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https://www.readbyqxmd.com/read/28214870/the-inhibitory-effect-of-s-777469-a-cannabinoid-type-2-receptor-agonist-on-skin-inflammation-in-mice
#1
Takayo Haruna, Masahiko Soga, Yasuhide Morioka, Kinichi Imura, Yoko Furue, Mina Yamamoto, Jun Hayakawa, Masashi Deguchi, Akinori Arimura, Kiyoshi Yasui
We investigated the effects of S-777469 (1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1, 2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid), a novel cannabinoid type 2 receptor (CB2) agonist, on 1-fluoro-2,4-dinitrobenzene (DNFB)-induced ear inflammation and mite antigen-induced dermatitis in mice. The oral administration of S-777469 significantly suppressed DNFB-induced ear swelling in a dose-dependent manner. In addition, S-777469 significantly alleviated mite antigen-induced atopic dermatitis-like skin lesions in NC/Nga mice...
February 18, 2017: Pharmacology
https://www.readbyqxmd.com/read/28214849/lipopeptide-induced-suicidal-erythrocyte-death-correlates-with-the-degree-of-acylation
#2
Abdulla Al Mamun Bhuyan, Minh-Thu Nguyen, Rosi Bissinger, Friedrich Götz, Florian Lang
BACKGROUND/AIMS: Consequences of bacterial infection include anemia, which could result from stimulation of suicidal erythrocyte death or eryptosis, characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. Bacterial components known to stimulate eryptosis include lipopeptides. Signaling mediating the triggering of eryptosis include increased cytosolic Ca2+ activity ([Ca2+]<Sub>i</Sub>), oxidative stress and cellular accumulation of ceramide...
January 24, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28214842/inhibition-of-methylglyoxal-induced-ages-rage-expression-contributes-to-dermal-protection-by-n-acetyl-l-cysteine
#3
Chun-Tao Yang, Fu-Hui Meng, Li Chen, Xiang Li, Lai-Jian Cen, Yu-Hua Wen, Cai-Chen Li, Hui Zhang
BACKGROUND/AIM: Accumulation of advanced glycation end products (AGEs) is a major cause of diabetes mellitus (DM) skin complications. Methylglyoxal (MGO), a reactive dicarbonyl compound, is a crucial intermediate of AGEs generation. N-acetyl-L-cysteine (NAC), an active ingredient of some medicines, can induce endogenous GSH and hydrogen sulfide generation, and set off a condensation reaction with MGO. However, there is rare evidence to show NAC can alleviate DM-induced skin injury through inhibition of AGEs generation or toxicity...
13, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28214607/real-time-liver-uptake-and-biodistribution-of-magnetic-nanoparticles-determined-by-ac-biosusceptometry
#4
Caio C Quini, André G Próspero, Marcos F F Calabresi, Gustavo M Moretto, Nicholas Zufelato, Sunil Krishnan, Diana R Pina, Ricardo B Oliveira, Oswaldo Baffa, Andris F Bakuzis, Jose R A Miranda
We describe the development of a joint in vivo/ex vivo protocol to monitor magnetic nanoparticles in animal models. Alternating current biosusceptometry (ACB) enables the assessment of magnetic nanoparticle accumulation, followed by quantitative analysis of concentrations in organs of interest. We present a study of real-time liver accumulation, followed by the assessment of sequential biodistribution using the same technique. For quantification, we validated our results by comparing all of the data with electron spin resonance (ESR)...
February 15, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28214545/potential-of-amphiphilic-graft-copolymer-%C3%AE-tocopherol-succinate-g-carboxymethyl-chitosan-in-modulating-the-permeability-and-anticancer-efficacy-of-tamoxifen
#5
Sunil K Jena, Sanjaya K Samal, Shamandeep Kaur, Mahesh Chand, Abhay T Sangamwar
Recent studies showed an enhanced oral bioavailability of tamoxifen (TMX) by hydrophobically modified α-tocopherol succinate-g-carboxymethyl chitosan (Cmc-TS) micelles. As a continued effort, here we evaluated TMX-loaded polymeric micelles (TMX-PMs) for its enhanced permeability with increased anticancer efficacy and decreased hepatotoxicity. We employed co-solvent evaporation technique to encapsulate TMX into Cmc-TS. Apparent permeability assay of TMX-PMs was performed on Caco-2 cell line. The absorptive transport of TMX increased significantly about 3...
February 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28213091/convergence-of-hepcidin-deficiency-systemic-iron-overloading-heme-accumulation-and-rev-erb%C3%AE-%C3%AE-activation-in-aryl-hydrocarbon-receptor-elicited-hepatotoxicity
#6
Kelly A Fader, Rance Nault, Mathew P Kirby, Gena Markous, Jason Matthews, Timothy R Zacharewski
Persistent aryl hydrocarbon receptor (AhR) agonists elicit dose-dependent hepatic lipid accumulation, oxidative stress, inflammation, and fibrosis in mice. Iron (Fe) promotes AhR-mediated oxidative stress by catalyzing reactive oxygen species (ROS) production. To further characterize the role of Fe in AhR-mediated hepatotoxicity, male C57BL/6 mice were orally gavaged with sesame oil vehicle or 0.01-30μg/kg 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) every 4days for 28days. Duodenal epithelial and hepatic RNA-Seq data were integrated with hepatic AhR ChIP-Seq, capillary electrophoresis protein measurements, and clinical chemistry analyses...
February 14, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28212986/correlating-the-effects-of-antimicrobial-preservatives-on-conformational-stability-aggregation-propensity-and-backbone-flexibility-of-an-igg1-monoclonal-antibody
#7
Jayant Arora, Sangeeta B Joshi, C Russell Middaugh, David D Weis, David B Volkin
Multi-dose formulations of biotherapeutics, which offer better dosage management and reduced production costs, require the addition of antimicrobial preservatives (APs). APs have been shown, however, to decrease protein stability in solution and cause protein aggregation. In this report, the effect of four APs, m-cresol, phenol, phenoxyethanol and benzyl alcohol, on conformational stability, aggregation propensity and backbone flexibility of an IgG1 monoclonal antibody, mAb-4, is investigated. Compared to no preservative control, each of the APs decreased the conformational stability of mAb-4 as measured by DSC and extrinsic fluorescence spectroscopy...
February 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28212863/yghj-the-secreted-metalloprotease-of-pathogenic-e-coli-induces-hemorrhagic-fluid-accumulation-in-mouse-ileal-loop
#8
Rima Tapader, Dipro Bose, Amit Pal
YghJ, also known as SsLE (Secreted and surface associated lipoprotein) is a cell surface associated and secreted lipoprotein harbouring M60 metalloprotease domain. Though the gene is known to be conserved among both pathogenic and commensal E. coli isolates, the expression and secretion of YghJ was found to be higher among diverse Escherichia coli pathotypes. YghJ, secreted from intestinal pathogens such as enterotoxigenic E. coli (ETEC) and enteropathogenic E. coli (EPEC) has been demonstrated to possess mucinase activity and hence facilitates colonization of these enteric pathogens to intestinal epithelial cells...
February 14, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28212817/in-vivo-toxicity-of-copper-oxide-lead-oxide-and-zinc-oxide-nanoparticles-acting-in-different-combinations-and-its-attenuation-with-a-complex-of-innocuous-bio-protectors
#9
Ilzira A Minigalieva, Boris A Katsnelson, Vladimir G Panov, Larisa I Privalova, Anatoly N Varaksin, Vladimir B Gurvich, Marina P Sutunkova, Vladimir Ya Shur, Ekaterina V Shishkina, Irene E Valamina, Ilya V Zubarev, Oleg H Makeyev, Ekaterina Y Meshtcheryakova, Svetlana V Klinova
Stable suspensions of metal oxide nanoparticles (Me-NPs) obtained by laser ablation of 99.99% pure copper, zinc or lead under a layer of deionized water were used separately, in three binary combinations and a triple combination in two independent experiments on rats. In one of the experiments the rats were instilled with Me-NPs intratracheally (i.t.) (for performing a broncho-alveolar lavage in 24hrs to estimate the cytological and biochemical indices of the response of the lower airways), while in the other, Me-NPs were repeatedly injected intraperitoneally (i...
February 14, 2017: Toxicology
https://www.readbyqxmd.com/read/28209479/subacute-immunotoxicity-of-the-marine-phycotoxin-yessotoxin-in-rats
#10
Sara F Ferreiro, Natalia Vilariño, Cristina Carrera, M Carmen Louzao, Germán Santamarina, Antonio G Cantalapiedra, J Manuel Cifuentes, Andrés C Vieira, Luis M Botana
Yessotoxin (YTX) is a marine phycotoxin produced by dinoflagellates and accumulated in filter feeding shellfish. YTX content in shellfish is regulated by many food safety authorities to protect human health, although currently no human intoxication episodes have been unequivocally related to YTX presence in food. The immune system has been proposed as one of the target organs of YTX due to alterations of lymphoid tissues and cellular and humoral components. The aim of the present study was to explore subacute immunotoxicity of YTX in rats by evaluating the hematological response, inflammatory cytokine biomarkers and the presence of YTX-induced structural alterations in the spleen and thymus...
February 13, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28209351/an-indirect-stereoselective-analysis-of-nebivolol-glucuronides-in-plasma-by-lc-ms-ms-application-to-clinical-pharmacokinetics
#11
Carolina Pinto Vieira, Daniel Valente Neves, Evandro José Cesarino, Adriana Rocha, Séverine Poirier, Vera Lucia Lanchote
Nebivolol is a racemate of the d-isomer responsible for β1 adrenergic receptor antagonism and the l-isomer responsible for the release of nitric oxide from endothelial cells. Nebivolol is mainly metabolized to nebivolol glucuronide, which also contribute to the nebivolol β1 adrenoreceptor antagonism. This study reports the development and validation of an indirect stereoselective method of analysis of nebivolol glucuronides in plasma by LC-MS/MS. The method was applied to the investigation of stereoselectivity in the glucuronidation of nebivolol in elderly hypertensive patients (n=11) CYP2D6 phenotyped as EM and treated with a single oral dose of the racemate...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28208108/dietary-administration-of-edc-mixtures-a-focus-on-fish-lipid-metabolism
#12
O Carnevali, V Notarstefano, I Olivotto, M Graziano, P Gallo, I Di Marco Pisciottano, L Vaccari, A Mandich, E Giorgini, F Maradonna
Many man-made chemical compounds are recognized as endocrine disruptors and once released into the environment are likely to spread and bioaccumulate in wild species. Due to their lipophilic nature, these substances pass through the cell membrane or bind to specific receptors activating physiological responses that in the long run can cause reproductive impairment, physiological disorders, including the occurrence of metabolic syndromes. One significant source of contamination is represented by the consumption of polluted food...
February 6, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28208058/monitoring-of-macrophage-accumulation-in-statin-treated-atherosclerotic-mouse-model-using-sodium-iodide-symporter-imaging-system
#13
Ran Ji Yoo, Min Hwan Kim, Sang-Keun Woo, Kwang Il Kim, Tae Sup Lee, Yang-Kyu Choi, Joo Hyun Kang, Sang Moo Lim, Yong Jin Lee
INTRODUCTION: Macrophages play a key role in atherosclerotic plaque formation in atherosclerosis, but its detailed understanding has poorly investigated until now. Thus, we sought to demonstrate a noninvasive technique for macrophage tracking to atherosclerotic lesions in apolipoprotein E(-/-)(ApoE(-/-)) mice with an imaging system based on sodium iodide symporter (NIS) gene coupled with (99m)Tc-single-photon emission computed tomography (SPECT). METHODS AND RESULTS: Macrophage cells (RAW264...
January 25, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28208011/glucosylsphingosine-activates-serotonin-receptor-2a-and-2b-implication-of-a-novel-itch-signaling-pathway
#14
Ramsha Afzal, Won-Sik Shim
Recent reports claimed that glucosylsphingosine (GS) is highly accumulated and specifically evoking itch-scratch responses in the skins of atopic dermatitis (AD) patients. However, it was unclear how GS can trigger itch-scratch responses, since there were no known molecular singling pathways revealed yet. In the present study, it was verified for the first time that GS can activate mouse serotonin receptor 2a (mHtr2a) and 2b (mHtr2b), but not 2c (mHtr2c) that are expressed in HEK293T cells. Specifically, effects of GS on all mouse serotonin receptor 2 subfamily were evaluated by calcium imaging techniques...
February 17, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28207834/a-cyclin-dependent-kinase-inhibitor-dinaciclib-in-preclinical-treatment-models-of-thyroid-cancer
#15
Shu-Fu Lin, Jen-Der Lin, Chuen Hsueh, Ting-Chao Chou, Richard J Wong
BACKGROUND: We explored the therapeutic effects of dinaciclib, a cyclin-dependent kinase (CDK) inhibitor, in the treatment of thyroid cancer. MATERIALS AND METHODS: Seven cell lines originating from three pathologic types of thyroid cancer (papillary, follicular and anaplastic) were studied. The cytotoxicity of dinaciclib was measured using a lactate dehydrogenase assay. The expression of proteins associated with cell cycle and apoptosis was assessed using Western blot analysis and immunofluorescence microscopy...
2017: PloS One
https://www.readbyqxmd.com/read/28206821/simulated-space-radiation-impact-of-four-different-types-of-high-dose-ionizing-radiation-on-the-lichen-xanthoria-elegans
#16
Annette Brandt, Joachim Meeßen, Reiner U Jänicke, Marina Raguse, Sieglinde Ott
This study addresses the viability of the lichen Xanthoria elegans after high-dose ionizing irradiation in the frame of the STARLIFE campaign. The first set of experiments was intended to resemble several types of galactic cosmic radiation (GCR) as present beyond the magnetic shield of Earth. In the second set of experiments, γ radiation up to 113 kGy was applied to test the limit of lichen resistance to ionizing radiation. Entire thalli of Xanthoria elegans were irradiated in the anhydrobiotic state. After STARLIFE 1, the metabolic activity of both symbionts was quantified by live/dead staining with confocal laser scanning microscopy...
February 2017: Astrobiology
https://www.readbyqxmd.com/read/28204913/accumulation-of-alpha-fluoro-beta-alanine-and-fluoro-mono-acetate-in-a-patient-with-5-fluorouracil-associated-hyperammonemia
#17
Yoshitaka Nishikawa, Taro Funakoshi, Takahiro Horimatsu, Shin'ichi Miyamoto, Takeshi Matsubara, Motoko Yanagita, Shunsaku Nakagawa, Atsushi Yonezawa, Kazuo Matsubara, Manabu Muto
PURPOSE: High-dose 5-fluorouracil (5-FU) containing chemotherapy occasionally causes hyperammonemia and can be lethal. However, the mechanism of 5FU-associated hyperammonemia has not been known. The aim of this study was to reveal the pharmacokinetics of 5-FU-associated hyperammonemia in a recurrent colorectal cancer patient with end-stage renal disease (ESRD). METHODS: We experienced a case of hyperammonemia during mFOLFOX6 plus bevacizumab therapy for recurrent colorectal cancer...
February 15, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28203068/ectopic-fat-accumulation-in-patients-with-copd-an-eclipse-substudy
#18
Mickaël Martin, Natalie Almeras, Jean-Pierre Després, Harvey O Coxson, George R Washko, Isabelle Vivodtzev, Emiel Fm Wouters, Erica Rutten, Michelle C Williams, John T Murchison, William MacNee, Don D Sin, François Maltais
BACKGROUND: Obesity is increasingly associated with COPD, but little is known about the prevalence of ectopic fat accumulation in COPD and whether this can possibly be associated with poor clinical outcomes and comorbidities. The Evaluation of COPD Longitudinally to Identify Predictive Surrogate Endpoints (ECLIPSE) substudy tested the hypothesis that COPD is associated with increased ectopic fat accumulation and that this would be associated with COPD-related outcomes and comorbidities...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/28202761/the-long-noncoding-rna-neat1-exerts-anti-hantaviral-effects-by-acting-as-a-positive-feedback-for-rig-i-signaling
#19
Hongwei Ma, Peijun Han, Wei Ye, Hesong Chen, Xuyang Zheng, Linfeng Cheng, Liang Zhang, Lan Yu, Xing'an Wu, Zhikai Xu, Yingfeng Lei, Fanglin Zhang
Hantavirus infection, which causes zoonotic diseases with a high mortality rate in humans, has long been a global public health concern. Over the past decades, accumulating evidence suggests that long noncoding RNAs (lncRNAs) play key regulatory roles in innate immunity. However, the involvement of host lncRNAs in hantaviral control remains uncharacterized. In this study, we identified the lncRNA, NEAT1, as a vital antiviral modulator. NEAT1 was dramatically upregulated after Hantaan virus (HTNV) infection, whereas its downregulation in vitro or in vivo delayed host innate immune responses and aggravated HTNV replication...
February 15, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28202290/effect-of-psychotropic-drug-treatment-on-sterol-metabolism
#20
Željka Korade, Wei Liu, Emily B Warren, Kristan Armstrong, Ned A Porter, Christine Konradi
Cholesterol metabolism is vital for brain function. Previous work in cultured cells has shown that a number of psychotropic drugs inhibit the activity of 7-dehydrocholesterol reductase (DHCR7), an enzyme that catalyzes the final steps in cholesterol biosynthesis. This leads to the accumulation of 7-dehydrocholesterol (7DHC), a molecule that gives rise to oxysterols, vitamin D, and atypical neurosteroids. We examined levels of cholesterol and the cholesterol precursors desmosterol, lanosterol, 7DHC and its isomer 8-dehydrocholesterol (8DHC), in blood samples of 123 psychiatric patients on various antipsychotic and antidepressant drugs, and 85 healthy controls, to see if the observations in cell lines hold true for patients as well...
February 12, 2017: Schizophrenia Research
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