis.DiscussionOur findings provide insight into GPs’ attitudes by exploring differences in perception and management of early diagnosis.
Reconciling the ecological and engineering definitions of resilience
Authors: Zampieri Matteo 
Published: February 2021

AbstractAssessing and managing the human influence on the natural and anthropic ecosystems strongly demands for robust measures of their resilience, especially in a world facing global changes as it is the Earth now. Many definitions of resilience have been proposed in order to cover different contexts. However, they are mostly derived either from the ecological or the engineering definitions of resilience, which substantially differ between each other. Here, following the strategy for measuring the system perturbations by the return period of their impacts on production (or equivalently by the inverse frequency), I demonstrate the mathematical equivalence of the ecological and engineering definitions of resilience for a special class of production systems. These finding provides additional robustness to resilience assessments based on the recently proposed annual production resilience indicator.
Diagnosis and Treatment of Iron Deficiency in Heart Failure: OFICSel study by the French Heart Failure Working Group
Authors: Pezel Theo , Audureau Etienne , Mansourati Jacques , Baudry Guillaume , Ben Driss Ahmed , Durup Florence , Fertin Marie , Godreuil Christian , Jeanneteau Julien , Kloeckner Martin , Koukoui François , Kesri‐Tartière Lamia , Laperche Thierry , Roubille François , Cohen‐Solal Alain , Damy Thibaud 
Published: February 2021

AbstractAimsIron deficiency (ID) occurs in about 50% of patients with heart failure (HF). The European Society of Cardiology (ESC) recommends ID diagnostic testing in newly diagnosed patients with HF and during follow‐up, with intravenous iron supplementation (IS) only recommended in patients with HF with reduced ejection fraction (HFrEF). This study aimed to assess prevalence, clinical characteristics, and application of ESC guidelines for ID and IS in patients with HF in the real‐life clinical setting.Methods and resultsThe French transversal multicentre OFICSel registry (300 cardiologists) conducted in 2017 included patients hospitalized for HF at least once in the previous 5 years. Diverse adult patients were eligible including inpatients and outpatients and those with acute and chronic HF. Data were collected from cardiologists and patients using study‐specific surveys. Data included demographic and clinical data, as well as HF and ID management data. Overall, 2822 patients, mainly male (69.3%) with a median age of 69 years (interquartile range 58–78), were included. A total of 1075 patients (38.1%) were tested for ID, with 364 (33.9%) diagnosed. Of these, 168 (46.2%) received IS: 128 (76.2%) intravenous IS and 40 (23.8%) oral. Among the 201 patients with HFrEF diagnosed with ID, 99 (49.3%) received IS: 79 (79.8%) intravenous IS and 20 (20.2%) oral.ConclusionsIn clinical practice, only one‐third of patients with HF had a diagnostic test for ID. In patients with ID with HFrEF, only 39.3% received intravenous IS as recommended. Thus, in general, cardiologists should be encouraged to follow the ESC guidelines to ensure optimal treatment for patients with HF.
Multiparameter diagnostic sensor measurements during clinically stable periods and worsening heart failure in ambulatory patients
Authors: Gardner Roy S. , Thakur Pramodsingh , Hammill Eric F. , Nair Devi G. , Eldadah Zayd , Stančák Branislav , Ferrick Kevin , Sriratanasathavorn Charn , Duray Gábor Zoltán , Wariar Ramesh , Zhang Yi , An Qi , Averina Viktoria , Boehmer John P. 
Published: February 2021

AbstractAimsThis study aims to characterize the range of implantable device‐based sensor values including heart sounds, markers of ventilation, thoracic impedance, activity, and heart rate for patients with heart failure (HF) when patients were deemed to be in clinically stable periods against the time course of acute decompensation and recovery from HF events.Methods and resultsThe MultiSENSE trial followed 900 patients implanted with a COGNIS CRT‐D for up to 1 year. Chronic, ambulatory diagnostic sensor data were collected and evaluated during clinically stable periods (CSP: unchanged NYHA classification, no adverse events, and weight change ≤2.27 kg), and in the timeframe leading up to and following HF events (HF admissions or unscheduled visits with intravenous HF treatment). Physiologic sensor data from 1667 CSPs occurring in 676 patients were compared with those data leading up to and following 192 HF events in 106 patients. Overall, the mean age was 66.6 years, and the population were predominantly male (73%). Patients were primarily in NYHA II (67%), with a mean LVEF of 29.6% and median NT‐proBNP of 754.5 pg/mL. Sensor values during CSP were poorer in patients who had HF events during the study period than those without HF events, including first heart sound (S1: 2.18 ± 0.84 mG vs. 2.62 ± 0.95 mG, P = 0.002), third heart sound (S3: 1.13 ± 0.36 mG vs. 0.91 ± 0.30 mG, P < 0.001), thoracic impedance (45.66 ± 8.78 Ohm vs. 50.33 ± 8.43 Ohm, P < 0.001), respiratory rate (19.09 ± 3.10 br/min vs. 17.66 ± 2.39 br/min, P = 0.002), night time heart rate (73.39 ± 8.36 b.p.m. vs. 69.56 ± 8.09 b.p.m., P = 0.001), patient activity (1.69 ± 1.84 h vs. 2.56 ± 2.20 h, P = 0.006), and HeartLogic index (11.07 ± 12.14 vs. 5.31 ± 5.13, P = 0.001). Sensor parameters measured worsening status leading up to HF events with recovery of values following treatment.ConclusionsDevice‐based physiologic sensors not only revealed progressive worsening leading up to HF events but also differentiated patients at increased risk of HF events when presumed to be clinically stable.
Phase‐Controlled Synthesis of Zeolites from Sodium Aluminosilicate under OSDA/Solvent‐Free Conditions
Authors: Mizuno Yoshitaka , Miyake Koji , Tanaka Shunsuke , Nishiyama Norikazu , Fukuhara Choji , Kong Chang Yi 
Published: February 2021

AbstractOSDA/solvent‐free synthesis of zeolites is suitable for practical commercialization due to low environmental damage and low cost. However, only a few types of zeolites have been successfully synthesized by this method. In this study, ANA, CAN, GIS, SOD, FAU and LTA type zeolites were synthesized by the OSDA/solvent‐free synthesis method by changing the Si/Al ratio and crystallization temperature in detail. At higher Si/Al ratios, FAU, GIS and ANA type zeolites were obtained with an increase of crystallization temperature. Meanwhile, at lower Si/Al ratios, LTA, SOD and CAN type zeolites were obtained with an increase of crystallization temperature. It was found that zeolites with high T atom density were synthesized with an increase of the crystallization temperature; zeolite with a high T atomic density is more stable. This work reveals the correlation between the Si / Al ratio and the crystallization temperature in OSDA/solvent‐free synthesis of zeolites, which provides a clear guideline for the OSDA/solvent‐free synthesis of zeolites.
Spiro‐2‐oxindoles via 1,3‐dipolar cycloadditions. A decade update
Authors: Molteni Giorgio , Silvani Alessandra 
Published: February 2021

AbstractThe great variety of spirooxindole three‐dimensional scaffolds encompasses relevant bioactive natural alkaloids as well as useful therapeutic agents. In view of the challenging features of the spirooxindole skeletons and their desirable properties, several synthetic routes have been devoted to their preparation. Because of the variety of both 1,3‐dipolar species and 2‐oxindoles bearing a C=X double bond (X=C<, N−, O) in the 3‐position, a prominent role relies upon a 1,3‐dipolar cycloaddition as the key step of the whole synthetic sequence. The present paper aims to discuss the developments in the field of spirooxindole synthesis via a 1,3‐dipolar cycloaddition occurred in the 2011–2020 decade. The literature data on this subject are reviewed in a systematic way according to the type of the 1,3‐dipole and the oxindole dipolarophile.
4‐Aryl‐2‐Imino‐1,3‐Dithiolanes from the Room Temperature Coupling of Sodium Dithiocarbamates with Sulfonium Salts
Authors: Bresciani Giulio , Marchetti Fabio , Ciancaleoni Gianluca , Pampaloni Guido 
Published: February 2021

AbstractA series of 4‐aryl‐2‐imino‐1,3‐dithiolanes was synthesized by means of a straightforward strategy starting from readily available precursors: reactions of dithiocarbamates and arylsulfonium salts, at room temperature in water/CH2Cl2 as biphasic medium, afforded the five‐membered cyclic products in good yields. The reaction mechanism was investigated by DFT calculations.