bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synephrine and phenylephrine act as α‐amylase, α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase enzymes inhibitors
Authors: Taslimi Parham , Akıncıoglu Hülya , Gülçin İlhami 
Published: August 2017

AbstractIn this paper, synephrine and phenylephrine compounds showed excellent inhibitory effects against human carbonic anhydrase (hCA) isoforms I and II, α‐amylase, α‐glycosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Synephrine and phenylephrine hadKivalues of 199.02 ± 16.01 and 65.01 ± 5.00 μM against hCA I and 336.02 ± 74.01 and 92.04 ± 18.03 μM against hCA II, respectively. On the other hand, theirKivalues were found to be 169.10 ± 80.03 and 88.03 ± 5.01 nM against AChE and 177.06 ± 6.01 and 78.03 ± 3.05 nM against BChE, respectively. α‐Amylase and α‐glycosidase enzymes were easily inhibited by these compounds. α‐Glycosidase inhibitors, generally defined to as starch blockers, are anti‐diabetic drugs that help to decrease post comestible blood glucose levels.
Antioxidant protection by β‐selenoamines against thioacetamide‐induced oxidative stress and hepatotoxicity in mice
Authors: Stefanello Sílvio Terra , Hartmann Diane Duarte , Amaral Guilherme Pires , Courtes Aline Alves , Leite Martim T. B. , da Silva Thayanara Cruz , Gonçalves Débora Farina , Souza Micaela B. , da Rosa Pâmela Carvalho , Dornelles Luciano , Soares Félix Alexandre Antunes 
Published: August 2017

AbstractThioacetamide (TAA) is a hepatotoxin that rapidly triggers the necrotic process and oxidative stress in the liver. Nevertheless, organic selenium compounds, such as β‐selenoamines, can be used as pharmacological agents to diminish the oxidative damage. Thus, the aim of this study was to investigate the protective effect of the antioxidant β‐selenoamines on TAA‐induced oxidative stress in mice. Here, we observed that a single intraperitoneal injection of TAA (200 mg/kg) dramatically elevated some parameters of oxidative stress, such as lipid peroxidation and reactive oxygen species (ROS) production, as well as depleted cellular antioxidant defenses. In addition, TAA‐induced edema and morphological changes in the liver, which correlate with high serum aspartate and alanine aminotransferase enzyme activities, and a decrease in cell viability. Conversely, a significant reduction in liver lipid peroxidation, ROS production, and edema was observed in animals that received an intraperitoneal injection of β‐selenoamines (15.6 mg/kg) 1 h after TAA administration.
TPX2‐p53‐GLIPR1 regulatory circuitry in cell proliferation, invasion, and tumor growth of bladder cancer
Authors: Yan Liang , Li Qi , Yang Juan , Qiao Baoping 
Published: August 2017

AbstractThe targeting protein for Xenopus kinesin‐like protein 2 (TPX2) is associated with the metastasis and prognosis of bladder cancer. p53 is closely related to the progression of bladder cancer. Human glioma pathogenesis‐related protein 1 (GLIPR1) is a p53 target gene with antitumor activity. This study aims to explore the interplay between TPX2, p53, and GLIPR1 and its correlation with cell proliferation, invasion, and tumor growth in bladder cancer. Here, Western blot and qRT‐PCR analysis revealed that TPX2 at both mRNA and protein levels was up‐regulated in bladder carcinoma tissues compared to their paired adjacent normal tissues. Additionally, tissues expressing high TPX2 level exhibited high p53 level and low GLIPR1 level. The expressions of TPX2 and p53 in non‐muscle‐invasive bladder cancer cells (KK47 and RT4) were lower than those in muscle‐invasive bladder cancer cells (T24, 5637, and UM‐UC‐3), while GLIPR1 showed the converse expression pattern. Further investigation revealed that TPX2 activated the synthesis of p53; and GLIPR1 is up‐regulated by wild‐type (wt)‐p53 but not affected by mutated p53; Additionally, GLIPR1 inhibited TPX2. These data suggested a TPX2‐p53‐GLIPR1 regulatory circuitry. Meanwhile, TPX2 overexpression promoted while overexpression of GLIPR1 or p53 inhibited bladder cancer growth. Interestingly, in T24 cells with mutated p53, p53 silence suppressed bladder cancer growth. This study identified a novel TPX2‐p53‐GLIPR1 regulatory circuitry which modulated cell proliferation, migration, invasion, and tumorigenicity of bladder cancer. Our findings provide new insight into underlying mechanisms of tumorigenesis and novel therapeutic options in bladder cancer.
Pharmacokinetics, Safety, and Tolerability of Glecaprevir and Pibrentasvir in Healthy White, Chinese, and Japanese Adult Subjects
Authors: Lin Chih‐Wei , Dutta Sandeep , Ding Bifeng , Wang Tianli , Zadeikis Neddie , Asatryan Armen , Kort Jens , Campbell Andrew , Podsadecki Thomas , Liu Wei 
Published: August 2017

AbstractGlecaprevir and pibrentasvir are direct‐acting antiviral agents being developed as combination therapy for the treatment of chronic hepatitis C virus infection. The aim of the present studies was to assess the effect of race and ethnicity (white, Han Chinese, Japanese) on the pharmacokinetics and safety of multiple oral doses of glecaprevir and pibrentasvir given alone and in combination. Two multiple‐dose, single‐center, phase 1 studies were conducted in healthy adult male and female subjects (n = 170) of respective Asian and white race/ethnicity. Glecaprevir (100, 200, 300, or 700 mg once daily) and pibrentasvir (80, 120, or 160 mg once daily) were administered alone for 7 days followed by the combination of both direct‐acting antiviral agents for another 7 days. Intensive blood sampling was performed, and pharmacokinetic parameters were estimated by noncompartmental analyses. ANOVA was employed to evaluate for differences of steady‐state glecaprevir and pibrentasvir exposures between Asian (Japanese or Han Chinese) and white subjects. Glecaprevir and pibrentasvir exposures in Han Chinese and Japanese were similar to those in whites across dose levels. The nonlinear dose‐exposure relationships for glecaprevir and pibrentasvir were similar across Japanese, Han Chinese, and white subjects, and the safety profiles of the agents were comparable across these groups. The results of these studies demonstrate that race/ethnicity has no clinically meaningful impact on direct‐acting antiviral agent exposures, safety, or tolerability of the glecaprevir and pibrentasvir combination. This is supported in part by the large global registration program of the pangenotypic, coformulated fixed‐dose glecaprevir/pibrentasvir regimen and allows for inclusion of diverse ethnic populations.
Effects of bed compression on protein separation on gel filtration chromatography at bench and pilot scale
Authors: Kong Darryl YC , Gerontas Spyridon , McCluckie Ross A , Mewies Martin , Gruber David , Titchener‐Hooker Nigel J 
Published: August 2017

AbstractBACKGROUNDPoorly packed chromatography columns are known to reduce drastically the column efficiency and produce broader peaks. Controlled bed compression has been suggested to be a useful approach for solving this problem. Here the relationship between column efficiency and resolution of protein separation are examined when preparative chromatography media were compressed using mechanical and hydrodynamic methods. Sepharose CL‐6B, an agarose based size exclusion media was examined at bench and pilot scale. The asymmetry and height equivalent of a theoretical plate (HETP) was determined by using 2% v/v acetone, whereas the void volume and intraparticle porosity (ϵp) were estimated by using blue dextran. A protein mixture of ovalbumin (chicken), bovine serum albumin (BSA) and γ'‐ globulin (bovine) with molecular weights of 44, 67 and 158 kDa, respectively, were used as a ‘model’ separation challenge.RESULTSMechanical compression achieved a reduction in plate height for the column with a concomitant improvement in asymmetry. Furthermore, the theoretical plate height decreased significantly with mechanical compression resulting in a 40% improvement in purity compared with uncompressed columns at the most extreme conditions of compression used.CONCLUSIONThe results suggest that the mechanical bed compression of Sepharose CL‐6B can be used to improve the resolution of protein separation. © 2017 The Authors. Journal of Chemical Technology & Biotechnology published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
Ultrastructural characteristics of ovine bone marrow‐derived mesenchymal stromal cells cultured with a silicon stabilized tricalcium phosphate bioceramic
Authors: Desantis Salvatore , Accogli Gianluca , Burk Janina , Zizza Sara , Mastrodonato Maria , Francioso Edda G. , Rossi Roberta , Crovace Antonio , Resta Leonardo 
Published: August 2017

AbstractBioceramics are being used in experimental bone engineering application in association with bone marrow derived mesenchymal stem cells (BM‐MSCs) as a new therapeutic tool, but their effects on the ultrastructure of BM‐MSCs are yet unknown. In this study we report the morphological features of ovine (o)BM‐MSCs cultured with Skelite, a resorbable bioceramic based on silicon stabilized tricalcium phosphate (SiTCP), able to promote the repair of induced bone defect in sheep model. oBM‐MSCs were isolated from the iliac crest, cultured until they reached near‐confluence and incubated with SiTCP. After 48 hr the monolayers were highly damaged and only few cells adhered to the plastic. Thus, SiTCP was removed, and after washing the cells were cultured until they became confluent. Then, they were trypsinizated and processed for transmission electron microscopy (TEM) and RT‐PCR analysis. RT‐PCR displayed that oBM‐MSCs express typical surface marker for MSCs. TEM revealed the presence of electron‐lucent cells and electron‐dense cells, both expressing the CD90 surface antigen. The prominent feature of electron‐lucent cells was the concentration of cytoplasmic organelles around the nucleus as well as large surface blebs containing glycogen or profiles of endoplasmic reticulum. The dark cells had a multilocular appearance by the presence of peripheral vacuoles. Some dark cells contained endocytic vesicles, lysosomes, and glycogen aggregates. oBM‐MSCs showed different types of specialized interconnections. The comparison with ultrastructural features of untreated oBM‐MSCs suggests the light and dark cells are two distinct cell types which were differently affected by SiTCP bioceramic. Skelite cultured ovine BM‐MSCs display electron‐dense and electron‐lucent cells which are differently affected by this bioceramic. This suggests that they could play a different role in bioceramic based therapy.
Scanning electron microscope investigation on the process of healing of skin wounds in Cirrhinus mrigala
Authors: Verma Neeraj , Kumari Usha , Mittal Swati , Mittal Ajay Kumar 
Published: August 2017

AbstractPresent scanning electron microscope study, reports healing of excised skin wounds in Cirrhinus mrigala. Healing process of wounds, inflicted on head skin, using biopsy punch was observed at intervals—0 hour (h), 1, 2, 4, 6, 12 h, 1 day (d) 2 and 4 d. Accumulation of mucus in wound region within 1h after infliction of wound has been considered an immediate measure to provide protection to injured skin from microbial invasion and other external environmental hazards. On infliction of wound, mobilization of epithelial cells at wound edge is associated with disturbance of coaptive relationship of epithelial cells till original coaptive stability is reached. At 6–12 h appearance of epidermal ridge in region of contact of migrating fronts is due to piling up of epithelial cells. This is associated with cessation of migration of epithelial cells and their simultaneous continual arrival in the region. Speedy epithelialization of skin wounds in C. mrigala like in other fishes, compared to that of mammals and other higher vertebrates, is possibly facilitated owing to surrounding wet external environment. Microridges in initial stages of wound healing appear fragmented without particular orientation. Further, epithelial cells in epithelium in wound region and in region adjacent to wound elongate. These changes are associated with the stretching of epithelial cells indicating their streaming and migration, toward wound. Presence of superficial neuromasts, smallest functional units of lateral line system, a hydrodynamic sensory system, has been associated with important functional significance in fish.
Attitude determination by combining arrays of MEMS accelerometers, gyros, and magnetometers via quaternion‐based complementary filter
Authors: Ghasemi‐Moghadam S. , Homaeinezhad M. R. 
Published: August 2017

AbstractIn this study, an Attitude and Heading Reference System (AHRS) consisting of 5 modules is designed where each module has a triaxial gyroscope, accelerometer, and magnetometer. First, a method based on the Levenberg‐Marquardt algorithm (LMA) is utilized to correct the bias error, scale factor and axes nonorthogonality. Also, the data from the 5 modules of AHRS are ensemble averaged to reduce the adverse effects of high‐frequency noises. Then, the obtained trends are used in an orientation estimation algorithm based on a complementary filter algorithm. In this algorithm, the dynamical accelerations are first decreased via a low‐pass filter. Afterwards, it is determined using an algorithm whether the system is experiencing magnetic distortion or not. If distortion is verified, magnetometers' data are discarded, as it will introduce noticeable error in estimating heading angle. In this case, the heading angle starts to diverge; however, employing 5 modules in the system decreases divergence rate noticeably, such that after 2 minutes in quasi‐static conditions, the pitch, roll, and heading angles' errors decrease, respectively, from 36.195°, 23.201°, and 12.541° when only 1 module is used to 2.511°, 3.972°, and 0.984° when all 5 modules are used. Moreover, in dynamical conditions, these errors decrease from 37.916°, 13.633°, and 13.071° to 6.514°, 5.961°, and 0.284°. Once the distortion is removed from magnetic field, the magnetometers' data are used again to correct the heading error. The obtained results show that the root mean square (RMS) errors of pitch, roll, and heading angles in quasi‐static conditions are 0.536°, 0.323°, and 0.601°, whereas in dynamical condition, they are 1.267°, 1.535°, and 0.994°, respectively.
Macronutrients and metals released from soils by solutions of naturally occurring phenols
Authors: Schmidt Michael A. , Halvorson Jonathan J. , Hagerman Ann E. , Gonzalez Javier M. 
Published: August 2017

AbstractPhenolic compounds produced by plants enter the soil by leaching and litter decomposition. The goal of this work is to determine the effect of phenolic compounds on solubility of plant macronutrients and metals in agroforestry systems. Soils from forest and pasture systems were repeatedly extracted with water (control) or phenolic solutions and then compared to a Mehlich 3 reference. The phenolics were aqueous solutions of tannic acid or β–1,2,3,4,6‐penta‐O‐galloyl‐D‐glucose (PGG) (hydrolyzable tannins), procyanidin (condensed tannin), or small phenolics catechin, gallic acid, or methyl gallate. The concentration of the macronutrients Ca, Mg, K, P, and S, and the metals Fe, Al, Mn, and Zn in the supernatants was determined by inductively‐coupled plasma spectroscopy. Cumulative extraction of macronutrients was generally similar to or less than the amount obtained by the Mehlich 3 extraction with the lowest recoveries obtained with the water control, PGG, and procyanidin. Metals tended to be somewhat more extractable from forest soil, especially with gallic acid, tannic acid or PGG treatments. Three mechanisms affected extraction of analytes by phenol‐containing solutions: (1) pH‐driven dissolution (Ca and Mg), (2) chelation of the metal (Al) by the polyphenol, or (3) reduction of the metal (Fe and Mn). Relatively low extraction of nutrients by some polyphenols is attributed to the tendency of some phenols to sorb to soil. This study demonstrates that tannins and related compounds change the solubility of macronutrients and metals in soils by a complex process that is not easily predictable from simple chemical properties of the phenolics.
Physico‐chemical properties and extrusion behaviour of selected common bean varieties
Authors: Natabirwa Hedwig , Muyonga John H , Nakimbugwe Dorothy , Lungaho Mercy 
Published: August 2017

AbstractBACKGROUNDExtrusion processing offers the possibility of processing common beans industrially into highly nutritious and functional products. However, there is limited information on properties of extrudates from different bean varieties and their association with raw material characteristics and extrusion conditions. In this study, physico‐chemical properties of raw and extruded Bishaz, K131, NABE19, Roba1 and RWR2245 common beans were determined. The relationships between bean characteristics and extrusion conditions on the extrudate properties were analysed.RESULTSExtrudate physico‐chemical and pasting properties varied significantly (P < 0.05) among bean varieties. Expansion ratio and water solubility decreased, while bulk density, water absorption, peak and breakdown viscosities increased as feed moisture increased. Protein exhibited significant positive correlation (P < 0.05) with water solubility index, and negative correlations (P < 0.05) with water absorption, bulk density and pasting viscosities. Iron and dietary fibre showed positive correlation while total ash exhibited negative correlation with peak viscosity, final viscosity and setback. Similar trends were observed in principal component analysis.CONCLUSIONExtrudate physico‐chemical properties were found to be associated with beans protein, starch, iron, zinc and fibre contents. Therefore, bean chemical composition may serve as an indicator for beans extrusion behaviour and could be useful in selection of beans for extrusion. © 2017 Society of Chemical Industry
Investigating inhibitory activity of novel synthetic sericin peptide on α‐D‐glucosidase: kinetics and interaction mechanism study using a docking simulation
Authors: Xie Fan , Wang Shaoyun , Zhang Li , Wu Jinhong , Wang Zhengwu 
Published: August 2017

AbstractBACKGROUNDWe synthesised a novel sericin peptide (SP‐GI) with α‐d‐glucosidase inhibitory activity, which has a sequence of SEDSSEVDIDLGN. The kinetics of its peptide‐induced inhibition on α‐d‐glucosidase activity and its interaction mechanism merging with molecular docking were both investigated.RESULTSSP‐GI exhibited significant inhibitory activity with an IC50 of 2.9 ± 0.1 µmol L−1 and this inhibition was reversible and non‐competitive with a Ki value of 1.0 ± 0.1 µmol L−1. An interaction study with SP‐GI revealed it bound to α‐d‐glucosidase at a single binding site, resulting in alterations in α‐d‐glucosidase secondary structure. This led to quenching of intrinsic α‐d‐glucosidase fluorescence by a static quenching mechanism. Molecular docking results showed that the SP‐GI binding site on α‐d‐glucosidase differed from acarbose, with hydrogen bonding and van der Waals forces being the main binding drivers.CONCLUSIONThese findings suggest the potential use for SP‐GI or other natural sericin peptides as dietary supplements for the treatment of type 2 diabetes. © 2017 Society of Chemical Industry
Exploring the microbial diversity in Jordanian hot springs by comparative metagenomic analysis
Authors: Hussein Emad I. , Jacob Jacob H. , Shakhatreh Muhamad Ali K. , Abd Al‐razaq Mutaz A. , Juhmani Abdul‐salam F. , Cornelison Christopher T. 
Published: August 2017

AbstractA culture‐independent approach was utilized in this study to reveal the microbial diversity in Jordanian hot springs represented by Ma'in and Afra hot springs. Water samples from Ma'in and Afra hot springs were collected in June 2015. The in situ temperature of water samples range was 38–59°C and the pH range was 7.4–8.4. The metagenome was extracted and analyzed using the next generation technology (bTEFAP®). A total of 314,310 sequences were parsed and 288,452 were then clustered. The sequences were predominated by bacteria (>84%) and the relative abundance of archaea in each sample was <1%. Eukaryotic microorganisms were detected but with varying abundances (0.6%–15%). Because most of the detected sequences were found to belong to the domain of bacteria (196,936 sequences out 288,452), the bacterial sequences were utilized for further microbial analyses. With respect to alpha and beta diversity, samples were rarefied to 30,000 sequences and bootstrapped at 10,000 sequences. The Shannon–Wiener Index curve plot reaches a plateau at approximately 3,000 sequences indicating that sequencing depth was sufficient to capture the full scope of microbial diversity. By examining the relative abundance of phyla detected in each sample, it appears that the biota of both Jordanian hot springs sampled are compositionally similar, with over 50% of the microbial community of each sample being comprised of the phylum Proteobacteria. The second most abundant phylum was the phylum Bacteroidetes which represents more than 13% in each sample. The phylum Firmicutes was also detected with a significant abundance. However, lower abundance of Deinococcus, Verrucomicrobia, Planctomycetes, and Chloroflexi was detected. A principal coordinate analysis plot was generated based upon the weighted UniFrac distance matrix. By utilizing Monte Carlo simulations, we were able to determine that there were no significant differences in the microbial diversity between each sample.
CCR2+ monocytic myeloid‐derived suppressor cells (M‐MDSCs) inhibit collagen degradation and promote lung fibrosis by producing transforming growth factor‐β1
Authors: Lebrun Astrid , Lo Re Sandra , Chantry Mathilde , Izquierdo Carerra Xavier , Uwambayinema Francine , Ricci Doriana , Devosse Raynal , Ibouraadaten Saloua , Brombin Lisa , Palmai‐Pallag Mihaly , Yakoub Yousof , Pasparakis Manolis , Lison Dominique , Huaux François 
Published: August 2017

AbstractMonocytes infiltrating scar tissue are predominantly viewed as progenitor cells. Here, we show that tissue CCR2+ monocytes have specific immunosuppressive and profibrotic functions. CCR2+ monocytic cells are acutely recruited to the lung before the onset of silica‐induced fibrosis in mice. These tissue monocytes are defined as monocytic myeloid‐derived suppressor cells (M‐MDSCs) because they significantly suppress T‐lymphocyte proliferation in vitro. M‐MDSCs collected from silica‐treated mice also express transforming growth factor (TGF)‐β1, which stimulates lung fibroblasts to release tissue inhibitor of metalloproteinase (TIMP)‐1, an inhibitor of metalloproteinase collagenolytic activity. By using LysMCreCCR2loxP/loxP mice, we show that limiting CCR2+ M‐MDSC accumulation reduces the pulmonary contents of TGF‐β1, TIMP‐1 and collagen after silica treatment. M‐MDSCs do not differentiate into lung macrophages, granulocytes or fibrocytes during pulmonary fibrogenesis. Collectively, our data indicate that M‐MDSCs contribute to lung fibrosis by specifically promoting a non‐degrading collagen microenvironment. Copyright © 2017 Pathological Society of Great Britain and Ireland. Published by John Wiley & Sons, Ltd.