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https://www.readbyqxmd.com/read/28544938/sex-steroids-and-metabolic-responses-in-mussels-mytilus-galloprovincialis-exposed-to-drospirenone
#1
Tiziana Cappello, Denise Fernandes, Maria Maisano, Andrea Casano, Marta Bonastre, Maria João Bebianno, Angela Mauceri, Salvatore Fasulo, Cinta Porte
Drospirenone (DRO) is a synthetic progestin derived from 17α-spironolactone with a pharmacological mechanism of action similar to progesterone. Despite its wide use as pharmaceutical and consequent continuous release into the aquatic environment, DRO effects have been poorly investigated on aquatic biota. In order to unravel the toxicity mechanisms of DRO, mussels Mytilus galloprovincialis were exposed for 7 days to different concentrations of DRO, namely 20ng/L (Low; L), 200ng/L (Medium; M), 2000ng/L (High; H) and 10μg/L (Super High; SH) nominal doses...
May 22, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28537194/an-investigation-into-the-potential-role-of-brain-angiogenesis-inhibitor-protein-3-bai3-in-the-tumorigenesis-of-small-cell-carcinoma-a-review-of-the-surrounding-literature
#2
Michael Thomas, David Snead, Daniel Mitchell
Brain angiogenesis inhibitor protein 3 (BAI3) is from the adhesion group of seven-transmembrane spanning G protein-coupled receptors (GPCRs) and has been identified via gene expression profiling as being upregulated in small-cell lung cancer (SCLC) tumors. It has subsequently been validated as a sensitive and specific immunohistochemical marker for SCLC, helping to differentiate these tumors from morphologically similar large-cell neuroendocrine (LCNEC) malignancies. It is, however, still unclear as to the role BAI3 proteins might play in SCLC and indeed how they might contribute to tumorigenesis...
May 24, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28528487/role-of-medicines-of-unknown-identity-in-adverse-drug-reaction-related-hospitalizations-in-developing-countries-evidence-from-a-cross-sectional-study-in-a-teaching-hospital-in-the-lao-people-s-democratic-republic
#3
Céline Caillet, Chanvilay Sichanh, Gaëtan Assemat, Myriam Malet-Martino, Agnès Sommet, Haleh Bagheri, Noudy Sengxeu, Niphonh Mongkhonmath, Mayfong Mayxay, Lamphone Syhakhang, Maryse Lapeyre-Mestre, Paul N Newton, Anne Roussin
INTRODUCTION: The health dangers of medicines of unknown identity (MUIs) [loose pharmaceutical units repackaged in individual bags without labelling of their identity] have been suspected in L/MICs. Using visual and analytical tools to identify MUIs, we investigated the frequency of, and factors associated with, adverse drug reaction (ADR)-related hospitalizations in a central hospital in Vientiane Capital, Lao People's Democratic Republic (PDR). METHODS: All unplanned admissions, except for acute trauma and intentional overdose, were prospectively recorded during a 7-week period in 2013, leading to include 453 adults hospitalized for ≥24 h...
May 20, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28527464/-14-n-nqr-lineshape-in-nanocrystals-an-ab-initio-investigation-of-urea
#4
Alan Gregorovič
(14)N nuclear quadrupole resonance (NQR) lineshapes mostly contain information of low interest, although in nanocrystals they may display some unexpected behaviour. In this work, we present an ab initio computational study of the (14)N NQR lineshapes in urea nanocrystals as a function of the nanocrystal size and geometry, focusing on the surface induced broadening of the lineshapes. The lineshapes were obtained through a calculation of the electric field gradient for each nitrogen site in the nanocrystal separately, taking into account the individual crystal field by embedding the molecule of interest in a suitable lattice of point multipoles representing other urea molecules in the nanocrystal...
May 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28487608/role-of-%C3%AE-133p53-isoform-in-nf-%C3%AE%C2%BAb-inhibitor-pdtc-mediated-growth-inhibition-of-mkn45-gastric-cancer-cells
#5
Hong-Mei Zhang, Xiao-Guang Sang, Yan-Ze Wang, Can Cui, Li Zhang, Wan-Sheng Ji
AIM: To investigate the role of Δ133p53 isoform in nuclear factor-κB (NF-κB) inhibitor pyrrolidine dithiocarbamate (PDTC)-mediated growth inhibition of MKN45 gastric cancer cells. METHODS: The growth rate of MKN45 cells after treatment with different concentrations of only PDTC or PTDC in combination with cisplatin was detected by the CCK-8 assay. mRNA expression levels of Δ133p53, p53β, and the NF-κB p65 subunit and p65 protein levels were detected by reverse transcription-polymerase chain reaction (RT-PCR) and immunofluorescence, respectively...
April 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28483880/the-c-domain-of-oleuropein-%C3%AE-glucosidase-assists-in-protein-folding-and-sequesters-the-enzyme-in-nucleus
#6
Konstantinos Koudounas, Margarita Thomopoulou, Christos Michaelidis, Efstathia Zevgiti, Georgios Papakostas, Paraskevi Tserou, Gerasimos Daras, Polydefkis Hatzopoulos
Oleuropein, a terpene-derived glycosylated secoiridoid biosynthesized exclusively by members of the Oleaceae family, is involved in a two-component defense system comprising a β-glucosidase that activates oleuropein into a toxic glutaraldehyde-like structure. Oleuropein and its deglycosylated derivatives have high pharmaceutical interest. In the present study we determined that the in planta heterologous expressed OeGLU, an oleuropein-specific β-glucosidase from olive (Olea europaea) had enzymatic kinetics similar to the olive native enzyme...
May 8, 2017: Plant Physiology
https://www.readbyqxmd.com/read/28458018/anti-inflammatory-effects-of-novel-polygonum-multiflorum-compound-via-inhibiting-nf-%C3%AE%C2%BAb-mapk-and-upregulating-the-nrf2-pathways-in-lps-stimulated-microglia
#7
Sun Young Park, Mei Ling Jin, Nam Jun Kang, Geuntae Park, Young-Whan Choi
The incorporation of Polygonum multiflorum into the diet can result in anti-aging effects owing to its wide range of biological and pharmaceutical properties. We investigated the anti-neuroinflammatory properties of CRPE56IGIH isolated from P. multiflorum by focusing on its role in the induction of phase II antioxidant enzymes and the modulation of upstream signaling pathways. In microglia, CRPE56IGIH significantly inhibited lipopolysaccharide (LPS)-stimulated nitric oxide and prostaglandin E2 production with nonspecific cytotoxicity...
April 27, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28455777/insights-into-nano-and-micron-scale-phase-separation-in-amorphous-solid-dispersions-using-fluorescence-based-techniques-in-combination-with-solid-state-nuclear-magnetic-resonance-spectroscopy
#8
Hitesh S Purohit, James D Ormes, Sugandha Saboo, Yongchao Su, Matthew S Lamm, Amanda K P Mann, Lynne S Taylor
PURPOSE: Miscibility between the drug and the polymer in an amorphous solid dispersion (ASD) is considered to be one of the most important factors impacting the solid state stability and dissolution performance of the active pharmaceutical ingredient (API). The research described herein utilizes emerging fluorescence-based methodologies to probe (im)miscibility of itraconazole (ITZ)-hydroxypropyl methylcellulose (HPMC) ASDs. METHODS: The ASDs were prepared by solvent evaporation with varying evaporation rates and were characterized by steady-state fluorescence spectroscopy, confocal imaging, differential scanning calorimetry (DSC), and solid state nuclear magnetic resonance (ssNMR) spectroscopy...
April 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28454189/assessment-of-the-authenticity-of-herbal-dietary-supplements-comparison-of-chemical-and-dna-barcoding-methods
#9
Rahul S Pawar, Sara M Handy, Raymond Cheng, Nicole Shyong, Erich Grundel
About 7 % of the U. S. population reports using botanical dietary supplements. Increased use of such supplements has led to discussions related to their authenticity and quality. Reports of adulteration with substandard materials or pharmaceuticals are of concern because such substitutions, whether inadvertent or deliberate, may reduce the efficacy of specific botanicals or lead to adverse events. Methods for verifying the identity of botanicals include macroscopic and microscopic examinations, chemical analysis, and DNA-based methods including DNA barcoding...
April 28, 2017: Planta Medica
https://www.readbyqxmd.com/read/28451739/understanding-renal-nuclear-protein-accumulation-an-in-vitro-approach-to-explain-an-in-vivo-phenomenon
#10
Lisanne Luks, Marcia Y Maier, Silvia Sacchi, Loredano Pollegioni, Daniel R Dietrich
Proper subcellular trafficking is essential to prevent protein mislocalization and aggregation. Transport of the peroxisomal enzyme D-amino acid oxidase (DAAO) appears dysregulated by specific pharmaceuticals, e.g., the anti-overactive bladder drug propiverine or a norepinephrine/serotonin reuptake inhibitor (NSRI), resulting in massive cytosolic and nuclear accumulations in rat kidney. To assess the underlying molecular mechanism of the latter, we aimed to characterize the nature of peroxisomal and cyto-nuclear shuttling of human and rat DAAO overexpressed in three cell lines using confocal microscopy...
April 27, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28447451/improvement-of-a-p450-based-recombinant-escherichia-coli-whole-cell-system-for-the-production-of-oxygenated-sesquiterpene-derivatives
#11
Thuy T B Ly, Alexander Schifrin, Bach Duc Nguyen, Rita Bernhardt
Sesquiterpenes are common constituents of essential oil in plants. Their oxygenated derivatives often possess desirable flavor, fragrance, and pharmaceutical properties. Recently, the CYP264B1-based recombinant Escherichia coli whole-cell system has been constructed for the oxidation of sesquiterpenes. However, limiting factors of this system related to the high volatility of substrates and the suitability of the P450 redox partner need to be addressed. In this work, the improvement of the system was implemented with (+)-α-longipinene as a model substrate...
May 4, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28445526/biosynthesis-of-the-oxygenated-diterpene-nezukol-in-the-medicinal-plant-isodon-rubescens-is-catalyzed-by-a-pair-of-diterpene-synthases
#12
Kyle A Pelot, David M Hagelthorn, J Bennett Addison, Philipp Zerbe
Plants produce an immense diversity of natural products (i.e. secondary or specialized metabolites) that offer a rich source of known and potentially new pharmaceuticals and other desirable bioproducts. The Traditional Chinese Medicinal plant Isodon rubescens (Lamiaceae) contains an array of bioactive labdane-related diterpenoid natural products. Of these, the ent-kauranoid oridonin is the most prominent specialized metabolite that has been extensively studied for its potent antimicrobial and anticancer efficacy...
2017: PloS One
https://www.readbyqxmd.com/read/28445076/image-based-phenotypic-screening-with-human-primary-t-cells-using-one-dimensional-imaging-cytometry-with-self-tuning-statistical-gating-algorithms
#13
Steve S Wang, Daniel J Ehrlich
The parallel microfluidic cytometer (PMC) is an imaging flow cytometer that operates on statistical analysis of low-pixel-count, one-dimensional (1D) line scans. It is highly efficient in data collection and operates on suspension cells. In this article, we present a supervised automated pipeline for the PMC that minimizes operator intervention by incorporating multivariate logistic regression for data scoring. We test the self-tuning statistical algorithms in a human primary T-cell activation assay in flow using nuclear factor of activated T cells (NFAT) translocation as a readout and readily achieve an average Z' of 0...
April 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28437741/use-of-nuclear-receptor-luciferase-based-bioassays-to-detect-endocrine-active-chemicals-in-a-biosolids-biochar-amended-soil
#14
Carolyn G Anderson, Geetika Joshi, Daniel A Bair, Charlotte Oriol, Guochun He, Sanjai J Parikh, Michael S Denison, Kate M Scow
Biosolids are a potentially valuable source of carbon and nutrients for agricultural soils; however, potential unintended impacts on human health and the environment must be considered. Virtually all biosolids contain trace amounts endocrine-disrupting chemicals derived from human use of pharmaceuticals and personal care products (PPCPs). One potential way to reduce the bioavailability of PPCPs is to co-apply biosolids with biochar to soil, because biochar's chemical (e.g., aromaticity) and physical properties (e...
April 8, 2017: Chemosphere
https://www.readbyqxmd.com/read/28435985/elucidating-the-a%C3%AE-42-anti-aggregation-mechanism-of-action-of-tramiprosate-in-alzheimer-s-disease-integrating-molecular-analytical-methods-pharmacokinetic-and-clinical-data
#15
Petr Kocis, Martin Tolar, Jeremy Yu, William Sinko, Soumya Ray, Kaj Blennow, Howard Fillit, John A Hey
BACKGROUND: Amyloid beta (Aβ) oligomers play a critical role in the pathogenesis of Alzheimer's disease (AD) and represent a promising target for drug development. Tramiprosate is a small-molecule Aβ anti-aggregation agent that was evaluated in phase III clinical trials for AD but did not meet the primary efficacy endpoints; however, a pre-specified subgroup analysis revealed robust, sustained, and clinically meaningful cognitive and functional effects in patients with AD homozygous for the ε4 allele of apolipoprotein E4 (APOE4/4 homozygotes), who carry an increased risk for the disease...
April 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28429292/preparation-of-chloramphenicol-amino-acid-combinations-exhibiting-enhanced-dissolution-rates-and-reduced-drug-induced-oxidative-stress
#16
Vanesa B Sterren, Virginia Aiassa, Claudia Garnero, Yamila Garro Linck, Ana K Chattah, Gustavo A Monti, Marcela R Longhi, Ariana Zoppi
Chloramphenicol is an old antibiotic agent that is re-emerging as a valuable alternative for the treatment of multidrug-resistant pathogens. However, it exhibits suboptimal biopharmaceutical properties and toxicity profiles. In this work, chloramphenicol was combined with essential amino acids (arginine, cysteine, glycine, and leucine) with the aim of improving its dissolution rate and reduce its toxicity towards leukocytes. The chloramphenicol/amino acid solid samples were prepared by freeze-drying method and characterized in the solid state by using Fourier transform infrared spectroscopy, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and solid-state nuclear magnetic resonance...
April 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28425152/nmr-structures-and-molecular-dynamics-simulation-of-hylin-a1-peptide-analogs-interacting-with-micelles
#17
Edson Crusca, Amanda Souza Câmara, Carolina Oliveira Matos, Reinaldo Marchetto, Eduardo Maffud Cilli, Luciano Morais Lião, Aline Lima de Oliveira
Antimicrobial peptides are recognized candidates with pharmaceutical potential against epidemic emerging multi-drug resistant bacteria. In this study, we use nuclear magnetic resonance spectroscopy and molecular dynamics simulations to determine the unknown structure and evaluate the interaction with dodecylphosphatidylcholine (DPC) and sodium dodecylsulphate (SDS) micelles with three W(6) -Hylin-a1 analogs antimicrobial peptides (HyAc, HyK, and HyD). The HyAc, HyK, and HyD bound to DPC micelles are all formed by a unique α-helix structure...
April 20, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28423670/invasive-fusobacterium-nucleatum-activates-beta-catenin-signaling-in-colorectal-cancer-via-a-tlr4-p-pak1-cascade
#18
Yongyu Chen, Yan Peng, Jiahui Yu, Ting Chen, Yaxin Wu, Lei Shi, Qing Li, Jiao Wu, Xiangsheng Fu
The underlying mechanism of Fusobacterium nucleatum (Fn) in the carcinogenesis of colorectal cancer (CRC) is poorly understood. Here, we examined Fn abundance in CRC tissues, as well as β-catenin, TLR4 and PAK1 protein abundance in Fn positive and Fn negative CRCs. Furthermore, we isolated a strain of Fn (F01) from a CRC tissue and examined whether Fn (F01) infection of colon cancer cells activated β-catenin signaling via the TLR4/P-PAK1/P-β-catenin S675 cascade. Invasive Fn was abundant in 62.2% of CRC tissues...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28416656/effect-of-cholesterol-on-the-molecular-structure-and-transitions-in-a-clinical-grade-lung-surfactant-extract
#19
Jenny Marie Andersson, Carl Grey, Marcus Larsson, Tiago Mendes Ferreira, Emma Sparr
The lipid-protein film covering the interface of the lung alveolar in mammals is vital for proper lung function and its deficiency is related to a range of diseases. Here we present a molecular-level characterization of a clinical-grade porcine lung surfactant extract using a multitechnique approach consisting of [Formula: see text]-[Formula: see text] solid-state nuclear magnetic spectroscopy, small- and wide-angle X-ray scattering, and mass spectrometry. The detailed characterization presented for reconstituted membranes of a lung extract demonstrates that the molecular structure of lung surfactant strongly depends on the concentration of cholesterol...
May 2, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28415422/synthesis-and-characterization-of-redox-sensitive-heparin-%C3%AE-sitosterol-micelles-their-application-as-carriers-for-the-pharmaceutical-agent-doxorubicin-and-investigation-of-their-antimetastatic-activities-in-vitro
#20
Tilahun Ayane Debele, Shewaye Lakew Mekuria, Hsieh-Chih Tsai
Although there are several clinical attempts to treat tumors at the primary site, only few therapies can inhibit the spread of metastatic cancers. In this study, we synthesized redox-sensitive heparin-β-sitosterol micelles that show antimetastatic activity. Proton nuclear magnetic resonance and Fourier transform infrared analyses confirmed the formation of bioreducible heparin-β-sitosterol (bHSC) conjugates, whereas dynamic light scattering was used to measure the particle size and zeta potential. Both 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and flow cytometry assays confirmed the low toxicity of the synthesized micelles...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
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