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https://www.readbyqxmd.com/read/29793215/in-silico-insight-into-voltage-gated-sodium-channel-1-7-inhibition-for-anti-pain-drug-discovery
#1
Mingxing Wang, Wei Li, Ying Wang, Yongbo Song, Jian Wang, Maosheng Cheng
Studies on human genetics have implicated the voltage-gated sodium channel Nav1.7 as an appealing target for the treatment of pain. In this study, we put forward a ligand-based pharmacophore for the first time, which was generated by a set of multiple chemical scaffolds including sulfonamide and non-sulfonamide derivatives and consisted of four chemical features: an aromatic ring, a hydrophobic group and two hydrogen acceptors. The active cavity was divided into three regions according to the properties of the amino acids surrounded and was used for the docking of 16 known active inhibitors...
May 18, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#2
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#3
Andrea Chicca, Chiara Arena, Simone Bertini, Francesca Gado, Elena Ciaglia, Mario Abate, Maria Digiacomo, Margherita Lapillo, Giulio Poli, Maurizio Bifulco, Marco Macchia, Tiziano Tuccinardi, Jürg Gertsch, Clementina Manera
The endocannabinoid system (ECS) represents one of the major neuromodulatory systems involved in different physiological and pathological processes. Multi-target compounds exert their activities by acting via multiple mechanisms of action and represent a promising pharmacological modulation of the ECS. In this work we report 4-substituted and 4,5-disubstituted 1,2-dihydro-2-oxo-pyridine-3-carboxamide derivatives with a broad spectrum of affinity and functional activity towards both cannabinoid receptors and additional effects on the main components of the ECS...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793208/enhanced-phosphate-removal-from-wastewater-by-using-in-situ-generated-fresh-trivalent-fe-composition-through-the-interaction-of-fe-ii-on-caco-3
#4
Yujie Li, Xiaoman He, Huimin Hu, Tingting Zhang, Jun Qu, Qiwu Zhang
Excessive existences of nutrients such as phosphate in the aqueous environment remain as a heavy concern although many researches have been reported for dealing with their removal. Based on the understanding toward the interactions of Fe compounds with phosphate and carbonate from many available researches, we designed a very simple and efficient approach for phosphate removal by using in situ generated fresh trivalent Fe composition through the interaction of Fe(II) as FeSO4 on CaCO3 . Addition and agitation of Fe(II) and CaCO3 simultaneously to phosphate solution allowed an amorphous Fe(III)-P or Ca-Fe(III)-P precipitation, with a phosphate removal rate close to 100%, to reduce the residual phosphorus concentration less than 0...
May 21, 2018: Journal of Environmental Management
https://www.readbyqxmd.com/read/29793206/effects-on-the-hepatic-transcriptome-of-chicken-embryos-in-ovo-exposed-to-phenobarbital
#5
Jiahua Guo, Shohei Ito, Hoa Thanh Nguyen, Kimika Yamamoto, Hisato Iwata
This work aimed at evaluating the toxic effects of in ovo exposure to phenobarbital (PB) and unveiling the mode of action by transcriptome analysis in the embryonic liver of a model avian species, chicken (Gallus gallus). Embryos were initially treated with saline or 1 μg PB /g egg at Hamburger Hamilton Stage (HHS) 1 (1st day), followed by 20 days of incubation to HHS 46. At 21st day, chicks that pipped successfully were euthanized and dissected for assessing the PB caused effects on phenotypes and the liver transcriptome in both genders...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793205/comprehensive-assessment-of-three-typical-antibiotics-on-cyanobacteria-microcystis-aeruginosa-the-impact-and-recovery-capability
#6
Yingxiang Du, Jing Wang, Fengyi Zhu, Dina Mai, Zhongrun Xiang, Jianqiu Chen, Ruixin Guo
This innovative study provided a comprehensive evaluation of the effects of three typical antibiotics exposures (cefradine, norfloxacin and amoxicillin) on Microcystis aeruginosa in two periods (exposure and post-exposure) at a new perspective. The results indicated that the irreversible growth inhibition of M. aeruginosa attributed to the norfloxacin in the exposure and the re-exposure stages. In contrast, although the algal cell size recovered to the control level after the exposure of 20 mg/L of cefradine, the significant stimulation on glutathione (GSH) still persisted even if the contaminants were removed...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793204/influence-of-isolated-bacterial-strains-on-the-in-situ-biodegradation-of-endosulfan-and-the-reduction-of-endosulfan-contaminated-soil-toxicity
#7
Lingfen Kong, Yu Zhang, Lusheng Zhu, Jinhua Wang, Jun Wang, Zhongkun Du, Cheng Zhang
The recently discovered endosulfan-degrading bacterial strains Pusillimonas sp. JW2 and Bordetella petrii NS were isolated from endosulfan-polluted water and soil environments. The optimal conditions for the growth and biodegradation activity of the strains JW2 and NS were studied in detail. In addition, the ability of the strains JW2 and NS to biodegrade endosulfan in soils during in situ bioremediation experiments was investigated. At a concentration of 2 mg of endosulfan per kilogram of soil, both JW2 and NS had positive effects on the degradation of endosulfan; JW2 degraded 100% and 91...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793199/effects-of-acute-and-chronic-exposures-of-fluoxetine-on-the-chinese-fish-topmouth-gudgeon-pseudorasbora-parva
#8
Hongxing Chen, Xiangfeng Zeng, Lei Mu, Liping Hou, Bin Yang, Jianliang Zhao, Daniel Schlenk, Wu Dong, Lingtian Xie, Qianru Zhang
Fluoxetine is a selective serotonin reuptake inhibitor used as an antidepressant and has been frequently detected in aquatic environments. However, its effects in fish from Asia remain relatively less studied. In this study, the topmouth gudgeon Pseudorasbora parva was exposed to 0, 50, and 200 µg/L of fluoxetine for 4 h and 42 d. The effects of fluoxetine on biometrics were compared to biochemical endpoints indicative of stress in different fish tissues (brain, liver, gills and intestine) following exposures...
May 21, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29793198/assessment-of-cu-sub-lethal-toxicity-lc-50-in-the-cold-water-gorgonian-dentomuricea-meteor-under-a-deep-sea-mining-activity-scenario
#9
Inês Martins, António Godinho, Joana Goulart, Marina Carreiro-Silva
Previous aquaria-based experiments have shown dissolution and leaching of metals, especially copper (Cu), from the simulated sediment plumes generated during mining activities resulting in a pronounced increase of Cu contamination in the surrounding seawater. Metals are bioavailable to corals with food, through ingestion (particulate phase) and through tissue-facilitated transport (passive diffusion). With corals being particularly vulnerable to metal contamination, resuspension of metal-bearing sediments during mining activities represents an important ecological threat...
May 21, 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29793192/how-did-older-adults-respond-to-challenges-after-an-earthquake-results-from-a-qualitative-study-in-iran
#10
Shokoufeh Ahmadi, Hamidreza Khankeh, Robab Sahaf, Asghar Dalvandi, Seyed Ali Hosseini, Fardin Alipour
OBJECTIVES: In many areas, natural disasters are a major challenge for life and property of people. Earthquake is one of the most devastating natural disasters. This study aimed to explore how older adults responded to challenges after the earthquake in Iran. METHODS: This study was based on qualitative analysis. Data were collected through in-depth and semi-structured interviews. 29 participants including 18 older adult survivors of the earthquake-stricken areas, four lay caregivers, and three health professionals in disasters, one social worker, two relief worker and one disaster psychologist were interviewed...
May 17, 2018: Archives of Gerontology and Geriatrics
https://www.readbyqxmd.com/read/29793189/effects-of-exposure-to-anti-vaping-public-service-announcements-among-current-smokers-and-dual-users-of-cigarettes-and-electronic-nicotine-delivery-systems
#11
Andy S L Tan, Vaughan W Rees, Justin Rodgers, Emeka Agudile, Natasha A Sokol, Kyeungyeun Yie, Ashley Sanders-Jackson
INTRODUCTION: Anti-vaping public service announcements (PSAs) are intended to discourage vaping or use of electronic nicotine delivery systems (ENDS). However, vaping portrayals in PSAs may have unintended effects if they increase smoking or vaping urges. This study examined benefits and unintended effects of anti-vaping PSAs with vapor portrayals on smoking and vaping-related outcomes. METHODS: Young adult smokers (N = 171) and dual users (N = 122) aged 21-30 years were randomly assigned to view: 1) anti-vaping PSAs with vapor; 2) anti-vaping PSAs without vapor; 3) physical activity PSAs; or 4) anti-smoking PSAs with smoking cues...
May 16, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29793186/excess-sludge-disruption-and-pollutant-removal-from-tannery-effluent-by-upgraded-activated-sludge-system
#12
Vijay Sodhi, Ajay Bansal, Mithilesh Kumar Jha
This study proposed a maintenance metabolism based upgraded activated sludge as MANODOX system that restricts excess biosludge generation from high strength real tannery effluent. The MANODOX experimental demonstration has been done using a sequenced operational arrangement of a MBBR, anaerobic digester, and oxidation ditch connected to CAS reactor, discussed in detail manner. Experimental trends revealed a prominently lower sludge yield upto 0.271 gVSS/gCOD (72% overall sludge reduction) that corresponds to parallel run CAS (0...
April 30, 2018: Bioresource Technology
https://www.readbyqxmd.com/read/29793185/production-of-biogas-methane-and-hydrogen-from-anaerobic-digestion-of-hemicellulosic-hydrolysate-generated-in-the-oxidative-pretreatment-of-coffee-husks
#13
Lívia Caroline Dos Santos, Oscar Fernando Herrera Adarme, Bruno Eduardo Lobo Baêta, Leandro Vinícius Alves Gurgel, Sérgio Francisco de Aquino
Ozone pretreatment of coffee husks (CH) was evaluated to generate hydrolysates for biogas production and to preserve cellulose of the solid phase for 2G ethanol production. Pretreatment variables included liquid-to-solid ratio (LSR), pH and specific applied ozone load (SAOL). Considering single-stage anaerobic digestion (AD), the highest methane production (36 NmL CH4 /g CH) was achieved with the hydrolysate generated in the experiment using LSR 10 mL/g, pH 11 and SAOL 18.5 mg O3 /g CH, leading to 0...
May 21, 2018: Bioresource Technology
https://www.readbyqxmd.com/read/29793180/insulin-is-a-potential-antioxidant-for-diabetes-associated-cognitive-decline-via-regulating-nrf2-dependent-antioxidant-enzymes
#14
Ying Song, Wei Ding, Yun Bei, Yan Xiao, Hai-Da Tong, Li-Bo Wang, Li-Yao Ai
PURPOSE: To investigate the neuroprotective effects of insulin on diabetic encephalopathy and its mechanism. EXPERIMENTAL AND APPROACH: The diabetic model was established by injection of streptozotocin. Behavior examinations were conducted by the Morris water maze. Histopathological alterations were detected by HE staining. ROS, CAT levels and SOD activity were measured using a microplate reader. In vitro, the viability of wild type and knock-down PC12 cells was detected by MTT assay, the morphology of cells was monitored under a microscope...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793179/nano-strategies-for-berberine-delivery-a-natural-alkaloid-of-berberis
#15
REVIEW
Elaheh Mirhadi, Mehdi Rezaee, Bizhan Malaekeh-Nikouei
Berberine, as a phytochemical component of some medicinal Chinese herbs (most frequently Berberis vulgaris), is an isoquinoline alkaloid with many therapeutic effects including anti-viral, anti-microbial, anti-diarrhea, anti-inflammatory and anti-tumor effects. Berberine has some significant effects on type 2 diabetes through adenosine monophosphate-activated protein kinase activation, glycolysis stimulation, and mitochondrial function inhibition which subsequently improves both lipid and glucose metabolism...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793178/nrf2-p-glycoprotein-axis-is-associated-with-clinicopathological-characteristics-in-colorectal-cancer
#16
Mohammad Reza Sadeghi, Farhad Jeddi, Narges Soozangar, Mohammad Hossein Somi, Masoud Shirmohamadi, Vahid Khaze, Nasser Samadi
Colorectal cancer (CRC) is the fourth leading cause of cancer-related death worldwide. Activation of ABCB1 gene and its main product, P-glycoprotein, is the common reason for chemoresistance. The nuclear factor-erythroid 2-related factor2 (Nrf2) is directly regulated by Kelch like ECH-associated protein1 (Keap1). In addition, Nrf2 is a key transcriptional factor that regulates efflux transporters, including P-gp. The aim of this study was to investigate the expression levels of Nrf2, Keap1 and ABCB1 in the biopsy samples and their association with clinicopathological features in CRC patients...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793177/long-noncoding-rna-gas5-suppresses-triple-negative-breast-cancer-progression-through-inhibition-of-proliferation-and-invasion-by-competitively-binding-mir-196a-5p
#17
Shuqin Li, Jun Zhou, Zhaoxin Wang, Peishun Wang, Xitao Gao, Yan Wang
Triple-negative breast cancer (TNBC) is considered to be the most aggressive and lethal type of breast cancer. Many studies have suggested that the dysfunction of long noncoding RNAs (lncRNAs) is correlated with breast cancer metastasis and progression. Here, we show that levels of the lncRNA, growth arrest-specific transcript 5 (GAS5), are decreased in TNBC tissues, and this down-regulation of GAS5 is associated with an aggressive tumor phenotype in patients, affecting clinical stage, lymph node metastasis and overall survival...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793176/non-ldl-dyslipidemia-is-prevalent-in-the-young-and-determined-by-lifestyle-factors-and-age-the-lifelines-cohort
#18
Jeroen K de Vries, Jan W Balder, Michelle J Pena, Petra Denig, Andries J Smit
BACKGROUND AND AIMS: Non-LDL dyslipidemia (NLD) confers cardiovascular risk, and prevalence rates appear to be high in elderly populations. Small cohorts have identified several lifestyle, anthropometric, and medical factors associated with NLD. We aimed to assess sex- and age-specific prevalence of NLD in a contemporary population cohort (n = 167 729), and to identify independent determinants of NLD, focusing on lifestyle, anthropometric, and medical factors. METHODS: The prevalence of NLD was assessed per 10-year age intervals in adults without cardiovascular disease not using lipid-modifying drugs from the Dutch LifeLines cohort...
May 21, 2018: Atherosclerosis
https://www.readbyqxmd.com/read/29793173/ag-nanoparticles-loading-of-polypyrrole-coated-superwetting-mesh-for-on-demand-separation-of-oil-water-mixtures-and-catalytic-reduction-of-aromatic-dyes
#19
Sun Yihan, Liu Mingming, Zhiguang Guo
Herein, a catalytic mesh with unique wettability, high oil-water separation efficiency and excellent catalytic performance towards aromatic dyes was fabricated. Polypyrrole (PPy) was firstly pre-coated on pristine stainless-steel mesh (SSM) surface via cyclic voltammetry approach. Subsequently, a simple electrodeposition process was performed to prepare and anchor Ag nanoparticles (AgNPs) onto the PPy-coated SSM surface. The PPy-coated mesh with anchored AgNPs was denoted as PPy/AgNPs-coated SSM. The obtained PPy/AgNPs-coated SSM exhibited dual superlyophobic properties and were able to achieve on-demand separation to deal with various of light oil (ρoil  < ρwater ) and heavy oil (ρoil  > ρwater )-water mixtures...
May 19, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29793172/on-the-autonomous-motion-of-active-drops-or-bubbles
#20
Yuri S Ryazantsev, Manuel G Velarde, Eduardo Guzman, Ramón G Rubio, Francisco Ortega, Juan-Jose Montoya
Thermo-capillary stresses on the surface of a drop can be the result of a non-isothermal surface chemical conversion of a reactant dissolved in the host fluid. The strength of heat production (with e.g. absorption) on the surface is ruled by the diffusion of the reactant and depends on the state of motion of the drop. Such thermo-capillary stresses can provoke the motion of the drop or its motionless state in the presence of an external body force. If in the balance of forces, including indeed viscous drag, the net resultant force vanishes there is the possibility of autonomous motion with constant velocity of the drop...
May 19, 2018: Journal of Colloid and Interface Science
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