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Quincy A Edwards, Sergei M Kulikov, Leah D Garner-O'Neale, Chris D Metcalfe, Tamanna Sultana
Contaminants of emerging concern (CECs), including pharmaceuticals, artificial sweeteners, steroid hormones, and current-use pesticides have been detected in surface waters around the world, but to date, there have been no reports in the peer-reviewed literature on the levels of these classes of contaminants in freshwater resources in the Caribbean region. In the present study, multi-residue solid phase extraction (SPE) and liquid chromatography with tandem mass spectroscopy (LC-MS/MS) were used to analyze grab samples of surface waters collected from five different watersheds in Barbados, West Indies...
November 14, 2017: Environmental Monitoring and Assessment
Arshag D Mooradian, Meridith Smith, Masaaki Tokuda
The rapid increase in the prevalence of obesity worldwide has been partially attributed to the overconsumption of added sugars. Recent guidelines call for limiting the consumption of simple sugars to less than 10% of daily caloric consumption. High intensity sweeteners are regulated as food additives and include aspartame, acesulfame-k, neotame, saccharin, sucralose, cyclamate and alitame. Steviol glycosides and Luo Han Guo fruit extracts are high intensity sweeteners that are designated as generally recognized as safe (GRAS)...
April 2017: Clinical Nutrition ESPEN
Manjula M Weerasekera, Thilini A Jayarathna, Gayan K Wijesinghe, Chinthika P Gunasekara, Neluka Fernando, Nilwala Kottegoda, Lakshman P Samaranayake
OBJECTIVE: To determine the effect of glucose, sucrose, and saccharin on growth, adhesion and biofilm formation of Candida albicans and C.tropicalis. MATERIALS AND METHODS: The growth rates of mono-cultures of planktonic C. albicans and C. tropicalis and co-cultures (1:1), were determined in yeast nitrogen broth supplemented with 5% (30 mM) and 10% (60 mM) of glucose, sucrose, and saccharin, using optical density measurements at 2h intervals over a 14h period. Adhesion and biofilm growth were performed and the growth quantified using standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay...
November 1, 2017: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
Emily C Eastwood, Amy J Eshleman, Aaron Janowsky, Tamara J Phillips
A quantitative trait locus (QTL) on proximal chromosome (Chr) 10 accounts for > 50% of the genetic variance in methamphetamine (MA) intake in mice selectively bred for high (MAHDR) and low (MALDR) voluntary MA drinking. The µ-opioid receptor (MOP-r) gene, Oprm1, resides at the proximal end of Chr 10, and buprenorphine reduces MA intake in MAHDR mice. However, this drug has only partial agonist effects at MOP-r. We investigated the impact of a full MOP-r agonist, morphine, on MA intake and saccharin intake, measured MOP-r density and affinity in several brain regions of the MA drinking lines and their C57BL/6J (B6) and DBA/2J (D2) progenitor strains, and measured MA intake in two congenic strains of mice to verify the QTL and reduce the QTL interval...
November 10, 2017: Mammalian Genome: Official Journal of the International Mammalian Genome Society
Zoe Thompson, Erik M Kolb, Theodore Garland
To explore reward substitution in the context of voluntary exercise, female mice from four replicate high-runner (HR) lines (bred for wheel running) and four non-selected control (C) lines were given simultaneous access to wheels and palatable solutions as competing rewards (two doses of saccharin [0.1, 0.2% w/v]; two doses of common artificial sweetener blends containing saccharin [Sweet 'N Low(®): 0.1, 0.2% w/v], aspartame [Equal(®): 0.04, 0.08% w/v], or sucralose [Splenda(®): 0.08, 0.16% w/v]; or two doses of sucrose [3...
November 7, 2017: Behavioural Processes
Martin Pedard, Céline Demougeot, Clément Prati, Christine Marie
OBJECTIVES: Both peripheral and central brain-derived neurotrophic factor (BDNF) levels are decreased in depression and normalized by efficient anti-depressive therapies. While depression symptoms are frequent in rheumatoid arthritis, BDNF has been poorly investigated in this pathology. Therefore, the present study explored cerebral and peripheral BDNF in arthritis rats as well as the link between brain BDNF and the two factors recently involved in the pathogenesis of depression and present in rheumatoid arthritis namely inflammation and endothelial dysfunction...
November 7, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
Sezen Kislal, David A Blizard
We compared the rate of acquisition and strength of retention of conditioned context aversion (CCA) with conditioned taste aversion (CTA) using pigmented, genetically heterogeneous mice (derived from Large and Small strains). Extending previous findings, in Experiment 1, mice accustomed to drinking from large glass bottles in the colony room learned to avoid graduated tubes after a single conditioning trial when drinking from these novel tubes was paired with injections of LiCl. The results also showed that CCA could be developed even when there was a 30-minute delay between conditioned stimulus and unconditioned stimulus...
November 9, 2017: Learning & Behavior
Liang Wu, Qihang Shao, Guoqiang Yang, Wanbin Zhang
A Co(II)/Box-catalyzed enantioselective addition of potassium allyltrifluoroborate to cyclic ketimines was developed, providing the corresponding chiral α-tertiary amines in high yields and with good enantioselectivities. Alkoxycarbonyl and alkyl substituted saccharin-derived ketimines are suitable substrates for this allylation reaction. The product can be converted to complex molecules over several simple steps, including a precursor of MK-0371, which is a kinesin spindle protein inhibitor. In addition, this catalytic system showed a strong positive non-linear effect...
November 9, 2017: Chemistry: a European Journal
Ryusuke Yoshida, Shingo Takai, Keisuke Sanematsu, Robert F Margolskee, Noriatsu Shigemura, Yuzo Ninomiya
Bitter taste serves as an important signal for potentially poisonous compounds in foods to avoid their ingestion. Thousands of compounds are estimated to taste bitter and presumed to activate taste receptor cells expressing bitter taste receptors (Tas2rs) and coupled transduction components including gustducin, phospholipase Cβ2 (PLCβ2) and transient receptor potential channel M5 (TRPM5). Indeed, some gustducin-positive taste cells have been shown to respond to bitter compounds. However, there has been no systematic characterization of their response properties to multiple bitter compounds and the role of transduction molecules in these cells...
November 4, 2017: Neuroscience
Hong Chen, Bing-Bing Xu, Tao Sun, Zhan Zhou, Hui-Yuan Ya, Mu Yuan
Prostate cancer is a major public health problem worldwide. For the development of potential anti-prostate cancer agents, a series of novel arylpiperazine derivatives containing the saccharin moiety based on previous studies was designed, synthesized, and evaluated in prostate (PC-3, LNCaP, and DU145) cancer cell lines for their anticancer activities. The majority of the compounds exhibited excellent selective activity for the tested cancer cells. Compounds 4 and 12 exhibited strong cytotoxic activities against DU145 cells (half maximal inhibitory concentration (IC50) < 2 μM)...
October 29, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Andrea Balla, Bin Dong, Borehalli M Shilpa, Kiran Vemuri, Alexandros Makriyannis, Subhash C Pandey, Henry Sershen, Raymond F Suckow, K Yaragudri Vinod
Binge alcohol (ethanol) drinking is associated with profound adverse effects on our health and society. Rimonabant (SR141716A), a CB1 receptor inverse agonist, was previously shown to be effective for nicotine cessation and obesity. However, studies using rimonabant were discontinued as it was associated with an increased risk of depression and anxiety. In the present study, we examined the pharmacokinetics and effects of AM4113, a novel CB1 receptor neutral antagonist on binge-like ethanol drinking in C57BL/6J mice using a two-bottle choice drinking-in-dark (DID) paradigm...
November 3, 2017: Neuropharmacology
Mark Z Chen, Joshua C Chang, Jose Zavala-Solorio, Lance Kates, Minh Thai, Annie Ogasawara, Xiaobo Bai, Sean Flanagan, Victor Nunez, Khanhky Phamluong, James Ziai, Robert Newman, Søren Warming, Ganesh Kolumam, Junichiro Sonoda
OBJECTIVE: Fibroblast Growth Factor 21 (FGF21) is a potent stimulator of brown fat thermogenesis that improves insulin sensitivity, ameliorates hepatosteatosis, and induces weight loss by engaging the receptor complex comprised of Fibroblast Growth Factor Receptor 1 (FGFR1) and the requisite coreceptor βKlotho. Previously, recombinant antibody proteins that activate the FGFR1/βKlotho complex were proposed to act as an FGF21-mimetic; however, in vivo action of these engineered proteins has not been well studied...
November 2017: Molecular Metabolism
Jesús-Servando Medel-Matus, Don Shin, Raman Sankar, Andrey Mazarati
Anxiety is one of the most common comorbidities of epilepsy, which has major detrimental effects on the quality of life. Generalized anxiety disorder (GAD) associated with epilepsy has been receiving most attention. However, several other forms of anxiety reportedly present in patients with epilepsy, including panic disorder (PD). In this study, using an animal model of limbic epilepsy, we examined the interplay between epilepsy and panic-like behavior (PLB). Further, considering the high degree of comorbidity between depression on the one hand, and both epilepsy and PD on the other hand, we studied whether and how the presence of PLB in animals with epilepsy would affect their performance in depression-relevant tests...
October 26, 2017: Epilepsy & Behavior: E&B
Seyhan Dülger, Önder Akdeniz, Fevzi Solmaz, Özlem Şengören Dikiş, Tekin Yildiz
BACKGROUND AND AIM: Nasal muco-ciliary clearance time (NMCT) can be measured with the saccharine clearance test which is an inexpensive and easy method. The aim of the present study was to compare and evaluate NMCT using the saccharine clearance test in smokers and non-smokers. MATERIALS AND METHODS: Eighty-five patients whose ages ranged from 18 to 65 years were included in the study. Fifty of the patients were smokers (Group 1) while 35 were healthy, non-smoking volunteers (Group 2)...
November 4, 2017: Clinical Respiratory Journal
Yan Zhou, Marcelo Rubinstein, Malcolm Low, Mary Jeanne Kreek
BACKGROUND: A recent clinical trial found that pharmacological blockade of V1b receptors reduces alcohol relapse in alcohol-dependent patients. SSR149415 is a selective V1b receptor antagonist that has potential for development as an alcohol dependency treatment. In this study, we investigated whether SSR149415 alone or in combination with the mu-opioid receptor [MOP-r] antagonist naltrexone (NTN) would alter excessive alcohol drinking in mice. METHODS: Both sexes of C57BL/6J (B6) mice were subjected to a chronic intermittent access (IA) drinking paradigm (two-bottle choice, 24-h access every other day) for 3 weeks...
November 3, 2017: Alcoholism, Clinical and Experimental Research
Daniela Vullo, R Siva Sai Kumar, Andrea Scozzafava, James G Ferry, Claudiu T Supuran
The β-carbonic anhydrases (CAs, EC from the pathogenic bacterium Clostridium perfringens (CpeCA) was recently characterised kinetically and for its anion inhibition profile. In the search of effective CpeCA inhibitors, possibly useful to inhibit the growth/pathogenicity of this bacterium, we report here an inhibition study of this enzyme with a panel of aromatic, heterocyclic and sugar sulphonamides/sulphamates. Some sulphonamides, such as acetazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, sulthiame and 4-(2-hydroxymethyl-4-nitrophenyl-sulphonamido)ethylbenzenesulphonamide were effective CpeCA inhibitors, with KIs in the range of 37...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Katie L Cavanagh, Chinmay Maheshwari, Naír Rodríguez-Hornedo
This work challenges the popular notion that pharmaceutical salts are more soluble than cocrystals. There are cocrystals that are more soluble than salt forms of a drug and vice-versa. It all depends on the interplay between the chemistry of both the solid and solution phases. Aqueous solubility, pHmax, and supersaturation index (SA =SCC or Ssalt/SD) of cocrystals and salts of a basic drug, Lamotrigine (LTG), were determined, and mathematical models that predict the influence of cocrystal/salt Ksp and Ka were derived...
October 30, 2017: Journal of Pharmaceutical Sciences
Paola Palombo, Rodrigo M Leao, Paula C Bianchi, Paulo E C de Oliveira, Cleopatra da Silva Planeta, Fábio C Cruz
Evidence indicates that drug relapse in humans is often provoked by exposure to the self-administered drug-associated context. An animal model called "ABA renewal procedure" has been used to study the context-induced relapse to drug seeking. Here, we reported a new and feasible training procedure for the ABA renewal method to explore the role of the prelimbic cortex in context-induced relapse to ethanol seeking. By using a saccharin fading technique, we trained rats to self-administer ethanol (10%). The drug delivery was paired with a discrete tone-light cue...
2017: Frontiers in Pharmacology
Rong-San Jiang, Chih-Wen Twu, Kai-Li Liang
BACKGROUND: Previous studies have shown controversial results of topical amphotericin B (AMB) nasal irrigation for chronic rhinosinusitis (CRS). The purpose of this study was to evaluate the efficacy of 200 μg/mL AMB nasal irrigation as an adjuvant therapy after functional endoscopic sinus surgery (FESS). METHODS: Patients with CRS who had received FESS for treatment were recruited and assigned to 1 of 2 groups at random at 1 month postsurgery. In the AMB group patients received nasal irrigation with 200 μg/mL of AMB for 2 months on a daily basis...
October 30, 2017: International Forum of Allergy & Rhinology
Wendy J Lynch, Lillian Tan, Syeda Narmeen, Rebecca Beiter, Darlene H Brunzell
Recent evidence suggests that adolescent and young adult females may be particularly responsive to nicotine use interventions that include exercise or environmental enrichment. This possibility was addressed in the current study by comparing the efficacy of exercise versus non-exercise environmental enrichment (saccharin) during abstinence at reducing subsequent nicotine-seeking/relapse vulnerability in an adolescent-onset rat model. The efficacy of each intervention was examined as a function of estrous cycle phase given findings indicating that hormonal status influences relapse vulnerability and treatment outcome in females...
October 30, 2017: Physiology & Behavior
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