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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/29793195/alcohol-and-drugs-use-among-drivers-injured-in-road-accidents-in-campania-italy-a-8-years-retrospective-analysis
#3
Anna Carfora, Carlo Pietro Campobasso, Paola Cassandro, Raffaella Petrella, Renata Borriello
A recent update of the Italian Road Traffic Law (RTL 41/2016), established severe penal sanctions when drivers, driving under the influence of alcohol (DUI) or drugs (DUID), are involved in road accident that results in death or injuries. A study was carried out to assess the trends of consumption of alcohol, illicit drugs or pharmaceutical among injured drivers suspected for DUI or DUID from 2009 to 2016 in the region of Campania (Italy). Confirmation toxicological analyses were performed on 780 blood samples and 1017 urine samples collected from 1797 injured drivers...
May 9, 2018: Forensic Science International
https://www.readbyqxmd.com/read/29793190/comparative-hazards-of-acute-myocardial-infarction-among-hospitalized-patients-with-methamphetamine-or-cocaine-use-disorders-a-retrospective-cohort-study
#4
Russell C Callaghan, Montana Halliday, Jodi Gatley, Jenna Sykes, Lawren Taylor, Claire Benny, Stephen J Kish
BACKGROUND: It is assumed that recreational use of methamphetamine can trigger acute myocardial infarction (AMI) events, but estimates of longitudinal hazards of AMI among methamphetamine users are lacking. METHODS: Retrospective cohort study: Competing-risks analysis was used to estimate time-to-AMI patterns in methamphetamine versus matched appendicitis (population-proxy) and matched cocaine (drug-control) groups. Cohorts were propensity-score-matched using demographic and clinical variables...
April 26, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29793176/non-ldl-dyslipidemia-is-prevalent-in-the-young-and-determined-by-lifestyle-factors-and-age-the-lifelines-cohort
#5
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/29793153/effects-of-mg-2-on-recovery-of-nmda-receptors-from-inhibition-by-memantine-and-ketamine-reveal-properties-of-a-second-site
#6
Nathan G Glasgow, Madeleine R Wilcox, Jon W Johnson
Memantine and ketamine are NMDA receptor (NMDAR) open channel blockers that are thought to act via similar mechanisms at NMDARs, but exhibit divergent clinical effects. Both drugs act by entering open NMDARs and binding at a site deep within the ion channel (the deep site) at which the endogenous NMDAR channel blocker Mg2+ also binds. Under physiological conditions, Mg2+ increases the IC50 s of memantine and ketamine through competition for binding at the deep site. Memantine also can inhibit NMDARs after associating with a second site accessible in the absence of agonist, a process termed second site inhibition (SSI) that is not observed with ketamine...
May 12, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29793150/exploring-the-victimization%C3%A2-early-substance-misuse-relationship-in-search-of-moderating-and-mediating-effects
#7
Glenn D Walters, Dorothy L Espelage
This study was designed to address two research questions. The first research question asked whether physical abuse victimization at the hands of parents/guardians, bullying victimization at the hands of peers, and the abuse x bullying interaction encouraged early involvement in substance misuse. The second research question inquired as to whether the victimization‒substance misuse relationship was mediated by variables proposed by various theories and research studies-specifically, cognitive impulsivity, negative affect, and low self-esteem...
May 21, 2018: Child Abuse & Neglect
https://www.readbyqxmd.com/read/29793142/synthesis-of-aryl-pyrazole-via-suzuki-coupling-reaction-in-vitro-mushroom-tyrosinase-enzyme-inhibition-assay-and-in-silico-comparative-molecular-docking-analysis-with-kojic-acid
#8
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Bakhtawar Batool, Saima Kalsoom, M M Hasan, Mauricio F Erben, Hesham R El-Seedi, Musrat Ali, Zaman Ashraf
Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50  = 1.568 ± 0.01 µM) showed relatively better potential compared to reference kojic acid (IC50  = 16...
April 30, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793128/convolutional-neural-networks-for-seizure-prediction-using-intracranial-and-scalp-electroencephalogram
#9
Nhan Duy Truong, Anh Duy Nguyen, Levin Kuhlmann, Mohammad Reza Bonyadi, Jiawei Yang, Samuel Ippolito, Omid Kavehei
Seizure prediction has attracted growing attention as one of the most challenging predictive data analysis efforts to improve the life of patients with drug-resistant epilepsy and tonic seizures. Many outstanding studies have reported great results in providing sensible indirect (warning systems) or direct (interactive neural stimulation) control over refractory seizures, some of which achieved high performance. However, to achieve high sensitivity and a low false prediction rate, many of these studies relied on handcraft feature extraction and/or tailored feature extraction, which is performed for each patient independently...
May 7, 2018: Neural Networks: the Official Journal of the International Neural Network Society
https://www.readbyqxmd.com/read/29793094/effects-of-chronic-antipsychotic-drug-exposure-on-the-expression-of-translocator-protein-and-inflammatory-markers-in-rat-adipose-tissue
#10
Anita Calevro, Marie-Caroline Cotel, Sridhar Natesan, Michel Modo, Anthony C Vernon, Valeria Mondelli
The precise effect of antipsychotic drugs on either central or peripheral inflammation remains unclear. An important issue in this debate is to what extent the known peripheral metabolic effects of antipsychotics, including increased adiposity, may contribute to increased inflammation. Adipose tissue is known to contribute to the development of systemic inflammation, which can eventually lead to insulin resistance and metabolic dysregulation. As a first step to address this question, we evaluated whether chronic exposure to clinically comparable doses of haloperidol or olanzapine resulted in the immune activation of rat adipose tissue...
May 16, 2018: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29793092/a-combined-ftir-and-dsc-study-on-the-bilayer-stabilising-effect-of-electrostatic-interactions-in-ion-paired-lipids
#11
Maximilian Schmid, Christian Wölk, Julia Giselbrecht, K L Andrew Chan, Richard D Harvey
Investigating lipid ion pair formation is important for understanding the mechanisms of lipid-mediated drug resistance in bacteria. In this study we have used the charged amphiphiles dipalmitoylphosphatidylglycerol (DPPG) and dihexadecyldimethylammonium bromide (DHDAB), as a model to evaluate the formation of ion pairs by a combined Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) analysis. FTIR was employed to study the environment of the DPPC headgroup phosphate and lipid/surfactant alkane chains, in vesicles formed by the two amphiphiles mixed in various molar ratios...
May 17, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29793073/bubble-generating-polymersomes-loaded-with-both-indocyanine-green-and-doxorubicin-for-effective-chemotherapy-combined-with-photothermal-therapy
#12
Dunwan Zhu, Fan Fan, Chenlu Huang, Zhiming Zhang, Yu Qin, Li Lu, Hai Wang, Xu Jin, Hanxue Zhao, Hu Yang, Chao Zhang, Jun Yang, Zhipeng Liu, Hongfan Sun, Xigang Leng, Deling Kong, Linhua Zhang
The combination of chemotherapy and photothermaltherapy (PTT) via stimuli-responsive nanovesicles has great potential in tumor treatment. In the present study, bubble-generating polymersomes, which can generate bubbles in response to low pH or hyperthermia, were fabricated to simultaneously encapsulate chemotherapeutic drug and photosensitizing agent for the synergistic chemo-photothermal tumor therapy. Photosensitizer indocyanine green (ICG) was encapsulated into the bilayer of polymersomes formed by amphiphilic triblock copolymer PCL8000 -PEG8000 -PCL8000 through thin film re-hydration method, while chemotherapeutic doxorubicin (DOX) was loaded into the hydrophilic lumen using a transmembrane ammonium bicarbonate gradient loading procedure...
May 21, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29793059/longitudinal-surveillance-of-drug-resistance-in-plasmodium-falciparum-isolates-from-the-china-myanmar-border-reveals-persistent-circulation-of-multidrug-resistant-parasites
#13
Yao Bai, Jiaqi Zhang, Jinting Geng, Shiling Xu, Shuang Deng, Weilin Zeng, Zenglei Wang, Huguette Gaelle Ngassa Mbenda, Jie Zhang, Na Li, Yanrui Wu, Cuiying Li, Huae Liu, Yonghua Ruan, Yaming Cao, Zhaoqing Yang, Liwang Cui
Multidrug-resistant Plasmodium falciparum in the Greater Mekong Subregion of Southeast Asia is a major threat to malaria elimination and requires close surveillance. In this study, we collected 107 longitudinal clinical samples of P. falciparum in 2007-2012 from the malaria hypoendemic region of the China-Myanmar border and measured their in vitro susceptibilities to 10 antimalarial drugs. Overall, parasites had significantly different IC50 values to all the drugs tested as compared to the reference 3D7 strain...
May 21, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29793058/the-transcription-factor-skn-1-and-detoxification-gene-ugt-22-alter-albendazole-efficacy-in-caenorhabditis-elegans
#14
Pauline Fontaine, Keith Choe
Parasitic nematodes infect over 1/4 th of the human population and are a major burden on livestock and crop production. Benzimidazole class anthelmintics are widely used to treat infections, but resistance is a widespread problem. Mutation of genes encoding the benzimidazole target β-tubulin is a well-established mechanism of resistance, but recent evidence suggests that metabolism of the drugs may also occur. Our objective was to investigate contributions of the detoxification-response transcription factor SKN-1 to anthelmintic drug resistance using C...
April 25, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29793051/promising-antileishmanial-activity-of-novel-imidazole-antifungal-drug-luliconazole-against-leishmania-major-in-vitro-and-in-silico-studies
#15
Azar Shokri, Mahdi Abastabar, Masoud Keighobadi, Saeed Emami, Mahdi Fakhar, Saeed Hosseini Teshnizi, Koichi Makimura, Ali Rezaei-Matehkolaei, Hassan Mirzaei
OBJECTIVES: Pentavalent antimonials have been used for the treatment of leishmaniasis for more than 70 years; however their toxicity limits their benefits. Unfortunately, the efficacy of the first line drugs has been decreased and resistance seems to be noticeable. Luliconazole is a new azole with unique effects on fungi which has not been tested on Leishmania parasites yet. METHODS: In the present study, we evaluated cytotoxicity and anti-leishmanial activities of Luliconazole on promastigotes and intracellular amastigotes of Leishmania major (L...
May 21, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29793039/antimicrobial-resistance-in-the-context-of-the-syrian-conflict-drivers-before-and-after-the-onset-of-conflict-and-key-recommendations
#16
REVIEW
Aula Abbara, Timothy M Rawson, Nabil Karah, Wael El-Amin, James Hatcher, Bachir Tajaldin, Osman Dar, Omar Dewachi, Ghassan Abu Sitta, Bernt Eric Uhlin, Annie Sparrow
Current evidence describing antimicrobial resistance (AMR) in the context of the Syrian conflict is of poor quality and sparse in nature. In this paper we explore and report the major drivers of AMR that were present in Syria pre-conflict and those that have emerged since its onset in March 2011. Drivers which existed before the conflict included a lack of enforcement of existing legislation to regulate over the counter antibiotics and notification of communicable diseases. This contributed to a number of drivers of AMR after the onset of conflict which were also compounded by the exodus of trained staff, the increase in overcrowding and unsanitary conditions, the increase in injuries and economic sanctions limiting the availability of required laboratory medical materials and equipment...
May 21, 2018: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/29793038/therapeutic-drug-monitoring-and-safety-of-voriconazole-therapy-in-patients-with-child-pugh-class-b-and-c-cirrhosis-a-multicenter-study
#17
Taotao Wang, Miao Yan, Dan Tang, Ling Xue, Tao Zhang, Yuzhu Dong, Li Zhu, Xinggang Wang, Yalin Dong
OBJECTIVES: The purpose of this study was to investigate the pharmacokinetic profile and safety of voriconazole treatment in patients with Child-Pugh class B and C cirrhosis. METHODS: Liver cirrhosis patients receiving recommended voriconazole maintenance dose (group A) and halved maintenance dose (group B) orally or intravenously were involved. Voriconazole-related adverse events (AEs) were defined according to Common Terminology Criteria for Adverse Events. RESULTS: A total of 110 voriconazole Cmin were monitored from 78 patients...
May 21, 2018: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/29793032/phosphorylated-and-non-phosphorylated-hck-kinase-domains-produced-by-cell-free-protein-expression
#18
Kazushige Katsura, Yuri Tomabechi, Takayoshi Matsuda, Mayumi Yonemochi, Junko Mikuni, Noboru Ohsawa, Takaho Terada, Shigeyuki Yokoyama, Mutsuko Kukimoto-Niino, Chie Takemoto, Mikako Shirouzu
Since phosphorylation is involved in various physiological events, kinases and interacting factors can be potential targets for drug discovery. For the development and improvement of inhibitors from the point of view of mechanistic enzymology, a cell-free protein synthesis system would be advantageous, since it could prepare mutant proteins easily. However, especially in the case of protein kinase, product solubility remains one of the major challenges. To overcome this problem, we prepared a chaperone-supplemented extract from Escherichia coli BL21 cells harboring a plasmid encoding a set of chaperone genes, dnaK, dnaJ, and grpE...
May 21, 2018: Protein Expression and Purification
https://www.readbyqxmd.com/read/29793000/effect-of-a-bisphosphonate-and-selective-estrogen-receptor-modulator-on-bone-remodeling-in-streptozotocin-induced-diabetes-and-ovariectomized-rat-model
#19
Young-Seok Lee, Rishab Gupta, Jeong-Taik Kwon, Dae-Chul Cho, Ye Jin Seo, Sung Young Seu, Eui Kyun Park, Inbo Han, Chi-Heon Kim, Joo-Kyung Sung, Kyoung-Tae Kim
BACKGROUND CONTEXT: Diabetes and menopause can cause severe osteoporosis. In general, menopause and diabetes can lead to an imbalance in bone turnover, which results in secondary osteoporosis. However, the efficacy of antiresorptive drugs against this form of osteoporosis has not been extensively evaluated. OBJECTIVE: The aim of this study was to determine the changes in vertebral bone remodeling when postmenopausal osteoporosis is accompanied by diabetes and the efficacy of bisphosphonates and selective estrogen-receptor modulators (SERMs) against these outcomes...
May 21, 2018: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/29792988/towards-quantitative-prediction-of-the-performance-of-dry-powder-inhalers-by-multi-scale-simulations-and-experiments
#20
Duy Nguyen, Johan Remmelgas, Ingela Niklasson Björn, Berend van Wachem, Kyrre Thalberg
This work demonstrates the use of multi-scale simulations coupled with experiments to build a quantitative prediction tool for the performance of adhesive mixtures in a dry powder inhaler (DPI). Using discrete element model (DEM), the behaviour of fine-carrier particle assemblies upon different mechanisms encountered during dose entrainment and dispersion can be described at the individual particle level. Combining these results with computational fluid dynamics (CFD) simulations, the complete dosing event from a DPI can be captured and key performance measures can be extracted...
May 21, 2018: International Journal of Pharmaceutics
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