bluuebunny/crossref_metadata_2025_split huggingface dataset:
Antitumor activity of potent pyruvate dehydrogenase kinase 4 inhibitors from plants in pancreatic cancer
Authors: Tambe Yukihiro , Terado Tokio , Kim Chul Jang , Mukaisho Ken‐ichi , Yoshida Saori , Sugihara Hiroyuki , Tanaka Hiroyuki , Chida Junji , Kido Hiroshi , Yamaji Kenzaburo , Yamamoto Tsuyoshi , Nakano Hirofumi , Omura Satoshi , Inoue Hirokazu 
Published: May 2019

AbstractPhosphorylation of pyruvate dehydrogenase by pyruvate dehydrogenase kinase 4 (PDK4) 4 inhibits its ability to induce a glycolytic shift. PDK4 expression is frequently upregulated in various cancer tissues, with its elevation being critical for the induction of the Warburg effect. PDK4 is an attractive target for cancer therapy given its effect on shifting glucose metabolism. Previous research has highlighted the necessity of identifying a potent compound to suppress PDK4 activity at the submicromolar concentrations. Here we identified natural diterpene quinones (KIS compounds) that inhibit PDK4 at low micromolar concentrations. KIS37 (cryptotanshinone) inhibited anchorage‐independent growth in three‐dimensional spheroid and soft agar colony formation assays of KRAS‐activated human pancreatic (MIAPaCa‐2 and Panc‐1) and colorectal (DLD‐1 and HCT116) cancer cell lines. KIS37 also suppressed KRAS protein expression in such cell lines. Furthermore, KIS37 suppressed phosphorylation of Rb protein and cyclin D1 protein expression via the PI3K‐Akt–mTOR signaling pathway under nonadherent culture conditions and suppressed the expression of cancer stem cell markers CD44, EpCAM, and ALDH1A1 in MIAPaCa‐2 cells. KIS37 also suppressed pancreatic cancer cell growth in both subcutaneous xenograft and orthotopic pancreatic tumor models in nude mice at 40 mg/kg (intraperitoneal dose) without any evident toxicity. Reduced ALDH1A1 expression was observed in KIS37‐treated pancreatic tumors, suggesting that cancer cell stemness was also suppressed in the orthotopic tumor model. The aforementioned results indicate that KIS37 administration is a novel therapeutic strategy for targeting PDK4 in KRAS‐activated intractable human pancreatic cancer.
The personality disorder patient pathway: Service user and clinical perspectives
Authors: Flynn S. , Raphael J. , Graney J. , Nyathi T. , Williams A. , Kapur N. , Appleby L. , Shaw J. 
Published: May 2019

AbstractAimsThere have been recent policy developments and research into care provision for service users with personality disorder. However, few studies have focused on service user and staff perspectives on how services could be improved.MethodsA qualitative study was undertaken in the UK between 2016 and 2017. We conducted six focus groups with clinicians in mental health services with experience of working with people with personality disorder. Using an online survey, we asked current and past service users with personality disorder to describe their experiences of mental health services and make recommendations for improvements. A thematic analysis was conducted.ResultsForty‐five clinicians participated in the focus group and 131 service users contributed to the online survey. The main areas of concern identified by both staff and patients were the diagnosis of personality disorder, the absence of a coherent care pathway, access to psychological treatment and staff training.ConclusionsThe care pathway for individuals with personality disorder is unclear to clinicians and service users, and elements of the pathway are disjointed and not working as effectively as they could. Guidelines recommended by National Institute for Health and Care Excellence are not being followed. Specialist psychological interventions should be available to ensure consistent and stable care provision. © 2019 John Wiley & Sons, Ltd.
Bereaved mothers' and fathers' prolonged grief and psychological health 1 to 5 years after loss—A nationwide study
Authors: Pohlkamp Lilian , Kreicbergs Ulrika , Sveen Josefin 
Published: May 2019

AbstractObjectiveTo assess differences in prolonged grief, depression, posttraumatic stress, and sleep disturbances in bereaved parents across years since loss (1‐5 years) and by gender and to assess potential interactive effects of time since loss and gender on bereavement outcomes.MethodsThis study examined symptom levels of prolonged grief disorder, depression, posttraumatic stress, and insomnia in bereaved parents. A sample, including 133 mothers and 92 fathers who had lost a child to cancer 1 to 5 years previously, subdivided to five subsamples, one for each year since loss. Analysis of variance (ANOVA) was used to assess differences in symptom levels, related to years since loss, and gender.ResultsRegardless of how many years had passed since the loss, symptom levels of prolonged grief, depression, posttraumatic stress symptoms, and insomnia were elevated in all subsamples. Mothers showed higher symptom levels of prolonged grief, depression, and posttraumatic stress than fathers. However, no significant interaction effects were found between years since loss and gender on any of the symptom levels.ConclusionsCancer‐bereaved mothers and fathers are vulnerable to prolonged grief and psychological symptoms up to 5 years after the death of their child. Findings highlight that bereaved parents may need long‐term support, and the results deserve further attention in research and clinical care.
Clustering of Iron Oxide Nanoparticles with Amphiphilic Invertible Polymer Enhances Uptake and Release of Drugs and MRI Properties
Authors: Price Paige M. , Dittmar Jasper W. , Carlson Kenneth , Lawson Bret P. , Reilly Austin K. , Stein Barry D. , Cheng Hu , Zholobko Oksana , Kohut Ananiy , Voronov Andriy , Bronstein Lyudmila M. 
Published: May 2019

AbstractA functionalization of iron oxide nanoparticles (NPs) of different diameters by the amphiphilic invertible polymer, (PEG600‐alt‐PTHF650)k (PEG and PTHF stand for poly(ethylene glycol) and poly(tetrahydrofuran), respectively), leads to different NP/polymer architectures for dye/drug uptake and release, as is reported here for the first time. It is demonstrated that 18.6 ± 1.4 and 11.9 ± 0.6 nm NPs are individually coated by this polymer, while 5.9 ± 0.6 nm NPs form nanoparticle clusters (NPCs) which could be isolated by either ultracentrifugation or magnetic separation. This phenomenon is most likely due to the character of the (PEG600‐alt‐PTHF650)k macromolecule with alternating hydrophilic and hydrophobic fragments and its dimensions sufficient to cause NP clustering. Utilizing Rhodamine B base (RBB) and doxorubicin (DOX), the data on uptake upon mixing and further release via inversion into octanol (mimicking the penetration of the cell biomembrane) are presented. The magnetic NPCs display enhanced uptake and release of both RBB and DOX most likely due to the higher retained polymer amount. The NPCs also display exceptional magnetic resonance imaging properties. This and the high uptake/release efficiency of the NPCs combined with easy magnetic separation make them promising for theranostic probes for magnetically targeted drug delivery.
A Novel Launching System Applying a Relay Chamber Technology and Its Optimization
Authors: Cao Runduo , Zhang Xiaobing 
Published: May 2019

AbstractThis paper investigates a novel launching system with a relay chamber using optimization method. For revealing the influences of new structures on the overall interior ballistic performance, the launching process of this novel system is modeled and a series of different schemes are simulated. In view of more design variables to be involved and conflicting objectives to be achieved, complete optimization of the interior ballistic performance is a complex process. A popular standard particle swarm optimization algorithm is used to obtain an optimal loading condition, together with a proper design of the relay chamber. Furthermore, for an existing cannon gun without modifying its structure, the charge system is re‐designed and simulated using the SPSO algorithm in this novel method and conventional method respectively. Compared with the original scheme, both optimal schemes could get higher muzzle velocity, while the novel method could improve by 16.5 % and the conventional method could improve by only 5.7 %. It means that this novel launch system could improve the interior ballistics performance obviously and it still has considerable potential to be ameliorated.
Photoselective exclusion netting in apple orchards: effectiveness against pests and impact on beneficial arthropods, fungal diseases and fruit quality
Authors: Candian Valentina , Pansa Marco G , Santoro Karin , Spadaro Davide , Tavella Luciana , Tedeschi Rosemarie 
Published: May 2019

AbstractBACKGROUNDFrequent pesticide treatments in fruit orchards increase hazards for workers, consumers and the environment. Moreover, the indiscriminate and excessive use of pesticides often induces resistance in pests. In the past few years, physical exclusion strategies have been proposed as an alternative for the control of insect pests. The goal of this study was to evaluate the effectiveness of anti‐hail photoselective netting in protecting apples against key and emerging pests, as well as the impact on beneficial arthropods, fungal diseases and fruit quality.RESULTSIn netted plots, a significant reduction in pest populations, i.e. fruit moths, Halyomorpha halys (Stål) and Drosophila suzukii (Matsumura), was recorded in comparison with un‐netted controls. Moreover, the damage on fruits caused by H. halys was reduced up to 62% compared with insecticidal treatments. The net did not negatively affect the abundance of predators and the incidence of post‐harvest rot. In addition, the incidence of bitter pit on apple was reduced up to 52%. Furthermore, fruit quality was unaffected by the net coverage (both at harvest and after 4 months of storage).CONCLUSIONAnti‐hail photoselective pearl netting proved a promising exclusion system that can prevent attack by more than one insect pest at a time, allowing for a strong reduction in insecticide treatments and relative costs. At the same time, the netting did not negatively influence the presence of predators, the incidence of fungal disease or fruit quality. © 2019 Society of Chemical Industry
Presence and roles of myrtenol, myrtanol and myrtenal in Dendroctonus armandi (Coleoptera: Curculionidae: Scolytinae) and Pinus armandi (Pinales: Pinaceae: Pinoideae)
Authors: Zhao Mingzhen , Liu Bin , Sun Yaya , Wang Yuanyuan , Dai Lulu , Chen Hui 
Published: May 2019

AbstractBACKGROUNDInsect pheromones and host volatiles are important for pest control due to their high efficiency and low potential for environmental pollution. The functions of myrtenol, myrtanol and myrtenal in pest–host interactions are unknown. This study aimed to determine the presence of myrtenol, myrtanol and myrtenal in newly emerged and emerged stages of Dendroctonus armandi, and in infected and healthy Pinus armandi, and to identify their roles in tree protection and pest management based on electroantennography (EAG), Y‐tube and toxicity experiments.RESULTSGas chromatographic and mass spectrometry (GC–MS) analyses, EAG, Y‐tube and toxicity assays revealed the following: (1) myrtenol was found in P. armandi phloem and did not exhibit significant toxicity towards D. armandi; (2) myrtanol was produced by infected P. armandi after D. armandi invasion and had significant toxicity towards D. armandi, especially females; and (3) myrtenal might represent an aggregation pheromone produced by female D. armandi to exert aggregation effects on other females, to help them overcome the resistance of P. armandi jointly and ensure a successful invasion, females remained in an aggregation state from leaving the host to mating in a new host.CONCLUSIONThese findings suggest that myrtanol as a repellent has potential for the protection of P. armandi and that myrtenal could be used to trap and disorient D. armandi. © 2019 Society of Chemical Industry
Revisiting the structural and electronic properties of neutral, mono‐ and di‐anionic titanium‐doped silicon clusters TiSin0/−/2− (n = 6‐16)
Authors: Dong Caixia , Han Limin , Yang Jucai , Cheng Lin 
Published: May 2019

AbstractThe systematic structures search for neutral and Zintl anionic Ti‐doped silicon clusters TiSin0/−/2− (n = 6‐16) have been carried out using the ABCluster global search technique combined with a double‐hybrid density functional method. Based on the predicted energies, adiabatic electron affinities, vertical detachment energies and the consistency between simulated and experimental photoelectron spectroscopy, the true global minimum structures are confirmed. The results show that structural growth pattern of neutral TiSin clusters is from linked structures (n = 10‐12) to encapsulated configurations (n = 13‐16). In contrast, the evolution pattern of Zintl anionic TiSin−/2− clusters begins with the pentagonal bipyramid structure (n = 6). As the Si atoms increase, these Si atoms attach to the surface adjacent to Ti atom, and gradually surround Ti atom. Eventually, the encapsulated structure is formed when n = 12. Moreover, two extra electrons not only perfect the structure of TiSi12 but also improve its chemical and thermodynamic stability.
TiK‐means: Transformation‐infusedK‐means clustering for skewed groups
Authors: Berry Nicholas S. , Maitra Ranjan 
Published: May 2019

AbstractTheK‐means algorithm is extended to allow for partitioning of skewed groups. Our algorithm is called TiK‐means and contributes aK‐means‐type algorithm that assigns observations to groups while estimating their skewness‐transformation parameters. The resulting groups and transformation reveal general‐structured clusters that can be explained by inverting the estimated transformation. Further, a modification of the jump statistic chooses the number of groups. Our algorithm is evaluated on simulated and real‐life data sets and then applied to a long‐standing astronomical dispute regarding the distinct kinds of gamma ray bursts.
Synthesis of New Chiral (R)‐BINOL Derivatives under Microwave Irradiation and Evaluation of Their Antibacterial and α‐Glucosidase Inhibitory Activity
Authors: Ankireddy Ashok Reddy , Paidikondala Kalyani , Gundla Rambabu , Balaraju Tuniki , Pagadala Ramakanth , Banothu Venkanna 
Published: May 2019

AbstractSeries of new 3,3’‐disubstituted chiral (R)‐BINOL compounds have been synthesized with good yields and short reaction time under microwave‐irradiation. The titled compounds showed great antibacterial activity against gram‐positive and gram‐negative organisms. The results indicated that two compounds (R)‐3,3′‐bis(3,5‐difluorophenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 a) and (R)‐3,3′‐bis(4‐nitrophenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 d) which bearing fluoro and nitro substitution on phenyl group has displayed highest inhibition against pathogens. All the derivatives evaluated in vitro against α‐glucosidase. The results indicates that all the target compounds have significant inhibitory activity and more potent than standard drug Acarbose (IC50 = 586.391 ± 14.017 μM). (R)‐3,3′‐bis(3,5‐dichlorophenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 b), (R)‐3,3′‐bis(3,5‐difluorophenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 a), (R)‐3,3′‐bis(4‐nitrophenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 d) and (R)‐3,3′‐bis(3,5‐dimethylphenyl)‐[1,1′‐binaphthalene]‐2,2′‐diol (6 f) compounds shows strong inhibitors of α‐glucosidase, with the IC50 values of 25.341 ± 0.009 μM, 29.215 ± 0.017 μM, 30.294 ± 0.012 μM and 32.402 ± 0.041 μM, respectively.
Synthesis of 21‐Alkylidenes and 21‐Alkylol Analogues of Uscharin and Their Effects on Intracellular Calcium in Cardiac Cells
Authors: Zhou Xiaobo , Chen Li , Jiang Zhi‐Hong , Chen Xiaoyi , Luo Pei , Bai Li‐Ping 
Published: May 2019

AbstractFive 21‐alkylidenes (2‐6) and a 21‐alkylol (7) derivatives of uscharin (1) were synthesized by aldol condensation reaction and aldol reaction of uscharin with aromatic aldehydes, respectively. We investigated the ability of uscharin and its derivatives to interfere with the intracellular calcium level by flow cytometry and contractile characteristics at the single cell level by time‐lapse microscopy in H9c2 cells. Changes of spontaneous calcium oscillations in beating HL‐1 cells were also studied by a high‐throughput Fluorometric Imaging Plate Reader (FLIPR) assay. We reported for the first time that uscharin could produce increased contraction strength in cardiac muscle cells while it showed a significant cytotoxicity to atrial cells. Unlike uscharin, 6 induced a marked increase of myocardial contractility, whereas 6 neither caused irregular frequency of oscillations nor cardiac cytotoxic effects under tested conditions. Structural modification on the butenolide moiety of uscharin showed a reduction of cardiac cytotoxicity and exhibited potential for use as an inotropic agent for the treatment of heart failure.
Layer by Layer Assembly of Zinc Oxide Nanotubes and Nanoflowers as Catalyst for Separate and Simultaneous Catalytic Degradation of Dyes and Fuel Additive
Authors: Khan Shanza Rauf , Abid Sobia , Jamil Saba , Aqib Amjad Islam , Faisal Muhammad Naeem , Ashraf Janjua Muhammad Ramzan Saeed 
Published: May 2019

AbstractZinc oxide nanotubes and nanoflowers are synthesized using urea as template through hydrothermal technique. XRD confirmed that product is consists of zinc and oxygen atoms forming a hexagonal crystal system with ZnO chemical formula. SEM showed that tubes and flower like particles are formed. ATR‐IR confirmed the presence of Zn−O bond as a functional group. UV‐VIS spectroscopic analysis exhibits that product has a band gap energy of 3.49 eV. Synthesized product due to its outstanding properties such as wide band gap semiconductor and large surface area to volume ratio is used as a catalyst for individual and simultaneous catalytic degradation of methylene blue (MB) and Congo red (CR) dyes. The apparent rate constant (kapp) value of individual and simultaneous catalytic degradation of CR dye is decreased with increase in catalyst dosage while kapp value of individual and simultaneous catalytic degradation of MB dye is increased with increase in catalyst dosage. The synthesized product is found more active towards CR dye as compared to MB dye. Small size and high surface area to volume ratio of product also make it a desirable additive for enhancing the efficiency of diesel fuel. Results obtained from fuel additive activity show that as the concentration of nanoadditive is increased from 20, 40, 60, 80 and 100 ppm the calorific value is increased which indicates the enhanced efficiency of fuel due to additive.
Synthesis of 5‐Carboxamidotriazoles via Azide‐Alkyne Cycloaddition–Aminocarbonylation Sequence
Authors: Szuroczki Péter , Sámson Judit , Kollár László 
Published: May 2019

Abstract5‐Carboxamidotriazoles were prepared in the palladium‐catalyzed aminocarbonylation of the corresponding iodotriazole using various amines as N‐nucleophiles under mild reaction conditions. The iodoheteroarene substrates were obtained in good yields in copper‐catalysed azide‐alkyne cycloaddition of iodoalkynes (2′‐iodophenylacetylene and ethyl iodopropiolate) and benzyl azide.
Unprecedented Synthesis of 4‐Ylidene (3 S)‐3‐hydroxy‐1‐aryl (alkyl)‐pyrrolidine‐2,5‐diones Based on 1,3‐Dipolar Cycloaddition of a Sugar‐derived Nitrone to N‐Substituted Maleimides
Authors: Ghannay Siwar , Alminderej Fahad , Msaddek Moncef , Praly Jean‐Pierre , Aouadi Kaïss 
Published: May 2019

Abstract1,3‐Dipolar cycloaddition of a sugar‐based nitrone to differently N‐substituted maleimides afforded mixtures of isoxazolidine‐based cycloadducts. The obtained predominant cycloadducts displayed three new contiguous stereogenic centers placing the protons in syn and anti‐relationship, respectively at the fused bond, and for H5 and H6. This was explained by an endo approach of the maleimide derivatives to the Si‐face of the nitrone reacting in its Z‐form. The mCPBA‐mediated oxidative cleavage N−O bond of the isoxazolidine occurred almost quantitatively to afford unprecedented sugar nitrones. Their pyrolysis under thermal or microwave activation led to new 4‐ylidene (3 S)‐3‐hydroxy‐1‐aryl (alkyl)‐pyrrolidine‐2,5‐diones.
A Mussel‐Inspired Persistent ROS‐Scavenging, Electroactive, and Osteoinductive Scaffold Based on Electrochemical‐Driven In Situ Nanoassembly
Authors: Zhou Ting , Yan Liwei , Xie Chaoming , Li Pengfei , Jiang Lili , Fang Ju , Zhao Cancan , Ren Fuzeng , Wang Kefeng , Wang Yingbo , Zhang Hongping , Guo Tailin , Lu Xiong 
Published: May 2019

AbstractConductive polymers are promising for bone regeneration because they can regulate cell behavior through electrical stimulation; moreover, they are antioxidative agents that can be used to protect cells and tissues from damage originating from reactive oxygen species (ROS). However, conductive polymers lack affinity to cells and osteoinductivity, which limits their application in tissue engineering. Herein, an electroactive, cell affinitive, persistent ROS‐scavenging, and osteoinductive porous Ti scaffold is prepared by the on‐surface in situ assembly of a polypyrrole‐polydopamine‐hydroxyapatite (PPy‐PDA‐HA) film through a layer‐by‐layer pulse electrodeposition (LBL‐PED) method. During LBL‐PED, the PPy‐PDA nanoparticles (NPs) and HA NPs are in situ synthesized and uniformly coated on a porous scaffold from inside to outside. PDA is entangled with and doped into PPy to enhance the ROS scavenging rate of the scaffold and realize repeatable, efficient ROS scavenging over a long period of time. HA and electrical stimulation synergistically promote osteogenic cell differentiation on PPy‐PDA‐HA films. Ultimately, the PPy‐PDA‐HA porous scaffold provides excellent bone regeneration through the synergistic effects of electroactivity, cell affinity, and antioxidative activity of the PPy‐PDA NPs and the osteoinductivity of HA NPs. This study provides a new strategy for functionalizing porous scaffolds that show great promise as implants for tissue regeneration.
A national survey of testing and management of asymptomatic carriage of C. difficile
Authors: Kutty Preeta K. , Beekmann Susan E. , Sinkowitz-Cochran Ronda L. , Dubberke Erik R. , Kuhar David T. , McDonald L. Clifford , Polgreen Philip M. 
Published: May 2019

AbstractA nationwide survey indicated that screening for asymptomatic carriers of C. difficile is an uncommon practice in US healthcare settings. Better understanding of the role of asymptomatic carriage in C. difficile transmission, and of the measures available to reduce that risk, are needed to inform best practices regarding the management of carriers.