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https://www.readbyqxmd.com/read/28800451/synthesis-antimicrobial-dna-cleavage-and-antioxidant-activities-of-tricyclic-sultams-derived-from-saccharin
#1
Ibrahim Elghamry, Magdy M Youssef, Mohammed A Al-Omair, Hany Elsawy
Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8-33 μg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28781184/contaminants-of-emerging-concern-in-the-open-sea-waters-of-the-western-mediterranean
#2
Miroslav Brumovský, Jitka Bečanová, Jiří Kohoutek, Mireno Borghini, Luca Nizzetto
Pollution by chemical substances is of concern for the maintenance of healthy and sustainable aquatic environments. While the occurrence and fate of numerous emerging contaminants, especially pharmaceuticals, is well documented in freshwater, their occurrence and behavior in coastal and marine waters is much less studied and understood. This study investigates the occurrence of 58 chemicals in the open surface water of the Western Mediterranean Sea for the first time. 70 samples in total were collected in 10 different sampling areas...
August 3, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28776509/molecular-structures-of-3-2-2-3-3-tetrafluoropropoxy-methyl-and-3-2-2-3-3-3-pentafluoropropoxy-methyl-pyridinium-saccharinates
#3
Norman Lu, Hsing Fang Chiang, Rong Jyun Wei, Yuh Sheng Wen, Ling Kang Liu
The salts 3-[(2,2,3,3-tetrafluoropropoxy)methyl]pyridinium saccharinate, C9H10F4NO(+)·C7H4NO3S(-), (1), and 3-[(2,2,3,3,3-pentafluoropropoxy)methyl]pyridinium saccharinate, C9H9F5NO(+)·C7H4NO3S(-), (2), i.e. saccharinate (or 1,1-dioxo-1λ(6),2-benzothiazol-3-olate) salts of pyridinium with -CH2OCH2CF2CF2H and -CH2OCH2CF2CF3 meta substituents, respectively, were investigated crystallographically in order to compare their fluorine-related weak interactions in the solid state. Both salts demonstrate a stable synthon formed by the pyridinium cation and the saccharinate anion, in which a seven-membered ring reveals a double hydrogen-bonding pattern...
August 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28769774/fenofibrate-administration-reduces-alcohol-and-saccharin-intake-in-rats-possible-effects-at-peripheral-and-central-levels
#4
Mario Rivera-Meza, Daniel Muñoz, Erik Jerez, María E Quintanilla, Catalina Salinas-Luypaert, Katia Fernandez, Eduardo Karahanian
We have previously shown that the administration of fenofibrate to high-drinker UChB rats markedly reduces voluntary ethanol intake. Fenofibrate is a peroxisome proliferator-activated receptor alpha (PPARα) agonist, which induces the proliferation of peroxisomes in the liver, leading to increases in catalase levels that result in acetaldehyde accumulation at aversive levels in the blood when animals consume ethanol. In these new studies, we aimed to investigate if the effect of fenofibrate on ethanol intake is produced exclusively in the liver (increasing catalase and systemic levels of acetaldehyde) or there might be additional effects at central level...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28763168/the-effect-of-nonnutritive-sweeteners-added-to-a-liquid-diet-on-volume-and-caloric-intake-and-weight-gain-in-rats
#5
David J Bissonnette, Samantha List, Penny Knoblich, M Hadley
OBJECTIVE: Long-term effects of diet beverage consumption on the regulation of caloric intake is unclear. The goal of this study was to investigate whether the chronic intake of a liquid diet with nonnutritive sweeteners (NNS) would lead to greater appetite and weight gain. METHODS: Wistar rats were fed a liquid diet (Osmolite) sweetened with nutritive sweetener (NS; sucrose) and NNS (stevia and saccharin) or a nonsweetened control. Intakes and weight gain were measured...
August 1, 2017: Obesity
https://www.readbyqxmd.com/read/28711215/changes-occurring-in-mucosal-contractility-of-the-inferior-turbinate-and-mucociliary-clearance-following-total-laryngectomy-a-prospective-clinical-trial
#6
Ilker Kocak, Remzi Dogan, Sabri Baki Eren, Selahattin Tugrul, Orhan Ozturan, Aysenur Meric Hafiz
OBJECTIVE: In this study, changes occurring in the contractility capacity of the inferior turbinate and mucociliary clearance time due to the interruption of nasal air flow were examined. MATERIAL & METHODS: A total of 23 patients undergone total laryngectomy between June 2010 and June 2012 were included in the study. Acoustic rhinometry test was performed in the patients before and after 0.05% oxymetazoline nasal topical decongestant administration. In addition, saccharin test was applied in order to measure mucociliary clearance...
July 12, 2017: Auris, Nasus, Larynx
https://www.readbyqxmd.com/read/28708901/sex-specific-enhancement-of-palatability-driven-feeding-in-adolescent-rats
#7
Andrew T Marshall, Angela T Liu, Niall P Murphy, Nigel T Maidment, Sean B Ostlund
It has been hypothesized that brain development during adolescence perturbs reward processing in a way that may ultimately contribute to the risky decision making associated with this stage of life, particularly in young males. To investigate potential reward dysfunction during adolescence, Experiment 1 examined palatable fluid intake in rats as a function of age and sex. During a series of twice-weekly test sessions, non-food-deprived rats were given the opportunity to voluntarily consume a highly palatable sweetened condensed milk (SCM) solution...
2017: PloS One
https://www.readbyqxmd.com/read/28708096/characterization-of-non-nutritive-sweetener-intake-in-rural-southwest-virginian-adults-living-in-a-health-disparate-region
#8
Valisa E Hedrick, Erin M Passaro, Brenda M Davy, Wen You, Jamie M Zoellner
Few data assessing non-nutritive sweetener (NNS) intake are available, especially within rural, health-disparate populations, where obesity and related co-morbidities are prevalent. The objective of this study is to characterize NNS intake for this population and examine the variance in demographics, cardio-metabolic outcomes, and dietary intake between NNS consumers and non-consumers. A cross-sectional sample (n = 301) of Virginian adults from a randomized controlled trial (data collected from 2012 to 2014) targeting sugar-sweetened beverage (SSB) intake completed three 24-h dietary recalls, and demographics and cardio-metabolic measures were assessed...
July 14, 2017: Nutrients
https://www.readbyqxmd.com/read/28699833/safety-assessment-of-16-sweeteners-for-the-korean-population-using-dietary-intake-monitoring-and-poundage-method
#9
MeeKyung Kim, Gunyoung Lee, Ho Soo Lim, Sang Soon Yun, Myungsil Hwang, Jin-Hwan Hong, Hoonjeong Kwon
A sweetener is a food additive that imparts a sweet taste to food products. Sweeteners have been increasingly used in Korea since the approval of sodium saccharin and d-sorbitol in 1962. Unlike food contaminants, humans are exposed to food additives only through the consumption of processed food products. For exposure assessments of sweeteners, the dietary intakes of food products containing acesulfame-K, aspartame, saccharin-Na, and sucralose were determined, and the resulting calculated estimated daily intake (EDI) values were compared directly with each additive's ADI...
July 12, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28681511/a-new-generation-of-mtorc1-inhibitor-attenuates-alcohol-intake-and-reward-in-mice
#10
Nadege Morisot, Christopher J Novotny, Kevan M Shokat, Dorit Ron
Alcohol use disorder (AUD) is a chronic condition associated with devastating socioeconomic consequences. Yet, pharmacotherapies to treat behavioral phenotypes such as uncontrolled heavy drinking are limited. Studies in rodents suggest that the mammalian target of rapamycin complex 1 (mTORC1) plays an important role in mechanisms underlying alcohol drinking behaviors as well as alcohol seeking and relapse. These preclinical evidence suggest that mTORC1 may be a therapeutic target for the treatment of AUD. Thus, the aim of the present study was to test the potential use of newly developed mTORC1 inhibitors, RapaLink-1 and MLN0128, in preclinical mouse models of AUD...
July 6, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28680497/late-term-effects-of-surgery-on-nasal-functions-in-patients-who-underwent-total-laryngectomy-surgery
#11
Deniz Karaoglu, Murat Kocyigit, Safiye Giran Ortekin, Mustafa Kemal Adali
Introduction  There is a common opinion that losing airway functions in total laryngectomy patients cause changes in nasal physiological rates. Studies conducted to review the subject present gaps, especially in terms of objective measurements. Objective  We evaluated late-term effects of surgery on nasal functions in patients who underwent total laryngectomy surgery more than two years ago. Methods  We included in the study 22 patients who had undergone total laryngectomy, as well as 24 healthy subjects with similar demographic characteristics as the control group...
July 2017: International Archives of Otorhinolaryngology
https://www.readbyqxmd.com/read/28675883/mass-loading-of-typical-artificial-sweeteners-in-a-pig-farm-and-their-dissipation-and-uptake-by-plants-in-neighboring-farmland
#12
Ling Ma, Yarui Liu, Jiayao Xu, Hongwen Sun, Hao Chen, Yiming Yao, Peng Zhang, Fengju Shen, Aldredo C Alder
Pig farm is an important potential source for artificial sweeteners (ASs) in the environment due to their wide use as additives in pig feed. The objective of this study was to evaluate the fate of typical ASs in pig farm and neighboring farmland. For this purpose, the levels of four typical artificial ASs, i.e. saccharin (SAC), cyclamate (CYC), acesulfame (ACE) and sucralose (SUC), in pig feed and manure from a pig farm and water samples from an on-farm wastewater treatment plant (WWTP) in Tianjin, China were measured and the mass loadings and removal efficiencies were assessed...
July 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28663116/short-term-selection-for-high-and-low-ethanol-intake-yields-differential-sensitivity-to-ethanol-s-motivational-effects-and-anxiety-like-responses-in-adolescent-wistar-rats
#13
Macarena Soledad Fernández, Bárbara Báez, Ana Bordón, Laura Espinosa, Eliana Martínez, Ricardo Marcos Pautassi
Alcohol use disorders are modulated by genetic factors, but the identification of specific genes and their concomitant biological changes that are associated with a higher risk for these disorders has proven difficult. Alterations in the sensitivity to the motivational effects of ethanol may be one way by which genes modulate the initiation and escalation of ethanol intake. Rats and mice have been selectively bred for high and low ethanol consumption during adulthood. However, selective breeding programs for ethanol intake have not focused on adolescence...
June 27, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28657910/a-palladium-ii-saccharinate-complex-of-terpyridine-exerts-higher-anticancer-potency-and-less-toxicity-than-cisplatin-in-a-mouse-allograft-model
#14
Yuksel Cetin, Zelal Adiguzel, Hivda U Polat, Tolga Akkoc, Arzu Tas, Buse Cevatemre, Gokalp Celik, Baris Carikci, Veysel T Yilmaz, Engin Ulukaya, Ceyda Acilan
The main aim of this study is to assess the safety and antitumor efficacy of a palladium(II) (Pd)-saccharinate complex with terpyridine. To characterize the Pd(II) complex in vitro, its cytotoxicity was evaluated using a water-soluble tetrazolium salt cell viability assay and the mechanism of cell death was assessed by DNA fragmentation/condensation and live cell imaging analyses. The antitumor efficacy and safety of the Pd(II) complex in-vivo were examined by analyzing reduction in tumor size, changes in body and organ weight, histopathological analysis of liver, kidney, and tumor sections, and biochemical analysis of serum in C57BL/6 mice...
June 27, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28645064/heroin-and-saccharin-demand-and-preference-in-rats
#15
Lindsay P Schwartz, Jung S Kim, Alan Silberberg, David N Kearns
BACKGROUND: Several recent studies have investigated the choice between heroin and a non-drug alternative reinforcer in rats. A common finding in these studies is that there are large individual differences in preference, with some rats preferring heroin and some preferring the non-drug alternative. The primary goal of the present study was to determine whether individual differences in how heroin or saccharin is valued, based on demand analysis, predicts choice. METHODS: Rats lever-pressed for heroin infusions and saccharin reinforcers on fixed-ratio schedules...
September 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28644870/effects-of-nicotine-on-corneal-wound-healing-following-acute-alkali-burn
#16
Jong Won Kim, Chae Woong Lim, Bumseok Kim
Epidemiological studies have indicated that smoking is a pivotal risk factor for the progression of several chronic diseases. Nicotine, the addictive component of cigarettes, has powerful pathophysiological properties in the body. Although the effects of cigarette smoking on corneal re-epithelialization have been studied, the effects of nicotine on corneal wound healing-related neovascularization and fibrosis have not been fully demonstrated. The aim of this study was to evaluate the effects of chronic administration of nicotine on corneal wound healing following acute insult induced by an alkali burn...
2017: PloS One
https://www.readbyqxmd.com/read/28637659/enduring-effects-of-perinatal-nicotine-exposure-on-murine-sleep-in-adulthood
#17
Jeremy Charles Borniger, Reuben F Don, Ning Zhang, Robert Thomas Boyd, Randy J Nelson
The long-term consequences of early life nicotine exposure are poorly defined. Approximately 8-10% of women report smoking during pregnancy, and this may promote aberrant development in the offspring. To this end, we investigated potential enduring effects of perinatal nicotine exposure on murine sleep and affective behaviors in adulthood (~13-15 weeks of age) in C57Bl6j mice. Mothers received a water bottle containing 200 µg/ml nicotine bitartrate dihydrate in 2% w/v saccharin or pH-matched 2% saccharin with 0...
June 21, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28626531/saccharin-aza-bioisosteres-synthesis-and-preclinical-property-comparisons
#18
Yantao Chen, Carl-Johan Aurell, Anna Pettersen, Richard J Lewis, Martin A Hayes, Matti Lepistö, Anna C Jonson, Hanna Leek, Linda Thunberg
Saccharin is a well-known scaffold in drug discovery. Herein, we report the synthesis and preclinical property comparisons of three bioisosteres of saccharin: aza-pseudosaccharins (cluster B), and two new types of aza-saccharins (clusters C and D). We demonstrate a convenient protocol to selectively synthesize products in cluster C or D when primary amines are used. Preclinical characterization of selected matched-pair products is reported. Through comparison of two diastereomers, we highlight how stereochemistry affects the preclinical properties...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28621396/sodium-saccharin-as-an-effective-catalyst-for-rapid-one-pot-pseudo-five-component-synthesis-of-dihydropyrano-2-3-g-chromenes-under-microwave-irradiation
#19
Leila Moradi, Aghamohammad Sadegh
One-pot microwave-assisted synthesis of dihydropyrano[2,3-g]chromenes catalyzed by sodium saccharin as an efficient, mild and green catalyst was studied. The method presented is a safe and eco-friendly approach for the multicomponent synthesis of dihydropyrano[2,3-g]chromene derivatives with many merits including short reaction times (in comparison with other reported results), high yields and easy work up.
June 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/28618238/antiglycating-potential-of-acesulfame-potassium-an-artificial-sweetener
#20
Ahmad Ali, Tejashree Anil More, Amaritpal Kaur Hoonjan, Subramanian Sivakami
Sweeteners have replaced the natural sugars in the food and beverage industry because of many reasons, such as hyperglycemia and cost. Saccharin, sucralose, aspartame and acesulfame-K are the most commonly used sweeteners. In the present study, the abovementioned artificial sweeteners were used to assess their glycating properties by established methods such as browning, fructosamine assay, determination of carbonyl content, protein aggregation, and measurement of fluorescence. Amadori and advanced glycation end products (AGEs) are formed as a result of the interaction between carbonyl groups of reducing sugars and amino groups of proteins and other macromolecules during glycation...
June 15, 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
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