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https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#1
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/29793153/effects-of-mg-2-on-recovery-of-nmda-receptors-from-inhibition-by-memantine-and-ketamine-reveal-properties-of-a-second-site
#2
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/29793152/identification-of-seven-polyamine-oxidase-genes-in-tomato-solanum-lycopersicum-l-and-their-expression-profiles-under-physiological-and-various-stress-conditions
#3
Yanwei Hao, Binbin Huang, Dongyu Jia, Taylor Mann, Xinyi Jiang, Yuxing Qiu, Masaru Niitsu, Thomas Berberich, Tomonobu Kusano, Taibo Liu
Polyamines (PAs) are implicated in developmental processes and stress responses of plants. Polyamine oxidases (PAOs), flavin adenine dinucleotide-dependent enzymes that function in PA catabolism, play a critical role. Even though PAO gene families of Arabidopsis and rice have been intensely characterized and their expression in response to developmental and environmental changes has been investigated, little is known about PAOs in tomato (Solanum lycopersicum). We found seven PAO genes in S. lycopersicum and named them SlPAO1∼7...
May 15, 2018: Journal of Plant Physiology
https://www.readbyqxmd.com/read/29793121/head-coaches-attitudes-towards-injury-prevention-and-use-of-related-methods-in-professional-basketball-a-survey
#4
J Wilke, D Niederer, L Vogt, W Banzer
OBJECTIVES: To investigate the practices and attitudes of professional basketball head coaches towards injury prevention. DESIGN: Survey. SETTING: Elite-level basketball. PARTICIPANTS: Head coaches of all 366 German professional teams. MAIN OUTCOME MEASURES: Use of injury risk screening methods, rated importance of different musculoskeletal injuries and rated effectiveness of preventive interventions...
April 17, 2018: Physical Therapy in Sport
https://www.readbyqxmd.com/read/29793103/disruption-of-the-gonadal-endocannabinoid-system-in-zebrafish-exposed-to-diisononyl-phthalate
#5
Isabel Forner-Piquer, Stefania Santangeli, Francesca Maradonna, Alessandro Rabbito, Fabiana Piscitelli, Hamid R Habibi, Vincenzo Di Marzo, Oliana Carnevali
DiNP (Di-isononyl phthalate) has been recently introduced as DEHP (Bis (2-ethylhexyl) phthalate) substitute and due to its chemical properties, DiNP is commonly used in a large variety of plastic items. The endocannabinoid system (ECS) is a lipid signaling system involved in a plethora of physiological pathways including the control of the reproductive and metabolic processes. In this study, the effects of DiNP on the ECS of zebrafish (male and female) gonads were analyzed. Adult zebrafish were chronically exposed for 21 days via water to 3 environmentally relevant concentrations of DiNP (42 μg/L; 4...
May 21, 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29793062/functional-mri-of-brain-physiology-in-aging-and-neurodegenerative-diseases
#6
J Jean Chen
Brain aging and associated neurodegeneration constitute a major societal challenge as well as one for the neuroimaging community. A full understanding of the physiological mechanisms underlying neurodegeneration still eludes medical researchers, fuelling the development of in vivo neuroimaging markers. Hence it is increasingly recognized that our understanding of neurodegenerative processes likely will depend upon the available information provided by imaging techniques. At the same time, the imaging techniques are often developed in response to the desire to observe certain physiological processes...
May 21, 2018: NeuroImage
https://www.readbyqxmd.com/read/29793032/phosphorylated-and-non-phosphorylated-hck-kinase-domains-produced-by-cell-free-protein-expression
#7
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/29793028/cytosolic-distributions-of-highly-toxic-metals-cd-and-tl-and-several-essential-elements-in-the-liver-of-brown-trout-salmo-trutta-l-analyzed-by-size-exclusion-chromatography-and-inductively-coupled-plasma-mass-spectrometry
#8
Zrinka Dragun, Nesrete Krasnići, Nicol Kolar, Vlatka Filipović Marijić, Dušica Ivanković, Marijana Erk
Cytosolic distributions of nonessential metals Cd and Tl and seven essential elements among compounds of different molecular masses were studied in the liver of brown trout (Salmo trutta) from the karstic Krka River in Croatia. Analyses were done by size exclusion high performance liquid chromatography and high resolution inductively coupled plasma mass spectrometry. Common feature of Cd and Tl, as highly toxic elements, was their distribution within only two narrow peaks. The increase of cytosolic Cd concentrations was reflected in marked increase of Cd elution within low molecular mass peak (maximum at ∼15 kDa), presumably containing metallothioneins (MTs), which indicated successful Cd detoxification in brown trout liver under studied exposure conditions...
May 15, 2018: Chemosphere
https://www.readbyqxmd.com/read/29793002/rasch-analysis-suggested-that-items-from-the-template-for-intervention-description-and-replication-tidier-checklist-can-be-summed-to-create-a-score
#9
Tie P Yamato, Chris G Maher, Bruno T Saragiotto, Mark J Catley, Anne M Moseley
OBJECTIVE: The aim of this study was to construct and evaluate a summary score of reporting completeness based on the Template for Intervention Description and Replication (TIDieR). STUDY DESIGN AND SETTING: We included 200 reports published in 2013 randomly selected from the Physiotherapy Evidence Database (PEDro). We summed the scores for the 12 items for the intervention and control groups for each trial in order to create a summary score from 0 to 24. Rasch analysis was used to investigate the item hierarchy, category function and reliability of the TIDieR checklist and determine the extent to which the summary score can be considered an interval-level measure...
May 21, 2018: Journal of Clinical Epidemiology
https://www.readbyqxmd.com/read/29792949/srnaome-and-transcriptome-analysis-provide-insight-into-chilling-response-of-cowpea-pods
#10
Jinhua Zuo, Yunxiang Wang, Benzhong Zhu, Yunbo Luo, Qing Wang, Lipu Gao
Cowpea is an important horticultural crop in tropical and subtropical areas of Asia, Africa, and Latin America, as well as parts of southern Europe and Central and South America. Chilling injury is a common physiological hazard of cowpea in cold chain logistics which reduce the cowpea pod's nutritional quality and product value. However, the molecular mechanism involved in chilling injury remains unclear in cowpea pods. RNA-Seq and sRNA-Seq technologies were employed to decipher the miRNAs and mRNAs expression profiles and their regulatory networks in cowpea pods involved in chilling stress...
May 21, 2018: Gene
https://www.readbyqxmd.com/read/29792944/enrichment-of-low-density-symbiont-dna-from-minute-insects
#11
Corinne M Stouthamer, Suzanne Kelly, Martha S Hunter
Symbioses between bacteria and insects are often associated with changes in important biological traits that can significantly affect host fitness. To a large extent, studies of these interactions have been based on physiological changes or induced phenotypes in the host, and the genetic mechanisms by which symbionts interact with their hosts have only recently become better understood. Learning about symbionts has been challenging in part due to difficulties such as obtaining enough high quality genomic material for high throughput sequencing technology, especially for symbionts present in low titers, and in small or difficult to rear non-model hosts...
May 21, 2018: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/29792940/a-randomized-control-trial-to-determine-the-effectiveness-and-physiological-effects-of-spinal-manipulation-and-spinal-mobilization-compared-to-each-other-and-a-sham-condition-in-patients-with-chronic-low-back-pain-study-protocol-for-the-relief-study
#12
Brian C Clark, David W Russ, Masato Nakazawa, Christopher R France, Stevan Walkowski, Timothy D Law, Megan Applegate, Niladri Mahato, Samuel Lietkam, James Odenthal, Daniel Corcos, Simeon Hain, Betty Sindelar, Robert J Ploutz-Snyder, James S Thomas
BACKGROUND: Low back pain (LBP) is one of the most common reasons for seeking medical care. Manipulative therapies are a common treatment for LBP. Few studies have compared the effectiveness of different types of manipulative therapies. Moreover, the physiologic mechanisms underlying these treatments are not fully understood. Herein, we present the study protocol for The Researching the Effectiveness of Lumbar Interventions for Enhancing Function Study (The RELIEF Study). METHODS AND STUDY DESIGN: The RELIEF Study is a Phase II RCT with a nested mechanistic design...
May 21, 2018: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29792923/high-throughput-sequencing-identifies-chilling-responsive-genes-in-sweetpotato-ipomoea-batatas-lam-during-storage
#13
Zeyi Xie, Zhilin Zhou, Hongmin Li, Jingjing Yu, Jiaojiao Jiang, Zhonghou Tang, Daifu Ma, Baohong Zhang, Yonghua Han, Zongyun Li
Sweetpotato (Ipomoea batatas L.) is a globally important economic food crop. It belongs to Convolvulaceae family and origins in the tropics; however, sweetpotato is sensitive to cold stress during storage. In this study, we performed transcriptome sequencing to investigate the sweetpotato response to chilling stress during storage. A total of 110,110 unigenes were generated via high-throughput sequencing. Differentially expressed genes (DEGs) analysis showed that 18,681 genes were up-regulated and 21,983 genes were down-regulated in low temperature condition...
May 21, 2018: Genomics
https://www.readbyqxmd.com/read/29792856/comparison-of-the-3-d-patterns-of-the-parasympathetic-nervous-system-in-the-lung-at-late-developmental-stages-between-mouse-and-chicken
#14
Tadayoshi Watanabe, Ryo Nakamura, Yuta Takase, Etsuo A Susaki, Hiroki R Ueda, Ryosuke Tadokoro, Yoshiko Takahashi
Although the basic schema of the body plan is similar among different species of amniotes (mammals, birds, and reptiles), the lung is an exception. Here, anatomy and physiology are considerably different, particularly between mammals and birds. In mammals, inhaled and exhaled airs mix in the airways, whereas in birds the inspired air flows unidirectionally without mixing with the expired air. This bird-specific respiration system is enabled by the complex tubular structures called parabronchi where gas exchange takes place, and also by the bellow-like air sacs appended to the main part of the lung...
May 21, 2018: Developmental Biology
https://www.readbyqxmd.com/read/29792855/the-versatile-hippo-pathway-in-oral-maxillofacial-development-and-bone-remodeling
#15
REVIEW
Lin Xiang, Hui Yu, Xinyuan Zhang, Bin Wang, Ying Yuan, Qin Zhang, Rui Ye, Ping Gong, Yingying Wu
The Hipposignaling pathway is implicated in key aspects of cell proliferation, control of organ size, stem cell functions and tumor suppression. Its functions are primarily mediated either through direct effects on transcription factors to influence target gene expression or through crosstalk with other signaling pathways that regulate multiple physiological activities. Studies are revealing Hippo pathway involvement in diverse functions including renewal of intestinal epithelium, promotion of myocardial cell proliferation, cancer suppression, etc...
May 21, 2018: Developmental Biology
https://www.readbyqxmd.com/read/29792723/-experimental-promotion-of-liver-regeneration-after-portal-vein-branch-ligation
#16
V Liška, V Třeška, H Mírka, O Vyčítal, J Brůha, L Haidingerová, J Beneš, Z Tonar, R Pálek, J Rosendorf
INTRODUCTION: Portal vein embolization or ligation (PVE/PVL) is part of most multi-stage liver procedures in the case of low future liver remnant volume (FLRV). PVE initiates compensatory hypertrophy of non-occluded liver parenchyma. This hypertrophy is stimulated by an increased volume of portal blood in the non-occluded veins. PVE results in adequate FLRV growth necessary for resection only in 63-96% patients. The aim of this publication is to summarize the possibilities of influencing liver regeneration after PVE/PVL in an experiment using cytokines (TNF-α, IL-6), a monoclonal antibody against TGF-β1 (MAB TGF-β1) and mesenchymal stem cells (MSC)...
2018: Rozhledy V Chirurgii: Měsíčník Československé Chirurgické Společnosti
https://www.readbyqxmd.com/read/29792708/nonalcoholic-fatty-liver-disease-and-diabetes-is-associated-with-decreased-cyp3a4-protein-expression-and-activity-in-human-liver
#17
Rohitash Jamwal, Suzanne M de la Monte, Ken Ogasawara, Sravani Adusumalli, Benjamin B Barlock, Fatemeh Akhlaghi
Nonalcoholic fatty liver disease (NAFLD) is a major cause of chronic liver disease in Western population. We investigated the effect of nonalcoholic fatty liver disease (NAFLD) and diabetes mellitus on CYP3A4 activity in human liver tissue from brain dead donors (N=74). Histopathologically graded livers were grouped into normal (n=24), nonalcoholic fatty liver (NAFL, n=26) and nonalcoholic steatohepatitis (NASH, n=24) categories. The rate of conversion of midazolam to its 1-hydroxy metabolite was used to assess in vitro CYP3A4 activity in human liver microsomes (HLM)...
May 24, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29792682/calix-4-arene-based-redox-sensitive-molecular-probe-for-sers-guided-recognition-of-labile-iron-pool-in-tumor-cells
#18
Padincharapad Sreedevi, Jyothi B Nair, Preethanuj Preethalayam, Benadicta S Jeeja, Cherumuttathu H Suresh, Kaustabh Kumar Maiti, Ramavarma Luxmi Varma
Targeting the intracellular 'labile' iron pool is turned as a key modulator for cancer progression since the former is responsible for several pathological processes in tumor cells. Herein, we report a non- fluorescent calix[4]arene based triazole appended molecular probe (PTBC) for redox-specific detection of Fe3+ under physiological condition by UV-vis, FT-IR, 1H NMR, HR-MS spectroscopies, ITC and the binding strategy between Calix[4]arene and Fe3+ was modeled by DFT calculations. As a new insight PTBC probe showed significant Raman fingerprint through surface enhanced Raman scattering (SERS) modality revealing the ultrasensitive detection of Fe3+ with a LOD of 2 nM...
May 24, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29792570/a-model-for-predicting-the-risk-of-musculoskeletal-disorders-among-computer-professionals
#19
Vishnu Sasikumar, Second Champakkadayil Abdul Basheer Binoosh
OBJECTIVE: The objective of this study was to develop a model for predicting the risk of musculoskeletal disorders among computer professionals. MATERIALS AND METHODS: A preliminary study with a modified Nordic musculoskeletal questionnaire was conducted to identify the risk in different body parts of the professionals during their work. A discrete postural evaluation of the dynamic postures involved in the work was assessed using rapid upper limb assessment. The postural, physiological and work-related factors were considered as the attributes of the model...
May 24, 2018: International Journal of Occupational Safety and Ergonomics: JOSE
https://www.readbyqxmd.com/read/29792553/mitochondrial-complex-i-defect-resulting-from-exercise-induced-lower-limb-ischemia-in-patients-with-peripheral-arterial-disease
#20
Isabelle Signolet, Pierre Abraham, Stéphanie Chupin, Myriam Ammi, Naïg Gueguen, Franck Letournel, Jean Picquet, Christophe Baufreton, Mickael Daligault, Vincent Procaccio, Pascal Reynier, Samir Henni
OBJECTIVE: This study aims to compare the structural and mitochondrial alterations between muscle segments affected by exercise-induced ischemia and segments of the same muscle without ischemia, in the same subject. METHODS: In a prospective analysis, 34 patients presenting either peripheral arterial disease or chronic coronary syndrome without any evidence of peripheral arterial disease were eligible for inclusion based on findings indicating a need for either a femoro-popliteal bypass or a saphenous harvesting for coronary bypass...
May 24, 2018: Journal of Applied Physiology
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