Base de dados : MEDLINE
Pesquisa : D02.886.952 [Categoria DeCS]
Referências encontradas : 876 [refinar]
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[PMID]:28346404
[Au] Autor:Kang HT; Park JT; Choi K; Kim Y; Choi HJC; Jung CW; Lee YS; Park SC
[Ad] Endereço:Well-Aging Research Center, Samsung Advanced Institute of Technology, Samsung Electronics, Suwon, Korea.
[Ti] Título:Chemical screening identifies ATM as a target for alleviating senescence.
[So] Source:Nat Chem Biol;13(6):616-623, 2017 06.
[Is] ISSN:1552-4469
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Senescence, defined as irreversible cell-cycle arrest, is the main driving force of aging and age-related diseases. Here, we performed high-throughput screening to identify compounds that alleviate senescence and identified the ataxia telangiectasia mutated (ATM) inhibitor KU-60019 as an effective agent. To elucidate the mechanism underlying ATM's role in senescence, we performed a yeast two-hybrid screen and found that ATM interacted with the vacuolar ATPase V subunits ATP6V1E1 and ATP6V1G1. Specifically, ATM decreased E-G dimerization through direct phosphorylation of ATP6V1G1. Attenuation of ATM activity restored the dimerization, thus consequently facilitating assembly of the V and V domains with concomitant reacidification of the lysosome. In turn, this reacidification induced the functional recovery of the lysosome/autophagy system and was coupled with mitochondrial functional recovery and metabolic reprogramming. Together, our data reveal a new mechanism through which senescence is controlled by the lysosomal-mitochondrial axis, whose function is modulated by the fine-tuning of ATM activity.
[Mh] Termos MeSH primário: Envelhecimento/efeitos dos fármacos
Sistemas de Liberação de Medicamentos
Morfolinas/farmacologia
Tioxantenos/farmacologia
[Mh] Termos MeSH secundário: Adenosina Trifosfatases/metabolismo
Animais
Proteínas Mutadas de Ataxia Telangiectasia/metabolismo
Núcleo Celular
Ativação Enzimática/efeitos dos fármacos
Citometria de Fluxo
Seres Humanos
Concentração de Íons de Hidrogênio
Lisossomos/enzimologia
Lisossomos/metabolismo
Camundongos
Mitocôndrias/enzimologia
Mitocôndrias/metabolismo
Fosforilação
Inibidores de Proteínas Quinases/farmacologia
Espécies Reativas de Oxigênio
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(2,6-dimethylmorpholin-4-yl)-N-(5-(6-morpholin-4-yl-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide); 0 (Morpholines); 0 (Protein Kinase Inhibitors); 0 (Reactive Oxygen Species); 0 (Thioxanthenes); EC 2.7.11.1 (Ataxia Telangiectasia Mutated Proteins); EC 3.6.1.- (Adenosine Triphosphatases)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170328
[St] Status:MEDLINE
[do] DOI:10.1038/nchembio.2342


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[PMID]:28237559
[Au] Autor:Luo L; Li Y; Qiang X; Cao Z; Xu R; Yang X; Xiao G; Song Q; Tan Z; Deng Y
[Ad] Endereço:Department of Medicinal Chemistry, Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
[Ti] Título:Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and ß-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
[So] Source:Bioorg Med Chem;25(6):1997-2009, 2017 Mar 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of 1-hydroxyl-3-aminoalkoxy-thioxanthone derivatives were designed, synthesized and evaluated as potential multifunctional agents against Alzheimer's disease (AD). The results indicated that most of these compounds exhibited good AChE and MAOs inhibitory activities, significant inhibition of self- and Cu -induced Aß aggregation, and moderate to good antioxidant activities. Specifically, compound 9e displayed high inhibitory potency toward AChE (IC =0.59±0.02µM), MAO-A and MAO-B (IC =1.01±0.02µM and 0.90±0.01µM respectively), excellent efficiency to block both self- and Cu -induced Aß aggregation (74.8±1.2% and 87.7±1.9% at 25µM, respectively), good metal-chelating property and a low toxicity in SH-SY5Y cells. Furthermore, kinetic and molecular modeling studies revealed that compound 9e binds simultaneously to the catalytic active site and peripheral anionic site of AChE, and could penetrate the BBB. Collectively, these results suggested that 9e might be a potential multifunctional agent for further development in the treatment of AD.
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Peptídeos beta-Amiloides/química
Inibidores da Colinesterase/farmacologia
Inibidores da Monoaminoxidase/farmacologia
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/efeitos dos fármacos
Doença de Alzheimer/enzimologia
Linhagem Celular
Inibidores da Colinesterase/química
Inibidores da Colinesterase/uso terapêutico
Seres Humanos
Cinética
Modelos Moleculares
Inibidores da Monoaminoxidase/química
Inibidores da Monoaminoxidase/uso terapêutico
Tioxantenos/química
Tioxantenos/farmacologia
Tioxantenos/uso terapêutico
Xantonas/química
Xantonas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Cholinesterase Inhibitors); 0 (Monoamine Oxidase Inhibitors); 0 (Thioxanthenes); 0 (Xanthones); EC 3.1.1.7 (Acetylcholinesterase); EOK1SAC304 (thioxanthone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170227
[St] Status:MEDLINE


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[PMID]:27465355
[Au] Autor:Ferreira AF; Ponte F; Silva R; Rocha-Pereira C; Sousa E; Pinto M; Bastos ML; Remião F
[Ad] Endereço:UCIBIO-REQUIMTE, Laboratório de Toxicologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
[Ti] Título:Quantification of 1-(propan-2-ylamino)-4-propoxy-9H-thioxanthen-9-one (TX5), a newly synthetized P-glycoprotein inducer/activator, in biological samples: method development and validation.
[So] Source:Biomed Chromatogr;31(2), 2017 Feb.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A simple, rapid and economical method was developed and validated for the analysis and quantification of 1-(propan-2-ylamino)-4-propoxy-9H-thioxanthen-9-one (TX5), a P-glycoprotein inducer/activator, in biological samples, using reverse-phase high-performance liquid chromatography (HPLC). A C column and a mobile phase composed of methanol-water (90/10, v/v) with 1% (v/v) triethylamine, at a flow rate of 1 mL/min, were used for chromatographic separation. TX5 standards (0.5-150 µm) were prepared in human serum. Methanol was used for TX5 extraction and serum protein precipitation. After filtration, samples were injected into the HPLC apparatus and TX5 was quantified by a conventional UV detector at 255 nm. The TX5 retention time was 13 min in this isocratic system. The method was validated according to ICH guidelines for specificity/selectivity, linearity, accuracy, precision, limits of detection and quantification (LOD and LOQ) and recovery. The method was proved to be selective, as there were no interferences of endogenous compounds with the same retention time of TX5. Also, the developed method was linear (r ≥ 0.99) for TX5 concentrations between 0.5 and 150 µm and the LOD and LOQ were 0.08 and 0.23 µm, respectively. The results indicated that the reported method could meet the requirements for TX5 analysis in the trace amounts expected to be present in biological samples.
[Mh] Termos MeSH primário: Subfamília B de Transportador de Cassetes de Ligação de ATP/agonistas
Cromatografia Líquida de Alta Pressão/métodos
Cromatografia de Fase Reversa/métodos
Xantonas/sangue
[Mh] Termos MeSH secundário: Seres Humanos
Limite de Detecção
Tioxantenos/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (ATP Binding Cassette Transporter, Sub-Family B); 0 (Thioxanthenes); 0 (Xanthones); EOK1SAC304 (thioxanthone)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160729
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.3802


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[PMID]:27735867
[Au] Autor:Lima RT; Sousa D; Paiva AM; Palmeira A; Barbosa J; Pedro M; Pinto MM; Sousa E; Vasconcelos MH
[Ad] Endereço:i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal. rlima@ipatimup.pt.
[Ti] Título:Modulation of Autophagy by a Thioxanthone Decreases the Viability of Melanoma Cells.
[So] Source:Molecules;21(10), 2016 Oct 10.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:(1) Background: Our previous studies unveiled the hit thioxanthone TXA1 as an inhibitor of P-glycoprotein (drug efflux pump) and of human tumor cells growth, namely of melanoma cells. Since TXA1 is structurally similar to lucanthone (an autophagy inhibitor and apoptosis inducer) and to -substituted phenoxazines (isosteres of thioxanthones, and autophagy inducers), this study aimed at further assessing its cytotoxic mechanism and evaluating its potential as an autophagy modulator in A375-C5 melanoma cells; (2) Methods: Flow cytometry with propidium iodide (PI) for cell cycle profile analysis; Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, flow cytometry with Annexin V/PI labeling and Western blot for apoptosis analysis were conducted. A pharmacophore approach was used for mapping TXA1 onto pharmacophores for autophagy induction. Autophagy analyses included transmission electron microscopy for visualization of autophagic structures, fluorescence microscopy for observation of monodansylcadaverine (MDC) staining, pattern of LC3 expression in the cells and acridine orange staining, and Western blot for autophagic proteins expression; (3) Results: TXA1 induced autophagy of melanoma cells at the GI concentration (3.6 µM) and apoptosis at twice that concentration. Following treatment with TXA1, autophagic structures were observed, together with the accumulation of autophagosomes and the formation of autophagolysosomes. An increase in LC3-II levels was also observed, which was reverted by 3-methyladenine (3-MA) (an early stage autophagy-inhibitor) but further increased by E-64d/pepstatin (late-stage autophagy inhibitors). Finally, 3-MA also reverted the effect of TXA1 in cellular viability; (4) Conclusion: TXA1 decreases the viability of melanoma cells by modulation of autophagy and may, therefore, serve as a lead compound for the development of autophagy modulators with antitumor activity.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Autofagia/efeitos dos fármacos
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Apoptose/efeitos dos fármacos
Biomarcadores
Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Expressão Gênica
Seres Humanos
Interações Hidrofóbicas e Hidrofílicas
Imuno-Histoquímica
Melanoma/genética
Melanoma/metabolismo
Melanoma/patologia
Melanoma/ultraestrutura
Modelos Moleculares
Conformação Molecular
Tioxantenos/química
Tioxantenos/farmacologia
Xantonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Biomarkers); 0 (Thioxanthenes); 0 (Xanthones); EOK1SAC304 (thioxanthone)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161014
[St] Status:MEDLINE


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[PMID]:27454205
[Au] Autor:Cocci P; Mozzicafreddo M; Angeletti M; Mosconi G; Palermo FA
[Ad] Endereço:School of Biosciences and Veterinary Medicine, University of Camerino, Via Gentile III Da Varano, I-62032 Camerino, MC, Italy. Electronic address: paolo.cocci@unicam.it.
[Ti] Título:In silico prediction and in vivo analysis of antiestrogenic potential of 2-isopropylthioxanthone (2-ITX) in juvenile goldfish (Carassius auratus).
[So] Source:Ecotoxicol Environ Saf;133:202-10, 2016 Nov.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Previous studies have shown both anti-estrogenic and anti-androgenic activities of 2-isopropylthioxanthone (2-ITX), a well known food contaminant, in in vitro assays. However, no data are available on the anti-estrogenic potentials and risks of 2-ITX in aquatic organisms. This work evaluated the potential endocrine disrupting effects of 2-ITX at the level of estrogen receptor (ER) signaling cascade using juvenile goldfish (Carassius auratus) as model. Firstly, we investigated the ligand binding efficiency of 2-ITX to the ligand binding domains (LBD) of goldfish ER subtypes using a molecular docking approach. Secondly, we assessed the effects of 2-ITX on E2-induced hepatic expression of ERα1, ERß1, ERß2, and vitellogenin (VTG) in vivo. Crosstalk between ER-VTG and aryl hydrocarbon receptor 2 (AhR2)-cytochrome P4501A (CYP1A) was also investigated. Fish were injected with increasing doses of 2-ITX ranging from 2 to 10µg/g BW, and results were compared to the effect of tamoxifen, a well-known ER modulator. We observed that compared to ERß, the interaction potentials of 2-ITX to goldfish ERα1 LBD was more stable in the inactive receptor conformation. The in silico docking simulation analysis also revealed that 2-ITX acted as agonist for the goldfish AhR2 LBDs suggesting the ability of this compound to activate the cross-talk between the ERα- and AhR-signaling pathways. In vivo experiments confirm in silico simulation predictions demonstrating that 2-ITX reduced the estrogenicity of E2 at both transcriptional and post-transcriptional levels, indicating a clear anti-estrogenic effect. Co-exposure of E2 and 2-ITX also resulted in a significant decrease of CYP1A gene expression with respect to 2-ITX alone. Results from these studies collectively revealed that the antiestrogenic property of 2-ITX can be ascribed to a combination of effects on multiple signaling pathways suggesting the potential for this environmental contaminant to affect the hormonal control of reproductive processes in fish.
[Mh] Termos MeSH primário: Simulação por Computador
Antagonistas de Estrogênios/toxicidade
Carpa Dourada/fisiologia
Simulação de Acoplamento Molecular
Tioxantenos/toxicidade
[Mh] Termos MeSH secundário: Adolescente
Animais
Disruptores Endócrinos/metabolismo
Receptor alfa de Estrogênio/metabolismo
Expressão Gênica
Carpa Dourada/metabolismo
Seres Humanos
Fígado/efeitos dos fármacos
Receptores de Hidrocarboneto Arílico/metabolismo
Vitelogeninas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Endocrine Disruptors); 0 (Estrogen Antagonists); 0 (Estrogen Receptor alpha); 0 (Receptors, Aryl Hydrocarbon); 0 (Thioxanthenes); 0 (Vitellogenins); 0 (isopropyl-9H-thioxanthen-9-one)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170125
[Lr] Data última revisão:
170125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160726
[St] Status:MEDLINE


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[PMID]:27168378
[Au] Autor:Yilmaz G; Guler E; Barlas FB; Timur S; Yagci Y
[Ad] Endereço:Department of Chemistry, Faculty of Science and Letters, Istanbul Technical University, 34469, Istanbul, Turkey.
[Ti] Título:Polymeric Thioxanthones as Potential Anticancer and Radiotherapy Agents.
[So] Source:Macromol Rapid Commun;37(13):1046-51, 2016 Jul.
[Is] ISSN:1521-3927
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Thioxanthone (TX) and its derivatives, which are widely used as photoinitiators in UV curing technology, hold promising research interest in biological applications. In particular, the use of TXs as anticancer agent has recently been manifested as an outstanding additional property of this class of molecules. Incorporation of TX molecules into specially designed polymers widens their practical use in such applications. In this study, two water-soluble, biocompatible, and stable polymers, namely poly(vinyl alcohol) and poly(ethylene glycol), possessing TX moieties at the side chains and chain ends, respectively, are prepared and used as anticancer and radiotherapy agents. The findings confirm that both polymers are potential candidates for therapeutic agents as they possess useful features including water-solubility, radiosensitizer effect, and anticancer activity in a polymeric scaffold.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Quimiorradioterapia
Neoplasias/terapia
Polietilenoglicóis/farmacologia
Álcool de Polivinil/farmacologia
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Neoplasias/tratamento farmacológico
Neoplasias/radioterapia
Polietilenoglicóis/síntese química
Polietilenoglicóis/química
Álcool de Polivinil/síntese química
Álcool de Polivinil/química
Relação Estrutura-Atividade
Tioxantenos/síntese química
Tioxantenos/química
Tioxantenos/farmacologia
Células Tumorais Cultivadas
Xantonas/síntese química
Xantonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Thioxanthenes); 0 (Xanthones); 30IQX730WE (Polyethylene Glycols); 9002-89-5 (Polyvinyl Alcohol); EOK1SAC304 (thioxanthone)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160512
[St] Status:MEDLINE
[do] DOI:10.1002/marc.201600189


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[PMID]:27146794
[Au] Autor:Van Den Houwe K; Evrard C; Van Loco J; Lynen F; Van Hoeck E
[Ad] Endereço:a Department of Food, Medicines and Consumer Safety , Scientific Institute of Public Health , Brussels , Belgium.
[Ti] Título:Migration of photoinitiators from cardboard into dry food: evaluation of Tenax® as a food simulant.
[So] Source:Food Addit Contam Part A Chem Anal Control Expo Risk Assess;33(5):913-20, 2016 May.
[Is] ISSN:1944-0057
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Photoinitiators are widely used to cure ink on packaging materials used in food applications such as cardboards for the packaging of dry foods. Conventional migration testing for long-term storage at ambient temperature with Tenax(®) was applied to paperboard for the following photoinitiators: benzophenone (BP), 4,4'-bis(diethylamino)benzophenone (DEAB), 2-chloro-9H-thioxanthen-9-one (CTX), 1-chloro-4-propoxy-9H-thioxanthen-9-one (CPTX), 4-(dimethylamino)benzophenone (DMBP), 2-ethylanthraquinone (EA), 2-ethylhexyl-4-dimethylaminobenzoate (EDB), ethyl-4-dimethylaminobenzoate (EDMAB), 4-hydroxybenzophenone (4-HBP), 2-hydroxy-4-methoxybenzophenone (HMBP), 2-hydroxy-4'-(2-hydroxyethoxy)-2-methylpropiophenone (HMMP), 2-isopropyl-9H-thioxanthen-9-one (ITX), 4-methylbenzophenone (MBP) and Michler's ketone (MK). Test conditions (10 days at 60°C) were according to Regulation (EU) No. 10/2011 and showed different migration patterns for the different photoinitiators. The results were compared with the migration in cereals after a storage of 6 months at room temperature. The simulation with Tenax at 60°C overestimated actual migration in cereals up to a maximum of 92%. In addition, the effect of a lower contact temperature and the impact of the Tenax pore size were investigated. Analogous simulation performed with rice instead of Tenax resulted in insufficiently low migration rates, showing Tenax is a much stronger adsorbent than rice and cereals.
[Mh] Termos MeSH primário: Contaminação de Alimentos/prevenção & controle
Embalagem de Alimentos
Teste de Materiais/métodos
Modelos Químicos
Papel
Fármacos Fotossensibilizantes/análise
Polímeros/química
[Mh] Termos MeSH secundário: Adsorção
Antraquinonas/análise
Antraquinonas/química
Bélgica
Benzofenonas/análise
Benzofenonas/química
Grãos Comestíveis/química
União Europeia
Embalagem de Alimentos/normas
Armazenamento de Alimentos
Temperatura Alta
Tinta
Cinética
Teste de Materiais/normas
Oryza/química
Papel/normas
Fármacos Fotossensibilizantes/química
Porosidade
Sementes/química
Tioxantenos/análise
Tioxantenos/química
para-Aminobenzoatos/análise
para-Aminobenzoatos/química
[Pt] Tipo de publicação:COMPARATIVE STUDY; EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthraquinones); 0 (Benzophenones); 0 (Photosensitizing Agents); 0 (Polymers); 0 (Thioxanthenes); 0 (para-Aminobenzoates); 24938-68-9 (tenax)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170201
[Lr] Data última revisão:
170201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160506
[St] Status:MEDLINE
[do] DOI:10.1080/19440049.2016.1179562


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[PMID]:27010861
[Au] Autor:Liu P; Zhao C; Zhang Y; Chen Y
[Ad] Endereço:College of Chemistry & Environmental Science, Hebei Univ, Baoding, 071000, China.
[Ti] Título:Simultaneous Determination of 10 Photoinitiators in Milk by Solid-Phase Microextraction Coupled with Gas Chromatography/Mass Spectrometry.
[So] Source:J Food Sci;81(5):T1336-41, 2016 May.
[Is] ISSN:1750-3841
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Photoinitiators (PIs) are widely used in food packaging materials, can migrate easily from packaging materials to food, and cause food contamination. It is essential to establish a method of determining PIs residues in food. A new method for simultaneously determining 10 kinds of PIs in milk has been established by using solid-phase microextraction (SPME) combined with a simple method of protein precipitation as the pretreatment approach and gas chromatography/mass spectrometry as the detecting technique. The limits of detection for 10 PIs in different milks were between 0.05 and 1.4 µg/L (skimmed milk), between 0.07 and 2.2 µg/L (semi-skimmed milk), between 0.11 and 4.4 µg/L (whole milk), respectively. The recoveries were from 71.5% to 133.5%, and the relative standard deviations were less than 15%. Twelve kinds of packed milk with different brands and fat contents were determined using this method.
[Mh] Termos MeSH primário: Contaminação de Alimentos/análise
Embalagem de Alimentos
Substâncias Perigosas/análise
Leite/química
[Mh] Termos MeSH secundário: Acetofenonas/análise
Animais
Benzofenonas/análise
Cromatografia Gasosa-Espectrometria de Massas/métodos
Seres Humanos
Microextração em Fase Sólida/métodos
Tioxantenos/análise
para-Aminobenzoatos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetophenones); 0 (Benzophenones); 0 (Hazardous Substances); 0 (Thioxanthenes); 0 (ethyl 4-N,N-dimethylaminobenzoate); 0 (isopropyl-9H-thioxanthen-9-one); 0 (para-Aminobenzoates)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160325
[St] Status:MEDLINE
[do] DOI:10.1111/1750-3841.13268


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[PMID]:26771595
[Au] Autor:Barbosa J; Lima RT; Sousa D; Gomes AS; Palmeira A; Seca H; Choosang K; Pakkong P; Bousbaa H; Pinto MM; Sousa E; Vasconcelos MH; Pedro M
[Ad] Endereço:CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, IUCS-Instituto Universitário de Ciências da Saúde, Rua Central de Gandra 1317, Gandra 4585-116, Portugal. j.filipebarbosa@hotmail.com.
[Ti] Título:Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis.
[So] Source:Molecules;21(1):81, 2016 Jan 13.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Our previous work has described a library of thioxanthones designed to have dual activity as P-glycoprotein modulators and antitumor agents. Some of these compounds had shown a significant cell growth inhibitory activity towards leukemia cell lines, without affecting the growth of non-tumor human fibroblasts. However, their effect in cell lines derived from solid tumors has not been previously studied. The present work aimed at: (i) screening this small series of compounds from an in-house library, for their in vitro cell growth inhibitory activity in human tumor cell lines derived from solid tumors; and (ii) initiate a study of the effect of the most potent compound on apoptosis. The tumor cell growth inhibitory effect of 27 compounds was first analysed in different human tumor cell lines, allowing the identification of a hit compound, TXA1. Its hydrochloride salt TXA1·HCl was then synthesized, to improve solubility and bioavailability. Both TXA1 and TXA1·HCl inhibited the growth of MCF-7, NCI-H460, A375-C5, HeLa, 786-O, Caki-2 and AGS cell lines. The effect of TXA1·HCl in MCF-7 cells was found to be irreversible and was associated, at least in part, with an increase in cellular apoptosis.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Bibliotecas de Moléculas Pequenas/farmacologia
Tioxantenos/farmacologia
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Linhagem Celular Tumoral
Células HeLa
Ensaios de Triagem em Larga Escala
Seres Humanos
Concentração Inibidora 50
Células MCF-7
Bibliotecas de Moléculas Pequenas/síntese química
Relação Estrutura-Atividade
Tioxantenos/síntese química
Xantonas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Small Molecule Libraries); 0 (Thioxanthenes); 0 (Xanthones)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160116
[St] Status:MEDLINE


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[PMID]:26649800
[Au] Autor:Liu R; Lin Y; Hu F; Liu R; Ruan T; Jiang G
[Ad] Endereço:State Key Laboratory of Environmental Chemistry and Ecotoxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences , Beijing, China , 100085.
[Ti] Título:Observation of Emerging Photoinitiator Additives in Household Environment and Sewage Sludge in China.
[So] Source:Environ Sci Technol;50(1):97-104, 2016 Jan 05.
[Is] ISSN:1520-5851
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Photoinitiators (PIs) are widely used additives in industrial polymerization process, the contamination of which through migration into foodstuffs has been subjected to increasing public scrutiny. Nevertheless, little attention has been paid to the PI residue levels and potential exposure pathways from other environmental compartments. In the present study, the occurrence of PI additives with discrete molecular structures, that is, nine benzophenones (BZPs), four thioxanthones (TXs), and eight amine co-initiators (ACIs), was investigated in commercial products, indoor dust and sewage sludge samples. Nine PI compounds were positively detected in ultraviolet curable resins with concentrations of ∑PIs (sum of the detected PIs) up to 2.51 × 10(4) ng/g, and 20 PIs can be found in food contact materials with concentrations of ∑PIs varying from 65.9 to 6.93 × 10(3) ng/g. The wide usage of PIs in commercial products led to the occurrence of 19 PIs in indoor dust, with concentrations of ∑PIs in the range of 245-5.68 × 10(3) ng/g. Meanwhile, all 21 targeted PIs could be identified in the sewage sludge, with concentrations from 67.6 to 2.03 × 10(3) ng/g. Distinct PI composition profiles were observed in different investigated compartments, and BZPs were the dominant homologues in all samples. Most of the target PIs were further identified as class III chemicals by toxic hazard estimation algorithm (Toxtree), which indicates the compounds might be of significant toxicity or have reactive functional groups.
[Mh] Termos MeSH primário: Benzofenonas/análise
Poluentes Ambientais/análise
Esgotos/química
Xantonas/análise
[Mh] Termos MeSH secundário: China
Poeira
Monitoramento Ambiental
Características da Família
Tioxantenos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzophenones); 0 (Dust); 0 (Environmental Pollutants); 0 (Sewage); 0 (Thioxanthenes); 0 (Xanthones); EOK1SAC304 (thioxanthone)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151210
[St] Status:MEDLINE
[do] DOI:10.1021/acs.est.5b04977



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