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https://www.readbyqxmd.com/read/28225057/intracellular-drug-bioavailability-a-new-predictor-of-system-dependent-drug-disposition
#1
André Mateus, Andrea Treyer, Christine Wegler, Maria Karlgren, Pär Matsson, Per Artursson
Intracellular drug exposure is influenced by cell- and tissue-dependent expression of drug-transporting proteins and metabolizing enzymes. Here, we introduce the concept of intracellular bioavailability (Fic) as the fraction of extracellular drug available to bind intracellular targets, and we assess how Fic is affected by cellular drug disposition processes. We first investigated the impact of two essential drug transporters separately, one influx transporter (OATP1B1; SLCO1B1) and one efflux transporter (P-gp; ABCB1), in cells overexpressing these proteins...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28222143/antidepressive-and-antinociceptive-effects-of-ethanolic-extract-and-fruticuline-a-from-salvia-lachnostachys-benth-leaves-on-rodents
#2
Joyce Alencar Santos, Ana Claudia Piccinelli, Maira Dante Formagio, Cristhian Santos Oliveira, Elide Pereira Dos Santos, Maria Élida Alves Stefanello, Ubirajara Lanza Junior, Rodrigo Juliano Oliveira, Mário Mateus Sugizaki, Cândida Aparecida Leite Kassuya
OBJECTIVES: This study investigated the antidepressant and antinociceptive effects of ethanolic extract (SLEE) and pure fruticuline A obtained from Salvia lachnostachys leaves on rats and mice. METHODS: In this study, SLEE (100 mg/kg, p.o. route) was evaluated for its effects on spared nerve injury (SNI) in rats. The animals were submitted to mechanical sensitivity, forced swim (FST) and cold sensitivity tests 10 and 15 days after surgery. SLEE (100 mg/kg, p.o.) and fruticuline A (3 mg/kg, p...
2017: PloS One
https://www.readbyqxmd.com/read/28219103/digoxin-induces-cardiac-hypertrophy-without-negative-effects-on-cardiac-function-and-physical-performance-in-trained-normotensive-rats
#3
Claodete Hasselstrom Neves, Ramires Alsamir Tibana, Jonato Prestes, Fabricio Azevedo Voltarelli, Andreo Fernando Aguiar, Gustavo Augusto Ferreira Mota, Sergio Luiz Borges de Sousa, Andre Soares Leopoldo, Ana Paula Lima Leopoldo, Andre Mueller, Danilo Henrique Aguiar, James Wilfred Navalta, Mario Mateus Sugizaki
Cardiotonic drugs and exercise training promote cardiac inotropic effects, which may affect training-induced cardiac adaptations. This study investigated the effects of long-term administration of digoxin on heart structure and function, and physical performance of rats submitted to high-intensity interval training (HIIT). Male Wistar rats, 60 days old, were divided into control (C), digoxin (DIGO), trained (T), and trained with digoxin (TDIGO). Digoxin was administered by gavage (30 µg/kg/day) for 75 days...
February 20, 2017: International Journal of Sports Medicine
https://www.readbyqxmd.com/read/28216567/wine-flavonoids-in-health-and-disease-prevention
#4
Iva Fernandes, Rosa Pérez-Gregorio, Susana Soares, Nuno Mateus, Victor de Freitas
Wine, and particularly red wine, is a beverage with a great chemical complexity that is in continuous evolution. Chemically, wine is a hydroalcoholic solution (~78% water) that comprises a wide variety of chemical components, including aldehydes, esters, ketones, lipids, minerals, organic acids, phenolics, soluble proteins, sugars and vitamins. Flavonoids constitute a major group of polyphenolic compounds which are directly associated with the organoleptic and health-promoting properties of red wine. However, due to the insufficient epidemiological and in vivo evidences on this subject, the presence of a high number of variables such as human age, metabolism, the presence of alcohol, the complex wine chemistry, and the wide array of in vivo biological effects of these compounds suggest that only cautious conclusions may be drawn from studies focusing on the direct effect of wine and any specific health issue...
February 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28202703/investigations-in-gabaa-receptor-antibody-associated-encephalitis
#5
Marianna Spatola, Mar Petit-Pedrol, Mateus Mistieri Simabukuro, Thaís Armangue, Fernanda J Castro, Maria I Barcelo Artigues, Maria R Julià Benique, Leslie Benson, Mark Gorman, Ana Felipe, Ruben L Caparó Oblitas, Myrna R Rosenfeld, Francesc Graus, Josep Dalmau
OBJECTIVE: To report the clinical features, comorbidities, receptor subunit targets, and outcome in patients with anti-GABAA receptor (GABAAR) encephalitis. METHODS: Clinical study of 26 patients, including 17 new (April 2013-January 2016) and 9 previously reported patients. Antibodies to α1, β3, and γ2 subunits of the GABAAR were determined using reported techniques. RESULTS: Patients' median age was 40.5 years (interquartile range 48...
February 15, 2017: Neurology
https://www.readbyqxmd.com/read/28181220/eslicarbazepine-acetate-as-adjunctive-therapy-in-clinical-practice-esladoba-study
#6
J Chaves, P Breia, J Pimentel, R Pelejão, M Carvalho, P Mateus, H Grebe, A Mestre, H Fernandes, R Sousa, A Gala
OBJECTIVE: To assess seizure control and tolerability of eslicarbazepine acetate (ESL) as adjunctive therapy to one baseline antiepileptic drug (AED), in adults with partial-onset seizures (POS) with or without secondary generalization. METHODS: Multicenter, non-interventional, prospective cohort study conducted between March 2012 and September 2014 at 12 neurology departments in Portugal. Adults with POS not controlled with one AED who had initiated ESL as adjunctive treatment were enrolled...
February 8, 2017: Acta Neurologica Scandinavica
https://www.readbyqxmd.com/read/28178778/malvidin-3-glucoside-fatty-acid-conjugates-from-hydrophilic-toward-novel-lipophilic-derivatives
#7
Luís Cruz, Marta Guimarães, Paula Araújo, Ana Évora, Victor de Freitas, Nuno Mateus
This work describes the lipophilization reactions of malvidin 3-glucoside with different saturated fatty acid chain lengths using an enzymatic synthesis and the study of their physical-chemical and antioxidant properties. The lipophilic anthocyanins were obtained with satisfactory yields (22-40%) after column chromatography purifications, and they revealed the same appealing chromatic features of the parent anthocyanin. All of the compounds were characterized by mass spectrometry, confirming the regioselective acylation on the glucose moiety...
February 16, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28177709/effects-of-resistance-training-and-estrogen-replacement-on-adipose-tissue-inflammation-in-ovariectomized-rats
#8
Maria Fernanda Cury Rodrigues, Fabiano Candido Ferreira, Natália Santanielo Silva-Magosso, Marina Rodrigues Barbosa, Markus Vinicius Campos Souza, Mateus Moraes Domingos, Gustavo Henrique Rigo Canevazzi, Uliana Sbeguen Stotzer, Sabrina Messa Peviani, Fábio Santos de Lira, Heloísa Sobreiro Selistre de Araújo, Sérgio Eduardo de Andrade Perez
Estrogen deficiency is directly related to central obesity and low-grade inflammation. Hormonal replacement and exercise training are both able to decrease fat accumulation and inflammation in postmenopausal women. However, the efficiency of resistance training (RT) and estrogen replacement (ER) in minimizing adiposity and inflammation in the visceral adipose tissue (VAT) of ovariectomized (OVX) rats has not yet been elucidated. In this study, Sprague-Dawley rats were divided into the following six groups: the sham-operated sedentary (Sham-Sed), ovariectomized sedentary (OVX-Sed), sham-operated resistance training (Sham-RT), OVX-RT, OVX-Sed-ER and OVX-RT-ER groups...
January 25, 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/28175054/p315-gastrointestinal-immune-related-adverse-events-associated-with-programmed-death-1-blockade
#9
M Collins, J-M Michot, F-X Danlos, S Champiat, C Mussini, E Soularue, C Mateus, D Loirat, A Buisson, I Rosa, O Lambotte, S Laghouati, A-L Voisin, J-C Soria, A Marabelle, C Robert, F Carbonnel
No abstract text is available yet for this article.
February 1, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28174009/ceramic-strengthening-by-tuning-the-elastic-moduli-of-resin-based-luting-agents
#10
Aloísio O Spazzin, Ataís Bacchi, Rodrigo Alessandretti, Mateus B Santos, Gabriela R Basso, Jason Griggs, Rafael R Moraes
OBJECTIVE: Resin-based luting agents (RBLAs) with tuned elastic moduli (E) were prepared and their influence on the strengthening, reliability, and mode of failure of luted feldspar ceramic was investigated. METHODS: RBLAs with low E (2.6GPa), intermediate E (6.6GPa), and high E (13.3GPa) were prepared and used to coat acid-etched ceramic disks. Positive (untreated ceramic) and negative (acid-etched ceramic) control groups were tested. The response variables (n=30) were biaxial flexural strength (σbf, MPa), characteristic strength (σ0, MPa), and Weibull modulus at the ceramic surface (z=0) and luting agent surface (z=-t2)...
February 4, 2017: Dental Materials: Official Publication of the Academy of Dental Materials
https://www.readbyqxmd.com/read/28168267/stability-and-optical-and-electronic-properties-of-ultrathin-h-bnc
#11
Andressa C Bevilacqua, Mateus Henrique Köhler, Sérgio Azevedo, Rogério J Baierle
Spin polarized density functional theory has been used to study the stability, and electronic and optical properties when BN nanodomains are embedded in graphene and carbon patches are embedded in a single layer of h-BN forming h-BNC nanosystems. Our results show that graphene doped with BN nanodomains exhibits a non-zero gap, which depends on the nanodomain's shape and width. For h-BN with C domains we observe that we can tune the h-BN gap into the visible region, making the h-BNC a promising material for catalysis using solar energy...
February 7, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28159241/cattle-naturally-infected-by-eurytrema-coelomaticum-relation-between-adenosine-deaminase-activity-and-zinc-levels
#12
Hyolanda M Grosskopf, Claiton I Schwertz, Gustavo Machado, Nathieli B Bottari, Ester S da Silva, Mateus E Gabriel, Neuber J Lucca, Mariana S Alves, Maria Rosa C Schetinger, Vera M Morsch, Ricardo E Mendes, Aleksandro S da Silva
The enzyme adenosine deaminase (ADA) is critical for modulating the immune system, and in the presence of zinc, its activity is catalyzed. The aim of this study was to evaluate the ADA activity in pancreas of cattle naturally infected by Eurytrema coelomaticum in relation to the results of zinc levels, pathological findings and parasite load. For this study 51 slaughtered cattle were used. The animals were divided into two groups: Group A consisting of animals naturally infected by E. coelomaticum (n=33) and Group B of uninfected animals (n=18)...
February 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28157580/physiological-highlights-of-manganese-toxicity-symptoms-in-soybean-plants-mn-toxicity-responses
#13
Elcio Ferreira Santos, José Mateus Kondo Santini, Amanda Pereira Paixão, Enes Furlani Júnior, José Lavres, Marcelo Campos, André Rodrigues Dos Reis
Manganese (Mn) is an essential element for plants; however, high concentrations in certain soil conditions can cause toxicity symptoms in the plant tissue. Here, we describe Mn toxicity symptoms and Mn toxicity responses in soybean plants. Soybean plants exposed to excess Mn showed reductions in the CO2 assimilation rate and stomatal conductance, which in turn resulted in decreased shoot biomass. Furthermore, peroxidase (POD), superoxide dismutase (SOD), and catalase (CAT) activity were higher in plants grown with the highest Mn concentration...
January 25, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28146169/chagas-disease-transmission-by-consumption-of-game-meat-systematic-review
#14
Luiz Henrique Conde Sangenis, Marco Antonio Prates Nielebock, Ceumara da Silva Santos, Mateus Curty Carriello da Silva, Glauber Motta Ribeiro Bento
Objective: To evaluate the influence of game meat consumption in Chagas disease (CD) transmission, the conditions under which it occurs and the frequency of reports in the literature. Methods: Through systematic review, databases PubMed, LILACS, MEDLINE, and SciELO were consulted, and articles written in Portuguese, English, and Spanish were included, with no limitation over publication date. We used the following descriptors: oral, transmission, meat, wild animals, hunt, carnivory, and Chagas disease...
October 2016: Revista Brasileira de Epidemiologia, Brazilian Journal of Epidemiology
https://www.readbyqxmd.com/read/28145708/identification-of-triazolothiadiazoles-as-potent-inhibitors-of-the-dctp-pyrophosphatase-1
#15
Sabin Llona-Minguez, Anders Höglund, Elisee Wiita, Ingrid Almlöf, André Mateus, José Manuel Calderón-Montaño, Cindy Cazares-Körner, Evert J Homan, Olga Loseva, Pawel Baranczewski, Ann-Sofie Jemth, Maria Häggblad, Ulf Martens, Bo Lundgren, Per Artursson, Thomas Lundbäck, Annika Jenmalm-Jensen, Ulrika Warpman Berglund, Martin Scobie, Thomas Helleday
The dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression. Here we report on the discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. Compound 16 and 18 display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit-to-lead development.
February 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28137365/in-vitro-protective-effects-of-botryosphaeran-a-1%C3%A2-3-1%C3%A2-6-%C3%AE-d-glucan-against-mutagens-in-normal-and-tumor-rodent-cells
#16
Leandra E Kerche-Silva, Ilce M S Cólus, Maressa Malini, Mateus Prates Mori, Robert F H Dekker, Aneli M Barbosa-Dekker
Botryosphaeran (BOT) is an exocellular β-d-glucan (carbohydrate biopolymer) of the (1→3;1→6)-linked type produced by Botryosphaeria rhodina MAMB-05. The cytotoxic, mutagenic, genotoxic, and protective effects of this substance were evaluated in Chinese hamster lung fibroblasts (V79) and rat hepatocarcinoma cells (HTC) by the micronucleus test (MN) and the comet assay. BOT was not genotoxic in either cell line; it decreased the clastogenic effects of doxorubicin, H2O2, and benzo[a]pyrene. These results indicate that BOT may have potential as a therapeutic agent...
February 2017: Mutation Research
https://www.readbyqxmd.com/read/28122331/integrative-mirna-and-mrna-analysis-in-penile-carcinomas-reveals-markers-and-pathways-with-potential-clinical-impact
#17
Hellen Kuasne, Mateus C Barros-Filho, Ariane Busso-Lopes, Fábio A Marchi, Maisa Pinheiro, Juan J M Muñoz, Cristovam Scapulatempo-Neto, Eliney F Faria, Gustavo C Guimarães, Ademar Lopes, José C S Trindade-Filho, Maria Aparecida C Domingues, Sandra A Drigo, Silvia R Rogatto
Penile carcinoma (PeCa) is an important public health issue in poor and developing countries, and has only recently been explored in terms of genetic and epigenetic studies. Integrative data analysis is a powerful method for the identification of molecular drivers involved in cancer development and progression. miRNA and mRNA expression profiles followed by integrative analysis were investigated in 23 PeCa and 12 non-neoplastic penile tissues (NPT). Expression levels of eight miRNAs and 10 mRNAs were evaluated in the same set of samples used for microarray and in a validation set of cases (PeCa = 36; NPT = 27)...
January 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28120837/suggestive-association-between-variants-in-il1rapl-and-asthma-symptoms-in-latin-american-children
#18
Cintia Rodrigues Marques, Gustavo No Costa, Thiago Magalhães da Silva, Pablo Oliveira, Alvaro A Cruz, Neuza Maria Alcantara-Neves, Rosemeire L Fiaccone, Bernardo L Horta, Fernando Pires Hartwig, Esteban G Burchard, Maria Pino-Yanes, Laura C Rodrigues, Maria Fernanda Lima-Costa, Alexandre C Pereira, Mateus H Gouveia, Hanaisa P Sant Anna, Eduardo Tarazona-Santos, Maurício Lima Barreto, Camila Alexandrina Figueiredo
Several genome-wide association studies have been conducted to investigate the influence of genetic polymorphisms in the development of allergic diseases, but few of them have included the X chromosome. The aim of present study was to perform an X chromosome-wide association study (X-WAS) for asthma symptoms. The study included 1307 children of which 294 were asthma cases. DNA was genotyped using 2.5 HumanOmni Beadchip from Illumina. Statistical analyses were performed in PLINK 1.9, MACH 1.0 and Minimac2. The variant rs12007907 (g...
January 25, 2017: European Journal of Human Genetics: EJHG
https://www.readbyqxmd.com/read/28101706/comparative-assessment-of-leca-and-spartina-maritima-to-remove-emerging-organic-contaminants-from-wastewater
#19
Ana Rita Ferreira, Paula Guedes, Eduardo P Mateus, Alexandra B Ribeiro, Nazaré Couto
The present work aimed to evaluate the capacity of constructed wetlands (CWs) to remove three emerging organic contaminants with different physicochemical properties: caffeine (CAF), oxybenzone (MBPh), and triclosan (TCS). The simulated CWs were set up with a matrix of light expanded clay aggregates (LECA) and planted with Spartina maritima, a salt marsh plant. Controlled experiments were carried out in microcosms using deionized water and wastewater collected at a wastewater treatment plant (WWTP), with different contaminant mass ranges, for 3, 7, and 14 days...
January 18, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28099630/the-brain-derived-neurotrophic-factor-bdnf-gene-val66met-polymorphism-affects-memory-performance-in-older-adults
#20
Lucas A de Azeredo, Tatiana De Nardi, Mateus L Levandowski, Saulo G Tractenberg, Julia Kommers-Molina, Andrea Wieck, Tatiana Q Irigaray, Irênio G da Silva, Rodrigo Grassi-Oliveira
Objective: Memory impairment is an important contributor to the reduction in quality of life experienced by older adults, and genetic risk factors seem to contribute to variance in age-related cognitive decline. Brain-derived neurotrophic factor (BDNF) is an important nerve growth factor linked with development and neural plasticity. The Val66Met polymorphism in the BDNF gene has been associated with impaired episodic memory in adults, but whether this functional variant plays a role in cognitive aging remains unclear...
January 12, 2017: Revista Brasileira de Psiquiatria
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