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https://www.readbyqxmd.com/read/27923180/insight-into-the-structure-and-stability-of-tc-and-re-dmsa-complexes-a-computational-study
#1
Daniel Hernández-Valdés, Alejandro Blanco-González, Ariel García-Fleitas, Zalua Rodríguez-Riera, Giuseppe Meola, Roger Alberto, Ulises Jáuregui-Haza
Meso-2,3-dimercaptosuccinic acid (DMSA) is used in nuclear medicine as ligand for preparation of diagnostic and therapy radiopharmaceuticals. DMSA has been the subject of numerous investigations during the past three decades and new and significant information of the chemistry and pharmacology of DMSA complexes have emerged. In comparison to other ligands, the structure of some DMSA complexes is unclear up today. The structures and applications of DMSA complexes are strictly dependent on the chemical conditions of their preparation, especially pH and components ratio...
November 27, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27922827/gold-nanoparticles-as-scaffolds-for-poor-water-soluble-and-difficult-to-vehiculate-antiparkinson-codrugs
#2
A Di Crescenzo, I Cacciatore, M Petrini, M D'Alessandro, N Petragnani, P Del Boccio, P Di Profio, S Boncompagni, G Spoto, H Turkez, P Ballerini, A Di Stefano, A Fontana
We report the facile and non-covalent preparation of gold nanoparticles (AuNPs) stabilized by an antiparkinson codrug based on lipoic acid (LA). The obtained AuNPs appear stable in both dimethyl sulfoxide and fetal bovine serum and able to load an amount of codrug double the weight of gold. These NPs were demonstrated to be safe and biocompatible towards primary human blood cells and human neuroblastoma cells, one of the most widely used cellular models to study dopaminergic neural cells, therefore are ideal drug carriers for difficult to solubilize molecules...
December 6, 2016: Nanotechnology
https://www.readbyqxmd.com/read/27922213/quantitative-maldi-ms-binding-assays-an-alternative-to-radiolabeling
#3
Maxime Rossato, Guillaume Miralles, Céline M'Kadmi, Mathieu Maingot, Muriel Amblard, Bernard Mouillac, Didier Gagne, Jean Martinez, Gilles Subra, Christine Enjalbal, Sonia Cantel
Radiolabeling of ligands is still the gold standard in the study of high-affinity receptor-ligand interactions. In an effort toward safer and simpler alternatives to the use of radioisotopes, we developed a quantitative and highly sensitive matrix-assisted laser desorption ionization mass spectrometry (MALDI-MS) method that relies on the use of chemically tagged ligands designed to be specifically detectable when present as traces in complex biological mixtures such as cellular lysates. This innovative technology allows easy, sensitive detection and accurate quantification of analytes at the sub-nanomolar level...
December 6, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27922194/pharmacodynamic-response-profiles-of-anxiolytic-and-sedative-drugs
#4
Xia Chen, Freerk Broeyer, Marieke de Kam, Joke Baas, Adam Cohen, Joop van Gerven
INTRODUCTION: Centrally-acting acutely anxiolytic drugs, like benzodiazepines, barbiturates and gabapentinoids, affect various central nervous system (CNS) functions, which reflect not only their anxiolytic effects but also neuropsychological side-effects. To validate the pharmacodynamic biomarkers for GABA-ergic anxiolytics, this study determined the pharmacodynamics of two anxiolytics and a non-anxiolytic control and linked them to their anxiolytic and sedative effects, during an anxiety-challenge study day...
December 6, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27921428/-promising-molecules-for-treatment-of-hyperglycemia-in-patients-with-type-2-diabetes
#5
Milan Kvapil
New antidiabetic drugs are being developed today that expand the range of pharmacological intervention, in particular for patients with type 2 diabetes (imeglimin, semaglutide, dulaglutide, FGF 21 analogue). At the same time innovations take place that "better" the well-proven molecules, they offer new application forms we have no experience of diabetology (osmotic pump for exenatide, faster acting insulin aspart). New properties are brought by just the change of concentration (insulin glargine in a concentration of 300 U/ml), unexpected positive results are also brought by new fixed-ratio combinations of antidiabetics (fixed-ratio combination of insulin degludec and liraglutide, fixed-ratio combination of insulin glargine and lixisenatide)...
2016: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/27921374/efficacy-of-a-novel-granulocyte-monocyte-apheresis-adsorber-device-in-the-treatment-of-inflammatory-bowel-diseases-a-pilot-study
#6
Maria Di Girolamo, Alessandro Sartini, Rosina Critelli, Angela Bertani, Alberto Merighi, Erica Villa
Granulocyte monocyte apheresis (GMA) is a non-pharmacological treatment for inflammatory bowel disease. In our study, we tested a novel GMA adsorber device in terms of clinical efficacy and safety in patients' non-response to pharmacological therapy. Secondary outcomes were the evaluation of adsorber's technical performance, the reduction of inflammatory markers and the improvement of patients' life quality. The prospective study included 18 patients enrolled from 2011 to 2012 with a monitoring of 48 weeks...
December 5, 2016: Therapeutic Apheresis and Dialysis
https://www.readbyqxmd.com/read/27921338/melancholic-and-atypical-depression-as-predictor-and-moderator-of-outcome-in-cognitive-behavior-therapy-and-pharmacotherapy-for-adult-depression
#7
Pim Cuijpers, Erica Weitz, Femke Lamers, Brenda W Penninx, Jos Twisk, Robert J DeRubeis, Sona Dimidjian, Boadie W Dunlop, Robin B Jarrett, Zindel V Segal, Steven D Hollon
BACKGROUND: Melancholic and atypical depression are widely thought to moderate or predict outcome of pharmacological and psychological treatments of adult depression, but that has not yet been established. This study uses the data from four earlier trials comparing cognitive behavior therapy (CBT) versus antidepressant medications (ADMs; and pill placebo when available) to examine the extent to which melancholic and atypical depression moderate or predict outcome in an "individual patient data" meta-analysis...
December 6, 2016: Depression and Anxiety
https://www.readbyqxmd.com/read/27920947/the-daniel-k-inouye-college-of-pharmacy-scripts-poha-berry-physalis-peruviana-with-potential-anti-inflammatory-and-cancer-prevention-activities
#8
Leng Chee Chang, Mayuramas Sang-Ngern, John M Pezzuto, Carolyn Ma
The Daniel K. Inouye College of Pharmacy, during a historic event in Spring 2016, graduated the first two students in the Pacific region to earn a PhD in pharmaceutical sciences at the University of Hawai'i at Hilo. The college offers PhD programs in these five disciplines: Cancer Biology, Medicinal Chemistry, Pharmaceutics, Pharmacognosy, and Pharmacology. One of the Pharmacognosy dissertations focused on plant-derived natural products with potential anti-inflammatory and cancer chemopreventive activities...
November 2016: Hawai'i Journal of Medicine & Public Health: a Journal of Asia Pacific Medicine & Public Health
https://www.readbyqxmd.com/read/27920820/protective-effect-of-melissa-officinalis-extract-against-h2o2-induced-oxidative-stress-in-human-vascular-endothelial-cells
#9
Leila Safaeian, Seyyed Ebrahim Sajjadi, Shaghayegh Haghjooy Javanmard, Hossein Montazeri, Fariba Samani
Melissa officinalis L. is a medicinal plant with a large variety of pharmacological effects and traditional applications. This study aimed to evaluate the protective and antioxidant activities of the extract of M. officinalis aerial parts on human umbilical vein endothelial cells (HUVECs) under oxidative stress induced by H2O2. Cells were incubated with H2O2 (0.5 mM, 2 h) after pretreatment with M. officinalis extract (25-500 μg/mL). Cell viability was evaluated by 3-(4, 5- Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay...
October 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27920817/pharmacological-characterization-of-liquiritigenin-a-chiral-flavonoid-in-licorice
#10
Samaa Alrushaid, Neal M Davies, Stephanie E Martinez, Casey L Sayre
Liquiritigenin is a chiral flavonoid present in plant based food, nutraceuticals, and traditional medicines. It is also an important ingredient present in licorice. The purpose of this study is to explore the pharmacological activity of racemic liquiritigenin utilizing several in vitro assays with relevant roles in colon cancer and diabetes. Where possible, the pure enantiomers were tested to identify the stereospecific contribution to the activity. In vitro antioxidant, anticancer, anti-inflammatory activities (cyclooxygenase inhibition), antidiabetic activities (alpha-amylase and alpha-glucosidase inhibition) as well as cytochrome P450 (CYP450) inhibitory activities were assessed...
October 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27920809/rates-and-reasons-for-lack-of-persistence-with-anti-osteoporotic-drugs-analysis-of-the-campania-region-database
#11
Giovanni Iolascon, Francesca Gimigliano, Antimo Moretti, Ilaria Riccio, Massimo Di Gennaro, Maddalena Illario, Valeria Marina Monetti, Valentina Orlando, Enrica Menditto
Subjects with chronic diseases are more likely to be nonpersistent to pharmacological treatment. Lack of persistence is common among subjects using oral anti-osteoporotic drugs, and leads to increased risk of fragility fracture. The aim of our retrospective study is to analyze the rates and reasons for discontinuation of anti-osteoporotic drugs in the Campania Region. Subjects aged over 40 years were included if they had received at least one prescription for any anti-osteoporotic drugs. Data were obtained from an administrative database of regional data on outpatient drug prescriptions reimbursed by the National Health Service...
May 2016: Clinical Cases in Mineral and Bone Metabolism
https://www.readbyqxmd.com/read/27920795/donepezil-enhances-frontal-functional-connectivity-in-alzheimer-s-disease-a-pilot-study
#12
Ludovica Griffanti, Gordon K Wilcock, Natalie Voets, Guendalina Bonifacio, Clare E Mackay, Mark Jenkinson, Giovanna Zamboni
BACKGROUND: We have previously shown that increased resting-state functional magnetic resonance imaging (fMRI)-based functional connectivity (FC) within the frontal resting-state networks in Alzheimer's disease (AD) patients reflects residual, possibly compensatory, function. This suggests that symptomatic treatments should aim to enhance FC specifically in these networks. METHODS: 18 patients with probable AD underwent brain MRI and neuropsychological assessment at baseline and after 12 weeks of treatment with donepezil...
September 2016: Dementia and Geriatric Cognitive Disorders Extra
https://www.readbyqxmd.com/read/27920724/insulin-induces-relaxation-and-decreases-hydrogen-peroxide-induced-vasoconstriction-in-human-placental-vascular-bed-in-a-mechanism-mediated-by-calcium-activated-potassium-channels-and-l-arginine-nitric-oxide-pathways
#13
Lissette Cabrera, Andrea Saavedra, Susana Rojas, Marcela Cid, Cristina Valenzuela, David Gallegos, Pamela Careaga, Emerita Basualto, Astrid Haensgen, Eduardo Peña, Coralia Rivas, Juan Carlos Vera, Victoria Gallardo, Leandro Zúñiga, Carlos Escudero, Luis Sobrevia, Mark Wareing, Marcelo González
HIGHLIGHTS Short-term incubation with insulin increases the L-arginine transport in HUVECs.Short-term incubation with insulin increases the NO synthesis in HUVECs.Insulin induces relaxation in human placental vascular bed.Insulin attenuates the constriction induced by hydrogen peroxide in human placenta.The relaxation induced by insulin is dependent on BKCa channels activity in human placenta. Insulin induces relaxation in umbilical veins, increasing the expression of human amino acid transporter 1 (hCAT-1) and nitric oxide synthesis (NO) in human umbilical vein endothelial cells (HUVECs)...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27920663/asd-and-genetic-associations-with-receptors-for-oxytocin-and-vasopressin-avpr1a-avpr1b-and-oxtr
#14
Sunday M Francis, Soo-Jeong Kim, Emily Kistner-Griffin, Stephen Guter, Edwin H Cook, Suma Jacob
Background: There are limited treatments available for autism spectrum disorder (ASD). Studies have reported significant associations between the receptor genes of oxytocin (OT) and vasopressin (AVP) and ASD diagnosis, as well as ASD-related phenotypes. Researchers have also found the manipulation of these systems affects social and repetitive behaviors, core characteristics of ASD. Consequently, research involving the oxytocin/vasopressin pathways as intervention targets has increased. Therefore, further examination into the relationship between these neuropeptides and ASD was undertaken...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27920467/possible-therapeutic-role-of-ige-blockade-in-irritable-bowel-syndrome
#15
EDITORIAL
Eli Magen, Tinatin Chikovani
Omalizumab is a humanized monoclonal antibody that binds to the high-affinity type-I IgE Fc receptors on mast cells (MCs) and basophils, inhibiting the IgE immune pathway. Irritable bowel syndrome (IBS) is the most common functional gastrointestinal disorder, and dysregulation of the immune system likely contributes to its etiology and/or symptomatology. Colonic biopsies from patients with IBS demonstrate considerable increase in the number of degranulating MCs releasing histamine in proximity to nerves, and this event may underlie the common IBS symptom of abdominal pain...
November 21, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/27920229/octreotide-use-in-post-cardiac-surgery-chylothorax-a-12-year-perspective
#16
Abdulrazaq Sheikh Aljazairi, Tauhid Ahmed Bhuiyan, Abdullah Hasan Alwadai, Rayd Abdulaziz Almehizia
BACKGROUND: Chylothorax following cardiothoracic surgery is a rare condition in pediatric patients with significant morbidity and mortality. Pharmacological management with octreotide suggests possible efficacy; however, current evidence is inadequate. The objective of this study was to assess the safety and efficacy of octreotide as a therapeutic option in this clinical setting. METHODS: This was a 12-year single-center retrospective cohort study of all patients (birth to 18-years old) who received octreotide for management of post-cardiac surgery chylothorax between January 2003 to August 2015...
December 5, 2016: Asian Cardiovascular & Thoracic Annals
https://www.readbyqxmd.com/read/27919942/a-single-intravesical-instillation-of-vax014-inhibits-orthotopic-superficial-bladder-tumor-implantation-to-increase-survival
#17
Bryan M Hancock, Kathleen L McGuire, Shingo Tsuji, Katherine Reil, Veronica Hernandez, Matthew J Giacalone, W T Godbey
BACKGROUND/AIM: VAX014 minicells (VAX014) have been previously characterized as an integrin-specific oncolytic biotherapeutic agent. The present study was designed to evaluate the potential of VAX014 as an immediate post-operative intravesical adjuvant therapy in the treatment of non-muscle invasive bladder cancer (NMIBC). MATERIALS AND METHODS: The ability of VAX014 to kill a panel of dissociated urothelial carcinoma cell lines was tested in vitro. In vivo experiments were conducted using a single intravesical dose of VAX014 in the anti-implantation variation of the MB49 syngeneic orthotopic bladder cancer model with tumor implantation and overall survival rates serving as study endpoints...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919935/secondary-prevention-lifestyle-interventions-initiated-within-90-days-after-tia-or-minor-stroke-a-systematic-review-and-meta-analysis-of-rehabilitation-programmes
#18
Neil Heron, Frank Kee, Christopher Cardwell, Mark A Tully, Michael Donnelly, Margaret E Cupples
BACKGROUND: Strokes are often preceded by a transient ischaemic attack (TIA) or 'minor' stroke. The immediate period after a TIA/minor stroke is a crucial time to initiate secondary prevention. However, the optimal approach to prevention, including non-pharmacological measures, after TIA is not clear. AIM: To systematically review evidence about the effectiveness of delivering secondary prevention, with lifestyle interventions, in comprehensive rehabilitation programmes, initiated within 90 days of a TIA/minor stroke...
December 5, 2016: British Journal of General Practice: the Journal of the Royal College of General Practitioners
https://www.readbyqxmd.com/read/27919830/newly-acquired-and-reactivated-contextual-fear-memories-are-more-intense-and-prone-to-generalize-after-activation-of-prelimbic-cortex-nmda-receptors
#19
Ana C Vanvossen, Marina A M Portes, Rafael Scoz-Silva, Hugo B Reichmann, Cristina A J Stern, Leandro J Bertoglio
Activity in the rodent prelimbic (PL) cortex contributes to consolidation, retrieval and reconsolidation of learned fear. The PL cortex is considered homologous to the primate dorsal anterior cingulate cortex (dACC). In patients with post-traumatic stress disorder (PTSD), the dACC is often reported to be hyperactive after acquisition and/or around the retrieval of the traumatic memory. It is still unknown, however, whether there is a relationship between altered dACC functioning at these time points and PTSD-associated behavioral outcomes, such as fear overgeneralization...
December 2, 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/27919827/pkc%C3%AE-ii-mediated-cross-talk-of-trpv1-cb2-modulates-the-glucocorticoid-induced-osteoclast-overactivity
#20
Giulia Bellini, Marco Torella, Iolanda Manzo, Chiara Tortora, Livio Luongo, Francesca Punzo, Nicola Colacurci, Bruno Nobili, Sabatino Maione, Francesca Rossi
In this study, we investigated the role of the endovanilloid/endocannabinoid system in the glucocorticoid-induced osteoclast overactivity. Receptorial and enzymatic component of the endovanilloid/endocannabinoid system are expressed in bone cells, and dysregulated when bone mass is reduced. Moreover, blockade or desensitization of vanilloid receptor 1 (TRPV1) and/or stimulation of cannabinoid receptor 2 (CB2) are beneficial for reducing number and activity of the bone cells modulating resorption, the osteoclasts...
December 2, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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