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https://www.readbyqxmd.com/read/29150561/influence-of-enzalutamide-on-cabazitaxel-pharmacokinetics-a-drug-drug-interaction-study-in-metastatic-castration-resistant-prostate-cancer-mcrpc-patients
#1
Bodine P S Belderbos, Sander Bins, Roelof W F van Leeuwen, Esther Oomen-de Hoop, Nelly van der Meer, Peter de Bruijn, Paul Hamberg, Esther N M Overkleeft, Wendy M van der Deure, Martijn Lolkema, Ronald de Wit, Ron H J Mathijssen
PURPOSE: In ongoing clinical research on metastatic castration-resistant prostate cancer (mCRPC) treatment, the potential enhanced efficacy of the combination of taxanes with AR-targeted agents, i.e. enzalutamide and abiraterone, is currently being explored. Since enzalutamide induces the CYP3A4 enzyme and taxanes are metabolized by this enzyme, a potential drug-drug interaction needs to be investigated. DESIGN: Therefore, we performed a pharmacokinetic cross-over study in mCRPC patients who were scheduled for treatment with cabazitaxel Q3W (25 mg/m(2))...
November 17, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29150544/estimation-of-circulating-drug-metabolite-exposure-in-human-using-in-vitro-data-and-physiologically-based-pharmacokinetic-modelling-example-of-a-high-metabolite-parent-drug-ratio
#2
R Scott Obach, Jian Lin, Emi Kimoto, Sridhar Duvvuri, Timothy Nicholas, Eugene P Kadar, Larry M Tremaine, Aarti Sawant Basak
TBPT ((R)-4-((4-(((4-((tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol), a serotonin-4 receptor partial agonist, is metabolized to two metabolites: an N-dealkylation product (M1) and a cyclized oxazolidine structure (M2). After administration to humans, the exposure to M1 was low and the exposure to M2 was high, relative to the parent drug, despite this being the opposite in vitro. In this study, projection of the plasma metabolite/parent ratios for M1 and M2 was attempted, using in vitro metabolism, binding, and permeability data in static and dynamic PBPK models...
November 17, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29149454/melatonin-alleviates-adipose-inflammation-through-elevating-%C3%AE-ketoglutarate-and-diverting-adipose-derived-exosomes-to-macrophages-in-mice
#3
Zhenjiang Liu, Lu Gan, Tiantian Zhang, Qian Ren, Chao Sun
Obesity is associated with macrophage infiltration and metabolic inflammation, both of which promote metabolic disease progression. Melatonin is reported to possess anti-inflammatory properties by inhibiting inflammatory response of adipocytes and macrophages activation. However, the effects of melatonin on the communication between adipocytes and macrophages during adipose inflammation remain elusive. Here, we demonstrated melatonin alleviated inflammation and elevated α-ketoglutarate (αKG) level in adipose tissue of obese mice...
November 17, 2017: Journal of Pineal Research
https://www.readbyqxmd.com/read/29149305/rituximab-for-non-responsive-idiopathic-membranous-nephropathy-in-a-chinese-cohort
#4
Xin Wang, Zhao Cui, Yi-Miao Zhang, Zhen Qu, Fang Wang, Li-Qiang Meng, Xu-Yang Cheng, Gang Liu, Fu-de Zhou, Ming-Hui Zhao
Background: Rituximab had been shown to be effective in inducing remission of nephrotic syndrome in patients with idiopathic membranous nephropathy (iMN). This study applied rituximab therapy for 36 non-responsive iMN patients to investigate its effects and safety. Methods: Thirty-six iMN patients who were non-responsive to prior immunosuppression were enrolled. Rituximab was used for B-cell depletion in patients, with a goal of <5 B cells/mm3 in the circulation...
November 14, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/29148706/porous-carbon-with-willow-leaf-shaped-pores-for-high-performance-supercapacitors
#5
Yanhong Shi, Lin-Lin Zhang, Tyler B Schon, Huan-Huan Li, Chao-Ying Fan, Xiao-Ying Li, Hai-Feng Wang, Xing-Long Wu, Haiming Xie, Haizhu Sun, Dwight S Seferos, Jingping Zhang
A novel kind of biomass-derived high oxygen containing carbon materials doped with nitrogen that have willow leaf shaped pores was synthesized. The obtained carbon materials have an exotic hierarchical pore structure composed of bowl shaped macropores, willow leaf shaped pores, and an abundance of micropores. This unique hierarchical porous structure provides an effective combination of high current densities with high capacitance due to a pseudocapacitive component that is afforded by the introduction of nitrogen and oxygen dopants...
November 17, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29148629/carbohydrate-mouth-rinse-improves-cycling-performance-carried-out-until-the-volitional-exhaustion
#6
Bruno Bavaresco Gambassi, Ylana Gomes de Santana Barros Leal, Edson R Pinheiro Dos Anjos, Bruna A Antonelli, Daniela C Gomes Gonçalves E Silva, Iracema H Pires de Mélo Montenegro, Rita di Cássia de Oliveira Angelo, Isis S Correia Moura, Paulo A Schwingel
BACKGROUND: Carbohydrates (CHO) are among the most investigated nutritional ergogenic aids, and may be consumed in different forms, e.g., mouth rinse with carbohydrate solution (MRCS). In this sense, the aim of this study was to evaluate the impact of MRCS on the performance of physically active individuals undergoing a physical exercise session carried out until the volitional exhaustion. METHODS: This is a counter-balanced randomized study, with a double-blind design...
November 17, 2017: Journal of Sports Medicine and Physical Fitness
https://www.readbyqxmd.com/read/29148627/assessment-of-endpoint-criteria-and-perceived-barriers-during-maximal-cardiorespiratory-fitness-testing-among-pregnant-women
#7
Caitlin M Hesse, Rachel A Tinius, Bailey J Cooley, Alyssa A Olenick, Maire M Blankenship, Donald L Hoover, Jill M Maples
BACKGROUND: A plateau in volume of oxygen consumption (VO2) is the primary indicator for determining if an individual has reached their maximal aerobic capacity. However, secondary criteria can also be used to identify maximal effort (i.e. lactate level, rating of perceived exertion (RPE), percent of age-predicted maximal heart rate (HR) and respiratory exchange ratio (RER)). Age and gender-specific secondary criteria have been developed for the general population, but no secondary criteria have been established for pregnant women...
November 17, 2017: Journal of Sports Medicine and Physical Fitness
https://www.readbyqxmd.com/read/29148603/mcp2-activates-nf-%C3%AE%C2%BAb-signaling-pathway-promoting-the-migration-and-invasion-of-escc-cells
#8
Jian Zhou, Shutao Zheng, Tao Liu, Qing Liu, Yumei Chen, Doudou Tan, Rong Ma, Xiaomei Lu
MCP2, aliased CCL8, has been suggested to be implicated in the metastasis of cancer cells; however no direct evidence has been established in esophageal squamous cell carcinoma (ESCC). In our present study, to investigate the role MCP2 played in the metastasis of ESCC cells; in vitro cell co-culture system was established. Wound-healing and Transwell assays were used to evaluate the migratory and invasive variation of ESCC cells before and after treatment with recombinant human MCP2. It was shown that MCP2 was able to activate the NF-κB signaling pathway inducing the epithelial-mesenchymal transition (EMT) and promoting the migration and invasion of ESCC cells in vitro...
November 17, 2017: Cell Biology International
https://www.readbyqxmd.com/read/29148269/salidroside-attenuates-neuroinflammation-and-improves-functional-recovery-after-spinal-cord-injury-through-microglia-polarization-regulation
#9
Chenggui Wang, Qingqing Wang, Yiting Lou, Jianxiang Xu, Zhenhua Feng, Yu Chen, Qian Tang, Gang Zheng, Zengjie Zhang, Yaosen Wu, Naifeng Tian, Yifei Zhou, Huazi Xu, Xiaolei Zhang
Spinal cord injury (SCI) is a severe neurological disease; however, few drugs have been proved to treat SCI effectively. Neuroinflammation is the major pathogenesis of SCI secondary injury and considered to be the therapeutic target of SCI. Salidroside (Sal) has been reported to exert anti-inflammatory effects in airway, adipose and myocardial tissue; however, the role of Sal in SCI therapeutics has not been clarified. In this study, we showed that Sal could improve the functional recovery of spinal cord in rats as revealed by increased BBB locomotor rating scale, angle of incline, and decreased cavity of spinal cord injury and apoptosis of neurons in vivo...
November 17, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29147994/printability-of-papers-recycled-from-toner-and-inkjet-printed-papers-after-deinking-and-recycling-processes
#10
Arif Karademir, Cem Aydemir, Dogan Tutak, Raja Aravamuthan
BACKGROUND: In our contemporary world, while part of the fibers used in the paper industry is obtained from primary fibers such as wood and agricultural plants, the rest is obtained from secondary fibers from waste papers. To manufacture paper with high optical quality from fibers of recycled waste papers, these papers require deinking and bleaching of fibers at desired levels. High efficiency in removal of ink from paper mass during recycling, and hence deinkability, are especially crucial for the optical and printability quality of the ultimate manufactured paper...
November 11, 2017: Journal of Applied Biomaterials & Functional Materials
https://www.readbyqxmd.com/read/29147812/geissoschizine-synthase-controls-flux-in-the-formation-of-monoterpenoid-indole-alkaloids-in-a-catharanthus-roseus-mutant
#11
Yang Qu, Antje M K Thamm, Matthew Czerwinski, Sayaka Masada, Kyung Hee Kim, Graham Jones, Ping Liang, Vincenzo De Luca
A Catharanthus roseus mutant accumulates high levels of ajmalicine at the expense of catharanthine and vindoline. The altered chemistry depends on increased expression and biochemical activities of strictosidine β-glucosidase and ajmalicine synthase activities and reduced expression and biochemical activity of geissoschizine synthase. The Madagascar periwinkle [Catharanthus roseus (L.) G. Don] is a commercially important horticultural flower species and is a valuable source for several monoterpenoid indole alkaloids (MIAs), such as the powerful antihypertensive drug ajmalicine and the antineoplastic agents, vinblastine and vincristine...
November 17, 2017: Planta
https://www.readbyqxmd.com/read/29146830/mechanical-thrombectomy-performs-similarly-in-real-world-practice-a-2016-nationwide-study-from-the-czech-republic
#12
Ondrej Volny, Antonin Krajina, Silvie Belaskova, Michal Bar, Petra Cimflova, Roman Herzig, Daniel Sanak, Ales Tomek, Martin Köcher, Miloslav Rocek, Radek Padr, Filip Cihlar, Miroslava Nevsimalova, Lubomir Jurak, Roman Havlicek, Martin Kovar, Petr Sevcik, Vladimir Rohan, Jan Fiksa, Bijoy K Menon, Robert Mikulik
BACKGROUND: Randomized clinical trials have proven mechanical thrombectomy (MT) to be a highly effective and safe treatment in acute stroke. The purpose of this study was to compare neurothrombectomy data from the Czech Republic (CR) with data from the HERMES meta-analysis. METHODS: Available nationwide data for the CR from 2016 from the Safe Implementation of Treatments in Stroke-Thrombectomy (SITS-TBY) registry for patients with terminal internal carotid artery (ICA) and/or middle cerebral artery (MCA) occlusions were compared with data from HERMES...
November 16, 2017: Journal of Neurointerventional Surgery
https://www.readbyqxmd.com/read/29146235/macrophages-their-role-activation-and-polarization-in-pulmonary-diseases
#13
REVIEW
Shweta Arora, Kapil Dev, Beamon Agarwal, Pragnya Das, Mansoor Ali Syed
Macrophages, circulating in the blood or concatenated into different organs and tissues constitute the first barrier against any disease. They are foremost controllers of both innate and acquired immunity, healthy tissue homeostasis, vasculogenesis and congenital metabolism. Two hallmarks of macrophages are diversity and plasticity due to which they acquire a wobbling array of phenotypes. These phenotypes are appropriately synchronized responses to a variety of different stimuli from either the tissue microenvironment or - microbes or their products...
November 12, 2017: Immunobiology
https://www.readbyqxmd.com/read/29146225/response-comparison-of-multiple-myeloma-and-monoclonal-gammopathy-of-undetermined-significance-to-the-same-anti-myeloma-therapy-a-retrospective-cohort-study
#14
John P Campbell, Jennifer L J Heaney, Sankalp Pandya, Zaheer Afzal, Martin Kaiser, Roger Owen, J Anthony Child, David A Cairns, Walter Gregory, Gareth J Morgan, Graham H Jackson, Chris M Bunce, Mark T Drayson
BACKGROUND: Multiple myeloma is consistently preceded by monoclonal gammopathy of undetermined significance (MGUS), which is usually only treated by a form of anti-multiple myeloma therapy if it is causing substantial disease through deposition of secreted M proteins. However, studies comparing how MGUS and multiple myeloma plasma cell clones respond to these therapies are scarce. Biclonal gammopathy multiple myeloma is characterised by the coexistence of an active multiple myeloma clone and a benign MGUS clone, and thus provides a unique model to assess the responses of separate clones to the same anti-multiple myeloma therapy, in the same patient, at the same time...
November 13, 2017: Lancet Haematology
https://www.readbyqxmd.com/read/29145924/pharmacokinetic-interaction-between-bedaquiline-and-clofazimine-in-patients-with-drug-resistant-tuberculosis
#15
G Maartens, M J E Brill, M Pandie, E M Svensson
<h2>BACKGROUND:</h2>Bedaquiline (BDQ) and clofazimine (CFZ) are both recommended for treating drug-resistant tuberculosis (DR-TB). As CFZ is an inhibitor of the cytochrome P450 isoenzyme 3A4 (CYP3A4) in vitro, and BDQ a substrate of CYP3A4, there is a potential for pharmacokinetic (PK) drug-drug interaction that may result in increased BDQ exposure when co-administered with CFZ, which could increase the toxicity of BDQ.<h2>METHODS:</h2>We assessed the effect of co-administered CFZ on BDQ bioavailability, or on clearance of BDQ and its N-monodesmethyl metabolite (M2), in patients with DR-TB using a population PK model developed from data of patients with DR-TB...
November 16, 2017: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/29145790/innate-immunity-in-cardiac-myxomas-and-its-pathological-and-clinical-correlations
#16
Anna Di Vito, Gianluca Santise, Chiara Mignogna, Eusebio Chiefari, Gabriella Cardillo, Ivan Presta, Franco Arturi, Natalia Malara, Francesco Brunetti, Annalidia Donato, Domenico Maisano, Stefania Leonetti, Daniele Maselli, Tullio Barni, Giuseppe Donato
Cardiac myxomas are the most common benign cardiac tumor. We investigated the immunohistochemical properties of 11 surgically excised cardiac myxomas, in order to analyze the correlation between macrophages and mast cell populations and clinical parameters. CD68(+)/CD163(-)/iNOS(-) (M0) cells represent the most abundant macrophage phenotype; however, CD68(+)/CD163(+) cells (M2) were also frequent. CD68(+)/iNOS(+) (M1) elements were rare. Mast cells, defined as a population of c-kit (CD117)(+) and/or tryptase(+) cells were also detected...
January 1, 2017: Innate Immunity
https://www.readbyqxmd.com/read/29145722/outcomes-of-beating-heart-on-pump-utilizing-a-miniature-bypass-circuit-versus-off-pump-cardiac-bypass-at-a-veterans-affairs-medical-center
#17
Matthew Skancke, Kendal Endicott, Richard Amdur, Michael Greenberg, Gregory Trachiotis
BACKGROUND: Off-pump coronary artery bypass grafting (OPCAB) helps reduce systemic inflammatory changes by maintaining native pulsatile flow. This analysis evaluates the outcomes of OPCAB at a Veterans Affairs Medical Center (VAMC) and evaluates the use of beating heart on-pump (BHOP) bypass grafting as an empiric therapy for high-risk patients. METHODS: We performed a retrospective analysis of 756 patients who underwent coronary bypass grafting between 2004-2015 at a single VAMC...
November 16, 2017: Journal of Cardiovascular Surgery
https://www.readbyqxmd.com/read/29145517/which-patients-recur-as-atrial-tachycardia-rather-than-atrial-fibrillation-after-catheter-ablation-of-atrial-fibrillation
#18
Pil-Sung Yang, Young-Ah Park, Tae-Hoon Kim, Jae-Sun Uhm, Boyoung Joung, Moon-Hyoung Lee, Hui-Nam Pak
INTRODUCTION: The ablation gaps have been known as the main mechanism of recurrence as atrial tachycardia (AT) rather than atrial fibrillation (AF) after AF catheter ablation. However, AF organization due to reduction of critical mass or focal trigger may also be the mechanism of AT recurrence. We sought to find out the main clinical factors of recurrence as AT rather than AF after AF ablation in the absence of antiarrhythmic drug effect. METHODS: We analyzed 521 patients (70...
2017: PloS One
https://www.readbyqxmd.com/read/29145484/lifestyle-intervention-program-in-deprived-obese-adult-patients-and-their-non-deprived-counterparts
#19
Celine Loddo, Emilie Pupier, Rémy Amour, Maud Monsaingeon-Henry, Kamel Mohammedi, Blandine Gatta-Cherifi
INTRODUCTION: Although it is known that the prevalence of obesity is high in deprived patients, the link between deprivation and obesity, and the impact of deprivation on compliance and efficacy of a lifestyle intervention program are not known. MATERIALS AND METHODS: Deprivation was assessed in 40 patients (23 Females, mean±SD age: 49±17 years) from the diabetology department and 140 patients (101 Females, age: 50±15 years) from the nutrition department of Bordeaux University hospital...
2017: PloS One
https://www.readbyqxmd.com/read/29145305/prognostic-significance-of-metabolic-enzyme-pyruvate-kinase-m2-in-breast-cancer-a-meta-analysis
#20
Yiming Yang, Ke Wu, Yulin Liu, Liang Shi, Kaixiong Tao, Guobin Wang
BACKGROUNDS: Numerous studies have reported that aberrant pyruvate kinase M2 isoform (PKM2) expressed in cancer, indicating that PKM2 plays a critical role in tumor initiation and progression. Nevertheless, its prognostic value in breast cancer tumor is yet contentious. Therefore, we performed this meta-analysis to evaluate the prognostic significance of PKM2 in breast cancer. METHODS: Eligible relevant literatures were retrieved by searching PubMed, the Cochrane Library, Embase through December 2016...
November 2017: Medicine (Baltimore)
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