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https://www.readbyqxmd.com/read/29347850/feasibility-of-electrospray-deposition-for-rapid-screening-of-the-cocrystal-formation-and-single-step-continuous-production-of-pharmaceutical-nanococrystals
#1
Shahram Emami, Mohammadreza Siahi-Shadbad, Mohammad Barzegar-Jalali, Khosro Adibkia
OBJECTIVES: This study employed electrospray deposition (ESD) for simultaneous synthesis and particle engineering of cocrystals. SIGNIFICANCE: Exploring new methods for the efficient production of cocrystals with desired particle properties is an essential demand. METHODS: The possibility of cocrystal formation by ESD was examined for indomethacin-saccharin, indomethacin-nicotinamide, naproxen-nicotinamide, and naproxen-iso-nicotinamide cocrystals...
January 18, 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29341907/molecular-level-elucidation-of-saccharin-assisted-rapid-dissolution-and-high-supersaturation-level-of-drug-from-eudragit%C3%A2-e-solid-dispersion
#2
Keisuke Ueda, Harunobu Kanaya, Kenjirou Higashi, Keiji Yamamoto, Kunikazu Moribe
In this work, the effect of saccharin (SAC) addition on the dissolution and supersaturation level of phenytoin (PHT)/Eudragit® E (EUD-E) solid dispersion (SD) at neutral pH was examined. The PHT/EUD-E SD showed a much slower dissolution of PHT compared to the PHT/EUD-E/SAC SD. EUD-E formed a gel layer after the dispersion of the PHT/EUD-E SD into an aqueous medium, resulting in a slow dissolution of PHT. Pre-dissolving SAC in the aqueous medium significantly improved the dissolution of the PHT/EUD-E SD. Solid-state 13C NMR measurements showed an ionic interaction between the tertiary amino group of EUD-E and the amide group of SAC in the EUD-E gel layer...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29307532/analysis-of-acetylcholinesterase-inhibitors-by-extraction-in-choline-saccharinate-aqueous-biphasic-systems
#3
Milen G Bogdanov, Ivan Svinyarov
Ionic liquid-based aqueous biphasic systems (IL-ABS) formed by ILs composed of ions of low toxicity, choline ([Chol]+) coupled with saccharinate ([Sac]-) and acesulfamate ([Ace]-), and inorganic salts with distinct water-structuring properties were employed for simultaneous extraction and concentration of acetylcholinesterase (AChE) inhibitors - galantamine (gal), N-desmethyl galantamine (des) and ungiminorine (ung). Comprehensive experiments aimed to assess the influence of salt and IL type and concentration, as well as the pH and temperature on the phase-forming ability and distribution of the target alkaloids between the two phases formed reveled that the IL anion and pH are the most important factors...
January 3, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29302964/n-thiocyanatosaccharin-a-sweet-electrophilic-thiocyanation-reagent-and-the-synthetic-applications
#4
Di Wu, Jiashen Qiu, Pran Gopal Karmaker, Hongquan Yin, Fu-Xue Chen
N-Thiocyanatosaccharin (R1) was readily prepared from the sweet additive Saccharin in two steps with 71% overall yield. Applying this new reagent to diverse nucleophiles such as benzothiophenes, indoles, oxindoles, aromatic amines, phenols, β-keto carbonyl compounds, aromatic ketones, a novel electrophilic thiocyanation reaction was achieved with high yields (up to 99%). The potential recycling of saccharin, wide scope of substrates, and the mild reaction conditions made this protocol much more practical.
January 5, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29283203/synthesis-structure-and-cytotoxicity-of-a-novel-sulphanyl-bridged-thiadiazolyl-saccharinate-conjugate-the-relevance-of-s%C3%A2-n-interaction
#5
Lilia Cabral, Elisa Brás, Marta Henriques, Catia Marques, Luís Frija, Luísa Barreira, José António Paixão, Rui Fausto, Maria Lurdes Cristiano
Reports showing that the copper concentration is considerably higher in neoplasms than in normal tissues prompted the need to develop selective copper chelators. We disclosed recently that some N-linked tetrazole-saccharinates bind selectively to copper, forming complexes that are highly cytotoxic towards cancer cells. Because tetrazole-saccharinates are photolabile, due to the photoreactivity of tetrazoles, we proposed thiadiazolyl-saccharinates. Herein we describe the synthesis, structure and monomeric photochemistry of a sulphanyl-bridged thiadiazolyl-saccharinate, MTSB...
December 28, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29280297/hypercrosslinked-particles-for-the-extraction-of-sweeteners-using-dispersive-solid-phase-extrction-from-environmental-samples
#6
Sameer S Lakade, Qing Zhou, Aimin Li, Francesc Borrull, Núria Fontanals, Rosa M Marcé
This work presents a new extraction material, namely, Q-100, based on hypercrosslinked magnetic particles, which was tested in dispersive solid-phase extraction for a group of sweeteners from environmental samples. The hypercrosslinked Q-100 magnetic particles had the advantage of suitable pore size distribution and high surface area, and showed good retention behavior towards sweeteners. Different dispersive solid-phase extraction parameters such as amount of magnetic particles or extraction time were optimized...
December 26, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29262312/effects-of-daily-exposure-to-saccharin-sodium-and-rebaudioside-a-on-the-ovarian-cycle-and-steroidogenesis-in-rats
#7
Jingle Jiang, Lina Qi, Quanwei Wei, Fangxiong Shi
Saccharin sodium and rebaudioside A are widely used as non-caloric sweeteners in our daily life; however, the impacts and regulatory mechanisms of such sweeteners on reproduction remain unclear. In the present study, we used rats as animal models to evaluate the effects of daily exposure to saccharin sodium and rebaudioside A on ovarian biologic functions. Weanling rats were distributed into five experimental groups receiving normal water, 1.5 or 7.5 mM saccharin sodium solution, or 0.5 or 2.5 mM rebaudioside A solution for 48 days of exposure...
December 17, 2017: Reproductive Toxicology
https://www.readbyqxmd.com/read/29258553/prenatal-alcohol-exposure-is-a-risk-factor-for-adult-neuropathic-pain-via-aberrant-neuroimmune-function
#8
Joshua J Sanchez, Shahani Noor, Suzy Davies, Daniel Savage, Erin D Milligan
BACKGROUND: Clinical studies show that prenatal alcohol exposure (PAE) results in effects that persist into adulthood. Experimental animal models of moderate PAE demonstrate that young adults with PAE display potentiated sensitivity to light touch, clinically termed allodynia, following sciatic nerve chronic constriction injury (CCI) that coincides with heightened spinal glial, spinal macrophage, and peripheral immune responses. However, basal touch sensitivity and corresponding glial and leukocyte activation are unaltered...
December 19, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29250448/glucose-intake-alters-expression-of-neuropeptides-derived-from-proopiomelanocortin-in-the-lateral-hypothalamus-and-the-nucleus-accumbens-in-fructose-preference-rats
#9
Guangfa Jiao, Guozhong Zhang, Haiying Wang, Weilin Zhao, Yanwei Cui, Yongjing Liu, Feng Gao, Fang Yuan, Yi Zhang
To study the neuroendocrine mechanism of sugar preference, we investigated the role of glucose feeding in the regulation of expression levels of neuropeptides derived from proopiomelanocortin (POMC) in the lateral hypothalamus (LH) and nucleus accumbens (NAc) in fructose preference rats. Fructose preference rats were induced by using the lithium chloride backward conditioning procedure. The fructose preference was confirmed by the two-bottle test. The drinking behavior of rats was assessed by the fructose concentration gradient test...
2017: Neural Plasticity
https://www.readbyqxmd.com/read/29231885/development-of-a-sequential-injection-analysis-system-for-the-determination-of-saccharin
#10
Budi Wibowotomo, Jong-Bang Eun, Jong Il Rhee
Saccharin is a powerfully sweet nonnutritive sweetener that has been approved for food-processing applications within the range of 100-1200 mg/kg. A simple, rapid, and cost-effective sequential injection analysis (SIA) technique was developed to determine the saccharin level. This method is based on the reaction of saccharin with p-chloranil in an ethanol medium with a hydrogen peroxide (H₂O₂) acceleration, and the resultant violet-red compound was detected using a UV-Vis spectrophotometer at λmax = 420 nm...
December 12, 2017: Sensors
https://www.readbyqxmd.com/read/29225095/restriction-of-dietary-protein-leads-to-conditioned-protein-preference-and-elevated-palatability-of-protein-containing-food-in-rats
#11
Michelle Murphy, Kate Z Peters, Bethany S Denton, Kathryn A Lee, Heramb Chadchankar, James E McCutcheon
The mechanisms by which intake of dietary protein is regulated are poorly understood despite their potential involvement in determining food choice and appetite. In particular, it is unclear whether protein deficiency results in a specific appetite for protein and whether influences on diet are immediate or develop over time. To determine the effects of protein restriction on consumption, preference, and palatability for protein we assessed patterns of intake for casein (protein) and maltodextrin (carbohydrate) solutions in adult rats...
December 7, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/29224235/long-term-cardiovascular-re-programming-by-short-term-perinatal-exposure-to-nicotine-s-main-metabolite-cotinine
#12
Stefano Bastianini, Viviana Lo Martire, Alessandro Silvani, Giovanna Zoccoli, Chiara Berteotti, Hugo Lagercrantz, Anders Arner, Gary Cohen
AIM: Gather "proof-of-concept" evidence of the adverse developmental potential of cotinine (a seemingly benign biomarker of recent nicotine / tobacco smoke exposure). METHODS: Pregnant C57 mice drank nicotine or cotinine-laced water for 6wks from conception (NPRE = 2% saccharin+100μg nicotine/ml; CPRE = 2% saccharin + 10μg cotinine/ml) or 3wks after birth (CPOST = 2% saccharin + 30μg cotinine/ml). Controls drank 2% saccharin (CTRL). At 17±1weeks (male pups; CTRL n=6; CPOST n=6; CPRE n=8; NPRE n=9) we assessed (i) cardiovascular control during sleep; (ii) arterial reactivity ex vivo; (iii) expression of genes involved in arterial constriction / dilation...
December 9, 2017: Acta Paediatrica
https://www.readbyqxmd.com/read/29217834/gender-specific-alteration-of-energy-balance-and-circadian-locomotor-activity-in-the-crtc1-knockout-mouse-model-of-depression
#13
Clara Rossetti, Daniel Sciarra, Jean-Marie Petit, Chin B Eap, Olivier Halfon, Pierre J Magistretti, Benjamin Boutrel, Jean-René Cardinaux
Obesity and depression are major public health concerns, and there is increasing evidence that they share etiological mechanisms. CREB-regulated transcription coactivator 1 (CRTC1) participates in neurobiological pathways involved in both mood and energy balance regulation. Crtc1 -/- mice rapidly develop a depressive-like and obese phenotype in early adulthood, and are therefore a relevant animal model to explore possible common mechanisms underlying mood disorders and obesity. Here, the obese phenotype of male and female Crtc1 -/- mice was further characterized by investigating CRTC1's role in the homeostatic and hedonic regulation of food intake, as well as its influence on daily locomotor activity...
December 8, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/29210609/dietary-intakes-of-six-intense-sweeteners-by-irish-adults
#14
Maria Buffini, Séverine Goscinny, Joris Van Loco, Anne P Nugent, Janette Walton, Albert Flynn, Michael J Gibney, Breige A McNulty
This research investigated the intakes of six intense sweeteners: acesulfame-K (E950), aspartame (E951), cyclamate (E952), saccharin (E954), sucralose (E955), and steviol glycosides (E960) in the diets of Irish adults, using data from the National Adult Nutrition Survey. A food label survey that included products currently available on the Irish market supplemented the analysis. Sweetener intakes were investigated using three different exposure scenarios; beginning with a crude assessment which assumed that all foods permitted to contain the additives of interest always did contain them, and at their maximum permitted level (Tier 1)...
December 28, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29210144/adolescent-impulsivity-as-a-sex-dependent-and-subtype-dependent-predictor-of-impulsivity-alcohol-drinking-and-dopamine-d2-receptor-expression-in-adult-rats
#15
Lindsey R Hammerslag, Amogh P Belagodu, Olubankole A Aladesuyi Arogundade, Angela G Karountzos, Qingrou Guo, Roberto Galvez, Brent W Roberts, Joshua M Gulley
Impulsivity is a personality trait associated with a heightened risk for drug use and other psychiatric conditions. Because impulsivity-related disorders typically emerge during adolescence, there has been interest in exploring methods for identifying adolescents that will be at risk to develop substance use disorders in adulthood. Here, we used a rodent model to assess inhibitory control (impulsive action) and impulsive decision making (impulsive choice) during adolescence (43-50 days old) or adulthood (93-100 days old) and then examined the impact of development on these impulsivity traits by re-testing rats 50 days later...
December 5, 2017: Addiction Biology
https://www.readbyqxmd.com/read/29198469/novel-small-molecule-inhibitors-of-protein-kinase%C3%A2-c-epsilon-reduce-ethanol-consumption-in%C3%A2-mice
#16
Angelo Blasio, Jingyi Wang, Dan Wang, Florence P Varodayan, Matthew B Pomrenze, Jacklyn Miller, Anna M Lee, Thomas McMahon, Sandeep Gyawali, Hua-Yu Wang, Marisa Roberto, Stanton McHardy, Michael A Pleiss, Robert O Messing
BACKGROUND: Despite the high cost and widespread prevalence of alcohol use disorders, treatment options are limited, underscoring the need for new, effective medications. Previous results using protein kinase C epsilon (PKCε) knockout mice, RNA interference against PKCε, and peptide inhibitors of PKCε predict that small-molecule inhibitors of PKCε should reduce alcohol consumption in humans. METHODS: We designed a new class of PKCε inhibitors based on the Rho-associated protein kinase (ROCK) inhibitor Y-27632...
December 1, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/29197983/reduced-sensitivity-to-reinforcement-in-adolescent-compared-to-adult-sprague-dawley-rats-of-both-sexes
#17
Emily R Hankosky, Sara R Westbrook, Rachel M Haake, Michela Marinelli, Joshua M Gulley
RATIONALE: Adolescence is a period of considerable development of brain and behavior and is the time during which most drug use is initiated. OBJECTIVE: Age-dependent differences in motivated behaviors may be one of the factors that contribute to heightened vulnerability to developing substance use disorders, so we sought to compare age differences in methamphetamine (METH) and saccharin seeking. METHODS: Beginning during adolescence or adulthood, male and female Sprague-Dawley rats were trained to self-administer 0...
December 2, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29195134/developing-cellulosic-waste-products-as-platform-chemicals-protecting-group-chemistry-of-%C3%AE-glucoisosaccharinic-acid
#18
Michael Almond, Mustapha G Suleiman, Matthew Hawkins, Daniel Winder, Thomas Robshaw, Megan Waddoups, Paul N Humphreys, Andrew P Laws
Alpha and beta-glucoisosaccharinic acids ((2S,4S)-2,4,5-trihydroxy-2-(hydroxymethyl)pentanoic acid and (2R,4S)-2,4,5-trihydroxy-2-(hydroxymethyl)pentanoic acid) which are produced when cellulosic materials are treated with aqueous alkali are potentially valuable platform chemicals. Their highly functionalised carbon skeleton, with fixed chirality at C-2 and C-4, makes them ideal starting materials for use in synthesis. In order to assess the potential of these saccharinic acids as platform chemicals we have explored the protecting group chemistry of the lactone form of alpha-glucoisosaccharinic acid (α-GISAL)...
November 26, 2017: Carbohydrate Research
https://www.readbyqxmd.com/read/29194387/preparation-and-characterization-of-cabamazepine-cocrystal-in-polymer-solution
#19
Hao Zhang, Ying Zhu, Ning Qiao, Yang Chen, Linghuan Gao
In this study, we attempted to prepare carbamazepine (CBZ) cocrystal through the solution method in ethanol-water solvent mixture (volume ratio 1:1) and polyvinyl pyrrolidone (PVP) solution. Nicotinamide (NIC) and saccharin (SAC) were selected as cocrystal coformers. Cocrystal screening products were characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD) techniques. Characterization results show that in ethanol-water solvent mixture, pure CBZ-NIC cocrystal can be prepared, while CBZ-SAC cocrystal cannot be obtained...
December 1, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29185711/discovery-and-biological-evaluation-of-potent-and-selective-n-methylene-saccharin-derived-inhibitors-for-rhomboid-intramembrane-proteases
#20
Parul Goel, Thorsten Jumpertz, David C Mikles, Anezka Ticha, Minh T N Nguyen, Steven H L Verhelst, Martin Hubalek, Darren C Johnson, Daniel Bachovchin, Isabella Ogorek, C U Pietrzik, Kvido Strisovsky, Boris Schmidt, Sascha Weggen
Rhomboids are intramembrane serine proteases and belong to the structurally and biochemically most comprehensively characterized membrane proteins. They are highly conserved, ubiquitously distributed in all kingdoms of life, and they function in a wide range of biological processes including epidermal growth factor signaling, mitochondrial dynamics, and apoptosis. Importantly, rhomboids have been associated with multiple diseases including Parkinson's, type 2 diabetes and malaria. However, despite a thorough understanding of many structural and functional aspects of rhomboids, potent and selective inhibitors for these intramembrane proteases are still not available...
November 29, 2017: Biochemistry
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