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https://www.readbyqxmd.com/read/27916811/design-synthesis-and-biological-evaluation-of-novel-primaquine-cinnamic-acid-conjugates-of-the-amide-and-acylsemicarbazide-type
#1
Kristina Pavić, Ivana Perković, Petra Gilja, Filip Kozlina, Katja Ester, Marijeta Kralj, Dominique Schols, Dimitra Hadjipavlou-Litina, Eleni Pontiki, Branka Zorc
In this paper design and synthesis of a scaffold comprising primaquine (PQ) motif and cinnamic acid derivatives (CADs) bound directly (compounds 3a-k) or via a spacer (compounds 7a-k) are reported. In the first series of compounds, PQ and various CADs were connected by amide bonds and in the second series by acylsemicarbazide functional groups built from the PQ amino group, CONHNH spacer and the carbonyl group originating from the CADs. PQ-CAD amides 3a-k were prepared by a simple one-step condensation reaction of PQ with a series of CAD chlorides (method A) or benzotriazolides 2 (method B)...
November 28, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27916716/effects-of-a-non-competitive-n-methyl-d-aspartate-nmda-antagonist-tiletamine-in-adult-zebrafish
#2
Tatiana O Kolesnikova, Sergey L Khatsko, Vadim A Shevyrin, Yuri Yu Morzherin, Allan V Kalueff
Tiletamine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist chemically related to ketamine and phencyclidine. A common veterinary anesthetic drug, tiletamine is currently a Schedule III controlled substance. This compound exerts sedative effects in humans and animals, also having an abuse potential, toxicity and dissociative hallucinogenic properties clinically. However, the neurotropic profile of tiletamine remains poorly understood, necessitating novel models and in-vivo screens, including non-mammalian species...
December 1, 2016: Neurotoxicology and Teratology
https://www.readbyqxmd.com/read/27913853/the-role-of-intestinal-oxalate-transport-in-hyperoxaluria-and-the-formation-of-kidney-stones-in-animals-and-man
#3
REVIEW
Jonathan M Whittamore, Marguerite Hatch
The intestine exerts a considerable influence over urinary oxalate in two ways, through the absorption of dietary oxalate and by serving as an adaptive extra-renal pathway for elimination of this waste metabolite. Knowledge of the mechanisms responsible for oxalate absorption and secretion by the intestine therefore have significant implications for understanding the etiology of hyperoxaluria, as well as offering potential targets for future treatment strategies for calcium oxalate kidney stone disease. In this review, we present the recent developments and advances in this area over the past 10 years, and put to the test some of the new ideas that have emerged during this time, using human and mouse models...
December 2, 2016: Urolithiasis
https://www.readbyqxmd.com/read/27913606/acute-administration-of-acyl-but-not-desacyl-ghrelin-decreases-blood-pressure-in-healthy-humans
#4
Cecilia J Zhang, Martin Bidlingmaier, Mekibib Altaye, Laura C Page, David D'Alessio, Matthias H Tschöp, Jenny Tong
OBJECTIVE: To compare the effects of acyl ghrelin (AG) and desacyl ghrelin (DAG) on blood pressure (BP), heart rate (HR) and other autonomic parameters in healthy humans and to elucidate the hormonal mechanisms through which AG could exert its cardiovascular effects. DESIGN: Seventeen healthy participants underwent frequent monitoring of systolic (sBP) and diastolic blood pressure (dBP), HR, respiratory rate (RR) and body surface temperature (Temp) during continuous infusion of AG, DAG, combined AG + DAG or saline control before and during an IV glucose tolerance test on 4 separate days...
February 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/27913354/a-novel-elastic-force-field-to-influence-mediolateral-foot-placement-during-walking
#5
Elizabeth Nyberg, Jordan Broadway, Christian Finetto, Jesse Dean
Bipedal gait can be stabilized through mechanically-appropriate mediolateral foot placement, although this strategy is disrupted in a subset of neurologically injured individuals with balance deficits. The goal of the present work was to develop a device to influence mediolateral foot placement during treadmill walking. We created a novel force-field using a combination of passive elasticity and active control; wires in series with extension springs run parallel to the treadmill belts and can be rapidly repositioned to exert mediolateral forces on the legs of users...
December 1, 2016: IEEE Transactions on Neural Systems and Rehabilitation Engineering
https://www.readbyqxmd.com/read/27912883/miltirone-protects-human-ea-hy926-endothelial-cells-from-oxidized-low-density-lipoprotein-derived-oxidative-stress-via-a-heme-oxygenase-1-and-mapk-nrf2-dependent-pathway
#6
Liu Zhang, Hui Zhang, Xueyan Li, Bingjie Jia, Yuyu Yang, Ping Zhou, Ping Li, Jun Chen
BACKGROUND: Oxidized low-density lipoprotein (ox-LDL) is an underlying cause of endothelial dysfunction, which is an early event in the pathogenesis of atherosclerosis. In our previous study, we established an ARE-driven luciferase reporter system and screened out several potential Nrf2 activators from Salvia miltiorrhiza Bunge. PURPOSE: Since miltirone showed the most potent ARE-driven luciferase activity, the aim of this study was to test the protective role of miltirone against oxidative stress in endothelial cell and to investigate the underlying mechanistic signaling pathways...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27904901/effect-of-ticagrelor-on-endothelial-calcium-signalling-and-barrier-function
#7
Dursun Gündüz, Christian Tanislav, Klaus-Dieter Schlüter, Rainer Schulz, Christian Hamm, Muhammad Aslam
The P2Y12 receptor is a Gi-coupled receptor whose activation inhibits adenylyl cyclase and thereby reduces the concentration of intracellular cAMP. Here the hypothesis was tested whether AR-C 66096 or ticagrelor, two direct-acting and reversibly binding P2Y12 receptor antagonists, protect endothelial cell (EC) barrier function by raising intracellular cAMP in ECs. The study was carried out on primary human umbilical vein ECs (HUVECs) and human pulmonary microvascular ECs (hPMECs). AR-C66096 (10 µM) induced a 50 % increase in cAMP in ECs whereas ticagrelor (2-10 µM) had no effect...
December 1, 2016: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/27904472/clearing-the-corpses-regulatory-mechanisms-novel-tools-and-therapeutic-potential-of-harnessing-microglial-phagocytosis-in-the-diseased-brain
#8
REVIEW
Irune Diaz-Aparicio, Sol Beccari, Oihane Abiega, Amanda Sierra
Apoptosis is a widespread phenomenon that occurs in the brain in both physiological and pathological conditions. Dead cells must be quickly removed to avoid the further toxic effects they exert in the parenchyma, a process executed by microglia, the brain professional phagocytes. Although phagocytosis is critical to maintain tissue homeostasis, it has long been either overlooked or indirectly assessed based on microglial morphology, expression of classical activation markers, or engulfment of artificial phagocytic targets in vitro...
October 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/27895800/a-novel-curcumin-analogue-is-a-potent-chemotherapy-candidate-for-human-hepatocellular-carcinoma
#9
Ji-An Zhao, Mei-Xiang Sang, Cui-Zhi Geng, Shi-Jie Wang, Bao-En Shan
Curcumin (CUR) has been demonstrated to protect against carcinogenesis and to prevent tumor development in cancer; however, the clinical application of CUR is limited by its instability and poor metabolic properties. The present study offers an strategy for a novel CUR analogue, (1E,4E)-1,5-bis(2-bromophenyl)penta-1,4-dien-3-one (GL63), to be used as a potential therapeutic agent for hepatocellular carcinoma (HCC) in vitro and in vivo. The current study demonstrated that GL63 exhibited more potent inhibition of proliferation of HCC cells than CUR...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27895776/establishment-of-specific-cytotoxic-t-lymphocyte-culture-system-and-its-inhibitory-effect-on-ovarian-cancer
#10
Mingxing Sui, Lihui Si, Tianmin Xu, Manhua Cui
The present study aimed to establish a novel method for efficiently inducing cytotoxic T lymphocytes (CTLs) in vitro, in order to develop an immune-based therapy for suppressing and killing ovarian cancer cells with a high safety and efficacy. Peripheral blood mononuclear cells (PBMCs) were stimulated with CpG oligodeoxynucleotide (CpGODN) and ginsenoside Rg1, which were united as an immune adjuvant, and human epidermal growth factor receptor 2 (HER2/neu) antigen peptide, in order to establish a specific CTL culture system in vitro...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27894189/ziprasidone-induces-cytotoxicity-and-genotoxicity-in-human-peripheral-lymphocytes
#11
Haluk Kefelioğlu, Zülal Atlı Şekeroğlu, Gamze Coşguner, Seval Kontaş Yedier, Vedat Şekeroğlu
It has been stated that some antipsychotic drugs might cause genotoxic and carcinogenic effects. Ziprasidone (ZIP) is commonly used an antipsychotic drug. However, its genotoxicity and carcinogenicity data are very limited. The cytotoxicity and genotoxicity of ZIP on human peripheral blood lymphocytes were examined in vitro by sister chromatid exchange (SCE), chromosome aberration (CA) and micronucleus (MN) tests in this study. Lymphocyte cultures were treated with 50, 75 and 100 μg/ml of ZIP in the presence and absence of a metabolic activator (S9 mix)...
November 29, 2016: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/27894091/preclinical-study-of-cinobufagin-as-a-promising-anti-colorectal-cancer-agent
#12
Xing-Sheng Lu, Yin-Biao Qiao, Ya Li, Bo Yang, Min-Bin Chen, Chun-Gen Xing
Here, we assessed the anti-colorectal cancer (CRC) cell activity of cinobufagin (CBG). We found that CBG exerted potent cytotoxic and anti-proliferative activity against CRC lines (HCT-116 and HT-29) and primary human CRC cells. Meanwhile, it activated apoptosis, and disrupted cell-cycle progression in the cells. At the signaling level, CBG treatment in CRC cells provoked endoplasmic reticulum stress (ER stress), the latter was evidenced by caspase-12 activation, CHOP expression, as well as PERK and IRE1 phosphorylations...
November 23, 2016: Oncotarget
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#13
Jocelien D A Olivier, Diana C Esquivel Franco, Ronald Oosting, Marcel Waldinger, Zoltan Sarnyai, Berend Olivier
Tramadol is a well-known and effective analgesic. Recently it was shown that tramadol is also effective in human premature ejaculation. The inhibitory effect of tramadol on the ejaculation latency is probably due to its mechanism of action as a μ-opioid receptor agonist and noradrenaline/serotonin (5-HT) reuptake inhibitor. In order to test this speculation, we tested several doses of tramadol in a rat model of male sexual behavior and investigated two types of drugs interfering with the μ-opioid and the 5-HT system...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27888799/new-bipyridine-gold-iii-dithiocarbamate-containing-complexes-exerted-a-potent-anticancer-activity-against-cisplatin-resistant-cancer-cells-independent-of-p53-status
#14
Muhammad Altaf, Muhammad Monim-Ul-Mehboob, Abdel-Nasser Kawde, Giuseppe Corona, Roberto Larcher, Marcia Ogasawara, Naike Casagrande, Marta Celegato, Cinzia Borghese, Zahid H Siddik, Donatella Aldinucci, Anvarhusein A Isab
We synthesized, characterized and tested in a panel of cancer cell lines, nine new bipyridine gold(III) dithiocarbamate-containing complexes. In vitro studies demonstrated that compounds 1, 2, 4, 5, 7 and 8 were the most cytotoxic in prostate, breast, ovarian cancer cell lines and in Hodgkin lymphoma cells with IC50 values lower than the reference drug cisplatin. The most active compound 1 was more active than cisplatin in ovarian (A2780cis and 2780CP-16) and breast cancer cisplatin-resistant cells. Compound 1 determined an alteration of the cellular redox homeostasis leading to increased ROS levels, a decrease in the mitochondrial membrane potential, cytochrome-c release from the mitochondria and activation of caspases 9 and 3...
November 18, 2016: Oncotarget
https://www.readbyqxmd.com/read/27884749/celecoxib-exerts-antitumor-effects-in-hl-60-acute-leukemia-cells-and-inhibits-autophagy-by-affecting-lysosome-function
#15
Ying Lu, Xiang-Fu Liu, Ting-Rong Liu, Rui-Fang Fan, Yi-Chuan Xu, Xiang-Zhong Zhang, Ling-Ling Liu
Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, has been demonstrated to exert antitumor activity in a variety of cancer cells. The underlying mechanism involves inhibition of cell cycle progression and induction of apoptosis. Besides, celecoxib has also been found to induce autophagy in some solid tumor cells. The aim of this study was to investigate the effect of celecoxib on cell proliferation in HL-60 human acute leukemia cells and to explore the potential mechanism. HL-60 cells were exposed to various concentrations of celecoxib and cell viability was evaluated by the MTT assay...
November 21, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27879653/ellagic-acid-inhibits-bladder-cancer-invasiveness-and-in-vivo-tumor-growth
#16
Claudia Ceci, Lucio Tentori, Maria Grazia Atzori, Pedro M Lacal, Elena Bonanno, Manuel Scimeca, Rosella Cicconi, Maurizio Mattei, Maria Gabriella de Martino, Giuseppe Vespasiani, Roberto Miano, Grazia Graziani
Ellagic acid (EA) is a polyphenolic compound that can be found as a naturally occurring hydrolysis product of ellagitannins in pomegranates, berries, grapes, green tea and nuts. Previous studies have reported the antitumor properties of EA mainly using in vitro models. No data are available about EA influence on bladder cancer cell invasion of the extracellular matrix triggered by vascular endothelial growth factor-A (VEGF-A), an angiogenic factor associated with disease progression and recurrence, and tumor growth in vivo...
November 22, 2016: Nutrients
https://www.readbyqxmd.com/read/27871958/current-perspectives-on-stem-cell-therapy-for-erectile-dysfunction
#17
REVIEW
Taylor C Peak, James Anaissie, Wayne J G Hellstrom
INTRODUCTION: Erectile dysfunction (ED) is a common sexual disorder that affects the lives of millions of male patients and their partners. Various medical and surgical therapies exist, with the most common being oral intake of phosphodiesterase 5 inhibitors. One therapeutic strategy in preclinical development to treat ED is stem cell transplantation. AIM: To examine the studies that have investigated stem cells for the treatment of ED. METHODS: A literature review was performed through PubMed focusing on stem cells and ED...
July 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27867276/ursolic-acid-a-natural-pentacylcic-triterpene-from-ochrosia-elliptica-and-its-role-in-the-management-of-certain-neglected-tropical-diseases
#18
Rola M Labib, Sherif S Ebada, Fadia S Youssef, Mohamed L Ashour, Samir A Ross
BACKGROUND: Leishmaniasis and African trypanosomiasis are recognized as the leading causes of mortality and morbidity with the greatest prevalence in the developing countries. They affect more than one billion of the poorest people on the globe. OBJECTIVE: To find a cheap, affordable, safe, and efficacious antileshmanial and antitrypanosomal natural drug and to elucidate its probable mode of action. MATERIALS AND METHODS: Phytochemical investigation of the non-polar fraction of the methanol extract of leaves of Ochrosia elliptica Labill...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27866267/luminol-testing-in-detecting-modern-human-skeletal-remains-a-test-on-different-types-of-bone-tissue-and-a-caveat-for-pmi-interpretation
#19
Giorgio Caudullo, Valentina Caruso, Annalisa Cappella, Emanuela Sguazza, Debora Mazzarelli, Alberto Amadasi, Cristina Cattaneo
When forensic pathologists and anthropologists have to deal with the evaluation of the post-mortem interval (PMI) in skeletal remains, luminol testing is frequently performed as a preliminary screening method. However, the repeatability of this test on the same bone, as well as comparative studies on different bones of the same individual, has never been performed. Therefore, with the aim of investigating the influence that different types of bones may exert on the response to the luminol test, the present study analysed three different skeletal elements (femoral diaphysis, vertebra and cranial vault), gathered from ten recent exhumed skeletons (all with a 20-year PMI)...
November 19, 2016: International Journal of Legal Medicine
https://www.readbyqxmd.com/read/27861949/absolute-quantification-of-micrornas-in-green-tea-camellia-sinensis-by-stem-loop-quantitative-real-time-pcr
#20
Ying-Hui Hou, Anburaj Jeyaraj, Xiao Zhang, Chao-Ling Wei
BACKGROUND: There are some studies to show that food-derived plant microRNAs (miRNAs) may be detected in mammals. The research evidence has being provoked a considerable debate whether plant-derived miRNAs exert the same regulatory functions as endogenous animal miRNAs. To test the hypothesis, the methods of highly sensitive absolute quantification miRNAs have been developed. However, absolute miRNA quantification of green tea has not yet been reported. In this study, it is the first to build an absolute quantification method to detect miRNAs level in green tea using stem-loop quantitative real-time PCR (qRT-PCR)...
November 12, 2016: Journal of the Science of Food and Agriculture
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