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Maret G Traber, Eunice Mah, Scott W Leonard, Gerd Bobe, Richard S Bruno
BACKGROUND: Vitamin E supplementation improves liver histology in patients with nonalcoholic steatohepatitis, which is a manifestation of the metabolic syndrome (MetS). We reported previously that α-tocopherol bioavailability in healthy adults is higher than in those with MetS, thereby suggesting that the latter group has increased requirements. OBJECTIVE: We hypothesized that α-tocopherol catabolites α-carboxyethyl hydroxychromanol (α-CEHC) and α-carboxymethylbutyl hydroxychromanol (α-CMBHC) are useful biomarkers of α-tocopherol status...
January 11, 2017: American Journal of Clinical Nutrition
Konstantinos Ypsilantis, Theodoros Tsolis, Andreas Kourtellaris, Manolis J Manos, John C Plakatouras, Achilleas Garoufis
Platinum(ii) complexes of the formula PtLCl2 [L = 2-(2'-pyridyl)quinoxaline, (pqx) (1), 2,(2'-pyridyl)benzo[g]quinoxaline, (pbqx) (3) and 2,(2'-pyridyl)quinoline, (pqn) (5)] were synthesized and characterized by spectroscopic and X-ray diffraction methods. Also, monodentate coordination of the ligands pqx and pbqx formed the complexes trans-Pt(DMSO)pqxCl2 (2) and trans-Pt(DMSO)pbqxCl2 (4) as it is indicated from X-ray crystal structure and NMR studies. The reaction of the complexes (1), (3) and (5) with DMSO-d6 revealed a ligand-release solvolysis, which was studied by means of NMR techniques...
January 11, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Yvonne W S Jauw, Josée M Zijlstra, Daphne de Jong, Danielle J Vugts, Sonja Zweegman, Otto S Hoekstra, Guus A M S van Dongen, Marc C Huisman
PURPOSE: Treatment of patients with diffuse large B cell lymphoma (DLBCL) includes rituximab, an anti-CD20 monoclonal antibody (mAb). Insufficient tumor targeting might cause therapy failure. Tumor uptake of 89Zirconium (89Zr)-mAb is a potential imaging biomarker for tumor targeting, since it depends on target antigen expression and accessibility. The aim of this pilot study was to describe the performance of 89Zr-labeled-rituximab-PET to assess CD20 targeting in patients with relapsed/refractory DLBCL...
2017: PloS One
Guilherme R F Rosário, Diana S Vidal, Adriana V Silva, Antônio C C Franco
OBJECTIVE: This study aimed to correlate male age with embryo morphokinetic parameters on D3 considering the timing and the exact moment of embryo cleavage. METHODS: Time-lapse imaging was used to produce an ideal cleavage curve for the embryos analyzed. The percentage of embryos under the curve was analyzed and correlated with male age. RESULTS: 32.6% of the embryos from patients aged 28-33 years were under the curve; 36.2% of the embryos from patients aged 34-39 years were under the curve; 41...
December 1, 2016: JBRA Assisted Reproduction
Yihui Shi, Jaehyeon Park, Chandraiah Lagisetti, Wei Zhou, Lidia C Sambucetti, Thomas R Webb
The splicing of pre-mRNA is a critical process in normal cells and is deregulated in cancer. Compounds that modulate this process have recently been shown to target a specific vulnerability in tumors. We have developed a novel cell-based assay that specifically activates luciferase in cells exposed to SF3B1 targeted compounds, such as sudemycin D6. This assay was used to screen a combined collection of approved drugs and bioactive compounds. This screening approach identified several active hits, the most potent of which were CGP-74514A and aminopurvalanol A, both have been reported to be cyclin-dependent kinases (CDKs) inhibitors...
December 24, 2016: Bioorganic & Medicinal Chemistry Letters
Jian-Fen Zhang, Wei-Qing Chen, Hong Chen
In this study, we report the cloning and expression of a functional glucoside 3-dehydrogenase (G3DH) gene from Sphingobacterium faecium ZJF-D6. This gene is 1686 bp in length and encodes a peptide of 562 amino acids. The G3DH gene was successfully expressed in E. coli, and the recombinant enzyme could oxidize glucosides, galactosides and analogues at C-3 position. The sequence and multiple alignment analysis showed that the enzyme has highest identity with G3DHs from Paraglaciecola polaris LMG 21857, Aliiglaciecola lipolytica E3 and Halomonas sp...
February 2017: World Journal of Microbiology & Biotechnology
Ingjerd Sunde Krogseth, Michael John Whelan, Guttorm Normann Christensen, Knut Breivik, Anita Evenset, Nicholas Alexander Warner
Cyclic volatile methyl siloxanes (cVMS) are emitted to aquatic environments with wastewater effluents. Here, we evaluate the environmental behavior of three cVMS compounds (octamethylcyclotetrasiloxane (D4), decamethylcyclopentasiloxane (D5) and dodecamethylcyclohexasiloxane (D6)) in a high latitude lake (Storvannet, 70°N 23°E), experiencing intermittent wastewater emissions and high latitude environmental conditions (low temperatures and seasonal ice cover). Measured cVMS concentrations in lake water were below detection limits in both March and June 2014...
January 3, 2017: Environmental Science & Technology
Sanghoo Lee, Joo-Hoon Kim, Seol-A Kim, Yeoun-Soo Sun, Anna Lee, Seo-Jin Park, Yun-Tae Kim, Kyoung-Ryul Lee, Young-Jin Kim
BACKGROUND: Total 25-hydroxyvitamin D (25(OH)D) is well-known to be a reliable biomarker of human vitamin D status, with the recognition of widespread vitamin D insufficiency in general populations. The aims of this study are to validate a fast and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantifying 25(OH)D2 and 25(OH)D3 in serum and to compare two automated immunoassays with the LC-MS/MS method. METHODS: Samples were prepared by protein precipitation with ethanol including 25(OH)D3-d6, followed by a liquid-liquid extraction with hexane...
December 2016: Annals of Clinical and Laboratory Science
Kang Wang, Chun Xie, Jianan Zhang, Wenchao Zhang, Deqiang Yang, Lingxue Yu, Yifeng Jiang, Shen Yang, Fei Gao, Zhibiao Yang, Yanjun Zhou, Guangzhi Tong
Porcine epidemic diarrhea virus (PEDV) is a highly contagious coronavirus that causes severe diarrhea and death, particularly in neonatal piglets. The nucleocapsid protein (N protein) of PEDV presents strong immunogenicity and contributes to the cross-reactivity between PEDV and TGEV. However, the characterization of epitopes on the PEDV N protein remains largely unknown. Here, two monoclonal antibodies (MAbs) specific to the N protein of a PEDV strain, FJzz1/2011, were generated and screened against a partially overlapping library of 24 GST-fusion N protein-truncated constructs...
December 19, 2016: Scientific Reports
Huqun Li, Maosheng Fang, Mingzhen Xu, Shihong Li, Juan Du, Weiyong Li, Hui Chen
BACKGROUND: Atypical antipsychotics such as olanzapine cause metabolic side effects leading to obesity and insulin resistance. The underlying mechanisms remain elusive. In this study we investigated the effects of chronic treatment of olanzapine on the fatty acid composition of plasma in mice. METHODS: Twenty 8-week female Balb/c mice were randomly assigned to two groups: the OLA group and the control group. After treatment with olanzapine (10 mg/kg/day) or vehicle intraperitoneally for 8 weeks, fasting glucose, insulin levels and oral glucose tolerance test were determined...
2016: PloS One
Ricardo P Garay, George T Grossberg
Agitation is common and distressing in patients with Alzheimer-type dementia, but safe, effective treatments remain elusive. Psychological treatments are first-line options, but they have limited efficacy. Off-label psychotropic medications are frequently used, but they also have limited effectiveness, and their use may have harmful side effects, including death. Areas covered: This review discusses the history leading to the conception of AVP-786 (deuterated (d6)-dextromethorphan/quinidine), its pharmacokinetic and pharmacodynamic profiles and safety issues, together with an overview of recent clinical trials...
January 2017: Expert Opinion on Investigational Drugs
Qiansheng Zhan, Zhen Ye, Robert Clarke, Zev Rosenwaks, Nikica Zaninovic
OBJECTIVE: To investigate the prevalence, developmental potential, chromosomal constitution and clinical outcome of embryos with direct unequal cleavages (DUC). DESIGN: A retrospective observational study. SETTING: Academic Institution. PARTICIPANT: 21,261 embryos from 3,155 cycles cultured in EmbryoScope®. RESULTS: The total incidence of DUCs per embryo occupying the first three cleavages were 26...
2016: PloS One
T A T G van Kempen, M H Reijersen, C de Bruijn, S De Smet, J Michiels, M G Traber, C Lauridsen
Vitamin E is important for animal production because of its effects on health and product quality, but the amount and form required remains controversial. Our objective was to quantify the absolute bioavailability of oral -α-tocopheryl acetate (α-TAc) in swine (22 ± 1 kg and 8 wk old, fitted with jugular catheters) adapted to a diet supplemented with 75 mg/kg -α-TAc; 75 mg/kg was chosen because this level represents the nonweighted average inclusion level in piglet diets across Western key swine-producing countries...
October 2016: Journal of Animal Science
Makoto Kataoka, Chie Kojima, Kazuki Ueda, Keiko Minami, Haruki Higashino, Shinji Sakuma, Kazutaka Togashi, Kuninori Mutaguchi, Shinji Yamashita
The purpose of the present study is to demonstrate a useful approach (isotope-IV method) for analyzing drug-drug interactions (DDIs) following the oral administration of drugs using stable isotope-labeled compounds. Verapamil hydrochloride (VER) was used as a drug model. Deuterium-labeled VER (VER-d6, 0.005 mg/kg) was intravenously administered to rats with or without a pre-treatment with 1-aminobenzotriazole (ABT, 100 mg/kg), a potent CYP inhibitor, 1.5 h after the oral administration of VER (1 mg/kg)...
December 2016: Drug Metabolism and Pharmacokinetics
Vera Homem, Daniela Capela, José Avelino Silva, Alessandra Cincinelli, Lúcia Santos, Arminda Alves, Nuno Ratola
Siloxane-based compounds are widely used in personal care, pharmaceutical and household products as well as in industrial applications. Among the wide variety of these chemicals, special attention has been given to volatile methylsiloxanes (VMSs). These compounds have been extensively detected in several environmental compartments, as they are not effectively removed from wastewater and may migrate through different matrices and being lipophilic, bioaccumulate and biomagnify in living organisms. In this work, a prioritisation methodology for several VMSs in different environmental matrices was applied, estimating a hazard quotient by combining exposure evaluation through measured or predicted environmental concentrations (MEC or PEC) and effects using ecotoxicity data to establish no effect concentrations (PNEC)...
February 1, 2017: Science of the Total Environment
F-D Kopinke, A Georgi, G Imfeld, H-H Richnow
Isotope fractionation between benzene-D0 and benzene-D6 caused by multi-step partitioning of the benzenes between water and two organic solvents, n-octane and 1-octanol, as well as between water and the gas phase, was measured. The obtained fractionation factors αH = KH/KD are αH = 1.080 ± 0.015 and αH = 1.074 ± 0.015 for extraction into n-octane and 1-octanol, respectively, and αH = 1.049 ± 0.010 for evaporation from aqueous solution. The comparison of solvent- and gas-phase partitioning reveals that about 2/3 of the driving force of fractionation is due to different interactions in the aqueous phase, whereas 1/3 is due to different interactions in the organic phase...
February 2017: Chemosphere
Georges Khalil, Christophe Orvain, Lu Fang, Laurent Barloy, Alain Chaumont, Christian Gaiddon, Marc Henry, Nathalie Kyritsakas, Pierre Mobian
This manuscript describes the synthesis of a series of neutral titanium(iv) monomeric complexes constructed around a TiO4N2 core. The two nitrogen atoms that compose the coordination sphere of the metallic center belong to 2,2'-bipyrimidine ligands homo-disubstituted in the 4 and 4' positions by methyl (2a), phenylvinyl (2b), naphthylvinyl (2c) or anthrylvinyl (2d) groups. The crystal structures of these complexes named [Ti(1)2(2a)], [Ti(1)2(2b)], [Ti(1)2(2c)] and [Ti(1)2(2d)] (where 1 is a 2,2'-biphenolato ligand substituted in the 6 and 6' positions by phenyl groups) are reported...
November 18, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Amali Subasinghe, Inoka C Perera, Svetlana Pakhomova, Theshini Perera
A novel ligand bearing a central piperidinyl sulfonamide group, N(SO2pip)dpa, and its corresponding Re tricarbonyl complex, [Re(CO)3(N(SO2pip)dpa)](+), have been synthesized in good yield. The methylene CH2 signal seen as a singlet (4.54 ppm) in a (1)H NMR spectrum of the ligand in DMSO-d6 appears as two doublets (5.39, 5.01 ppm) in a spectrum of the [Re(CO)3(N(SO2pip)dpa)](+) complex and confirms the presence of magnetically nonequivalent protons upon coordination to Re. Structural results revealed that the Re-N bond lengths fall within the normal range establishing coordination of ligand to metal...
2016: Bioinorganic Chemistry and Applications
Inês C R Barbosa, Hiromasa Shikata, Melina Zourelidou, Mareike Heilmann, Ingo Heilmann, Claus Schwechheimer
Polar transport of the phytohormone auxin through PIN-FORMED (PIN) auxin efflux carriers is essential for the spatiotemporal control of plant development. The Arabidopsis thaliana serine/threonine kinase D6 PROTEIN KINASE (D6PK) is polarly localized at the plasma membrane of many cells where it colocalizes with PINs and activates PIN-mediated auxin efflux. Here, we show that the association of D6PK with the basal plasma membrane and PINs is dependent on the phospholipid composition of the plasma membrane as well as on the phosphatidylinositol phosphate 5-kinases PIP5K1 and PIP5K2 in epidermis cells of the primary root...
December 15, 2016: Development
Faiz-Ur Rahman, Amjad Ali, Inam Ullah Khan, Hong-Quan Duong, Rong Guo, Hui Wang, Zhan-Ting Li, Dan-Wei Zhang
Novel phenylenediamine bridged mixed ligands dimetallic square planner Pt(II) complex (L-Pt-Py) was synthesized from simple commercially available precursors in good yield and characterized by (1)H, (13)C, 2D NOESY NMR and high resolution mass spectrometry (HR-ESI-MS). The stability of L-Pt-Py was checked by (1)H NMR in mixed DMSO-d6/D2O solvents. L-Pt-Py showed considerable in vitro cytotoxicity in lung (A549), breast (MCF-7) and liver (HepG2) cancer cell lines and strong in vivo growth inhibition in Escherichia coli (E...
January 5, 2017: European Journal of Medicinal Chemistry
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