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https://www.readbyqxmd.com/read/29448509/nicotinic-acid-coated-magnetite-nanorods-evaluation-by-lipid-profile-analysis-and-genetic-tests
#1
Olivia A Attallah, W K B Khalil, Mohamed M S Abdel Mottaleb, E Girgis
In our present work some biological tests were carried out to assess the biocompatibility of nicotinic acid coated magnetite nanorods. Pure and coated nanorods were injected intraperitoneally to cholesterol fed mice with dose values of 25, 50 mg/Kg. Investigations were done on treated mice with/without exposure to low frequency electromagnetic field (EMF) and samples were collected fourteen days post treatment. Toxicological effects were evaluated using Micronucleus and DNA fragmentation analysis. The results indicated that low dose (25 mg/Kg) nicotinic acid coated nanorods had insignificant toxicological effects in comparison to that of control group...
February 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29436756/alirocumab-versus-usual-lipid-lowering-care-as-add-on-to-statin-therapy-in-individuals-with-type-2-diabetes-and-mixed-dyslipidaemia-the-odyssey-dm-dyslipidemia-randomized-trial
#2
Kausik K Ray, Lawrence A Leiter, Dirk Müller-Wieland, Bertrand Cariou, Helen M Colhoun, Robert R Henry, Francisco J Tinahones, Maja Bujas-Bobanovic, Catherine Domenger, Alexia Letierce, Rita Samuel, Stefano Del Prato
AIMS: Individuals with type 2 diabetes (T2DM) and mixed dyslipidaemia represent a high-risk and difficult-to-treat population. ODYSSEY DM-DYSLIPIDEMIA (NCT02642159) compared alirocumab, a proprotein convertase subtilisin-kexin type 9 inhibitor, with usual care (UC) in individuals with T2DM and mixed dyslipidaemia not optimally managed by maximally-tolerated statins. MATERIALS AND METHODS: UC options (no additional lipid-lowering therapy; fenofibrate; ezetimibe; omega-3 fatty acid; nicotinic acid) were selected prior to stratified randomization to open-label alirocumab 75 mg every 2 weeks (Q2W; with increase to 150 mg Q2W at Week [W]12 if W8 non-high-density lipoprotein cholesterol [non-HDL-C] was ≥2...
February 13, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29429366/the-enhancement-of-serotonin-induced-contraction-of-rat-femoral-artery-is-mediated-by-angiotensin-ii-release-from-intact-endothelium
#3
Marko Stojanović, Milica Prostran, Miroslav Radenković
We have performed an in vitro study on isolated intact or denuded femoral artery (FA) of healthy, diabetic, and/or rats submitted to the FA occlusion. The aim was to determine the contribution of endothelium and endothelial dysfunction (ED) on serotonin-induced action in FA. Further, the contribution of angiotensin II and cyclooxygenase products of arachidonic acid was investigated. A marker of ED, vWF was measured in animal serum. Serotonin induced contraction-dependent contraction of isolated FA, which was increased in preparations with endothelium...
February 10, 2018: Archives of Physiology and Biochemistry
https://www.readbyqxmd.com/read/29421645/feeding-of-tobacco-blend-or-nicotine-induced-weight-loss-associated-with-decreased-adipocyte-size-and-increased-physical-activity-in-male-mice
#4
Mingxia Liu, Chia-Chi Chuang Key, Allison Weckerle, Elena Boudyguina, Janet K Sawyer, Abraham K Gebre, Wayne Spoo, Om Makwana, John S Parks
Although epidemiological data and results from rodent studies support an inverse relationship between nicotine consumption and body weight, the molecular mechanisms are poorly understood. CD-1 mice were fed a basal diet or a basal diet containing low or high dose smokeless tobacco blend or high dose nicotine tartrate for 14 weeks. High dose tobacco blend and nicotine tartrate diets vs. basal diet reduced mouse body weight (16.3% and 19.7%, respectively), epididymal (67.6% and 72.5%, respectively) and brown adipose weight (42% and 38%, respectively), epididymal adipocyte size (46...
February 5, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29417314/exploring-molecular-speciation-and-crystallization-mechanism-of-amorphous-2-phenylamino-nicotinic-acid
#5
Arjun Kalra, Joseph W Lubach, Eric J Munson, Tonglei Li
PURPOSE: Molecular understanding of phase stability and transition of the amorphous state helps in formulation and manufacturing of poorly-soluble drugs. Crystallization of a model compound, 2-phenylamino nicotinic acid (2PNA), from the amorphous state was studied using solid-state analytical methods. Our previous report suggests that 2PNA molecules mainly develop intermolecular -COOH∙∙∙pyridine N (acid-pyridine) interactions in the amorphous state. In the current study, the molecular speciation is explored with regard to the phase transition from the amorphous to the crystalline state...
February 7, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29393213/differential-neuroprotective-effects-of-interleukin-1-receptor-antagonist-on-spinal-cord-neurons-after-excitotoxic-injury
#6
Nikos Schizas, Sharn Perry, Brittmarie Andersson, Carolina Wählby, Klas Kullander, Nils P Hailer
Secondary damage following spinal cord injury (SCI) induces neuronal damage through inflammatory and excitotoxic pathways. We hypothesized that the interleukin-1 receptor antagonist (IL1RA) protects neuronal populations and suppresses apoptosis and gliosis after injury. Spinal cord slice cultures (SCSCs) were subjected to excitotoxic injury with N-methyl-D-aspartate (NMDA) and treated with IL1RA. Immunohistochemistry for neuronal nuclei (NeuN), MacII, glial fibrillary acidic protein, and TdT-mediated dUTP nick end labelling stains were used to evaluate neuronal survival, glial activation, and apoptosis...
January 26, 2018: Neuroimmunomodulation
https://www.readbyqxmd.com/read/29384531/triphenylbismuth-v-di-iso-nicotinates-transmetallation-agents-or-divergent-organometalloligands-first-organobismuth-v-based-silver-i-coordination-polymers
#7
Ahmad Ben Kiran, Teodora Mocanu, Alpár Pöllnitz, Sergiu Shova, Marius Andruh, Cristian Silvestru
The reaction of Ph3BiCl2 with alkali salts of isonicotinic and nicotinic acids afforded Ph3Bi[O(O)CC5H4N-4]2 (1) and Ph3Bi[O(O)CC5H4N-3]2 (2), respectively, which were characterized by multinuclear NMR spectroscopy in solution, mass spectrometry and IR spectroscopy in the solid state. Their molecular structures were established by single-crystal X-ray diffraction. For both 1 and 2 the molecules contain a trigonal bipyramidal C3BiO2 core, with the phenyl groups in equatorial positions. The potential use of 1 and 2 as ditopic organometalloligands was investigated...
January 31, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29382049/nicotinic-acid-long-term-effectiveness-in-a-patient-with-bipolar-type-ii-disorder-a-case-of-vitamin-dependency
#8
Bo H Jonsson
Nicotinic acid (NA), often called niacin, a form of vitamin B₃, is a water-soluble nutrient found in animal and vegetarian foods. Vitamin B₃ for healthy people is considered to be needed in doses of less than 20 mg daily. In higher doses, NA has been described to be beneficial in some patients with psychiatric disorders. This report describes a male patient with bipolar type II disorder who for many years had been treated with lithium and other medications applied in affective disorders. These pharmacological drugs had beneficial effects but were at times insufficient...
January 27, 2018: Nutrients
https://www.readbyqxmd.com/read/29381352/design-and-mechanism-of-s-3-amino-4-difluoromethylenyl-cyclopent-1-ene-1-carboxylic-acid-a-highly-potent-%C3%AE-aminobutyric-acid-aminotransferase-inactivator-for-the-treatment-of-addiction
#9
Jose I Juncosa, Kenji Takaya, Hoang V Le, Matthew J Moschitto, Pathum M Weerawarna, Romila Mascarenhas, Dali Liu, Stephen L Dewey, Richard B Silverman
γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system. Inhibition of GABA aminotransferase (GABA-AT), a pyridoxal 5'-phosphate (PLP)-dependent enzyme that degrades GABA, has been established as a possible strategy for the treatment of substance abuse. The raised GABA levels that occur as a consequence of this inhibition have been found to antagonize the rapid release of dopamine in the ventral striatum (nucleus accumbens) that follows an acute challenge by an addictive substance...
January 30, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29361723/treatment-strategy-for-dyslipidemia-in-cardiovascular-disease-prevention-focus-on-old-and-new-drugs
#10
Donatella Zodda, Rosario Giammona, Silvia Schifilliti
Prevention and treatment of dyslipidemia should be considered as an integral part of individual cardiovascular prevention interventions, which should be addressed primarily to those at higher risk who benefit most. To date, statins remain the first-choice therapy, as they have been shown to reduce the risk of major vascular events by lowering low-density lipoprotein cholesterol (LDL-C). However, due to adherence to statin therapy or statin resistance, many patients do not reach LDL-C target levels. Ezetimibe, fibrates, and nicotinic acid represent the second-choice drugs to be used in combination with statins if lipid targets cannot be reached...
January 21, 2018: Pharmacy (Basel, Switzerland)
https://www.readbyqxmd.com/read/29353067/antinociception-of-the-spirocyclopiperazinium-salt-compound-lxm-15-via-activating-%C3%AE-7-nachr-and-m4-machr-and-inhibiting-camkii%C3%AE-camp-creb-cgrp-signalling-pathway-in-mice
#11
Hua Yang, Qi Sun, Yingying Liang, Yimin Jiang, Runtao Li, Jia Ye
The aim of this study was to investigate the analgesic effect of the spirocyclopiperazinium salt compound LXM-15 by intragastric administration in thermal and chemical pain models and further to elucidate the possible molecular mechanisms. The results showed that LXM-15 exerted significant antinociception in hot-plate test, formalin test and acetic acid writhing test. Western blot analysis showed that LXM-15 significantly reduced the upregulation of phosphorylation of calcium/calmodulin -dependent protein kinaseⅡα (CaMKIIα) and cAMP response element-binding protein (CREB), and further decreased the elevation of calcitonin gene related peptide (CGRP) in the dorsal root ganglion (DRG) and spinal cord in mice...
January 15, 2018: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/29352227/ly2087101-and-dfbr-share-transmembrane-binding-sites-in-the-%C3%AE-4-3-%C3%AE-2-2-nicotinic-acetylcholine-receptor
#12
Farah Deba, Hamed I Ali, Abisola Tairu, Kara Ramos, Jihad Ali, Ayman K Hamouda
Positive allosteric modulators (PAMs) of nicotinic acetylcholine receptors (nAChRs) have potential therapeutic application in neuropathologies associated with decrease in function or loss of nAChRs. In this study, we characterize the pharmacological interactions of the nAChRs PAM, LY2087101, with the α4β2 nAChR using mutational and computational analyses. LY2087101 potentiated ACh-induced currents of low-sensitivity (α4)3(β2)2 and high-sensitivity (α4)2(β2)3 nAChRs with similar potencies albeit to a different maximum potentiation (potentiation I max  = ~840 and 450%, respectively)...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29341170/identification-and-characterization-of-a-new-three-component-nicotinic-acid-hydroxylase-nahab1-b2-from-pusillimonas-sp-strain-t2
#13
Mei Yuan, Yanting Zhang, Lingling Zhao, Yun Ma, Qin He, Jian He, Jiguo Qiu
Nicotinic acid (NA) is ubiquitous in nature and its microbial degradation mechanisms are diverse. In this study, Pusillimonas sp. strain T2 was found to be capable of utilizing NA as sole carbon and nitrogen sources. This strain could completely degrade 300 mg L-1 NA within 3.5 h at 30 °C and pH 7.0. And one of the degradation intermediate of NA was identified as 6-hydroxynicotinic acid (6HNA). The draft genome sequences of strain T2 was determined to have a total length of 3.3 M bp and 3,054 proteins were predicted...
January 16, 2018: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/29317496/a-functional-link-between-nad-homeostasis-and-n-terminal-protein-acetylation-in-saccharomyces-cerevisiae
#14
Trevor Croft, Christol James Theoga Raj, Michelle Salemi, Brett S Phinney, Su-Ju Lin
Nicotinamide adenine dinucleotide (NAD+) is an essential metabolite participating in cellular redox chemistry and signaling, and the complex regulation of NAD+ metabolism is not yet fully understood. To investigate this, we established a NAD+-intermediate specific reporter system to identify factors required for salvage of metabolically-linked nicotinamide (NAM) and nicotinic acid (NA). Mutants lacking components of the NatB complex, NAT3 and MDM20, appeared as hits in this screen. NatB is an Nα-terminal-acetyltransferase responsible for acetylation of the amino terminus of specific Met-retained peptides...
January 9, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29316708/carbon-monoxide-potentiates-high-temperature-induced-nicotine-biosynthesis-in-tobacco
#15
Tielong Cheng, Liwei Hu, Pengkai Wang, Xiuyan Yang, Ye Peng, Ye Lu, Jinhui Chen, Jisen Shi
Carbon monoxide (CO) acts as an important signal in many physiological responses in plants, but its role in plant secondary metabolism is still unknown. Nicotine is the main alkaloid generated in tobacco and the plant hormone jasmonic acid (JA) has previously been reported to efficiently induce its biosynthesis. Whether and how CO interacts with JA to regulate nicotine biosynthesis in tobacco remains elusive. In this study, we demonstrate that high temperature (HT) induces quick accumulation of nicotine in tobacco roots, combined with an increase in CO and JA concentration...
January 8, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29316071/signal-amplification-by-reversible-exchange-sabre-from-discovery-to-diagnosis
#16
Peter J Rayner, Simon Duckett
Signal Amplification by Reversible Exchange (SABRE) turns typically weak magnetic resonance responses into strong signals making previously impractical measurements possible. This technique has gained significant popularity due to its speed and simplicity. This minireview tracks the development of SABRE from the initial hyperpolarization of pyridine in 2009 to the point where 50% ¹H polarization levels have be achieved in a di-dueterio-nicotinate, a key step in the pathway to potential clinical use. Simple routes to efficient ¹⁵N hyperpolarization and the creation of hyperpolarized long-lived magnetic states are illustrated...
January 6, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29311484/molecular-determinants-of-%C3%AE-3%C3%AE-4-nicotinic-acetylcholine-receptors-inhibition-by-triterpenoids
#17
Sanung Eom, Yoon Suh Kim, Sung Bae Lee, Shinhwa Noh, Hye Duck Yeom, Hyunsu Bae, Jun-Ho Lee
In a previous work, we reported the regulatory role of the triterpenoids on 5-hydroxytryptamine (5-HT)3A receptors activity in Xenopus laevis oocytes (Eur. J. Pharmacol., 615, 2009, Lee et al.). In the present report, we studied the modulation of triterpenoids on the activity of the human nicotinic acetylcholine receptor type α3β4. Two-electrode voltage clamp experiments were used to test acetylcholine mediated inward current (IACh). Treatment with triterpenoids (dehydroeburicoic acid, 6α-hydroxypolyporenic acid C and pachymic acid) inhibited IACh in a concentration dependent and reversible manner...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29310282/use-of-polymer-inclusion-membranes-pims-as-support-for-electromembrane-extraction-of-non-steroidal-anti-inflammatory-drugs-and-highly-polar-acidic-drugs
#18
Román-Hidalgo Cristina, Martín-Valero María Jesús, Fernández-Torres Rut, Bello-López Miguel Ángel
The use of polymer inclusion membranes (PIMs) as support of 1-octanol liquid membrane in electromembrane extraction (EME) procedure is proposed. Synthesis of PIMs were optimized to a composition of 29% (w/w) of cellulose triacetate as base polymer and 71% (w/w) of Aliquat®336 as cationic carrier. Flat PIMs of 25µm thickness and 6mm diameter were used. EME protocol was implemented for the simultaneous extraction of four non-steroidal anti-inflammatory drugs (NSAIDs) (salicylic acid, ketoprofen, naproxen and ibuprofen) and four highly polar acidic drugs (anthranilic acid, nicotinic acid, amoxicillin and hippuric acid)...
March 1, 2018: Talanta
https://www.readbyqxmd.com/read/29300488/atp-binding-cassette-transporter-a-subfamily-8-is-a-sinusoidal-efflux-transporter-for-cholesterol-and-taurocholate-in-mouse-and-human-liver
#19
Kazunari Sasaki, Masanori Tachikawa, Yasuo Uchida, Satoshi Hirano, Fumito Kadowaki, Michitoshi Watanabe, Sumio Ohtsuki, Tetsuya Terasaki
The ATP-binding cassette (ABC) transporter A subfamily 8 (ABCA8) belongs to the ABCA6-like transporters subgroup, which is distinct from the ABCA1-like subgroup in the ABCA family. The expression and function of the short-size human ABCA8 lacking one of the two ATP-binding domains for ATP hydrolysis, which are regularly present in the other ABCA transporters, have been reported. However, the functional differences between the short-size human ABCA8 and full-size human ABCA8 which has the two ATP-binding domains, remain unknown...
January 4, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29286298/simple-purification-of-nicotiana-benthamiana-produced-recombinant-colicins-high-yield-recovery-of-purified-proteins-with-minimum-alkaloid-content-supports-the-suitability-of-the-host-for-manufacturing-food-additives
#20
Anett Stephan, Simone Hahn-Löbmann, Fred Rosche, Mirko Buchholz, Anatoli Giritch, Yuri Gleba
Colicins are natural non-antibiotic bacterial proteins with a narrow spectrum but an extremely high antibacterial activity. These proteins are promising food additives for the control of major pathogenic Shiga toxin-producing E. coli serovars in meats and produce. In the USA, colicins produced in edible plants such as spinach and leafy beets have already been accepted by the U. S. Food and Drug Administration (FDA) and U. S. Department of Agriculture (USDA) as food-processing antibacterials through the GRAS (generally recognized as safe) regulatory review process...
December 29, 2017: International Journal of Molecular Sciences
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