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https://www.readbyqxmd.com/read/28443803/a-strategy-for-early-risk-predictions-of-clinical-drug-drug-interactions-involving-the-gastroplus-tm-ddi-module-for-time-dependent-cyp-inhibitors
#1
Anna-Karin Sohlenius-Sternbeck, Gabrielle Meyerson, Ann-Louise Hagbjörk, Sanja Juric, Ylva Terelius
1. A set of reference compounds for time-dependent inhibition (TDI) of cytochrome P450 with available literature data for kinact and KI was used to predict clinical implications using the GastroPlus(TM) software. Comparisons were made to in vivo literature interaction data. 2. The predicted AUC ratios (AUC+inhibitor/AUCcontrol) could be compared with the observed ratios from literature for all compounds with detailed information about in vivo administration, pharmacokinetics and in vivo interactions (N = 21)...
April 26, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28439264/benthic-diatom-based-indices-for-water-quality-assessment-in-two-subtropical-streams
#2
Xiang Tan, Quanfa Zhang, Michele A Burford, Fran Sheldon, Stuart E Bunn
Benthic diatoms have been universally used as indicators to assess water quality in lotic ecosystems. However, most diatom-based indices developed in Europe have not been widely used or tested in other continents such as Asia or Oceania. This study compared the performance of 14 widely-applied diatom indices in assessing ecological conditions in subtropical streams in South East Queensland (SEQ) in Australia and in the upper Han River in China. Most water quality variables in the upper Han River including dissolved organic carbon (DOC), total nitrogen (TN), and soluble reactive phosphorus (SRP) had strong relationships with at least one diatom index, with the exception of IDAP (Index Diatom Artois-Picardie), and TDI (Trophic Diatom Index)...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28424878/oral-health-in-patients-with-renal-disease-a-longitudinal-study-from-predialysis-to-kidney-transplantation
#3
Karita M Nylund, Jukka H Meurman, Anna Maria Heikkinen, Jussi O Furuholm, Fernanda Ortiz, Hellevi M Ruokonen
OBJECTIVES: The aim of this longitudinal study was to compare the oral health of chronic kidney disease patients at the predialysis (baseline) and post-transplantation (follow-up) stages and to investigate differences in oral health between diabetic nephropathy and other kidney disease patients at follow-up. MATERIALS AND METHODS: Fifty-three kidney disease patients (34 men) aged 31-86 years were followed up to 157 months. Clinical and radiological oral examinations, salivary and laboratory analyses, and oral health behavior questionnaires were conducted at the predialysis and follow-up stages at Helsinki University Hospital, Finland...
April 20, 2017: Clinical Oral Investigations
https://www.readbyqxmd.com/read/28415122/p1138cardiac-shear-wave-velocity-in-healthy-individuals
#4
M Strachinaru, M L Geleijnse, J G Bosch, N De Jong, Afw Van Der Steen, B M Van Dalen, H J Vos
Background: The closure of the valves generates shear waves in the heart walls. The propagation velocity of shear waves relates to stiffness. This could potentially be used to estimate the stiffness of the myocardium, with huge potential implications in pathologies characterized by a deterioration of the diastolic properties of the left ventricle. In an earlier phantom study we already validated shear wave tracking with a clinical ultrasound system in cardiac mode. Purpose: In this study we aimed to measure the shear waves velocity in normal individuals...
December 1, 2016: European Heart Journal Cardiovascular Imaging
https://www.readbyqxmd.com/read/28415117/p1033echocardiographic-predictive-model-of-new-onset-postoperative-atrial-fibrillation-after-abdominal-surgery
#5
L Demirevska, D Gotchev
Background: and purpose: Postoperative atrial fibrillation (POAF) is a frequent complication post high-risk abdominal surgery in elderly patients. This study aimed to develop a predictive model of POAF based on preoperative transthoracic echocardiography (TTE) findings in these patients. Methods: We conducted a prospective study of 300 consecutive patients, age ≥ 65 years (mean age 72±6 years, 61% men), who underwent high-risk abdominal surgery under general anesthesia...
December 1, 2016: European Heart Journal Cardiovascular Imaging
https://www.readbyqxmd.com/read/28415097/p544the-importance-of-contractile-reserve-when-assessing-asymptomatic-patients-with-aortic-stenosis
#6
J J Van Zalen, S Badiani, L Hart, A Marshall, N Patel, G Lloyd
Asymptomatic patients may exhibit symptoms during objective exercise testing, but whether symptoms are due to the obstructively of the valve (typified by the mean gradient) or underlying ventricular function remains unknown. While the mean gradient is an easy parameter to measure no consensus about the measurement of contractile reserve exists. Longitudinal abnormalities may occur in the presence of a normal ejection fraction and the augmentation of these parameters is poorly described. To obtain an objective regarding patients exercise ability is best determined using cardiopulmonary exercise testing...
December 1, 2016: European Heart Journal Cardiovascular Imaging
https://www.readbyqxmd.com/read/28407489/exposure-to-the-plasticizer-di-2-ethylhexyl-terephthalate-dehtp-in-portuguese-children-urinary-metabolite-levels-and-estimated-daily-intakes
#7
Frederik Lessmann, Luísa Correia-Sá, Conceição Calhau, Valentina F Domingues, Tobias Weiss, Thomas Brüning, Holger M Koch
Classical ortho-phthalate plasticizers are, due to their endocrine disrupting potency and reproductive toxicity, increasingly replaced by alternative plasticizers. Di(2-ethylhexyl) terephthalate (DEHTP) is one of these substitutes. In this study, we investigated DEHTP exposure in 107 Portuguese children (4-17years old) by analyzing specific DEHTP metabolites in their urine using a newly developed LC-MS/MS method. We could detect the major, specific DEHTP metabolite mono(2-ethyl-5-carboxypentyl) terephthalate (5cx-MEPTP) in 100% of the samples with levels above the limit of quantification in 96% of the samples (median concentration 4...
April 10, 2017: Environment International
https://www.readbyqxmd.com/read/28405785/determination-of-the-potential-implementation-impact-of-2016-ministry-of-environmental-protection-generic-assessment-criteria-for-potentially-contaminated-sites-in-china
#8
Yuanyuan Cheng, Yu-Ting Tang, C Paul Nathanail
The Ministry of Environmental Protection of China issued a 3rd draft edition of risk-based Generic Assessment Criteria (the MEP-GAC) in March 2016. Since these will be the first authoritative GAC in China, their implementation is likely to have a significant impact on China's growing contaminated land management sector. This study aims to determine the potential implementation impact of the MEP-GAC through an in-depth analysis of the management context, land use scenarios, health criteria values adopted and exposure pathways considered...
April 12, 2017: Environmental Geochemistry and Health
https://www.readbyqxmd.com/read/28402044/reported-normal-values-and-weighted-means-for-commonly-used-echocardiography-pulsed-doppler-and-tissue-doppler-measurements
#9
REVIEW
Magnus Dencker, Martin Stagmo
Pulsed Doppler (PW) and tissue Doppler imaging (TDI) measurements are part of every echocardiography examination for evaluation of left ventricular (LV) diastolic function and filling pressure. The purpose of this study was to summarize published data on normal values for PW and TDI measurements. A PubMed search was performed on the 10th of October 2016 to identify relevant articles. Studies were considered relevant if they included more than 200 healthy individuals. A total of 13 studies were identified. Of these, 13 studies with 7777 subjects reported PW measurement over the mitral valve, six studies with 4082 subjects reported PW measurement in the pulmonary vein and 10 studies with 5988 subjects reported TDI...
April 12, 2017: Clinical Physiology and Functional Imaging
https://www.readbyqxmd.com/read/28400931/evaluation-of-cardiac-functions-in-children-and-adolescents-with-type-1-diabetes
#10
Faten M Abd-El Aziz, Shereen Abdelghaffar, Eman M Hussien, Aya M Fattouh
BACKGROUND: Cardiac dysfunction in patients with type 1 diabetes (T1D) represents one of the serious complications. To evaluate the cardiac function in children with T1D by conventional echocardiography and tissue Doppler imaging (TDI). METHODS: The study included 40 T1D patients (age between 6 and 16 years) with > 5 years duration of diabetes and 42 healthy control children. The patients were subjected to clinical evaluation and laboratory investigations [glycosylated hemoglobin A1c (HbA1c), serum lipids and lipoproteins]...
March 2017: Journal of Cardiovascular Ultrasound
https://www.readbyqxmd.com/read/28395467/-liquid-milk-exposure-and-risk-assessment-of-thiocyanate-in-chinese-populations
#11
L Yong, L Zhang, Y B N Wang, D J Yang, Z P Liu, T Wang, J P Huang, P P Zhou
Objective: To analyze liquid milk exposure of thiocyanate among Chinese population and preliminarily assess its health risk. Methods: A total of 2 059 raw milk samples were collected during 2013 and 2014 from 12 Chinese provinces, New Zealand and Netherlands. Farms were chosed according to the main sources of dairy companies, the distribution of farms and the yield of milk. Content of thiocyanate were detected by ion chromatography. Liquid milk consumption data were taken from Chinese beverage and alcoholic beverage consumption survey in 18 cities or counties in 9 provinces, including 16 775 subjects older than 3...
April 6, 2017: Zhonghua Yu Fang Yi Xue za Zhi [Chinese Journal of Preventive Medicine]
https://www.readbyqxmd.com/read/28394107/prevalence-type-and-etiology-of-dental-and-soft-tissue-injuries-in-children-in-croatia
#12
Josip Škaričić, Marko Vuletić, Sandra Hrvatin, Jesenka Jeličić, Ivana Čuković-Bagić
The prevalence, type and etiology of dental and soft tissue injuries and relationship between the time of arrival and sustaining soft tissue injury were analyzed in this retrospective study conducted at the Department of Pediatric Dentistry, University Dental Clinic in Zagreb, Croatia, during the 2010-2014 period using documentation on 447 patients (264 male and 183 female) aged 1-16 years with injuries of primary and permanent teeth. The highest prevalence of traumatic dental injury (TDI) was found in the 7-12 age group and maxillary central incisors were most frequently affected (80...
June 2016: Acta Clinica Croatica
https://www.readbyqxmd.com/read/28392276/studies-of-cdk-8-19-inhibitors-discovery-of-novel-and-selective-cdk8-19-dual-inhibitors-and-elimination-of-their-cyp3a4-time-dependent-inhibition-potential
#13
Jun Fujimoto, Takaharu Hirayama, Yasuhiro Hirata, Yukiko Hikichi, Saomi Murai, Maki Hasegawa, Yuka Hasegawa, Kazuko Yonemori, Akito Hata, Kazunobu Aoyama, Douglas R Cary
In this article, synthetic studies around a pyridylacrylamide-based hit compound (1), utilizing structure-based drug design guided by CDK8 docking models, is discussed. Modification of the pendant 4-fluorophenyl group to various heteroaromatic rings was conducted aiming an interaction with the proximal amino acids, and then replacement of the morpholine ring was targeted for decreasing potential of time-dependent CYP3A4 inhibition. These efforts led to the compound 4k, with enhanced CDK8 inhibitory activity and no apparent potential for time-dependent CYP3A4 inhibition (CDK8 IC50: 2...
March 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28388489/serial-measures-of-cardiac-performance-using-tissue-doppler-imaging-velocity-in-preterm-infants-29weeks-gestations
#14
Colm R Breatnach, Afif El-Khuffash, Adam James, Naomi McCallion, Orla Franklin
INTRODUCTION: Tissue Doppler imaging (TDI) is a useful marker of myocardial performance in preterm infants. We aimed to demonstrate serial changes in TDI velocity in preterm infants <29weeks gestation, to assess the impact of inotropes and a haemodynamically significant patent ductus arteriosus (hsPDA). METHODS: This was a prospective observational study of preterm infants <29weeks gestation. Echocardiography was performed at days 1, 2, 5-7 and at 36weeks, or before hospital discharge...
April 4, 2017: Early Human Development
https://www.readbyqxmd.com/read/28385400/nanomicelle-curcumin-induced-dna-fragmentation-in-testicular-tissue-correlation-between-mitochondria-dependent-apoptosis-and-failed-pcna-related-hemostasis
#15
Sana Moshari, Vahid Nejati, Gholamreza Najafi, Mazdak Razi
Current study was done to assess possible anti-proliferative effect of nanomicelle curcumin (NMCM) against germ cells in testicular tissue. For this purpose, 24 mature male Wistar rats were divided into control and test groups. The animals in test groups received 7.5mg/kg, 15mg/kg and 30mg/kg of NMC (NO=6 rats in each group). Following 48days, the expression of Bcl-2, Bax, caspase-3, P53 and proliferating cell nuclear antigen (PCNA) were evaluated by using reverse transcription-PCR and immunohistochemistry...
April 3, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28378431/left-ventricular-biomechanics-in-professional-football-players
#16
Thomas G von Lueder, Anders Hodt, Gard F Gjerdalen, Kjetil Steine
Chronic exercise induces adaptive changes of left ventricular (LV) ejection and filling capacities which may be detected by novel speckle-tracking echocardiography (STE) and tissue Doppler imaging (TDI)-based techniques. 103 consecutive male elite Norwegian soccer players and 46 age-matched healthy controls underwent echocardiography at rest. STE was used to assess LV torsional mechanics and LV systolic longitudinal strain (LS). Diastolic function was evaluated by trans-mitral blood flow, mitral annular velocities by TDI, and LV inflow propagation velocity by colour M-mode...
April 4, 2017: Scandinavian Journal of Medicine & Science in Sports
https://www.readbyqxmd.com/read/28351903/diaphragm-muscle-thinning-in-subjects-receiving-mechanical-ventilation-and-its-effect-on-extubation
#17
Horiana B Grosu, David E Ost, Young Im Lee, Juhee Song, Liang Li, Edward Eden, Keith Rose
BACKGROUND: Diaphragm muscle weakness and atrophy are consequences of prolonged mechanical ventilation. Our purpose was to determine whether thickness of the diaphragm (TDI) changes over time after intubation and whether the degree of change affects clinical outcome. METHODS: For this prospective, longitudinal observational study, we identified subjects who required mechanical ventilation and measured their TDI by ultrasonography. TDI was measured at baseline and repeated 72 h later and then weekly until the subject was either liberated from mechanical ventilation, was referred for tracheostomy, or died...
March 28, 2017: Respiratory Care
https://www.readbyqxmd.com/read/28329851/short-tslp-attenuates-toluene-diisocyanate-tdi-induced-airway-inflammation-and-inhibits-hmgb1-rage-and-long-tslp-expression
#18
Yanhong Wang, Yanqing Le, Wenqu Zhao, Yun Lin, Yue Wu, Changhui Yu, Jing Xiong, Fei Zou, Hangming Dong, Shaoxi Cai, Haijin Zhao
Short thymic stromal lymphopoietin (short TSLP), one of TSLP variants, exerts anti-inflammatory activities in endotoxin shock and colitis mouse models. Our latest work reported that short TSLP prevented house dust mite (HDM)-induced epithelial barrier disruption. Yet the role of short TSLP in toluene diisocyanate (TDI)-induced asthma is unknown. Male BALB/c mice were sensitized and challenged with TDI to generate a chemical-induced asthma model. Synthetic short TSLP peptides were given intranasally (i.n.) or intraperitoneally (i...
February 27, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28328090/bronchiolitis-score-of-sant-joan-de-d%C3%A3-u-brosjod-score-validation-and-usefulness
#19
Mònica Balaguer, Carme Alejandre, David Vila, Elisabeth Esteban, Josep L Carrasco, Francisco José Cambra, Iolanda Jordan
OBJECTIVE: To validate the bronchiolitis score of Sant Joan de Déu (BROSJOD) and to examine the previously defined scoring cutoff. PATIENTS AND METHODS: Prospective, observational study. BROSJOD scoring was done by two independent physicians (at admission, 24 and 48 hr). Internal consistency of the score was assessed using Cronbach's α. To determine inter-rater reliability, the concordance correlation coefficient estimated as an intraclass correlation coefficient (CCC) and limits of agreement estimated as the 90% total deviation index (TDI) were estimated...
April 2017: Pediatric Pulmonology
https://www.readbyqxmd.com/read/28324649/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-pharmacokinetics-and-metabolic-properties-to-obtain-atropisomeric-quinolinone-am-0466-that-affords-robust-in-vivo-activity
#20
Russell F Graceffa, Alessandro A Boezio, Jessica Able, Steven Altmann, Loren M Berry, Christiane Boezio, John R Butler, Margaret Chu-Moyer, Melanie Cooke, Erin F DiMauro, Thomas A Dineen, Elma Feric Bojic, Robert S Foti, Robert T Fremeau, Angel Guzman-Perez, Hua Gao, Hakan Gunaydin, Hongbing Huang, Liyue Huang, Christopher Ilch, Michael Jarosh, Thomas Kornecook, Charles R Kreiman, Daniel S La, Joseph Ligutti, Benjamin C Milgram, Min-Hwa Jasmine Lin, Isaac E Marx, Hanh N Nguyen, Emily A Peterson, Gwen Rescourio, John Roberts, Laurie Schenkel, Roman Shimanovich, Brian A Sparling, John Stellwagen, Kristin Taborn, Karina R Vaida, Jean Wang, John Yeoman, Violeta Yu, Dawn Zhu, Bryan D Moyer, Matthew M Weiss
Because of its strong genetic validation, NaV1.7 has attracted significant interest as a target for the treatment of pain. We have previously reported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. Herein, we report the discovery and optimization of a series of atropisomeric quinolinone sulfonamide inhibitors [ Bicyclic sulfonamide compounds as sodium channel inhibitors and their preparation . WO 2014201206, 2014 ] of NaV1...
April 20, 2017: Journal of Medicinal Chemistry
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