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Human exertion testing

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https://www.readbyqxmd.com/read/28325154/the-behavioral-profile-of-methylenedioxypyrovalerone-mdpv-and-%C3%AE-pyrrolidinopentiophenone-pvp-a-systematic-review
#1
Cornel N Stanciu, Thomas M Penders, Samantha A Gnanasegaram, Elvin Pirapakaran, Juvraj S Padda, Jeeven S Padda
BACKGROUND: New psychoactive substances are emerging at an alarming rate. With novel structures and properties they produce unique behavioral characteristics during intoxication. Synthetic cathinones are some of the most common. More and more are presenting to emergency departments due to consequences of use. Aside from isolated reports, little is known about these compounds. OBJECTIVE: Here we review literature pertaining to two common synthetic cathinones, MDPV and alphaPVP, and correlate clinically with guidance on management of intoxications...
March 21, 2017: Current Drug Abuse Reviews
https://www.readbyqxmd.com/read/28303774/physiological-evaluation-of-personal-protective-ensembles-recommended-for-use-in-west-africa
#2
Aitor Coca, Tyler Quinn, Jung-Hyun Kim, Tianzhou Wu, Jeff Powell, Raymond Roberge, Ronald Shaffer
OBJECTIVE: Personal protective equipment (PPE) provides health care workers with a barrier to prevent human contact with viruses like Ebola and potential transmission of the disease. However, PPE can also introduce an additional physiological burden from potentially increased heat stress. This study evaluated the human physiological and subjective responses to continuous light exercise within environmental conditions similar to those in West Africa while wearing 3 different, commonly used PPE ensembles (E1, E2, and E3)...
March 17, 2017: Disaster Medicine and Public Health Preparedness
https://www.readbyqxmd.com/read/28300789/anti-cancer-activity-of-resveratrol-and-derivatives-produced-by-grapevine-cell-suspensions-in-a-14-l-stirred-bioreactor
#3
Laetitia Nivelle, Jane Hubert, Eric Courot, Philippe Jeandet, Aziz Aziz, Jean-Marc Nuzillard, Jean-Hugues Renault, Christophe Clément, Laurent Martiny, Dominique Delmas, Michel Tarpin
In the present study, resveratrol and various oligomeric derivatives were obtained from a 14 L bioreactor culture of elicited grapevine cell suspensions (Vitis labrusca L.). The crude ethyl acetate stilbene extract obtained from the culture medium was fractionated by centrifugal partition chromatography (CPC) using a gradient elution method and the major stilbenes contained in the fractions were subsequently identified by using a (13)C-NMR-based dereplication procedure and further 2D NMR analyses including HSQC, HMBC, and COSY...
March 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28298694/isolation-molecular-characterization-and-screening-of-indigenous-lactobacilli-for-their-abilities-to-produce-bioactive-conjugated-linoleic-acid-cla
#4
Dinesh Kumar Dahiya, Anil Kumar Puniya
Ingestion of conjugated linoleic acid poised many health benefits; however, amount of CLA one can get through generalized diet in is inadequate in exerting the desired benefits. Therefore, presence of CLA producing lactobacilli in dairy fermented foods has a tremendous potential to increase the CLA content. Therefore, present study was focused to isolate and characterize CLA producing lactobacilli from different dairy products and human faeces. Arguably, 283 lactobacilli were isolated from various sources and tested for CLA production...
March 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28277037/fruit-extract-of-the-medicinal-plant-crataegus-oxyacantha-exerts-genotoxic-and-mutagenic-effects-in-cultured-cells
#5
Ana Paula Oliveira de Quadros, Dania Elisa Christofoletti Mazzeo, Maria Aparecida Marin-Morales, Fábio Ferreira Perazzo, Paulo Cesar Pires Rosa, Edson Luis Maistro
Crataegus oxyacantha, a plant of the Rosaceae family also known "English hawthorn, haw, maybush, or whitethorn," has long been used for medicinal purposes such as digestive disorders, hyperlipidemia, dyspnea, inducing diuresis, and preventing kidney stones. However, the predominant use of this plant has been to treat cardiovascular disorders. Due to a lack of studies on the genotoxicity of C. oxyacantha, this investigation was undertaken to determine whether its fruit extract exerts cytotoxic, genotoxic, or clastogenic/aneugenic effects in leukocytes and HepG2 (liver hepatocellular carcinoma) cultured human cells, or mutagenic effects in TA100 and TA98 strains of Salmonella typhimurium bacterium...
February 17, 2017: Journal of Toxicology and Environmental Health. Part A
https://www.readbyqxmd.com/read/28272349/the-influence-of-spirulina-platensis-filtrates-on-caco-2-proliferative-activity-and-expression-of-apoptosis-related-micrornas-and-mrna
#6
Agnieszka Śmieszek, Ewa Giezek, Martyna Chrapiec, Martyna Murat, Aleksandra Mucha, Izabela Michalak, Krzysztof Marycz
Spirulina platensis (SP) is a blue-green microalga that has recently raised attention not only as a nutritional component, but also as a source of bioactivities that have therapeutic effects and may find application in medicine, including cancer treatment. In the present study we determined the cytotoxic effect of S. platensis filtrates (SPF) on human colon cancer cell line Caco-2. Three concentrations of SPF were tested-1.25%, 2.5%, and 5% (v/v). We have found that the highest concentration of SPF exerts the strongest anti-proliferative and pro-apoptotic effect on Caco-2 cultures...
March 7, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28269396/investigation-of-a-passive-capstan-based-grasp-enhancement-feature-in-a-voluntary-closing-prosthetic-terminal-device
#7
Kevin D Gemmell, Michael T Leddy, Joseph T Belter, Aaron M Dollar
Body-powered prosthetic terminal devices fall into two main categories: voluntary-closing devices, which require the user to exert a force to maintain a grasp, and voluntary opening devices, which generally utilize springs to close and maintain a force. As a result, voluntary-closing devices often have a locking feature that allows the user to relax and transport objects while maintaining a firm grip. In this paper, we examine a new type of capstan-based passive brake mechanism in a voluntary-closing prosthetic terminal device...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28267389/molecular-requirements-involving-the-human-platelet-protease-activated-receptor-4-mechanism-of-activation-by-peptide-analogues-of-its-tethered-ligand
#8
I C Moschonas, T F Kellici, T Mavromoustakos, P Stathopoulos, V Tsikaris, V Magafa, A G Tzakos, A D Tselepis
Thrombin is the most potent agonist of human platelets and its effects are primarily mediated through the protease-activated receptors (PARs)-1 and -4. Although PAR-1 has higher affinity for thrombin than PAR-4, both receptors contribute to thrombin-mediated actions on platelets. Recently, a potent and selective PAR-1 antagonist (vorapaxar) was approved for clinical use in selected patients. In contrast, despite the fact that several PAR-4 antagonists have been developed, few of them have been tested in clinical trials...
March 7, 2017: Platelets
https://www.readbyqxmd.com/read/28266800/in-vitro-inhibition-of-human-erythrocyte-hexokinase-by-various-hyperglycemic-drugs
#9
Jalal A Aljamal, Muwaffag Badawneh
Hemolysis is the red blood cell abnormality most often associated with adverse effect of drug therapy. Drug-induced or drug-associated hyperglycemia could decrease the activity of hexokinase. The aim of this study was to investigate the inhibitory effects of some commonly used drugs that have hyperglycemic side effect on the human erythrocyte hexokinase enzyme in vitro. Hexokinase was purified from human erythrocytes using sequential chromatography, with a specific activity of 0.96 ± 0.18 U/g hemoglobin, and assayed in the presence of selected drugs that have hyperglycemic side effect...
March 7, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28264507/chemical-composition-antioxidant-antimicrobial-and-cytotoxic-activities-of-essential-oil-from-premna-microphylla-turczaninow
#10
Han-Yu Zhang, Yang Gao, Peng-Xiang Lai
Premna microphylla Turczaninow, an erect shrub, was widely used in Chinese traditional medicine to treat dysentery, appendicitis, and infections. In this study, the essential oil from P. microphylla Turcz. was obtained by hydrodistillation and analyzed by GC (Gas Chromatography) and GC-MS (Gas Chromatography-Mass Spectrometer). Fifty-six compounds were identified in the oil which comprised about 97.2% of the total composition of the oil. Major components of the oil were blumenol C (49.7%), β-cedrene (6.1%), limonene (3...
February 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28261092/screening-for-small-molecule-inhibitors-of-statin-induced-app-c-terminal-toxic-fragment-production
#11
Karen S Poksay, Douglas J Sheffler, Patricia Spilman, Jesus Campagna, Barbara Jagodzinska, Olivier Descamps, Olivia Gorostiza, Alex Matalis, Michael Mullenix, Dale E Bredesen, Nicholas D P Cosford, Varghese John
Alzheimer's disease (AD) is characterized by neuronal and synaptic loss. One process that could contribute to this loss is the intracellular caspase cleavage of the amyloid precursor protein (APP) resulting in release of the toxic C-terminal 31-amino acid peptide APP-C31 along with the production of APPΔC31, full-length APP minus the C-terminal 31 amino acids. We previously found that a mutation in APP that prevents this caspase cleavage ameliorated synaptic loss and cognitive impairment in a murine AD model...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28258008/high-content-screening-of-clinically-tested-anticancer-drugs-identifies-novel-inhibitors-of-human-mrp1-abcc1
#12
Brian G Peterson, Kee W Tan, Bremansu Osa-Andrews, Surtaj H Iram
Multidrug resistance protein 1 (MRP1/ABCC1), an integral transmembrane efflux transporter, belongs to the ATP-binding cassette (ABC) protein superfamily. MRP1 governs the absorption and disposition of a wide variety of endogenous and xenobiotic substrates including various drugs across organs and physiological barriers. Additionally, its overexpression has been implicated in multidrug resistance in chemotherapy of multiple cancers. Here, we describe the development of a high content imaging-based screening assay for MRP1 activity...
February 28, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28257828/directional-thyroid-hormone-distribution-via-the-blood-stream-to-target-sites
#13
Susanne T Janssen, Onno E Janssen
Thyroid hormones are bound to three major serum transport proteins, thyroxin-binding globulin (TBG), transthyretin (TTR) and human serum albumin (HSA). TBG has the strongest affinity for thyroid hormones, TTR is also found in the cerebrospinal fluid and HSA is the most abundant protein in plasma. Combination defects of either a high affinity TTR or HSA variant do not compensate TBG deficiency, underscoring the dominant role of TBG among the thyroid hormone transport proteins. On the other hand, coexistence of raised affinity TTR and HSA variants causes an augmented hyperthyroxinemia...
February 28, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28257822/characterization-of-6-methoxyflavanone-as-a-novel-anxiolytic-agent-a-behavioral-and-pharmacokinetic-approach
#14
Shehla Akbar, Fazal Subhan, Nasiara Karim, Urooj Aman, Sami Ullah, Muhammad Shahid, Nisar Ahmad, Khwaja Fawad, Robert D E Sewell
Benzodiazepines are regularly prescribed for treatment of anxiety though there are side effects. Flavonoids have selective affinity for GABAA receptors implicated in anxiolytic-like activity in rodents, but are devoid of the unwanted side effects of benzodiazepines. In this study, 6-methoxyflavanone (6-MeOF), a positive allosteric modulator of γ-amino butyric acid (GABA) responses at human recombinant GABAA receptors, was evaluated for its behavioral profile in the elevated plus-maze as well as the staircase- plus and open-field tests in mice...
February 28, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28255555/procalcitonin-impairs-liver-cell-viability-and-function-in-vitro-a-potential-new-mechanism-of-liver-dysfunction-and-failure-during-sepsis
#15
Martin Sauer, Sandra Doß, Johannes Ehler, Thomas Mencke, Nana-Maria Wagner
Purpose. Liver dysfunction and failure are severe complications of sepsis and result in poor outcome and increased mortality. The underlying pathologic mechanisms of hepatocyte dysfunction and necrosis during sepsis are only incompletely understood. Here, we investigated whether procalcitonin, a biomarker of sepsis, modulates liver cell function and viability. Materials and Methods. Employing a previously characterized and patented biosensor system evaluating hepatocyte toxicity in vitro, human hepatocellular carcinoma cells (HepG2/C3A) were exposed to 0...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28255085/effects-of-inspiratory-muscle-training-on-respiratory-muscle-electromyography-and-dyspnea-during-exercise-in-healthy-men
#16
Andrew H Ramsook, Yannick Molgat-Seon, Michele R Schaeffer, Sabrina S Wilkie, Pat G Camp, W Darlene Reid, Lee M Romer, Jordan A Guenette
Inspiratory muscle training (IMT) has consistently been shown to reduce exertional dyspnea in health and disease; however, the physiological mechanisms remain poorly understood. A growing body of literature suggests that dyspnea intensity can largely be explained by an awareness of increased neural respiratory drive, as indirectly measured using diaphragmatic electromyography (EMGdi). Accordingly, we sought to determine if improvements in dyspnea following IMT can be explained by decreases in inspiratory muscle EMG activity...
March 2, 2017: Journal of Applied Physiology
https://www.readbyqxmd.com/read/28252047/inhibition-of-proliferation-and-epithelial-mesenchymal-transition-in-retinal-pigment-epithelial-cells-by-heavy-chain-hyaluronan-pentraxin-3
#17
Hua He, Ajay E Kuriyan, Chen-Wei Su, Megha Mahabole, Yuan Zhang, Ying-Ting Zhu, Harry W Flynn, Jean-Marie Parel, Scheffer C G Tseng
Proliferative vitreoretinopathy (PVR) is mediated by proliferation and epithelial mesenchymal transition (EMT) of retinal pigment epithelium (RPE). Because heavy chain-hyaluronic acid/pentraxin 3 (HC-HA/PTX3) purified from human amniotic membrane exerts anti-inflammatory and anti-scarring actions, we hypothesized that HC-HA/PTX3 could inhibit these PVR-related processes in vitro. In this study, we first optimized an ARPE-19 cell culture model to mimic PVR by defining cell density, growth factors, and cultivation time...
March 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28250346/an-efficient-strategy-for-the-synthesis-of-1-trifluoromethylsulfonamido-propan-2-yl-esters-and-the-evaluation-of-their-cytotoxic-activity
#18
Omar Gómez-García, Elizabeth Gómez, César Monzón-González, Teresa Ramírez-Apan, Cecilio Álvarez-Toledano
An efficient method for the synthesis of 1-(trifluoromethylsulfonamido)propan-2-yl benzoates is described, the products of the reaction were characterized by heteronuclear single quantum coherence spectroscopy (HSQC), heteronuclear multiple bond correlation (HMBC) and NMR experiments. The overall process began with the activation of the oxazoline ring by triflic anhydride, followed by the opening of the five-membered ring in the 5-methyl-2-phenyl-4,5-dihydrooxazole system. The cytotoxic activity of the new trifluoromethyl sulfonamides was evaluated with six cancer cell lines and human gingival fibroblasts, posteriorly analyzing the influence on cytotoxicity exerted by the withdrawing and donor substituents at the para-position of the phenyl ring...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28249798/mesenchymal-stem-cells-derived-extracellular-vesicles-via-mir-210-improve-infarcted-cardiac-function-by-promotion-of-angiogenesis
#19
Na Wang, Caiyu Chen, Dezhong Yang, Qiao Liao, Hao Luo, Xinquan Wang, Faying Zhou, Xiaoli Yang, Jian Yang, Chunyu Zeng, Wei Eric Wang
Mesenchymal stem cells (MSCs) exert therapeutic effect on treating acute myocardial infarction. Recent evidence showed that paracrine function rather than direct differentiation predominately contributes to the beneficial effects of MSCs, but how the paracrine factors function are not fully elucidated. In the present study, we tested if extracellular vesicles (EVs) secreted by MSC promotes angiogenesis in infracted heart via microRNAs. Immunostaining of CD31 and matrigel plug assay were performed to detect angiogenesis in a mouse myocardial infarction (MI) model...
February 27, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28235702/design-synthesis-biological-evaluation-and-x-ray-structural-studies-of-potent-human-dihydroorotate-dehydrogenase-inhibitors-based-on-hydroxylated-azole-scaffolds
#20
Stefano Sainas, Agnese C Pippione, Marta Giorgis, Elisa Lupino, Parveen Goyal, Cristina Ramondetti, Barbara Buccinnà, Marco Piccinini, Rodolpho C Braga, Carolina H Andrade, Mikael Andersson, Ann-Christin Moritzer, Rosmarie Friemann, Stefano Mensa, Salam Al-Kadaraghi, Donatella Boschi, Marco L Lolli
A new generation of potent hDHODH inhibitors designed by a scaffold-hopping replacement of the quinolinecarboxylate moiety of brequinar, one of the most potent known hDHODH inhibitors, is presented here. Their general structure is characterized by a biphenyl moiety joined through an amide bridge with an acidic hydroxyazole scaffold (hydroxylated thiadiazole, pyrazole and triazole). Molecular modelling suggested that these structures should adopt a brequinar-like binding mode involving interactions with subsites 1, 2 and 4 of the hDHODH binding site...
March 31, 2017: European Journal of Medicinal Chemistry
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