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https://www.readbyqxmd.com/read/28548969/transcriptome-profiling-in-preadipocytes-identifies-long-noncoding-rnas-as-sam68-targets
#1
Naomi Li, Steven Hébert, Jingwen Song, Claudia L Kleinman, Stéphane Richard
The KH-type RNA binding protein Sam68 is required for adipogenesis. We have previously shown that Sam68-deficient mice have a lean phenotype and are protected against dietary-induced obesity due to defects in mTOR and S6K1 alternative splicing. Herein we profiled the transcriptome of Sam68 wild type and deficient 3T3-L1 mouse preadipocytes. We identified 652 protein-coding genes and 9 ncRNAs that were significantly altered with the loss of Sam68. As expected, downregulated genes were significantly associated with GO terms linked to cell migration, motility, and fat cell differentiation, while upregulated genes were mostly associated with GO terms linked to neurogenesis...
May 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28548843/zwitterionic-nanocarrier-surface-chemistry-improves-sirna-tumor-delivery-and-silencing-activity-relative-to-polyethylene-glycol
#2
Meredith A Jackson, Thomas A Werfel, Elizabeth J Curvino, Fang Yu, Taylor Elizabeth Kavanaugh, Samantha M Sarett, Mary D Dockery, Kameron V Kilchrist, Ayisha N Jackson, Todd D Giorgio, Craig L Duvall
Although siRNA-based nanomedicines hold promise for cancer treatment, conventional siRNA-polymer complex (polyplex) nanocarrier systems have poor pharmacokinetics following intravenous delivery, hindering tumor accumulation. Here, we determined the impact of surface chemistry on the in vivo pharmacokinetics and tumor delivery of siRNA polyplexes. A library of diblock polymers was synthesized, all containing the same pH-responsive, endosomolytic polyplex core-forming block but different corona blocks: 5 kDa (benchmark) and 20 kDa linear PEG, 10 kDa and 20 kDa brush-like poly(oligo ethylene glycol) (POEGMA), and 10 kDa and 20 kDa zwitterionic phosphorylcholine-based polymers (PMPC)...
May 26, 2017: ACS Nano
https://www.readbyqxmd.com/read/28543298/synthesis-and-preclinical-pharmacokinetic-study-of-dha-10-a-novel-potential-antifungal-pogostone-analogue
#3
Ming Liu, Yanfen Zhou, Jianwei Zhu, Bo Ma, Zheng Fang, Qi Zhang
OBJECTIVES: The emergence of fungal disease calls for the urgency of development of novel drug. In this study, we developed a novel pogostone analogue, DHA-10 and investigated its preclinical pharmacokinetics, tissue distribution, excretion and protein binding rate in rats. METHODS: DHA-10 was synthesized with dehydroacetic acid (DHA) as the starting material and the structure confirmed by NMR and HRMS. The LC-MS/MS was applied to quantitative analysis of DHA-10 concentrations in the biological samples...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28539253/documenting-the-kinetic-time-course-of-lambda-cyhalothrin-metabolites-in-orally-exposed-volunteers-for-the-interpretation-of-biomonitoring-data
#4
Rania Khemiri, Jonathan Côté, Hamadi Fetoui, Michèle Bouchard
Lambda-cyhalothrin is a pyrethroid pesticide largely used in agriculture. Exposure assessment can be performed by measuring key urinary metabolites. For a proper use of biomonitoring data, it is however important to gain information on the toxicokinetics of these key biomarkers of exposure. A human volunteer study was performed to document the plasma and urinary time courses of major lambda-cyhalothrin metabolites. Seven volunteers ingested 0.025mgkg(-1) body weight of lambda-cyhalothrin. Blood samples were withdrawn prior to dosing and at fixed time periods over the 72 h-period following ingestion and complete urine voids were collected pre-exposure and at pre-established intervals over 84h post-dosing...
May 21, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28534854/methodical-challenges-and-a-possible-resolution-in-the-assessment-of-receptor-reserve-for-adenosine-an-agonist-with-short-half-life
#5
Judit Zsuga, Tamas Erdei, Katalin Szabó, Nora Lampe, Csaba Papp, Akos Pinter, Andras Jozsef Szentmiklosi, Bela Juhasz, Zoltán Szilvássy, Rudolf Gesztelyi
The term receptor reserve, first introduced and used in the traditional receptor theory, is an integrative measure of response-inducing ability of the interaction between an agonist and a receptor system (consisting of a receptor and its downstream signaling). The underlying phenomenon, i.e., stimulation of a submaximal fraction of receptors can apparently elicit the maximal effect (in certain cases), provides an opportunity to assess the receptor reserve. However, determining receptor reserve is challenging for agonists with short half-lives, such as adenosine...
May 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28534402/passive-air-samplers-as-a-tool-for-assessing-long-term-trends-in-atmospheric-concentrations-of-semivolatile-organic-compounds
#6
Jiří Kalina, Martin Scheringer, Jana Boruvkova, Petr Kukucka, Petra Přibylová, Pernilla Bohlin-Nizzetto, Jana Klánová
Many attempts have been made to quantify the relationship between the amount of persistent organic pollutants sequestered by passive air sampling devices and their actual concentrations in ambient air. However, this information may not be necessary for some applications. In this study, two sets of 30 ten-year-long time series of simultaneous passive and high-volume active air sampling carried out at the Košetice observatory in the Czech Republic were used for a comparison of temporal trends. Fifteen polyaromatic hydrocarbons, seven polychlorinated biphenyls and eight organochlorine pesticides were investigated...
May 23, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28528081/click-strategy-using-disodium-salts-of-amino-acids-improves-the-water-solubility-of-plinabulin-and-kpu-300
#7
Fumika Yakushiji, Kyohei Muguruma, Yoshiki Hayashi, Takuya Shirasaka, Ryosuke Kawamata, Hironari Tanaka, Yushi Yoshiwaka, Akihiro Taguchi, Kentaro Takayama, Yoshio Hayashi
Plinabulin and KPU-300 are promising anti-microtubule agents; however, the low water solubility of these compounds (<0.1µg/mL) has limited their pharmaceutical advantages. Here, we developed five water-soluble derivatives of plinabulin and KPU-300 with a click strategy using disodium salts of amino acids. The mother skeleton, diketopiperazine (DKP), was transformed into a monolactim-type alkyne and a copper-catalyzed alkyne azide cycloaddition (CuAAC) combined azides that was derived from amino acids as a water-solubilizing moiety...
May 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28527785/the-effectiveness-of-a-fixed-dose-combination-pour-on-formulation-of-1-25-fipronil-and-2-5-fluazuron-against-economically-important-ectoparasites-and-associated-pharmacokinetics-in-cattle
#8
Welber Daniel Zanetti Lopes, Rafael Marin Chiummo, Luis Fernando Vettorato, Daniel de Castro Rodrigues, Rafael Bazaglia Sonada
The present work consisted of eight studies to evaluate the ectoparasiticidal spectrum and determine the pharmacokinetic parameters of a pour-on combination of fipronil 1.25mg/kg+fluazuron 2.5mg/kg for cattle against Rhipicephalus microplus, Haematobia irritans and the larvae of Dermatobia hominis and Cochliomyia hominivorax. The analysis fipronil and fluazuron were performed by liquid chromatography using a mass detector for the detection and quantification of analytes (LC-MS/MS). Additionally, in two of these studies, the animals were artificially infested with R...
May 17, 2017: Parasitology International
https://www.readbyqxmd.com/read/28513463/alzheimer-s-disease-against-peptides-products-of-enzymatic-cleavage-app-protein-biological-pathobiological-and-physico-chemical-properties-of-fibrillating-peptides
#9
Małgorzata Marszałek
Various peptides products of enzymatic cleavage of key for Alzheimer's disease Amyloid Precursor Protein (APP) are well known, but still are matter of scientific debate. The Aβ type products are especially challenging for experimental and medical research. This paper outlines several, still poorly known, biological and medical processes such as peptides biology, i.e., formation, biodistribution, translocation, transport and finally removal from brain compartments and body fluids like Intracellular Fluid (ICF), Cerebrospinal Fluid (CSF), Interstitial Fluid (ISF), blood serum or urine...
May 17, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28511818/-how-the-other-half-live-lay-perspectives-on-health-inequalities-in-an-age-of-austerity
#10
Kayleigh Garthwaite, Clare Bambra
This paper examines how people living in two socially contrasting areas of Stockton on Tees, North East England experience, explain, and understand the stark health inequalities in their town. Participants displayed opinions that fluctuated between a variety of converging and contrasting explanations. Three years of ethnographic observation in both areas (2014-2017) generated explanations which initially focused closely on behavioural and individualised factors, whilst 118 qualitative interviews subsequently revealed more nuanced justifications, which prioritised more structural, material and psychosocial influences...
May 10, 2017: Social Science & Medicine
https://www.readbyqxmd.com/read/28508378/population-pharmacokinetic-and-pharmacodynamic-modeling-of-etelcalcetide-in-patients-with-chronic-kidney-disease-and-secondary-hyperparathyroidism-receiving-hemodialysis
#11
Ping Chen, Adimoolam Narayanan, Benjamin Wu, Per Olsson Gisleskog, John P Gibbs, Andrew T Chow, Murad Melhem
INTRODUCTION: Etelcalcetide is a novel calcimimetic that binds and activates calcium-sensing receptors (CaSRs) for the treatment of secondary hyperparathyroidism (SHPT). METHODS: To assess titrated dosing regimens, population pharmacokinetic (PK) and PK/pharmacodynamic (PKPD) modeling of etelcalcetide was performed using NONMEM 7.2. In this analysis, plasma etelcalcetide, serum parathyroid hormone (PTH) and calcium (Ca) concentration-time data were collected from five phase I, II, and III clinical trials following single or multiple intravenous doses of etelcalcetide ranging from 2...
May 15, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28504822/equilibrium-kinetic-and-structural-properties-of-gallium-iii-and-some-divalent-metal-complexes-formed-with-the-new-datam-and-data5m-ligands
#12
Edit Farkas, Johannes Nagel, Bradley Waldron, David Parker, Imre Tóth, Ernő Brücher, Frank Rösch, Zsolt Baranyai
The development of 68Ge/68Ga generators has made the positron emitting 68Ga isotope widely accessible, raising interest in new chelate complexes of Ga3+. The hexadentate DATAm ligand and its bifunctional analogue, DATA5m, rapidly form complexes with 68Ga in high radiochemical yield. The stability constants of DATAm and DATA5m complexes formed with Ga3+, Zn2+, Cu2+, Mn2+ and Ca2+ have been determined by pH-potentiometry, spectrophotometry (Cu2+) and 1H- and 71Ga-NMR spectroscopy (Ga3+). The stability constants of Ga(DATAm) and Ga(DATA5m) complexes are slightly higher than those of the Ga(AAZTA)...
May 15, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28501802/stability-of-proteins-in-dried-blood-spot-biobanks
#13
Johan Björkesten, Stefan Enroth, Qiujin Shen, Lotta Wik, David Hougaard, Arieh Cohen, Lene Sörensen, Vilmantas Giedraitis, Martin Ingelsson, Anders Larsson, Masood Kamali-Moghaddam, Ulf Landegren
An important motivation for the construction of biobanks is to discover biomarkers that identify diseases at early, potentially curable stages. This will require biobanks from large numbers of individuals, preferably sampled repeatedly, where the samples are collected and stored under conditions that preserve potential biomarkers. Dried blood samples are attractive for biobanking because of the ease and low cost of collection and storage. Here we have investigated their suitability for protein measurements...
May 13, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28500968/stability-and-removal-of-selected-avobenzone-s-chlorination-products
#14
Cheng Wang, Mojca Bavcon Kralj, Berta Košmrlj, Jun Yao, Suzana Košenina, Olga V Polyakova, Viatcheslav B Artaev, Albert T Lebedev, Polonca Trebše
Stability studies of two avobenzone transformation products: chloro-avobenzone [2-chloro-1-(4-tert-butylphenyl)-3-(4-methoxyphenyl)-1,3-propanedione] and dichloro-avobenzone [2,2-dichloro-1-(4-tert-butylphenyl)-3-(4-methoxyphenyl)-1,3-propanedione] have been performed at different pHs values as well as under UV A light and compared with the stability of avobenzone, one of the mostly used UV A filter present in sunscreens. We have additionally investigated the possibility of application of TiO2 photocatalysis as a method for the removal of them...
May 6, 2017: Chemosphere
https://www.readbyqxmd.com/read/28495700/visualizing-dynamic-microvillar-search-and-stabilization-during-ligand-detection-by-t-cells
#15
En Cai, Kyle Marchuk, Peter Beemiller, Casey Beppler, Matthew G Rubashkin, Valerie M Weaver, Audrey Gérard, Tsung-Li Liu, Bi-Chang Chen, Eric Betzig, Frederic Bartumeus, Matthew F Krummel
During immune surveillance, T cells survey the surface of antigen-presenting cells. In searching for peptide-loaded major histocompatibility complexes (pMHCs), they must solve a classic trade-off between speed and sensitivity. It has long been supposed that microvilli on T cells act as sensory organs to enable search, but their strategy has been unknown. We used lattice light-sheet and quantum dot-enabled synaptic contact mapping microscopy to show that anomalous diffusion and fractal organization of microvilli survey the majority of opposing surfaces within 1 minute...
May 12, 2017: Science
https://www.readbyqxmd.com/read/28493602/avenacosides-metabolism-and-potential-use-as-exposure-biomarkers-of-oat-intake
#16
Pei Wang, Junli Yang, Aaron Yerke, Shengmin Sang
SCOPE: Exposure biomarkers used for objective estimation of whole-grain (WG) intake are essential for epidemiologic studies of WG consumption, however, up to now, no exposure biomarkers were developed for WG oat intake. This study investigates the potential of oat unique components, Avenacoside-B (AVE-B) and -A (AVE-A), as exposure biomarkers of oat intake. METHODS AND RESULTS: An in vivo study performed in mice and an in vitro batch fecalfermentation study were used to investigate the potential metabolic routes of AVE-B and -A...
May 11, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28488882/development-of-bioanalytical-assays-for-variegin-a-peptide-based-bivalent-direct-thrombin-inhibitor
#17
Norrapat Shih, Leonardo Pinto de Carvalho, Yie Hou Lee, Mauricio Macario Rocha, Adriano Henrique Pereira Barbosa, José Marconi A de Sousa, Antonio Carlos de C Carvalho, R Manjunatha Kini, Mark Y Chan
AIM: Variegin is an anticoagulant peptide that will be tested in porcine models of percutaneous coronary intervention. We developed three bioanalytical assays for variegin quantitation and utilized these methods to evaluate pharmacokinetics of variegin in pigs. Results & methodology: The LC-MS/MS, thrombin amidolytic and modified thrombin time assays had a quantitation range of 21.6-5541.7, 10.8-5541.7 and 5.4-5541.7 nM in human plasma, respectively. The elimination half-lives obtained using the LC-MS/MS, modified thrombin time and thrombin amidolytic assays were 52...
May 10, 2017: Bioanalysis
https://www.readbyqxmd.com/read/28486578/development-of-a-validated-comparative-stability-indicating-assay-method-for-some-h2-receptor-antagonists
#18
Sameh Ahmed, Salwa R Elshaboury, Niveen A Mohamed, Shereen Farrag
A comparative force degradation high performance thin layer chromatography (HPTLC) method was developed and validated for some H2-receptor antagonists. The studied H2-receptor antagonists were ranitidine (RAN), nizatidine (NIZ) and famotidine (FAM). The degradation behaviors of the studied H2-receptor antagonists were studied under different stress conditions (hydrolytic, thermal and oxidative) conditions as well as storage conditions according to International Conference on Harmonization (ICH) recommendations...
May 9, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28486182/dissipation-occurrence-and-risk-assessment-of-a-phenylurea-herbicide-tebuthiuron-in-sugarcane-and-aquatic-ecosystems-in-south-china
#19
Yuan Qian, Haruna Matsumoto, Xiaoyu Liu, Shuying Li, Xiao Liang, Yanan Liu, Guonian Zhu, Mengcen Wang
In this study, a modified QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) method coupled with UPLC-QqQ-MS/MS analysis was developed to detect tebuthiuron in sugarcane fields and the surrounding aquatic ecosystems. Methodological validation showed the method developed was of favorable sensitivity, reproducibility and accuracy. For assessment of its dietary and ecological risks, dissipation and occurrence of tebuthiuron in situ were further investigated through a supervised field trial and an aquatic environment monitoring carried out in six dominant sugarcane production regions in South China...
May 6, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28485745/the-half-life-of-25-oh-d-after-uvb-exposure-depends-on-gender-and-vitamin-d-receptor-polymorphism-but-mainly-on-the-start-level
#20
Pameli Datta, Peter A Philipsen, Peter Olsen, Morten K Bogh, Peter Johansen, Anne V Schmedes, Niels Morling, Hans C Wulf
The 25-hydroxy vitamin D (25(OH)D) production caused by UVB exposure is usually underestimated as the concurrent degradation of 25(OH)D is not considered. Therefore, the decrease in 25(OH)D was investigated during a 7-week period in winter when ambient UVB is negligible. Twenty-two healthy Danish individuals (113 samples) participated and had a mean and steady maximal 25(OH)D start level of 132 nmol l(-1) (range of 68-216 nmol l(-1)) due to long-term UVB treatment prior to this study. In this group with high 25(OH)D start levels, the decrease in 25(OH)D was best described by an exponential model...
May 9, 2017: Photochemical & Photobiological Sciences
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