Search results for "Saccharin"
showing 10 items of 13 documents
Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases
2017
Rhomboids are intramembrane serine proteases and belong to the group of structurally and biochemically most comprehensively characterized membrane proteins. They are highly conserved and ubiquitously distributed in all kingdoms of life and 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 disease, type 2 diabetes, and malaria. However, despite a thorough understanding of many structural and functional aspects of rhomboids, potent and selective inhibitors of these intramembrane proteases are still not available. In this …
[Saccharin test for the study of mucociliary clearance: reference values for a Spanish population].
2008
Objective Mucociliary transport is an important defense mechanism for the airways. The aim of this study was to establish reference values for nasal mucociliary clearance time (MCT) by means of the saccharin test. Subjects and Methods A cross-sectional, descriptive, observational study was performed. The variables studied were nasal MCT, age, and sex. We included 249 healthy nonsmokers (134 male and 115 female subjects) aged over 10 years and stratified the sample by age. To establish reference values, percentiles were calculated and lower and upper limits of normal were established at the 2.5 and 97.5 percentiles, respectively. The association between nasal MCT and the main study variables…
N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII.
2017
A series of N-substituted saccharins incorporating aryl, alkyl and alkynyl moieties, as well as some ring opened derivatives were prepared and investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The widespread cytosolic isoforms CA I and II were not inhibited by these sulfonamides whereas transmembrane, tumor-associated ones were effectively inhibited, with KIs in the range of 22.1-481nM for CA IX and of 3.9-245nM for hCA XII. Although the inhibition mechanism of these tertiary/secondary sulfonamides is unknown for the moment, the good efficacy and especially selectivity for the inhibition of the tumor-associated over the cytosolic, widespread isoforms, make…
Microwave-assisted catalytic esterification of α-glucoisosaccharino-1,4-lactone with tall oil fatty acids
2016
Background: Carbohydrates-rich materials are partly degraded during alkaline kraft pulping into a complex mixture of aliphatic carboxylic acids consisting of α-glucoisosaccharinic acid as one of the main acids. On the other hand, crude tall oil, containing significant amounts fatty acids, is obtained as a by-product from kraft pulping. One interesting novel approach is to utilize chemically both these side-streams by producing renewable surfactants from aliphatic carboxylic acids and fatty acids via esterification. Results: In this paper, lauric (C12:0) and oleic (C18:1) acids as well as a mixture of tall oil fatty acids were esterified with α-glucoisosaccharino-1,4-lactone in a microwave-a…
Impairment of nasal mucociliary clearance after radiotherapy for childhood head cancer.
2001
Background Radiotherapy of the head region in children is known to cause long-term sequelae, such as facial, dental, and ocular abnormalities. We investigated whether a decreased nasal mucociliary function occurs after radiotherapy of the head in children. Methods A saccharin/charcoal test was performed in 20 children treated with radiotherapy of the head and in 20 controls, age-matched and gender-matched. Results We found a decreased nasal mucociliary clearance (lower percentage of responses (p = 0083) and longer mucociliary transport times (p = .0001) in the patients compared with the controls. The radiotherapy dosage influenced the response to the test (p = .0046). Conclusions Irradiatio…
Perinatal xenohormone exposure impacts sweet preference and submandibular development in male rats.
2013
Objective To determine the effect of perinatal exposure to low doses of genistein and/or vinclozolin on submandibular salivary gland (SSG) development in juvenile and adult male rats and to establish a link with sweet preference. Material and Methods Female rats received orally (1 mg kg−1 body weight/day) genistein and vinclozolin, alone or in combination, from the first gestational day up to weaning. Sweet preference was assessed at weaning and in adulthood in male offspring; submandibular glands were then collected to study the morphogenesis and mRNA expression of steroid receptors, growth factors and taste related proteins. Results Exposure to genistein and/or vinclozolin resulted in a h…
Enantioselective zinc-mediated conjugate alkynylation of saccharin-derived 1-aza-butadienes
2020
The enantioselective 1,4-alkynylation of conjugated imines derived from saccharin with aryl- and alkyl-substituted terminal alkynes has been achieved. The reaction mediated by diethylzinc in the presence of a catalytic amount of a bis(hydroxy)malonamide chiral ligand provides the corresponding imines bearing a propargylic stereocenter with moderate yields and fair to excellent enantioselectivities.
Application of fractal geometry to dissolution kinetic study of a sweetener excipient
2001
Abstract In the context of relationship study between dissolution kinetic and particle morphology using the fractal geometry tool, we use a commercially available quality of saccharin powder. The characterization of molecular feature and image analysis study allows us to conclude to the statistic self-similarity of particles of four sieved particles size fractions, permitting the fractal approach. Calculation of reactive fractal dimension is performed using two forms of mass transfer equation: −d Q /d t = kQ D R /3 Δ C and −d Q /d t = k′R D R −3 Δ C , with Δ C ={ C f /[ln C s /( C s − C f )]}. Based on comparison of the surface fractal dimension D S on the two values of reactive fractal di…
Use of fractal geometry to dissolution study of a sweetener excipient
2002
International audience
Effects of oral Bisphenol A exposure on sweet preference and on submandibular salivary gland structure in male adult rat
2012
La Revue de Gériatrie; Objectifs: Le Bisphénol A (BPA) est un œstrogéno-mimétique qui entre dans la fabrication de plastiques en polycarbonate et de résines époxy destinés entre autres à l'élaboration d'emballages alimentaires, de matériel médical et d'amalgames dentaires. Pouvant atteindre des taux élevés dans la salive, l'objectif de cette étude était de vérifier l'innocuité du BPA au niveau buccal en recherchant les effets sur les préférences gustatives et sur les glandes saliuaires, deux paramètres sensibles aux œstrogènes. Matériels et Méthodes: Une étude effet-dose a été réalisée sur des rats Wistar adultes répartis en 5 groupes (n=12). Le Bisphénol A a été administré pendant 6 semain…