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https://www.readbyqxmd.com/read/28432980/discovery-of-potential-inhibitor-against-human-acetylcholinesterase-a-molecular-docking-and-molecular-dynamics-investigation
#1
Surya Pratap Singh, Dwijendra Gupta
Alzheimer's disease (AD) is a progressive neurodegenerative disease of central nervous system among elderly people. Human acetylcholinesterase (hAChE), an important enzyme in neuronal signaling, is responsible for the degradation of acetylcholine which in turn prevents the post synaptic signal transmissions. hAChE has been an attractive target of drug discovery for the search of therapeutics against AD. In the recent past hAChE has become hot target for the investigation of new potential therapeutics. We performed virtual screening of entire database against hAChE...
April 12, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28432957/nanoencapsulation-strategies-for-the-delivery-of-novel-bifunctional-antioxidant-%C3%AF-1-selective-ligands
#2
Claudia Carbone, Emanuela Arena, Veronica Pepe, Orazio Prezzavento, Ivana Cacciatore, Hasan Turkez, Agostino Marrazzo, Antonio Di Stefano, Giovanni Puglisi
Nowadays sigma-1 receptors are considered as new therapeutic objectives for central nervous system neurodegenerative diseases. Among different molecules, alpha lipoic acid has been identified as a natural potent antioxidant drug, whose therapeutic efficacy is limited by its many drawbacks, such as fast metabolism, poor bioavailability and high physico-chemical instability. Alfa-lipoic acid derivatives have been recently developed demonstrating their neuroprotective activity and effectiveness in different types of oxidative stress...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28432657/in-vitro-assay-for-measuring-real-time-topotecan-release-from-liposomes-release-kinetics-and-cellular-internalization
#3
Roger Gilabert-Oriol, Lina Chernov, Malathi Anantha, Wieslawa H Dragowska, Marcel B Bally
Topotecan is a drug that is under investigation for the treatment of neuroblastoma and has been encapsulated into liposomes to improve its therapeutic efficacy. However, liposomal formulations still need to be optimized for drug retention and new techniques to measure drug release are required to better understand this process. Here, a novel in vitro method based on fluorescence de-quenching and an automated microscopy imaging platform were developed for monitoring, in real time, the release of topotecan from a liposomal formulation...
April 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28432647/the-gender-attention-observational-study-gender-and-hormonal-status-differences-in-the-incidence-of-adverse-events-during-cyclosporine-treatment-in-psoriatic-patients
#4
Delia Colombo, Giuseppe Banfi, Nicoletta Cassano, Alessandra Graziottin, Gino Antonio Vena, Giovanni Gualberto Fiori, Emanuela Zagni, Luca Stingeni, Sergio Chimenti, Enzo Berardesca, Giuseppe Micali, Giuseppe Albertini, Clara De Simone, Gilberto Bellia
INTRODUCTION: Female sex has been shown to be a risk factor for the development of adverse drug reactions; however, this has not been studied for cyclosporine (CsA). The aim of this study was to investigate, in Italian dermatological practice, the influence of gender and menopause and related hormones on the incidence of adverse events (AEs) during CsA treatment in psoriatic patients. METHODS: Multicenter, prospective, observational study conducted from May 2011 to June 2013...
April 21, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#5
Abdelmoumin Zoghbi, Tianjiao Geng, Bo Wang
Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-β-cyclodextrin (HPβCD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HPβCD inclusion complex (KD)...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28432573/clinical-outcomes-in-trials-evaluating-lipid-lowering-drugs
#6
REVIEW
Julie Butters, Alex Brown, Liddy Griffith, Susan Kim, Stephen J Nicholls
While statins have formed the cornerstone of strategies for cardiovascular prevention, the residual risk related to low-density lipoprotein cholesterol (LDL-C) and other lipoprotein factors provides a landscape for development of new therapies. However, a number of lipid-modifying therapies have failed to reduce cardiovascular event rates in contemporary clinical trials of statin-treated patients. The factors considered in outcome measure selection for clinical trials of novel lipid-lowering therapies are reviewed...
April 21, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28432472/anti-infective-and-anti-inflammatory-pharmacotherapies
#7
Mark I Rosenblatt
Ocular infection and inflammation are common and are associated with myriad ocular conditions ranging from mild disease to blinding conditions. There are numerous anti-invectives with spectra against inciting pathogens. Given the potential for ocular infections to rapidly progress initial broad spectrum therapy is usually required, with therapy tailored as microbiological identification and sensitivities become available. The emergence of antibiotic resistance has become a major health problem. Anti-inflammatory therapy can be institutes to prevent ocular symptoms and end-organ damage...
April 22, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28432317/psiguajadials-a-k-unusual-psidium-meroterpenoids-as-phosphodiesterase-4-inhibitors-from-the-leaves-of-psidium-guajava
#8
Gui-Hua Tang, Zhen Dong, Yan-Qiong Guo, Zhong-Bin Cheng, Chu-Jun Zhou, Sheng Yin
Bioassay-guided fractionation of the ethanolic extract of the leaves of Psidium guajava led to the isolation of 11 new Psidium meroterpenoids, psiguajadials A-K (1-11), along with 17 known ones (12-28). Their structures and absolute configurations were elucidated by spectroscopic methods and comparison of experimental and calculated ECD. Compounds 1 and 2 represent two unprecedented skeletons of 3,5-diformyl-benzyl phloroglucinol-coupled sesquiterpenoid, while 3 is the first example of Psidium meroterpenoids coupling via an oxepane ring...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432280/small-molecules-targeting-histone-demethylase-genes-kdms-inhibit-growth-of-temozolomide-resistant-glioblastoma-cells
#9
Barbara Banelli, Antonio Daga, Alessandra Forlani, Giorgio Allemanni, Daniela Marubbi, Maria Pia Pistillo, Aldo Profumo, Massimo Romani
In glioblastoma several histone demethylase genes (KDM) are overexpressed compared to normal brain tissue and the development of Temozolomide (TMZ) resistance is accompanied by the transient further increased expression of KDM5A and other KDMs following a mechanism that we defined as "epigenetic resilience". We hypothesized that targeting KDMs may kill the cells that survive the cytotoxic therapy.We determined the effect of JIB 04 and CPI-455, two KDM inhibitors, on glioblastoma cells and found that both molecules are more effective against TMZ-resistant rather than native cells...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28432226/everolimus-plus-exemestane-in-advanced-breast-cancer-safety-results-of-the-ballet-study-on-patients-previously-treated-without-and-with-chemotherapy-in-the-metastatic-setting
#10
Daniele Generali, Filippo Montemurro, Roberto Bordonaro, Antonino Mafodda, Sante Romito, Andrea Michelotti, Pierluigi Piovano, Maria Teresa Ionta, Claudia Bighin, Donata Sartori, Antonio Frassoldati, Marina Elena Cazzaniga, Ferdinando Riccardi, Franco Testore, Patrizia Vici, Carlo Antonio Barone, Alessio Schirone, Federico Piacentini, Franco Nolè, Annamaria Molino, Luciano Latini, Edda Lucia Simoncini, Fausto Roila, Francesco Cognetti, Francesco Nuzzo, Jennifer Foglietta, Alessandro Marco Minisini, Francesca Goffredo, Giuseppe Portera, Gilda Ascione, Gabriella Mariani
BACKGROUND: The BALLET study was an open-label, multicenter, expanded access study designed to allow treatment with everolimus plus exemestane in postmenopausal women with hormone receptor-positive metastatic breast cancer progressed following prior endocrine therapy. A post hoc analysis to evaluate if previous chemotherapy in the metastatic setting affects the safety profile of the combination regimen of everolimus and exemestane was conducted on the Italian subset, as it represented the major part of the patients enrolled (54%)...
April 21, 2017: Oncologist
https://www.readbyqxmd.com/read/28432048/solithromycin-a-novel-ketolide-antibiotic
#11
Michael J Buege, Jack E Brown, Samuel L Aitken
PURPOSE: The pharmacology, pharmacokinetics, pharmacodynamics, antimicrobial activity, clinical safety, and current regulatory status of solithromycin are reviewed. SUMMARY: Solithromycin is a novel ketolide antibiotic developed for the treatment of community-acquired bacterial pneumonia (CABP). Its pharmacologic, pharmacokinetic, and pharmacodynamic properties provide activity against a broad range of intracellular organisms, including retained activity against pathogens displaying various mechanisms of macrolide resistance...
April 21, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28432031/membrane-lipid-replacement-for-chronic-illnesses-aging-and-cancer-using-oral-glycerolphospholipid-formulations-with-fructooligosaccharides-to-restore-phospholipid-function-in-cellular-membranes-organelles-cells-and-tissues
#12
REVIEW
Garth L Nicolson, Michael E Ash
Membrane Lipid Replacement is the use of functional, oral supplements containing mixtures of cell membrane glycerolphospholipids, plus fructooligosaccharides (for protection against oxidative, bile acid and enzymatic damage) and antioxidants, in order to safely replace damaged, oxidized, membrane phospholipids and restore membrane, organelle, cellular and organ function. Defects in cellular and intracellular membranes are characteristic of all chronic medical conditions, including cancer, and normal processes, such as aging...
April 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28431898/serum-potassium-concentrations-importance-of-normokalaemia
#13
REVIEW
Manuel Heras, María José Fernández-Reyes
Abnormalities in potassium concentrations are associated with morbidity and mortality. In recent years it has been considered that small variations in serum potassium concentrations within normal intervals may also be associated with mortality. Strategies for achieving normokalaemia include dietary measures, limiting the use of potassium retaining drugs, and use of conventional cation exchange resins (calcium/sodium polystyrene sulfonate) and/or the new non-absorbed cation exchange polymer (patiromer).
April 18, 2017: Medicina Clínica
https://www.readbyqxmd.com/read/28431810/in-vivo-ameliorative-effect-of-cerium-oxide-nanoparticles-in-isoproterenol-induced-cardiac-toxicity
#14
Shereen S El Shaer, Taher A Salaheldin, Nashwa M Saied, Sally M Abdelazim
BACKGROUND: Cerium oxide nanoparticles have gained much more attention especially in the field of nanomedicine. This work represents cerium oxide nanoparticles as a new prophylactic model for heart failure progression. OBJECTIVE: To investigate the potential protective effect of cerium oxide nanoparticles on Isoproterenol (ISO)-induced cardiac toxicity in rats. METHODS: Cerium oxide nanoparticles (5±1nm) were synthesized by reverse micelle method and characterized using High Resolution Transmission Electron Microscopy, X-Ray Diffraction and particle size analyzer...
April 18, 2017: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/28431803/reutilization-of-discarded-biomass-for-preparing-functional-polymer-materials
#15
REVIEW
Jianfeng Wang, Wenzhen Qian, Yufeng He, Yubing Xiong, Pengfei Song, Rong-Min Wang
Biomass is abundant and recyclable on the earth, which has been assigned numerous roles to human beings. However, over the past decades, accompanying with the rapid expansion of man-made materials, such as alloy, plastic, synthetic rubber and fiber, a great number of natural materials had been neglected and abandoned, such as straw, which cause a waste of resource and environmental pollution. In this review, based on introducing sources of discarded biomass, the main composition and polymer chains in discarded biomass materials, the traditional treatment and novel approach for reutilization of discarded biomass were summarized...
April 18, 2017: Waste Management
https://www.readbyqxmd.com/read/28431767/the-new-drug-conditional-approval-process-in-china-challenges-and-opportunities
#16
REVIEW
Xuefang Yao, Jinxi Ding, Yingfang Liu, Penghui Li
PURPOSE: Our aim was to characterize the newly established new drug conditional approval process in China and discuss the challenges and opportunities with respect to new drug research and development and registration. METHODS: We examined the new approval program through literature review, law analysis, and data analysis. Data were derived from published materials, such as journal articles, government publications, press releases, and news articles, along with statistical data from INSIGHT-China Pharma Databases, the China Food and Drug Administration website, the Center for Drug Evaluation website, the US Food and Drug Administration website, and search results published by Google...
April 18, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28431671/where-are-we-now-a-clinicians-guide-to-the-use-of-follow-on-insulin-for-patients-with-diabetes
#17
Steven V Edelman, Priscilla A Hollander, Eugene E Wright
Insulin has been used as a standard treatment for patients with diabetes for almost 100 years. Over time, advances in insulin development have improved its pharmacologic properties. (Online access: http://courses.elseviercme.com/t2dm/666). Most recently, the US Food and Drug Administration approved a novel, follow-on basal insulin agent, with more expected to be commercially available in the near future. With the imminent availability of follow-on basal insulin agents, clinicians need to be aware of the potential benefits and concerns in order to facilitate informed decision making and to provide the best possible advice and guidance to their patients with diabetes...
May 2017: American Journal of Medicine
https://www.readbyqxmd.com/read/28431634/multicenter-observational-study-of-abobotulinumtoxina-neurotoxin-in-cervical-dystonia-the-anchor-cd-registry
#18
Richard M Trosch, Alberto J Espay, Daniel Truong, Ramon Gil, Carlos Singer, Peter A LeWitt, Mark F Lew, Michele Tagliati, Charles H Adler, Jack J Chen, Dominic Marchese, Cynthia L Comella
BACKGROUND: The ANCHOR-CD prospective observational registry study evaluated the effectiveness of abobotulinumtoxinA in adult idiopathic cervical dystonia (CD) in clinical practice. METHODS: Adults with CD were eligible. Treating physicians determined abobotulinumtoxinA dose and treatment interval. The primary endpoint was patient response rate (Toronto Western Spasmodic Torticollis Rating Scale [TWSTRS] score reduction≥25% and Patient Global Impression of Change [PGIC] score of +2 or +3 at Week 4 of Cycle 1)...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28431589/t2-relaxometry-helps-prognosticate-seizure-outcome-in-patients-with-solitary-cerebral-cysticercosis
#19
Aaron de Souza, Atchayaram Nalini, Jitender Saini, Kandavel Thennarasu
OBJECTIVE: Correlate serial T2 relaxometry (T2R) values with long term seizure outcome in patients with solitary cerebral cysticercosis (SCC) in order to establish its usefulness as a prognostic marker in these patients. METHODS: Patients with new-onset seizures due to SCC were imaged serially using a pre-determined MRI protocol at enrolment and after 3, 6, 12 and 24months. T2 relaxometry was performed using a dual echo sequence with maps generated manually from the measured image intensities at the level of the lesion...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28431544/strategies-for-monitoring-and-combating-resistance-to-combination-kinase-inhibitors-for-cancer-therapy
#20
REVIEW
Leanne G Ahronian, Ryan B Corcoran
Targeted therapies such as kinase inhibitors and monoclonal antibodies have dramatically altered cancer care in recent decades. Although these targeted therapies have improved patient outcomes in several cancer types, resistance ultimately develops to these agents. One potential strategy proposed to overcome acquired resistance involves taking repeat tumor biopsies at the time of disease progression, to identify the specific molecular mechanism driving resistance in an individual patient and to select a new agent or combination of agents capable of surmounting that specific resistance mechanism...
April 21, 2017: Genome Medicine
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