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https://www.readbyqxmd.com/read/28550799/in%C3%A2-vivo-assessment-of-dermal-adhesion-penetration-and-bioavailability-of-tetrabromobisphenol-a
#1
Yunjiang Yu, Liangzhong Li, Hongyan Li, Xiaowei Yu, Yanping Zhang, Qiong Wang, Zhixiang Zhou, Dandan Gao, Hao Ye, Bigui Lin, Ruixue Ma
Individuals are exposed to brominated flame retardants (BFRs), including tetrabromobisphenol A (TBBPA), on a daily basis because of their widespread usage. These compounds may have adverse effects on human health. In the present study, dermal absorption experiments were conducted in vivo to predict the adhesion, penetration, and bioavailability of TBBPA. TBBPA was administered to Wistar rats for 6 h by repeated dermal exposure at doses of 20, 60, 200, and 600 mg of TBBPA per kg of body weight (bw). The skin adhesion coefficient (AC) was calculated using a difference-value method and ranged from 0...
May 24, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28550754/linear-polysialoside-outperforms-dendritic-analogs-for-inhibition-of-influenza-virus-infection-in%C3%A2-vitro-and-in%C3%A2-vivo
#2
Sumati Bhatia, Daniel Lauster, Markus Bardua, Kai Ludwig, Stefano Angioletti-Uberti, Nicole Popp, Ute Hoffmann, Florian Paulus, Matthias Budt, Marlena Stadtmüller, Thorsten Wolff, Alf Hamann, Christoph Böttcher, Andreas Herrmann, Rainer Haag
Inhibition of influenza A virus infection by multivalent sialic acid inhibitors preventing viral hemagglutinin binding to host cells of the respiratory tract is a promising strategy. However, optimal geometry and optimal ligand presentation on multivalent scaffolds for efficient inhibition both in vitro and in vivo application are still unclear. Here, by comparing linear and dendritic polyglycerol sialosides (LPGSA and dPGSA) we identified architectural requirements and optimal ligand densities for an efficient multivalent inhibitor of influenza virus A/X31/1 (H3N2)...
May 20, 2017: Biomaterials
https://www.readbyqxmd.com/read/28550753/catalase-loaded-cisplatin-prodrug-constructed-liposomes-to-overcome-tumor-hypoxia-for-enhanced-chemo-radiotherapy-of-cancer
#3
Rui Zhang, Xuejiao Song, Chao Liang, Xuan Yi, Guosheng Song, Yu Chao, Yu Yang, Kai Yang, Liangzhu Feng, Zhuang Liu
Aiming at improved therapeutic efficacies, the combination of chemotherapy and radiotherapy (chemo-radiotherapy) has been widely studied and applied in clinic. However, the hostile characteristics of tumor microenvironment such as hypoxia often limit the efficacies in both types of cancer therapies. Herein, catalase (CAT), an antioxidant enzyme, is encapsulated inside liposomes constituted by cisplatin (IV)-prodrug-conjugated phospholipid, forming CAT@Pt (IV)-liposome for enhanced chemo-radiotherapy of cancer...
May 18, 2017: Biomaterials
https://www.readbyqxmd.com/read/28550752/intracellular-delivery-of-oligonucleotides-in-helicobacter-pylori-by-fusogenic-liposomes-in-the-presence-of-gastric-mucus
#4
Rita S Santos, George R Dakwar, Elisa Zagato, Toon Brans, Céu Figueiredo, Koen Raemdonck, Nuno F Azevedo, Stefaan C De Smedt, Kevin Braeckmans
The rising antimicrobial resistance contributes to 25000 annual deaths in Europe. This threat to the public health can only be tackled if novel antimicrobials are developed, combined with a more precise use of the currently available antibiotics through the implementation of fast, specific, diagnostic methods. Nucleic acid mimics (NAMs) that are able to hybridize intracellular bacterial RNA have the potential to become such a new class of antimicrobials and additionally could serve as specific detection probes...
May 20, 2017: Biomaterials
https://www.readbyqxmd.com/read/28550732/reversing-the-polarization-of-tumor-associated-macrophages-inhibits-tumor-metastasis
#5
Rufei Yuan, Shengfu Li, Hua Geng, Xin Wang, Qinglin Guan, Xiaohuan Li, Changle Ren, Xiaolin Yuan
OBJECTIVE: The M2 phenotype is dominant in tumor associated macrophages (TAM), and plays a key role in promoting tumor growth, invasion and metastasis. Converting TAM polarization from M2 to M1 may contribute to eliciting anti-tumor-specific immune responses and inhibiting tumor metastasis. In this study, the effect of reversing the polarization of TAM on tumor metastasis was investigated. METHODS: Peritoneal macrophages were obtained from BABL/c mice, and M2 polarization was induced by IL-4...
May 24, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28550719/morphometric-analysis-of-thalamic-volume-in-progressive-supranuclear-palsy-in-vivo-evidence-of-regionally-specific-bilateral-thalamic-atrophy
#6
Brian D Power, David Jakabek, Mitchell Hunter-Dickson, Fiona A Wilkes, Danielle van Westen, Alexander F Santillo, Mark Walterfang, Dennis Velakoulis, Christer Nilsson, Jeffrey C L Looi
We investigated whether differences were detectable in the volume and shape of the dorsal thalamus on magnetic resonance imaging in patients with progressive supranuclear palsy (PSP). Manual segmentation of the left and right thalami on magnetic resonance imaging scans occurred in 22 patients with clinically diagnosed PSP and 23 healthy controls; thalamic volumes (left, right, total) were calculated. Between group differences were explored by multivariate analysis of co-variance, using age and intracranial volume as covariates...
May 17, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28550649/improved-formula-see-text-determination-in-23-na-35-cl-and-17-o-mri-using-iterative-partial-volume-correction-based-on-1-h-mri-segmentation
#7
Sebastian C Niesporek, Reiner Umathum, Thomas M Fiedler, Peter Bachert, Mark E Ladd, Armin M Nagel
OBJECTIVE: Functional parameters can be measured with the help of quantitative non-proton MRI where exact relaxometry parameters are needed. Investigation of [Formula: see text] is often biased by strong partial volume (PV) effects. Hence, in this work a PV correction algorithm approach was evaluated that uses iteratively adapted [Formula: see text]-values and high-resolution structural (1)H data to determine transverse relaxation in non-proton MRI more accurately. MATERIALS AND METHODS: Simulations, a phantom study and in vivo (23)Na, (17)O and (35)Cl MRI measurements of five healthy volunteers were performed to evaluate the algorithm...
May 26, 2017: Magma
https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#8
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28550532/drug-induced-hsp90-inhibition-alleviates-pain-in-monoarthritic-rats-and-alters-the-expression-of-new-putative-pain-players-at-the-drg
#9
Diana Sofia Marques Nascimento, Catarina Soares Potes, Miguel Luz Soares, António Carlos Ferreira, Marzia Malcangio, José Manuel Castro-Lopes, Fani Lourença Moreira Neto
Purinergic receptors (P2XRs) have been widely associated with pain states mostly due to their involvement in neuron-glia communication. Interestingly, we have previously shown that satellite glial cells (SGC), surrounding dorsal root ganglia (DRG) neurons, become activated and proliferate during monoarthritis (MA) in the rat. Here, we demonstrate that P2X7R expression increases in ipsilateral DRG after 1 week of disease, while P2X3R immunoreactivity decreases. We have also reported a significant induction of the activating transcriptional factor 3 (ATF3) in MA...
May 26, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28550455/-effects-of-the-novel-relatively-short-acting-kappa-opioid-receptor-antagonist-ly2444296-in-behaviors-observed-after-chronic-extended-access-cocaine-self-administration-in-rats
#10
Marta Valenza, Eduardo R Butelman, Mary Jeanne Kreek
RATIONALE: The recruitment of the stress circuitry contributes to a shift from positive to negative reinforcement mechanisms sustaining long-term cocaine addiction. The kappa opioid receptor (KOPr) signaling is upregulated by stress and chronic cocaine exposure. While KOPr agonists induce anhedonia and dysphoria, KOPr antagonists display antidepressant and anxiolytic properties. Most of the knowledge on KOPr antagonism is based on drugs with unusual pharmacokinetic and pharmacodynamic properties, complicating interpretation of results...
May 27, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28550454/oncogenic-roles-of-the-pi3k-akt-mtor-axis
#11
Masahiro Aoki, Teruaki Fujishita
The PI3K/AKT/mTOR pathway is frequently activated in various human cancers and has been considered a promising therapeutic target. Many of the positive regulators of the PI3K/AKT/mTOR axis, including the catalytic (p110α) and regulatory (p85α), of class IA PI3K, AKT, RHEB, mTOR, and eIF4E, possess oncogenic potentials, as demonstrated by transformation assays in vitro and by genetically engineered mouse models in vivo. Genetic evidences also indicate their roles in malignancies induced by activation of the upstream oncoproteins including receptor tyrosine kinases and RAS and those induced by the loss of the negative regulators of the PI3K/AKT/mTOR pathway such as PTEN, TSC1/2, LKB1, and PIPP...
May 28, 2017: Current Topics in Microbiology and Immunology
https://www.readbyqxmd.com/read/28550405/projective-biomechanical-depth-matching-for-soft-tissue-registration-in-laparoscopic-surgery
#12
Daniel Reichard, Dominik Häntsch, Sebastian Bodenstedt, Stefan Suwelack, Martin Wagner, Hannes Kenngott, Beat Müller-Stich, Lena Maier-Hein, Rüdiger Dillmann, Stefanie Speidel
PURPOSE: A key component of computer- assisted surgery systems is the accurate and robust registration of preoperative planning data with intraoperative sensor data. In laparoscopic surgery, this image-based registration remains challenging due to soft tissue deformations. This paper presents a novel approach for biomechanical soft tissue registration of preoperative CT data with stereo endoscopic image data. METHODS: The proposed method consists of two registrations steps...
May 26, 2017: International Journal of Computer Assisted Radiology and Surgery
https://www.readbyqxmd.com/read/28550404/development-of-an-imaging-system-for-in-vivo-real-time-monitoring-of-neuronal-activity-in-deep-brain-of-free-moving-rats
#13
Norio Iijima, Shinji Miyamoto, Keisuke Matsumoto, Ken Takumi, Yoichi Ueta, Hitoshi Ozawa
We have newly developed a system that allows monitoring of the intensity of fluorescent signals from deep brains of rats transgenically modified to express enhanced green fluorescent protein (eGFP) via an optical fiber. One terminal of the optical fiber was connected to a blue semiconductor laser oscillator/green fluorescence detector. The other terminal was inserted into the vicinity of the eGFP-expressing neurons. Since the optical fiber was vulnerable to twisting stresses caused by animal movement, we also developed a cage in which the floor automatically turns, in response to the turning of the rat's head...
May 26, 2017: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/28550361/prolyl-hydroxylase-inhibition-induces-sdf-1-associated-with-increased-cxcr4-cd11b-subpopulations-and-cardiac-repair
#14
Santhosh Kumar Ghadge, Moritz Messner, Thi Van Pham, Maximilian Doppelhammer, Andreas Petry, Agnes Görlach, Britta Husse, Wolfgang-Michael Franz, Marc-Michael Zaruba
SDF-1/CXCR4 activation facilitates myocardial repair. Therefore, we aimed to activate the HIF-1α target genes SDF-1 and CXCR4 by dimethyloxalylglycine (DMOG)-induced prolyl-hydroxylase (PH) inhibition to augment CXCR4+ cell recruitment and myocardial repair. SDF-1 and CXCR4 expression was analyzed under normoxia and ischemia ± DMOG utilizing SDF-1-EGFP and CXCR4-EGFP reporter mice. In bone marrow and heart, CXCR4-EGFP was predominantly expressed in CD45+/CD11b+ leukocytes which significantly increased after myocardial ischemia...
May 26, 2017: Journal of Molecular Medicine: Official Organ of the "Gesellschaft Deutscher Naturforscher und Ärzte"
https://www.readbyqxmd.com/read/28550358/visualization-of-a-cam-type-femoroacetabular-impingement-while-squatting-using-image-matching-techniques-a-case-report
#15
Kensei Yoshimoto, Satoshi Hamai, Hidehiko Higaki, Hirotaka Gondoh, Yasuharu Nakashima
The in vivo assessment of the three-dimensional (3D) kinematics of the hip in patients with femoroacetabular impingement (FAI) under weight-bearing conditions has not been previously reported. We evaluated the pre- and postoperative hip kinematics of a 34-year-old man, with a cam-type FAI while squatting, using image-matching techniques with measurement of the rim-neck distance. Post-osteochondroplasty, the α-angle improved from 51.0° to 35.5° and the head-neck offset ratio from 0.04 to 0.23. Coxalgia during squatting disappeared, and the Harris Hip Score improved from 79 to 92 at 1 year post-surgery...
May 27, 2017: Skeletal Radiology
https://www.readbyqxmd.com/read/28550311/organoid-based-epithelial-to-mesenchymal-transition-oemt-model-from-an-intestinal-fibrosis-perspective
#16
Soojung Hahn, Myeong-Ok Nam, Jung Hyun Noh, Dong Hyeon Lee, Hyun Wook Han, Duk Hwan Kim, Ki Baik Hahm, Sung Pyo Hong, Jun-Hwan Yoo, Jongman Yoo
The current in vitro or in vivo intestinal fibrosis models have many limitations. Recent advancements in the isolation and culturing of organoids has led to development of various three-dimensional (3D) intestinal disease models with in vivo physiology. In this study, we generated an organoid-based epithelial to mesenchymal transition (OEMT) model, which could be used as a novel intestinal fibrosis model. Intestinal epithelial organoids (IEOs) were isolated and cultured from the small intestines of normal mice...
May 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28550308/fortilin-binds-ire1%C3%AE-and-prevents-er-stress-from-signaling-apoptotic-cell-death
#17
Decha Pinkaew, Abhijnan Chattopadhyay, Matthew D King, Preedakorn Chunhacha, Zhihe Liu, Heather L Stevenson, Yanjie Chen, Patuma Sinthujaroen, Owen M McDougal, Ken Fujise
The endoplasmic reticulum, the cytoplasmic organelle that matures a massive amount of nascent secretory polypeptides, is particularly sensitive to stress. Endoplasmic reticulum stress causes unfolded proteins to populate the organelle, eliciting the unfolded protein response. During the unfolded protein response, GRP78-an endoplasmic reticulum master stress regulator-detaches from three endoplasmic reticulum stress sensors (IRE1α, PERK, and ATF6) and allows them to activate the apoptotic signaling pathway...
May 26, 2017: Nature Communications
https://www.readbyqxmd.com/read/28550295/effects-of-protein-corona-on-iapp-amyloid-aggregation-fibril-remodelling-and-cytotoxicity
#18
Emily H Pilkington, Yanting Xing, Bo Wang, Aleksandr Kakinen, Miaoyi Wang, Thomas P Davis, Feng Ding, Pu Chun Ke
Aggregation of islet amyloid polypeptide (IAPP), a peptide hormone co-synthesized and co-stored with insulin in pancreatic cells and also co-secreted to the circulation, is associated with beta-cell death in type-2 diabetes (T2D). In T2D patients IAPP is found aggregating in the extracellular space of the islets of Langerhans. Although the physiological environments of these intra- and extra-cellular compartments and vascular systems significantly differ, the presence of proteins is ubiquitous but the effects of protein binding on IAPP aggregation are largely unknown...
May 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28550279/cinnamon-induces-browning-in-subcutaneous-adipocytes
#19
Hiu Yee Kwan, Jiahui Wu, Tao Su, Xiao-Juan Chao, Bin Liu, Xiuqiong Fu, Chi Leung Chan, Rebecca Hiu Ying Lau, Anfernee Kai Wing Tse, Quan Bin Han, Wang Fun Fong, Zhi-Ling Yu
Browning is the process of increasing the number of brite cells, which helps to increase energy expenditure and reduce obesity. Consumption of natural and non-toxic herbal extracts that possess the browning effect is an attractive anti-obesity strategy. In this study, we examined the browning effect of cinnamon extract. We found that cinnamon extract (CE) induced typical brown adipocyte multiocular phenotype in 3T3-L1 adipocytes. The treatment also increased brown adipocytes markers and reduced white adipocytes markers in the 3T3-L1 adipocytes...
May 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#20
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
May 25, 2017: Journal of Alzheimer's Disease: JAD
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