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https://www.readbyqxmd.com/read/27903228/synthesis-and-evaluation-of-the-hypoglycemic-and-hypolipidemic-activity-of-novel-sulfonamide-benzothiazole-derivatives-of-benzylidene-2-4-thiazolidnedione
#1
Abbas Ahmadi, Mohsen Khalili, Lida Sohrabi, Nazanin Delzendeh, Babak Nahri-Niknafs, Fariba Ansari
Thiazolidinediones (TZDs) and sulfonamides are important and highly consumption class of antidiabetic drugs having insulin sensitizing and stimulating properties in patients with type 2 diabetes, respectively. In this paper, some novel benzothiazole derivatives of TZD-sulfonamides were synthesized (I-IV) and evaluated for anti-hyperglycemic and anti-hyperlipidemic activities in the STZ-induced diabetic rat model. Results indicated that all new conjugated drugs showed significant hypoglycemic activities compared to the control animals that were better for I and IV than others...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27900570/concomitant-use-of-statins-in-tocilizumab-treated-patients-with-rheumatoid-arthritis-a-post-hoc-analysis
#2
Martin Soubrier, Jinglan Pei, Frédérick Durand, Lars Gullestad, Ani John
INTRODUCTION: Patients with rheumatoid arthritis (RA) have decreased survival because of increased cardiovascular risk compared with the general population, and treatment with tocilizumab (TCZ) has been shown to increase lipid levels; however, the relationship between lipids and cardiovascular risk is unknown. This post hoc analysis expanded on previously reported 24-week results by characterizing statin use and subsequent changes in lipid parameters in patients with RA treated with intravenous or subcutaneous TCZ (TCZ-IV or TCZ-SC) over 2 years of treatment...
November 29, 2016: Rheumatology and Therapy
https://www.readbyqxmd.com/read/27898929/does-heat-stress-alter-the-pig-s-response-to-dietary-fat
#3
T A Kellner, L H Baumgard, K J Prusa, N K Gabler, J F Patience
Heat stress (HS) results in major losses to the pork industry via reduced growth performance and, possibly, carcass fat quality. The experimental objective was to measure the effects of HS on the pig's response to dietary fat in terms of lipid digestion, metabolism, and deposition over a 35-d finishing period. A total of 96 PIC 337 × C22/C29 (PIC, Inc., Hendersonville, TN) barrows (initial BW of 100.4 ± 1.2 kg) were randomly allotted to 1 of 9 treatments arranged as a 3 × 3 factorial: thermoneutral (TN; constant 24°C; ad libitum access to feed), pair-fed thermoneutral (PFTN; constant 24°C; limit fed based on previous HS daily feed intake), or HS (cyclical 28°C nighttime, 33°C from d 0 to 7, 33...
November 2016: Journal of Animal Science
https://www.readbyqxmd.com/read/27890592/small-particle-size-lipid-emulsions-satiety-and-energy-intake-in-lean-men
#4
Y K Chan, S C Budgett, A K MacGibbon, S Y Quek, S Kindleysides, S D Poppitt
Lipid emulsions have been proposed to suppress hunger and food intake. Whilst there is no consensus on optimal structural properties or mechanism of action, small particle size (small-PS) stable emulsions may have greatest efficacy. Fabuless®, a commercial lipid emulsion reported in some studies to decrease energy intake (EI), is a small-PS, 'hard' fat emulsion comprising highly saturated palm oil base (PS, 82nm). To determine whether small-PS dairy lipid emulsions can enhance satiety, firstly, we investigated 2 'soft' fat emulsions generated using dairy and soy emulsifying agents (PS, 114nm and 121nm) and a non-emulsified dairy control...
November 24, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27889890/protective-role-of-quercetin-against-hematotoxic-and-immunotoxic-effects-of-furan-in-rats
#5
Rasha T Alam, Ehsan H Abu Zeid, Tamer S Imam
Furan (Fu) is a liver carcinogen produced during heating process of food and concerns a public health problem. The current study was undertaken to evaluate the protective role of quercetin (Que) on Fu-induced hematological, immunological, and histopathological alterations in rats. Fifty male Sprague Dawley rats were divided into five equal groups. Group I (Cont) received distilled water, group II (CO) received corn oil, group III (Que) received Que at 50 mg/kg BW, group IV (Fu) received Fu at 16 mg/kg BW, and group V received Que + Fu simultaneously; all groups gavaged daily for 30 days...
November 26, 2016: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/27881716/influence-of-route-of-administration-and-lipidation-of-apolipoprotein-a-i-peptide-on-pharmacokinetics-and-cholesterol-mobilization
#6
Jie Tang, Dan Li, Lindsey Drake, Wenmin Yuan, Sarah Deshaine, Emily E Morin, Rose Ackermann, Karl Olsen, David E Smith, Anna Schwendeman
Apoliprotein A-I (apoA-I), apoA-I mimetic peptides and their lipid complexes or reconstituted high-density lipoprotein (HDL) have been studied as treatments for various pathologies. However, consensus is lacking about the best method for administration - by intravenous (IV) or intra-peritoneal (IP) routes, and formulation - as an HDL particle or in a lipid-free form. The objective of this study was to systematically examine peptide plasma levels, cholesterol mobilization and lipoprotein remodeling in vivo following administration of lipid-free apoA-I peptide (22A) or phospholipid reconstituted 22A-sHDL by IV and IP routes...
November 23, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27876644/dinotefuran-induced-morphophysiological-changes-in-semi-engorged-females-rhipicephalus-sanguineus-latreille-1806-acari-ixodidae-ticks-ultra-structural-evaluation
#7
Patrícia Rosa de Oliveira, Luis Adriano Anholeto, Gerváso Henrique Bechara, Maria Izabel Camargo Mathias
The present study demonstrated the effects of dinotefuran (active ingredient of the acaricide Protetor Pet(®)) on the ovary and midgut cells of semi engorged R. sanguineus females exposed to different concentrations of this chemical. For this, 120 semi-engorged females were divided into four treatment groups with 30 individuals each: group I or control (distilled water), group II (5000ppm), groups III (6250ppm) and group IV (8334ppm of dinotefuran). All the ticks were immersed in the different concentrations of dinotefuran or in distilled water for 5min and then dried and kept in BOD incubator for 7days...
November 19, 2016: Acta Tropica
https://www.readbyqxmd.com/read/27875537/effect-of-l-tryptophan-and-l-leucine-on-gut-hormone-secretion-appetite-feelings-and-gastric-emptying-rates-in-lean-and-non-diabetic-obese-participants-a-randomized-double-blind-parallel-group-trial
#8
Anne Christin Meyer-Gerspach, Simon Häfliger, Julian Meili, Alison Doody, Jens F Rehfeld, Jürgen Drewe, Christoph Beglinger, Bettina Wölnerhanssen
BACKGROUND/OBJECTIVES: Gut hormones such as cholecystokinin (CCK) and glucagon-like peptide-1 (GLP-1) play a role as satiation factors. Strategies to enhance satiation peptide secretion could provide a therapeutic approach for obesity. Carbohydrates and lipids have been extensively investigated in relation to peptide release. In contrast, the role of proteins or amino acids is less clear. Our aim was to compare the effects of the amino acids L-tryptophan (L-trp) and L-leucine (L-leu) separately on gastric emptying and gut peptide secretion...
2016: PloS One
https://www.readbyqxmd.com/read/27873387/physical-exercise-remodels-visceral-adipose-tissue-and-mitochondrial-lipid-metabolism-in-rats-fed-a-high-fat-diet
#9
Sílvia Rocha-Rodrigues, Amaia Rodríguez, Sara Becerril, Beatriz Ramírez, I O Gonçalves, Jorge Beleza, Gema Frühbeck, António Ascensão, José Magalhães
We aimed to investigate the effects of two physical exercise models, voluntary physical activity (VPA) and endurance training (ET) as preventive and therapeutic strategies, respectively, on lipid accumulation regulators and mitochondrial content in VAT of rats fed a high-fat diet (HFD). Sprague Dawley rats (6 wks old, n=60) were assigned into sedentary and VPA groups fed isoenergetic diets: standard (S, 35 kcal% fat) or HFD (71 kcal% fat). The VPA groups had free access to wheel running during the entire protocol...
November 22, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27871881/targeting-brain-and-peripheral-plasticity-of-the-lipidome-in-acute-kainic-acid-induced-epileptic-seizures-in-mice-via-quantitative-mass-spectrometry
#10
Raissa Lerner, Julia Post, Sebastian Loch, Beat Lutz, Laura Bindila
Epilepsy is a highly common chronic neurological disorder, manifested in many different types, affecting ~1% of the worldwide human population. The molecular mechanisms of epileptogenesis has not yet been clarified, and pharmacoresistance exhibited by 30-40% of epilepsy patients remains a major obstacle in medical care. Growing evidence indicates a role of lipid signalling pathways in epileptogenesis, thus lipid signals emerge as potential biomarkers for the onset and evolving course of the epileptic disorder, as well as potential therapeutic agents and targets...
November 15, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27867716/automatic-classification-of-atherosclerotic-plaques-imaged-with-intravascular-oct
#11
Jose J Rico-Jimenez, Daniel U Campos-Delgado, Martin Villiger, Kenichiro Otsuka, Brett E Bouma, Javier A Jo
Intravascular optical coherence tomography (IV-OCT) allows evaluation of atherosclerotic plaques; however, plaque characterization is performed by visual assessment and requires a trained expert for interpretation of the large data sets. Here, we present a novel computational method for automated IV-OCT plaque characterization. This method is based on the modeling of each A-line of an IV-OCT data set as a linear combination of a number of depth profiles. After estimating these depth profiles by means of an alternating least square optimization strategy, they are automatically classified to predefined tissue types based on their morphological characteristics...
October 1, 2016: Biomedical Optics Express
https://www.readbyqxmd.com/read/27861315/brincidofovir-is-not-a-substrate-for-the-human-organic-anion-transporter-1-oat1-a-mechanistic-explanation-for-the-lack-of-nephrotoxicity-observed-in-clinical-studies
#12
Timothy K Tippin, Marion E Morrison, Thomas M Brundage, Hervé Momméja-Marin
BACKGROUND: Brincidofovir (BCV) is an orally bioavailable lipid conjugate of cidofovir with increased in vitro potency relative to cidofovir against all five families of double-stranded DNA viruses that cause human disease. Following intravenous (IV) administration of cidofovir, the organic anion transporter 1 (OAT1) transports cidofovir from the blood into the renal proximal tubule epithelial cells with resulting dose-limiting nephrotoxicity. OBJECTIVE: To study whether OAT1 transports BCV and to evaluate the pharmacokinetic and renal safety profile of oral BCV compared with IV cidofovir...
November 16, 2016: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/27852753/thermal-sensitivity-and-phenotypic-plasticity-of-cardiac-mitochondrial-metabolism-in-european-perch-perca-fluviatilis
#13
Andreas Ekström, Erik Sandblom, Pierre U Blier, Bernard-Antonin Dupont Cyr, Jeroen Brijs, Nicolas Pichaud
Cellular and mitochondrial metabolic capacity of the heart has been suggested to limit performance of fish at warm temperatures. We investigated this hypothesis by studying the effects of acute temperature increases (16, 23, 30, 32.5 and 36°C) on the thermal sensitivity of 10 key enzymes governing cardiac oxidative and glycolytic metabolism in two populations of European perch (Perca fluviatilis) field-acclimated to 15.5 and 22.5°C, as well as the effects of acclimation on cardiac lipid composition. In both populations of perch, the activity of glycolytic (pyruvate kinase and lactate dehydrogenase) and tricarboxylic acid cycle (pyruvate dehydrogenase and citrate synthase) enzymes increased with acute warming...
November 16, 2016: Journal of Experimental Biology
https://www.readbyqxmd.com/read/27851688/brincidofovir-is-not-a-substrate-for-the-human-organic-anion-transporter-1-a-mechanistic-explanation-for-the-lack-of-nephrotoxicity-observed-in-clinical-studies
#14
Timothy K Tippin, Marion E Morrison, Thomas M Brundage, Hervé Momméja-Marin
BACKGROUND: Brincidofovir (BCV) is an orally bioavailable lipid conjugate of cidofovir (CDV) with increased in vitro potency relative to CDV against all 5 families of double-stranded DNA viruses that cause human disease. After intravenous (IV) administration of CDV, the organic anion transporter 1 (OAT1) transports CDV from the blood into the renal proximal tubule epithelial cells with resulting dose-limiting nephrotoxicity. OBJECTIVE: To study whether OAT1 transports BCV and to evaluate the pharmacokinetic and renal safety profile of oral BCV compared with IV CDV...
December 2016: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/27833513/plasma-and-urinary-type-iv-collagen-levels-for-early-detection-of-nephropathy-in-type-2-diabetes-mellitus-patients
#15
K Balu Mahendran, M Vijaya Bhaskar, K Santha, R Inmozhi, K K Perumal
BACKGROUND: Diabetic nephropathy is a major complication with high morbidity and mortality, and leads to end stage renal disease (ESRD). Type IV collagen is the main component of the glomerular basement membrane (GBM) and the extracellular matrix. The thickening of the GBM is due to accumulation of type IV collagen and alterations in its structure and composition. AIM: The aim of this study was to evaluate the association of plasma and urine type IV collagen with albuminuria status and to determine the clinical implications of type IV collagen as a marker in the early stage of diabetic nephropathy...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27829582/postprandial-hyperlipidemia-and-remnant-lipoproteins
#16
Daisaku Masuda, Shizuya Yamashita
Fasting hypertriglyceridemia is positively associated with the morbidity of coronary heart disease (CHD), and postprandial (non-fasting) hypertriglyceridemia is also correlated with the risk status for CHD, which is related to the increase in chylomicron (CM) remnant lipoproteins produced from the intestine. CM remnant particles, as well as oxidized low density lipoprotein (LDL) or very low density lipoprotein (VLDL) remnants, are highly atherogenic and act by enhancing systemic inflammation, platelet activation, coagulation, thrombus formation, and macrophage foam cell formation...
November 8, 2016: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/27827802/the-potential-protective-effect-of-%C3%AE-lipoic-acid-against-nanocopper-particle-induced-hepatotoxicity-in-male-rats
#17
A A Khalaf, A R Zaki, M K Galal, H A Ogaly, M A Ibrahim, A Hassan
The present research task is aimed to evaluate the role of exogenous α-lipoic acid (ALA) (100 mg/kg body weight) as hepatoprotective and potent antioxidant in amelioration of copper nanoparticle (CNP)-induced hepatotoxicity. Forty male rats were randomly assigned into four equal groups: group I (control), group II received CNPs, group III received CNPs + ALA, and finally group IV received ALA for 2 months. At the end of the experimental period, the rats were decapitated, and blood and liver tissue samples were collected for measurement of liver function tests, antioxidant status, lipid peroxidation (LPO), copper content, expression of some apoptotic genes, and histopathological analysis...
November 8, 2016: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/27826772/the-key-role-played-by-charge-in-the-interaction-of-cytochrome-c-with-cardiolipin
#18
Federica Sinibaldi, Lisa Milazzo, Barry D Howes, Maria Cristina Piro, Laura Fiorucci, Fabio Polticelli, Paolo Ascenzi, Massimo Coletta, Giulietta Smulevich, Roberto Santucci
Cytochrome c undergoes structural variations upon binding of cardiolipin, one of the phospholipids constituting the mitochondrial membrane. Although several mechanisms governing cytochrome c/cardiolipin (cyt c/CL) recognition have been proposed, the interpretation of the process remains, at least in part, unknown. To better define the steps characterizing the cyt c-CL interaction, the role of Lys72 and Lys73, two residues thought to be important in the protein/lipid binding interaction, were recently investigated by mutagenesis...
November 9, 2016: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/27815605/peptide-serum-markers-in-islet-autoantibody-positive-children
#19
Christine von Toerne, Michael Laimighofer, Peter Achenbach, Andreas Beyerlein, Tonia de Las Heras Gala, Jan Krumsiek, Fabian J Theis, Anette G Ziegler, Stefanie M Hauck
AIMS/HYPOTHESIS: We sought to identify minimal sets of serum peptide signatures as markers for islet autoimmunity and predictors of progression rates to clinical type 1 diabetes in a case-control study. METHODS: A double cross-validation approach was applied to first prioritise peptides from a shotgun proteomic approach in 45 islet autoantibody-positive and -negative children from the BABYDIAB/BABYDIET birth cohorts. Targeted proteomics for 82 discriminating peptides were then applied to samples from another 140 children from these cohorts...
November 4, 2016: Diabetologia
https://www.readbyqxmd.com/read/27813125/phosphatidylethanol-in-postmortem-brain-and-serum-ethanol-at-time-of-death
#20
Peter M Thompson, Nathalie Hill-Kapturczak, Marisa Lopez-Cruzan, Luis A Alvarado, Alok K Dwivedi, Martin A Javors
BACKGROUND: Phosphatidylethanol (PEth) is a metabolite of ethanol (EtOH), and its concentration in whole blood samples is a direct biomarker of alcohol consumption. Because PEth is also present in the brain and incorporated in lipid membranes, it can be used to classify deceased individuals on alcohol consumption status at the time of death. The purpose of this study was to detect PEth homologs in postmortem brains of individuals known to have had alcohol use disorder (AUD) and to determine the relationship between serum alcohol at the time of death and PEth in the cerebellum (CE) and orbital frontal cortex (OFC)...
December 2016: Alcoholism, Clinical and Experimental Research
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