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[PMID]:28457669
[Au] Autor:Kamens HM; Peck C; Garrity C; Gechlik A; Jenkins BC; Rajan A
[Ad] Endereço:Department of Biobehavioral Health, Penn State University, University Park, PA, USA; Center for Brain, Behavior, and Cognition, Penn State University, University Park, PA, USA. Electronic address: hmk123@psu.edu.
[Ti] Título:α6ß2 nicotinic acetylcholine receptors influence locomotor activity and ethanol consumption.
[So] Source:Alcohol;61:43-49, 2017 Jun.
[Is] ISSN:1873-6823
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Nicotinic acetylcholine receptors (nAChRs) in the mesolimbic dopamine system have been implicated in ethanol behaviors. In particular, work in genetically engineered mice has demonstrated that α6-containing nAChRs are involved in ethanol consumption and sedation. A limitation of these studies is that the alteration in the receptor was present throughout development. The recently described α6ß2 antagonist, N,N-decane-1,10-diyl-bis-3-picolinium diiodide (bPiDI), now makes it possible to test for the involvement of these receptors using a pharmacological approach. The aim of this study was to examine the role of α6ß2 nAChRs in ethanol behaviors using a pharmacological approach. Adolescent C57BL/6J mice were treated with bPiDI 30 min prior to testing the mice for binge-like ethanol consumption in the drinking-in-the-dark (DID) test, ethanol-induced motor incoordination using the balance beam, and ethanol-induced sedation using the Loss of Righting Reflex (LORR) paradigm. Adolescent animals were chosen because they express a high amount of α6 mRNA relative to adult animals. Control studies were also performed to determine the effect of bPiDI on locomotor activity and ethanol metabolism. Female mice treated with 20 mg/kg bPiDI had reduced locomotor activity compared to saline-treated animals during the first 30 min following an acute injection. Pretreatment with the α6ß2 antagonist reduced adolescent ethanol consumption but also reduced saccharin consumption. No significant effects were observed on ethanol-induced ataxia, sedation, or metabolism. This study provides evidence that α6ß2 nAChRs are involved in locomotor activity as well as ethanol and saccharin consumption in adolescent animals.
[Mh] Termos MeSH primário: Consumo de Bebidas Alcoólicas/fisiopatologia
Etanol/administração & dosagem
Locomoção/efeitos dos fármacos
Receptores Nicotínicos/fisiologia
[Mh] Termos MeSH secundário: Consumo de Bebidas Alcoólicas/prevenção & controle
Animais
Bebedeira/fisiopatologia
Etanol/efeitos adversos
Feminino
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Antagonistas Nicotínicos/farmacologia
Picolinas/farmacologia
Compostos de Piridínio/farmacologia
Sacarina/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (N,N-decane-1,10-diyl-bis-3-picolinium); 0 (Nicotinic Antagonists); 0 (Picolines); 0 (Pyridinium Compounds); 0 (Receptors, Nicotinic); 0 (alpha6beta2 nicotinic acetylcholine receptor); 3K9958V90M (Ethanol); FST467XS7D (Saccharin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE


  2 / 2712 MEDLINE  
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[PMID]:29053947
[Au] Autor:Munger SD
[Ad] Endereço:Center for Smell and Taste, University of Florida, Gainesville, FL 32610, USA; Department of Pharmacology & Therapeutics, University of Florida, Gainesville, FL 32610, USA; Department of Medicine, Division of Endocrinology, Diabetes, and Metabolism, University of Florida, Gainesville, FL 32610, USA. Electronic address: steven.munger@ufl.edu.
[Ti] Título:A Bitter Tale of Sweet Synergy.
[So] Source:Cell Chem Biol;24(10):1191-1192, 2017 Oct 19.
[Is] ISSN:2451-9456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Some sweeteners show a synergistic enhancement of perceived sweetness when they are tasted as binary mixtures. In this issue of Cell Chemical Biology, Behrens et al. (2017) find that a surprising explanation for this classic observation may lie in their reciprocal inhibition of bitter taste receptors.
[Mh] Termos MeSH primário: Edulcorantes/farmacologia
Percepção Gustatória/efeitos dos fármacos
[Mh] Termos MeSH secundário: Ciclamatos/farmacologia
Sinergismo Farmacológico
Sacarina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclamates); 0 (Sweetening Agents); FST467XS7D (Saccharin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171021
[St] Status:MEDLINE


  3 / 2712 MEDLINE  
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[PMID]:28919036
[Au] Autor:Behrens M; Blank K; Meyerhof W
[Ad] Endereço:German Institute of Human Nutrition Potsdam-Rehbruecke, Department Molecular Genetics, 14558 Nuthetal, Germany. Electronic address: behrens@dife.de.
[Ti] Título:Blends of Non-caloric Sweeteners Saccharin and Cyclamate Show Reduced Off-Taste due to TAS2R Bitter Receptor Inhibition.
[So] Source:Cell Chem Biol;24(10):1199-1204.e2, 2017 Oct 19.
[Is] ISSN:2451-9456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Non-caloric sweeteners are widely used for the formulation of calorie-reduced beverages for health-conscious consumers. However, disadvantages such as undesired off-tastes limit the use of non-nutritive sweeteners. Therefore, the food industry is constantly searching for novel sweeteners and frequently resorts to using blends combining non-caloric sweeteners in a single formulation. The earliest blend allowing higher sweetness levels with reduced bitter off-taste combined saccharin with cyclamate. However, the mechanism by which sweetener blends become superior to single compounds remained obscure. By functional expression of human bitter taste receptors, we found the explanation for the phenomenon observed ∼60 years ago. We demonstrate that cyclamate potently blocks the receptors responsible for saccharin's bitter off-taste. This effect occurs at concentrations where cyclamate itself does not elicit a side taste. Intriguingly, also saccharin inhibits cyclamate-activated bitter receptors. Our experiments demonstrate that heterologous assays are useful for understanding perceptual phenomena and the development of novel tastant formulations.
[Mh] Termos MeSH primário: Ciclamatos/farmacologia
Adoçantes não Calóricos/farmacologia
Receptores Acoplados a Proteínas-G/antagonistas & inibidores
Sacarina/farmacologia
Percepção Gustatória/efeitos dos fármacos
[Mh] Termos MeSH secundário: Interações Medicamentosas
Células HEK293
Seres Humanos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclamates); 0 (Non-Nutritive Sweeteners); 0 (Receptors, G-Protein-Coupled); FST467XS7D (Saccharin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170919
[St] Status:MEDLINE


  4 / 2712 MEDLINE  
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[PMID]:28800451
[Au] Autor:Elghamry I; Youssef MM; Al-Omair MA; Elsawy H
[Ad] Endereço:King Faisal University, College of Science, Department of Chemistry, P. O. Box 400 Al Hufuf, 31982 Al Ahsa, Saudi Arabia. Electronic address: ielghamry@kfu.edu.sa.
[Ti] Título:Synthesis, antimicrobial, DNA cleavage and antioxidant activities of tricyclic sultams derived from saccharin.
[So] Source:Eur J Med Chem;139:107-113, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo: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. And their antioxidant activities were also measured. Four carboxylate derivatives (3a, 5a, 5f and 5g) and one anilide (5d) of the tested compounds proved to be the highest activity all over the study.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Sacarina/química
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Antioxidantes/síntese química
Antioxidantes/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Clivagem do DNA/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Escherichia coli/efeitos dos fármacos
Seres Humanos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Pseudomonas aeruginosa/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Sulfonamides); FST467XS7D (Saccharin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE


  5 / 2712 MEDLINE  
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[PMID]:28690302
[Au] Autor:Tahara S; Yamamoto S; Yamajima Y; Miyakawa H; Uematsu Y; Monma K
[Ad] Endereço:Tokyo Metropolitan Institute of Public Health.
[Ti] Título:A Rapid Dialysis Method for Analysis of Artificial Sweeteners in Foods (2nd Report).
[So] Source:Shokuhin Eiseigaku Zasshi;58(3):124-131, 2017.
[Is] ISSN:1882-1006
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:Following the previous report, a rapid dialysis method was developed for the extraction and purification of four artificial sweeteners, namely, sodium saccharide (Sa), acesulfame potassium (AK), aspartame (APM), and dulcin (Du), which are present in various foods. The method was evaluated by the addition of 0.02 g/kg of these sweeteners to a cookie sample, in the same manner as in the previous report. Revisions from the previous method were: reduction of the total dialysis volume from 200 to 100 mL, change of tube length from 55 to 50 cm, change of dialysate from 0.01 mol/L hydrochloric aqueous solution containing 10% sodium chloride to 30% methanol solution, and change of dialysis conditions from ambient temperature with occasional shaking to 50℃ with shaking at 160 rpm. As a result of these revisions, the recovery reached 99.3-103.8% with one hour dialysis. The obtained recovery yields were comparable to the recovery yields in the previous method with four hour dialysis.
[Mh] Termos MeSH primário: Aspartame/análise
Aspartame/isolamento & purificação
Diálise/métodos
Análise de Alimentos/métodos
Compostos de Fenilureia/análise
Compostos de Fenilureia/isolamento & purificação
Sacarina/análise
Sacarina/isolamento & purificação
Edulcorantes/análise
Edulcorantes/isolamento & purificação
Tiazinas/análise
Tiazinas/isolamento & purificação
[Mh] Termos MeSH secundário: Carbonato de Cálcio
Cromatografia Líquida de Alta Pressão
Citratos
Soluções para Diálise
Combinação de Medicamentos
Temperatura Alta
Ácido Clorídrico
Óxido de Magnésio
Metanol
Cloreto de Sódio
Fatores de Tempo
Água
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Citrates); 0 (Dialysis Solutions); 0 (Drug Combinations); 0 (Phenylurea Compounds); 0 (Suby's G solution); 0 (Sweetening Agents); 0 (Thiazines); 059QF0KO0R (Water); 3A3U0GI71G (Magnesium Oxide); 451W47IQ8X (Sodium Chloride); 8U78KF577Z (dulcin); FST467XS7D (Saccharin); H0G9379FGK (Calcium Carbonate); MA3UYZ6K1H (acetosulfame); QTT17582CB (Hydrochloric Acid); Y4S76JWI15 (Methanol); Z0H242BBR1 (Aspartame)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170711
[St] Status:MEDLINE
[do] DOI:10.3358/shokueishi.58.124


  6 / 2712 MEDLINE  
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[PMID]:28506059
[Au] Autor:Logue C; Dowey LRC; Strain JJ; Verhagen H; McClean S; Gallagher AM
[Ad] Endereço:Nutrition Innovation Centre for Food and Health (NICHE), Ulster University , Coleraine, Northern Ireland BT52 1SA.
[Ti] Título:Application of Liquid Chromatography-Tandem Mass Spectrometry To Determine Urinary Concentrations of Five Commonly Used Low-Calorie Sweeteners: A Novel Biomarker Approach for Assessing Recent Intakes?
[So] Source:J Agric Food Chem;65(22):4516-4525, 2017 Jun 07.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although the use of low-calorie sweeteners (LCSs) is widespread, methods of assessing consumption within free-living populations have inherent limitations. Five commonly consumed LCSs, namely, acesulfame-K, saccharin, sucralose, cyclamate, and steviol glycosides, are excreted via the urine, and therefore a urinary biomarker approach may provide more objective LCS intake data. A LC-ESI-MS/MS method of simultaneously determining acesulfame-K, saccharin, sucralose, cyclamate, and the excretory metabolite of steviol glycosides, steviol glucuronide, in human urine was developed and validated. Linearity was observed over a concentration range of 10-1000 ng/mL with coefficients of determination ranging from 0.9969 to 0.9997. Accuracy ranged from 92 to 104%, and intrabatch and interday precisions were within acceptable limits with %CV below 8% for all compounds. A double-blind, randomized crossover dose-response study was conducted to assess the usefulness of urinary LCS excretions (from both fasting spot and a full 24-h urine collection) for investigating recent intakes. Both modes of sampling were useful for distinguishing between the three short-term intakes of acesulfame-K, saccharin, cyclamates, and steviol glycosides (p < 0.001), whereas for sucralose, urinary concentrations were useful for distinguishing between low (0.1% ADI) and high doses (10% ADI) only (p < 0.001). In summary, this biomarker approach may be useful for assessing intakes of five commonly consumed LCSs.
[Mh] Termos MeSH primário: Biomarcadores/urina
Cromatografia Líquida de Alta Pressão/métodos
Edulcorantes/análise
Espectrometria de Massas em Tandem/métodos
Urina/química
[Mh] Termos MeSH secundário: Biomarcadores/metabolismo
Ciclamatos/análise
Ciclamatos/metabolismo
Diterpenos Caurânicos/metabolismo
Diterpenos Caurânicos/urina
Seres Humanos
Sacarina/análise
Sacarina/metabolismo
Sacarose/análogos & derivados
Sacarose/análise
Sacarose/metabolismo
Sacarose/urina
Edulcorantes/metabolismo
Tiazinas/metabolismo
Tiazinas/urina
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Cyclamates); 0 (Diterpenes, Kaurane); 0 (Sweetening Agents); 0 (Thiazines); 4741LYX6RT (steviol); 57-50-1 (Sucrose); 96K6UQ3ZD4 (trichlorosucrose); FST467XS7D (Saccharin); MA3UYZ6K1H (acetosulfame)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170619
[Lr] Data última revisão:
170619
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170517
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.7b00404


  7 / 2712 MEDLINE  
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[PMID]:28482217
[Au] Autor:Kumar P; Dasari S; Patra AK
[Ad] Endereço:Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016, Uttar Pradesh, India.
[Ti] Título:Ruthenium(II) complexes of saccharin with dipyridoquinoxaline and dipyridophenazine: Structures, biological interactions and photoinduced DNA damage activity.
[So] Source:Eur J Med Chem;136:52-62, 2017 Aug 18.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Ruthenium complexes trans-[Ru(sac) (dpq) ] (1) and trans-[Ru(sac) (dppz) ] (2) where sac is artificial sweetener saccharin (o-sulfobenzimide; 1,2-benzothiazole-3(2H)-one1,1-dioxide (Hsac)), dpq = dipyrido[3,2-d:2',3'-f]quinoxaline and dppz = dipyrido[3,2-a:2',3'-c]phenazine have been synthesized and thoroughly characterized using various analytical and spectral techniques. Saccharin known to act as carbonic anhydrase IX (CA IX) inhibitor which is a biomarker for highly aggressive and proliferative tumor in hypoxic stress, so inhibition of CA IX is a potential strategy for anticancer chemotherapy. The solid state structures, photophysical properties, photostability, DNA and protein binding affinity, and DNA photocleavage activity were explored. The structural analysis revealed Ru(II) centre is in discrete mononuclear, distorted octahedral {RuN } coordination geometry with two monoanionic nitrogen donor saccharinate ligands and two neutral bidentate nitrogen donors ligands dpq and dppz. cis-[Ru(sac) (dppz) ] (cis-2) geometrical isomer was also isolated and structurally characterized by X-ray crystallography. The photo-induced dissociation of monodentate saccharin ligand is observed when irradiated at UV-A light of 365 nm. The complexes show significant binding affinity to the calf thymus DNA (K âˆ¼ 10 M ) through significant intercalation through planar dpq and dppz ligands. Interaction of complexes 1 and 2 with bovine serum albumin (BSA) showed remarkable tryptophan emission quenching (K ∼10 M ). The complexes showed appreciable photoinduced DNA cleavage activity upon irradiation of low power UV-A light of 365 nm from supercoiled (SC) to its nicked circular (NC) form at micromolar complex concentrations. Photocleavage mechanistic studies in presence of O reveals involvement of reactive oxygen species (ROS) mediated through ligand-centered ππ* and/or MLCT excited states generated upon photoactivation leads to nicking of supercoiled DNA to nicked circular form. In absence of O , we also observed photocleavage of DNA through formation of photoinduced ligand dissociated Ru-DNA complex involving PACT pathway.
[Mh] Termos MeSH primário: DNA/efeitos dos fármacos
Compostos Organometálicos/farmacologia
Fenazinas/farmacologia
Quinoxalinas/farmacologia
Rutênio/farmacologia
Sacarina/farmacologia
[Mh] Termos MeSH secundário: Animais
Bovinos
Dano ao DNA
Relação Dose-Resposta a Droga
Estrutura Molecular
Compostos Organometálicos/síntese química
Compostos Organometálicos/química
Fenazinas/química
Processos Fotoquímicos
Quinoxalinas/química
Rutênio/química
Sacarina/química
Relação Estrutura-Atividade
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organometallic Compounds); 0 (Phenazines); 0 (Quinoxalines); 7UI0TKC3U5 (Ruthenium); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA); FST467XS7D (Saccharin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170509
[St] Status:MEDLINE


  8 / 2712 MEDLINE  
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[PMID]:28472674
[Au] Autor:Bian X; Tu P; Chi L; Gao B; Ru H; Lu K
[Ad] Endereço:Department of Environmental Health Science, University of Georgia, Athens, GA 30602, United States.
[Ti] Título:Saccharin induced liver inflammation in mice by altering the gut microbiota and its metabolic functions.
[So] Source:Food Chem Toxicol;107(Pt B):530-539, 2017 Sep.
[Is] ISSN:1873-6351
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Maintaining the balance of the gut microbiota and its metabolic functions is vital for human health, however, this balance can be disrupted by various external factors including food additives. A range of food and beverages are sweetened by saccharin, which is generally considered to be safe despite controversial debates. However, recent studies indicated that saccharin perturbed the gut microbiota. Inflammation is frequently associated with disruptions of the gut microbiota. The aim of this study is to investigate the relationship between host inflammation and perturbed gut microbiome by saccharin. C57BL/6J male mice were treated with saccharin in drinking water for six months. Q-PCR was used to detect inflammatory markers in mouse liver, while 16S rRNA gene sequencing and metabolomics were used to reveal changes of the gut microbiota and its metabolomic profiles. Elevated expression of pro-inflammatory iNOS and TNF-α in liver indicated that saccharin induced inflammation in mice. The altered gut bacterial genera, enriched orthologs of pathogen-associated molecular patterns, such as LPS and bacterial toxins, in concert with increased pro-inflammatory metabolites suggested that the saccharin-induced liver inflammation could be associated with the perturbation of the gut microbiota and its metabolic functions.
[Mh] Termos MeSH primário: Microbioma Gastrointestinal
Trato Gastrointestinal/microbiologia
Hepatopatias/imunologia
Fígado/imunologia
Sacarina/efeitos adversos
Edulcorantes/efeitos adversos
[Mh] Termos MeSH secundário: Animais
Microbioma Gastrointestinal/efeitos dos fármacos
Trato Gastrointestinal/efeitos dos fármacos
Trato Gastrointestinal/metabolismo
Seres Humanos
Fígado/efeitos dos fármacos
Hepatopatias/etiologia
Hepatopatias/genética
Hepatopatias/microbiologia
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Fator de Necrose Tumoral alfa/genética
Fator de Necrose Tumoral alfa/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sweetening Agents); 0 (Tumor Necrosis Factor-alpha); FST467XS7D (Saccharin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE


  9 / 2712 MEDLINE  
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[PMID]:28416101
[Au] Autor:Ivanova J; Carta F; Vullo D; Leitans J; Kazaks A; Tars K; Zalubovskis R; Supuran CT
[Ad] Endereço:Latvian Institute of Organic Synthesis, Aizkraukles Str. 21, Riga LV-1006, Latvia; Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, Paula Valdena Str. 3/7, Riga LV-1048, Latvia.
[Ti] Título:N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII.
[So] Source:Bioorg Med Chem;25(13):3583-3589, 2017 Jul 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo: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 K s 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 these derivatives of considerable interest as enzyme inhibitors with various pharmacologic applications.
[Mh] Termos MeSH primário: Anidrase Carbônica IX/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Sacarina/farmacologia
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/metabolismo
Anidrase Carbônica IX/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Sacarina/síntese química
Sacarina/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Carbonic Anhydrase Inhibitors); EC 4.2.1.1 (CA9 protein, human); EC 4.2.1.1 (Carbonic Anhydrase IX); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase XII); FST467XS7D (Saccharin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170803
[Lr] Data última revisão:
170803
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170419
[St] Status:MEDLINE


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[PMID]:28334357
[Au] Autor:Dess NK; Dobson K; Roberts BT; Chapman CD
[Ad] Endereço:Department of Psychology, Occidental College, 1600 Campus Road, Los Angeles, CA 90041, USA.
[Ti] Título:Sweetener Intake by Rats Selectively Bred for Differential Saccharin Intake: Sucralose, Stevia, and Acesulfame Potassium.
[So] Source:Chem Senses;42(5):381-392, 2017 Jun 01.
[Is] ISSN:1464-3553
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Behavioral responses to sweeteners have been used to study the evolution, mechanisms, and functions of taste. Occidental low and high saccharin consuming rats (respectively, LoS and HiS) have been selectively outbred on the basis of saccharin intake and are a valuable tool for studying variation among individuals in sweetener intake and its correlates. Relative to HiS rats, LoS rats consume smaller amounts of all nutritive and nonnutritive sweeteners tested to date, except aspartame. The lines also differ in intake of the commercial product Splenda; the roles of sucralose and saccharides in the difference are unclear. The present study extends prior work by examining intake of custom mixtures of sucralose, maltodextrin, and sugars and Splenda by LoS and HiS rats (Experiment 1A-1D), stevia and a constituent compound (rebaudioside A; Experiment 2A-2E), and acesulfame potassium tested at several concentrations or with 4 other sweeteners at one concentration each (Experiment 3A-3B). Results indicate that aversive side tastes limit intake of Splenda, stevia, and acesulfame potassium, more so among LoS rats than among HiS rats. In addition, regression analyses involving 5 sweeteners support the idea that both sweetness and bitterness are needed to account for intake of nonnutritive sweeteners, more so among LoS rats. These findings contribute to well developed and emerging literatures on sweetness and domain-general processes related to gustation.
[Mh] Termos MeSH primário: Ingestão de Alimentos
Sacarina/administração & dosagem
Stevia/química
Sacarose/análogos & derivados
Edulcorantes/administração & dosagem
Paladar/efeitos dos fármacos
Paladar/genética
Tiazinas/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Ratos
Análise de Regressão
Sacarina/farmacologia
Sacarose/administração & dosagem
Sacarose/farmacologia
Edulcorantes/farmacologia
Paladar/fisiologia
Tiazinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sweetening Agents); 0 (Thiazines); 57-50-1 (Sucrose); 96K6UQ3ZD4 (trichlorosucrose); FST467XS7D (Saccharin); MA3UYZ6K1H (acetosulfame)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170913
[Lr] Data última revisão:
170913
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170324
[St] Status:MEDLINE
[do] DOI:10.1093/chemse/bjx017



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