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[PMID]:29385177
[Au] Autor:Dickel F; Münch D; Amdam GV; Mappes J; Freitak D
[Ad] Endereço:Centre of Excellence in Biological Interactions, Department of Biological and Environmental Science, University of Jyvaskyla, Jyvaskyla, Finland.
[Ti] Título:Increased survival of honeybees in the laboratory after simultaneous exposure to low doses of pesticides and bacteria.
[So] Source:PLoS One;13(1):e0191256, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recent studies of honeybees and bumblebees have examined combinatory effects of different stressors, as insect pollinators are naturally exposed to multiple stressors. At the same time the potential influences of simultaneously occurring agricultural agents on insect pollinator health remain largely unknown. Due to different farming methods, and the drift of applied agents and manure, pollinators are most probably exposed to insecticides but also bacteria from organic fertilizers at the same time. We orally exposed honeybee workers to sub-lethal doses of the insecticide thiacloprid and two strains of the bacterium Enterococcus faecalis, which can occur in manure from farming animals. Our results show that under laboratory conditions the bees simultaneously exposed to the a bacterium and the pesticide thiacloprid thiacloprid had significant higher survival rates 11 days post exposure than the controls, which surprisingly showed the lowest survival. Bees that were exposed to diet containing thiacloprid showed decreased food intake. General antibacterial activity is increased by the insecticide and the bacteria, resulting in a higher immune response observed in treated individuals compared to control individuals. We thus propose that caloric restriction through behavioural and physiological adaptations may have mediated an improved survival and stress resistance in our tests. However, the decreased food consumption could in long-term also result in possible negative effects at colony level. Our study does not show an additive negative impact of sub-lethal insecticide and bacteria doses, when tested under laboratory conditions. In contrast, we report seemingly beneficial effects of simultaneous exposure of bees to agricultural agents, which might demonstrate a surprising biological capacity for coping with stressors, possibly through hormetic regulation.
[Mh] Termos MeSH primário: Abelhas/efeitos dos fármacos
Abelhas/microbiologia
Enterococcus faecalis/patogenicidade
Inseticidas/toxicidade
Neonicotinoides/toxicidade
Tiazinas/toxicidade
[Mh] Termos MeSH secundário: Animais
Abelhas/fisiologia
Ingestão de Alimentos/efeitos dos fármacos
Hormese
Inseticidas/administração & dosagem
Neonicotinoides/administração & dosagem
Polinização
Estresse Fisiológico
Tiazinas/administração & dosagem
Virulência
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Insecticides); 0 (Neonicotinoids); 0 (Thiazines); DSV3A944A4 (thiacloprid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180201
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191256


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[PMID]:29232580
[Au] Autor:Solomon VR; Pundir S; Le HT; Lee H
[Ad] Endereço:Health Sciences North Research Institute, 41 Ramsey Lake Road, Sudbury, Ontario P3E 5J1, Canada. Electronic address: vrajasolomon@gmail.com.
[Ti] Título:Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
[So] Source:Eur J Med Chem;143:1028-1038, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:In an attempt to develop effective and safe anticancer agents, we designed, synthesized and examined 23 novel quinacrine (QC) derivatives by combining the 9-aminoacridine scaffold and the [1,3]thiazinan-4-ones group. Most of these hybrids showed strong anticancer activities, among which 3-(3-(6-chloro-2-methoxyacridin-9-ylamino)propyl)-2-(thiophen-2-yl)-1,3-thiazinan-4-one (25; VR151) effectively killed many different cancer cell types, including eight breast cancer cell lines with different genetic background, two prostate cancer and two lung cancer cell lines. In contrast, compound 25 is less effective against non-cancer cells, suggesting it may be less toxic to humans. Our data showed that cancer cells are arrested in S phase for a prolonged period due to the down-regulation of DNA replication, leading to eventual cell death. We have also shown that the S phase arrest may be resulted by the down-regulation of cyclin A coupled with the continued up-regulation of cyclin E, which coincide with the down-regulation of mTor-S6K and mTor-4EBP1 pathways.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Neoplasias da Mama/tratamento farmacológico
Desenho de Drogas
Quinacrina/análogos & derivados
Tiazinas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Neoplasias da Mama/patologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Feminino
Seres Humanos
Estrutura Molecular
Quinacrina/síntese química
Quinacrina/química
Quinacrina/farmacologia
Relação Estrutura-Atividade
Tiazinas/síntese química
Tiazinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Thiazines); H0C805XYDE (Quinacrine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE


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[PMID]:28782989
[Au] Autor:O'Sullivan AJ; Pigat S; O'Mahony C; Gibney MJ; McKevitt AI
[Ad] Endereço:a UCD Institute of Food and Health, School of Agriculture and Food Science , University College Dublin , Dublin , Republic of Ireland.
[Ti] Título:Longitudinal modelling of the exposure of young UK patients with PKU to acesulfame K and sucralose.
[So] Source:Food Addit Contam Part A Chem Anal Control Expo Risk Assess;34(11):1863-1874, 2017 Nov.
[Is] ISSN:1944-0057
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Artificial sweeteners are used in protein substitutes intended for the dietary management of inborn errors of metabolism (phenylketonuria, PKU) to improve the variety of medical foods available to patients and ensure dietary adherence to the prescribed course of dietary management. These patients can be exposed to artificial sweeteners from the combination of free and prescribed foods. Young children have a higher risk of exceeding acceptable daily intakes (ADI) for additives than adults, due to higher food intakes per kg body weight. Young patients with PKU aged 1-3 years can be exposed to higher levels of artificial sweeteners from these dual sources than normal healthy children and are at a higher risk of exceeding the ADI. Standard intake assessment methods are not adequate to assess the additive exposure of young patients with PKU. The aim of this study was to estimate the combination effect on the intake of artificial sweeteners and the impact of the introduction of new provisions for an artificial sweetener (sucralose, E955) on exposure of PKU patients using a validated probabilistic model. Food consumption data were derived from the food consumption survey data of healthy young children in the United Kingdom from the National Diet and Nutrition Survey (NDNS, 1992-2012). Specially formulated protein substitutes as foods for special medical purposes (FSMPs) were included in the exposure model to replace restricted foods. Inclusion of these protein substitutes is based on recommendations to ensure adequate protein intake in these patients. Exposure assessment results indicated the availability of sucralose for use in FSMPs for PKU leads to changes in intakes in young patients. These data further support the viability of probabilistic modelling as a means to estimate food additive exposure in patients consuming medical nutrition products.
[Mh] Termos MeSH primário: Aditivos Alimentares/administração & dosagem
Inquéritos Nutricionais
Fenilcetonúrias/metabolismo
Sacarose/análogos & derivados
Edulcorantes/administração & dosagem
Tiazinas/administração & dosagem
[Mh] Termos MeSH secundário: Pré-Escolar
Seres Humanos
Lactente
Estudos Longitudinais
Modelos Estatísticos
Fenilcetonúrias/dietoterapia
Sacarose/administração & dosagem
Reino Unido
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Food Additives); 0 (Sweetening Agents); 0 (Thiazines); 57-50-1 (Sucrose); 96K6UQ3ZD4 (trichlorosucrose); MA3UYZ6K1H (acetosulfame)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170808
[St] Status:MEDLINE
[do] DOI:10.1080/19440049.2017.1363417


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[PMID]:28770976
[Au] Autor:Eccleston C; Cooper TE; Fisher E; Anderson B; Wilkinson NM
[Ad] Endereço:Centre for Pain Research, University of Bath, Claverton Down, Bath, UK.
[Ti] Título:Non-steroidal anti-inflammatory drugs (NSAIDs) for chronic non-cancer pain in children and adolescents.
[So] Source:Cochrane Database Syst Rev;8:CD012537, 2017 08 02.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as important.We designed a suite of seven reviews on chronic non-cancer pain and cancer pain (looking at antidepressants, antiepileptic drugs, non-steroidal anti-inflammatory drugs, opioids, and paracetamol) in order to review the evidence for children's pain utilising pharmacological interventions.As the leading cause of morbidity in the world today, chronic disease (and its associated pain) is a major health concern. Chronic pain (that is pain lasting three months or longer) can arise in the paediatric population in a variety of pathophysiological classifications (nociceptive, neuropathic, or idiopathic) from genetic conditions, nerve damage pain, chronic musculoskeletal pain, and chronic abdominal pain, as well as for other unknown reasons.Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat pain, reduce fever, and for their anti-inflammation properties. They are commonly used within paediatric pain management. Non-steroidal anti-inflammatory drugs are currently licensed for use in Western countries, however they are not approved for infants under three months old. The main adverse effects include renal impairment and gastrointestinal issues. Common side effects in children include diarrhoea, headache, nausea, constipation, rash, dizziness, and abdominal pain. OBJECTIVES: To assess the analgesic efficacy and adverse events of NSAIDs used to treat chronic non-cancer pain in children and adolescents aged between birth and 17 years, in any setting. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL) via the Cochrane Register of Studies Online, MEDLINE via Ovid, and Embase via Ovid from inception to 6 September 2016. We also searched the reference lists of retrieved studies and reviews, as well as online clinical trial registries. SELECTION CRITERIA: Randomised controlled trials, with or without blinding, of any dose and any route, treating chronic non-cancer pain in children and adolescents, comparing any NSAID with placebo or an active comparator. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed studies for eligibility. We planned to use dichotomous data to calculate risk ratio and number needed to treat for one additional event, using standard methods. We assessed GRADE and created three 'Summary of findings' tables. MAIN RESULTS: We included seven studies with a total of 1074 participants (aged 2 to 18 years) with chronic juvenile polyarthritis or chronic juvenile rheumatoid arthritis. All seven studies compared an NSAID with an active comparator. None of the studies were placebo controlled. No two studies investigated the same type of NSAID compared with another. We were unable to perform a meta-analysis.Risk of bias varied. For randomisation and allocation concealment, one study was low risk and six studies were unclear risk. For blinding of participants and personnel, three studies were low risk and four studies were unclear to high risk. For blinding of outcome assessors, all studies were unclear risk. For attrition, four studies were low risk and three studies were unclear risk. For selective reporting, four studies were low risk, two studies were unclear risk, and one study was high risk. For size, three studies were unclear risk and four studies were high risk. For other potential sources of bias, seven studies were low risk. Primary outcomesThree studies reported participant-reported pain relief of 30% or greater, showing no statistically significant difference in pain scores between meloxicam and naproxen, celecoxib and naproxen, or rofecoxib and naproxen (P > 0.05) (low-quality evidence).One study reported participant-reported pain relief of 50% or greater, showing no statistically significant difference in pain scores between low-dose meloxicam (0.125 mg/kg) and high-dose meloxicam (0.25 mg/kg) when compared to naproxen 10 mg/kg (P > 0.05) (low-quality evidence).One study reported Patient Global Impression of Change, showing 'very much improved' in 85% of ibuprofen and 90% of aspirin participants (low-quality evidence). Secondary outcomesAll seven studies reported adverse events. Participants reporting an adverse event (one or more per person) by drug were: aspirin 85/202; fenoprofen 28/49; ibuprofen 40/45; indomethacin 9/30; ketoprofen 9/30; meloxicam 18/47; naproxen 44/202; and rofecoxib 47/209 (very low-quality evidence).All seven studies reported withdrawals due to adverse events. Participants withdrawn due to an adverse event by drug were: aspirin 16/120; celecoxib 10/159; fenoprofen 0/49; ibuprofen 0/45; indomethacin 0/30; ketoprofen 0/30; meloxicam 10/147; naproxen 17/285; and rofecoxib 3/209 (very low-quality evidence).All seven studies reported serious adverse events. Participants experiencing a serious adverse event by drug were: aspirin 13/120; celecoxib 5/159; fenoprofen 0/79; ketoprofen 0/30; ibuprofen 4/45; indomethacin 0/30; meloxicam 11/147; naproxen 10/285; and rofecoxib 0/209 (very low-quality evidence).There were few or no data for our remaining secondary outcomes: Carer Global Impression of Change; requirement for rescue analgesia; sleep duration and quality; acceptability of treatment; physical functioning as defined by validated scales; and quality of life as defined by validated scales (very low-quality evidence).We rated the overall quality of the evidence (GRADE rating) for our primary and secondary outcomes as very low because there were limited data from studies and no opportunity for a meta-analysis. AUTHORS' CONCLUSIONS: We identified only a small number of studies, with insufficient data for analysis.As we could undertake no meta-analysis, we are unable to comment about efficacy or harm from the use of NSAIDs to treat chronic non-cancer pain in children and adolescents. Similarly, we cannot comment on our remaining secondary outcomes: Carer Global Impression of Change; requirement for rescue analgesia; sleep duration and quality; acceptability of treatment; physical functioning; and quality of life.We know from adult randomised controlled trials that some NSAIDs, such as ibuprofen, naproxen, and aspirin, can be effective in certain chronic pain conditions.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/uso terapêutico
Artrite Juvenil/tratamento farmacológico
Artrite Reumatoide/tratamento farmacológico
Dor Crônica/tratamento farmacológico
[Mh] Termos MeSH secundário: Adolescente
Anti-Inflamatórios não Esteroides/efeitos adversos
Aspirina/efeitos adversos
Aspirina/uso terapêutico
Celecoxib/efeitos adversos
Celecoxib/uso terapêutico
Criança
Pré-Escolar
Doença Crônica
Fenoprofeno/efeitos adversos
Fenoprofeno/uso terapêutico
Seres Humanos
Ibuprofeno/efeitos adversos
Ibuprofeno/uso terapêutico
Lactonas/efeitos adversos
Lactonas/uso terapêutico
Metoxaleno/efeitos adversos
Metoxaleno/uso terapêutico
Naproxeno/efeitos adversos
Naproxeno/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Sulfonas/efeitos adversos
Sulfonas/uso terapêutico
Tiazinas/efeitos adversos
Tiazinas/uso terapêutico
Tiazóis/efeitos adversos
Tiazóis/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Lactones); 0 (Sulfones); 0 (Thiazines); 0 (Thiazoles); 0QTW8Z7MCR (rofecoxib); 57Y76R9ATQ (Naproxen); JCX84Q7J1L (Celecoxib); R16CO5Y76E (Aspirin); RA33EAC7KY (Fenoprofen); U4VJ29L7BQ (Methoxsalen); VG2QF83CGL (meloxicam); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170804
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD012537.pub2


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[PMID]:28750898
[Au] Autor:Caron-Beaudoin E; Viau R; Hudon-Thibeault AA; Vaillancourt C; Sanderson JT
[Ad] Endereço:INRS - Institut Armand-Frappier, Laval, QC H7V 1B7, Canada; Center for Interdisciplinary Research on Well-Being, Health, Society and Environment (CINBIOSE), Université du Québec à Montréal, Montreal, QC H3C 3P8, Canada. Electronic address: elyse.caron-beaudoin@iaf.inrs.ca.
[Ti] Título:The use of a unique co-culture model of fetoplacental steroidogenesis as a screening tool for endocrine disruptors: The effects of neonicotinoids on aromatase activity and hormone production.
[So] Source:Toxicol Appl Pharmacol;332:15-24, 2017 Oct 01.
[Is] ISSN:1096-0333
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Estrogen biosynthesis during pregnancy is dependent on the collaboration between the fetus producing the androgen precursors, and the placenta expressing the enzyme aromatase (CYP19). Disruption of estrogen production by contaminants may result in serious pregnancy outcomes. We used our recently developed in vitro co-culture model of fetoplacental steroidogenesis to screen the effects of three neonicotinoid insecticides on the catalytic activity of aromatase and the production of steroid hormones. A co-culture of H295R human adrenocortical carcinoma cells with fetal characteristics and BeWo human choriocarcinoma cells which display characteristics of the villous cytotrophoblast was exposed for 24h to various concentrations of three neonicotinoids: thiacloprid, thiamethoxam and imidacloprid. Aromatase catalytic activity was determined in both cell lines using the tritiated water-release assay. Hormone production was measured by ELISA. The three neonicotinoids induced aromatase activity in our fetoplacental co-culture and concordingly, estradiol and estrone production were increased. In contrast, estriol production was strongly inhibited by the neonicotinoids. All three pesticides induced the expression of CYP3A7 in H295R cells, and this induction was reversed by co-treatment of H295R cells with exogenous estriol. CYP3A7 is normally expressed in fetal liver and is a key enzyme involved in estriol synthesis. We suggest that neonicotinoids are metabolized by CYP3A7, thus impeding the 16α-hydroxylation of fetal DHEA(-sulfate), which is normally converted to estriol by placental aromatase. We successfully used the fetoplacental co-culture as a physiologically relevant tool to highlight the potential effects of neonicotinoids on estrogen production, aromatase activity and CYP3A7 expression during pregnancy.
[Mh] Termos MeSH primário: Aromatase/metabolismo
Técnicas de Cocultura/métodos
Disruptores Endócrinos/toxicidade
Inseticidas/toxicidade
Placenta/efeitos dos fármacos
[Mh] Termos MeSH secundário: Carcinoma Adrenocortical
Linhagem Celular Tumoral
Coriocarcinoma/induzido quimicamente
Coriocarcinoma/diagnóstico
Citocromo P-450 CYP3A/genética
Citocromo P-450 CYP3A/metabolismo
Estradiol/metabolismo
Estrogênios/metabolismo
Estrona/metabolismo
Feminino
Regulação da Expressão Gênica
Seres Humanos
Imidazóis/toxicidade
Neonicotinoides
Nitrocompostos/toxicidade
Oxazinas/toxicidade
Placenta/metabolismo
Gravidez
Piridinas/toxicidade
Tiazinas/toxicidade
Tiazóis/toxicidade
Neoplasias Uterinas/induzido quimicamente
Neoplasias Uterinas/diagnóstico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Endocrine Disruptors); 0 (Estrogens); 0 (Imidazoles); 0 (Insecticides); 0 (Neonicotinoids); 0 (Nitro Compounds); 0 (Oxazines); 0 (Pyridines); 0 (Thiazines); 0 (Thiazoles); 2DI9HA706A (Estrone); 3BN7M937V8 (imidacloprid); 4TI98Z838E (Estradiol); 747IC8B487 (thiamethoxam); DSV3A944A4 (thiacloprid); EC 1.14.14.1 (Aromatase); EC 1.14.14.1 (CYP19A1 protein, human); EC 1.14.14.1 (CYP3A7 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170729
[St] Status:MEDLINE


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[PMID]:28728107
[Au] Autor:Katselou MG; Matralis AN; Kourounakis AP
[Ad] Endereço:Division of Medicinal Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, 15771 Athens, Greece.
[Ti] Título:Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity.
[So] Source:Eur J Med Chem;138:748-760, 2017 Sep 29.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:For the treatment of multifactorial and complex diseases, it has become increasingly apparent that compounds acting at multiple targets often deliver superior efficacy compared to compounds with high specificity for only a single target. Based on previous studies demonstrating the important antioxidant and anti-hyperlipidemic effect of morpholine and 1,4-benzo(x/thi)azine derivatives (A-E), we hereby present the design, synthesis and pharmacological evaluation of novel dual-acting molecules as a therapeutic approach for atherosclerosis. Analogues 1-10 were rationally designed through structural modifications of their parent compounds (A-E) in order for structure-activity relationship studies to be carried out. Most compounds showed a significant inhibition against Squalene Synthase activity exhibiting at the same time a very potent multimodal antioxidant (against lipid peroxidation and as free-radical scavengers) effect, thus bringing to light the 2-aryl-1,4-benzo(x/thia)zin-2-ol scaffold as an outstanding pharmacophore for the design of potent antioxidants. Finally, the replacement of the octahydro-1,4-benzoxazine moiety of lead compound D with its respective 1,4-benzothiazine (compound 4), although conserved (anti-hypercholesterolemic) or even improved (anti-hyperlipidemic) activity, did not preserve the anti-diabetic effect of D.
[Mh] Termos MeSH primário: Aterosclerose/tratamento farmacológico
Diabetes Mellitus Tipo 2/tratamento farmacológico
Desenho de Drogas
Inibidores Enzimáticos/farmacologia
Farnesil-Difosfato Farnesiltransferase/antagonistas & inibidores
Hipolipemiantes/farmacologia
[Mh] Termos MeSH secundário: Animais
Ciclo-Oxigenase 1/metabolismo
Ciclo-Oxigenase 2/metabolismo
Diabetes Mellitus Tipo 2/induzido quimicamente
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Farnesil-Difosfato Farnesiltransferase/metabolismo
Seres Humanos
Hipolipemiantes/síntese química
Hipolipemiantes/química
Masculino
Camundongos
Camundongos Pelados
Estrutura Molecular
Morfolinas/síntese química
Morfolinas/química
Morfolinas/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Ratos
Relação Estrutura-Atividade
Tiazinas/síntese química
Tiazinas/química
Tiazinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,4-benzothiazine); 0 (Enzyme Inhibitors); 0 (Hypolipidemic Agents); 0 (Morpholines); 0 (Thiazines); 8B2ZCK305O (morpholine); EC 1.14.99.1 (Cyclooxygenase 1); EC 1.14.99.1 (Cyclooxygenase 2); EC 2.5.1.21 (Farnesyl-Diphosphate Farnesyltransferase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE


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[PMID]:28709952
[Au] Autor:Napolitano L; Scalise M; Koyioni M; Koutentis P; Catto M; Eberini I; Parravicini C; Palazzolo L; Pisani L; Galluccio M; Console L; Carotti A; Indiveri C
[Ad] Endereço:Department DiBEST (Biologia, Ecologia, Scienze della Terra) Unit of Biochemistry and Molecular Biotechnology, University of Calabria, Via P. Bucci 4C, 87036 Arcavacata di Rende, Italy.
[Ti] Título:Potent inhibitors of human LAT1 (SLC7A5) transporter based on dithiazole and dithiazine compounds for development of anticancer drugs.
[So] Source:Biochem Pharmacol;143:39-52, 2017 Nov 01.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The LAT1 transporter is acknowledged as a pharmacological target of tumours since it is strongly overexpressed in many human cancers. The purpose of this work was to find novel compounds exhibiting potent and prolonged inhibition of the transporter. To this aim, compounds based on dithiazole and dithiazine scaffold have been screened in the proteoliposome experimental model. Inhibition was tested on the antiport catalysed by hLAT1 as transport of extraliposomal [ H]histidine in exchange with intraliposomal histidine. Out of 59 compounds tested, 8 compounds, showing an inhibition higher than 90% at 100µM concentration, were subjected to dose-response analysis. Two of them exhibited IC lower than 1µM. Inhibition kinetics, performed on the two best inhibitors, indicated a mixed type of inhibition with respect to the substrate. Furthermore, inhibition of the transporter was still present after removal of the compounds from the reaction mixture, but was reversed on addition of dithioerythritol, a S-S reducing agent, indicating the formation of disulfide(s) between the compounds and the protein. Molecular docking of the two best inhibitors on the hLAT1 homology structural model, highlighted interaction with the substrate binding site and formation of a covalent bond with the residue C407. Indeed, the inhibition was impaired in the hLAT1 mutant C407A confirming the involvement of that Cys residue. Treatment of SiHa cells expressing hLAT1 at relatively high level, with the two most potent inhibitors led to cell death which was not observed after treatment with a compound exhibiting very poor inhibitory effect.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Descoberta de Drogas/métodos
Transportador 1 de Aminoácidos Neutros Grandes/metabolismo
Tiazinas/química
Tiazóis/química
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Células HEK293
Seres Humanos
Transportador 1 de Aminoácidos Neutros Grandes/genética
Simulação de Acoplamento Molecular
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Large Neutral Amino Acid-Transporter 1); 0 (Thiazines); 0 (Thiazoles)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170716
[St] Status:MEDLINE


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[PMID]:28692354
[Au] Autor:Kammoun I; Bkhairia I; Ben Abdallah F; Jaballi I; Ktari N; Boudawara O; Nasri M; Gharsallah N; Hakim A; Ben Amara I
[Ad] Endereço:a Unit of Functional Genomics and Plant Physiology , Higher Institute of Biotechnology of Sfax , Sfax , Tunisia.
[Ti] Título:Potential protective effects of polysaccharide extracted from Ulva lactuca against male reprotoxicity induced by thiacloprid.
[So] Source:Arch Physiol Biochem;123(5):334-343, 2017 Dec.
[Is] ISSN:1744-4160
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Polysaccharides (PSs) from seaweeds have been reported to possess biological activity of potential medicinal values. OBJECTIVE: The current study was conducted to establish the protective effects of PS extracted from Ulva lactuca against oxidative stress induced by Thiacloprid (THC) in the rat reproductive system. MATERIALS AND METHODS: Rats were exposed either to THC, THC + PS (100 mg/kg), or THC + PS (200 mg/kg). RESULTS: Our study showed that THC induced severe disorders in the functional sperm parameters. A decrease in antioxidant activities and their genes expression were observed in the same group, compared to the controls. Our molecular data showing also a severe DNA breakdown in the testis of THC treated group. Moreover, THC treated group showed severe histopathological changes. CONCLUSIONS: Our results revealed that PS extracted from Ulva lactuca alleviated the THC induced reprotoxicity and reduced oxidative stress damages, DNA breakdown and histological injuries in the testis.
[Mh] Termos MeSH primário: Polissacarídeos/isolamento & purificação
Polissacarídeos/farmacologia
Piridinas/toxicidade
Reprodução/efeitos dos fármacos
Tiazinas/toxicidade
Ulva/química
[Mh] Termos MeSH secundário: Animais
Antioxidantes/metabolismo
Compostos de Bifenilo/metabolismo
Fragmentação do DNA/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ingestão de Líquidos/efeitos dos fármacos
Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos
Masculino
Malondialdeído/metabolismo
Neonicotinoides
Estresse Oxidativo/efeitos dos fármacos
Picratos/metabolismo
Ratos
Ratos Wistar
Espermatozoides/efeitos dos fármacos
Espermatozoides/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Biphenyl Compounds); 0 (Neonicotinoids); 0 (Picrates); 0 (Polysaccharides); 0 (Pyridines); 0 (Thiazines); 4Y8F71G49Q (Malondialdehyde); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl); DSV3A944A4 (thiacloprid)
[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:170711
[St] Status:MEDLINE
[do] DOI:10.1080/13813455.2017.1347686


  9 / 3929 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


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[PMID]:28656780
[Au] Autor:Lusthaus JA; Goldberg I
[Ad] Endereço:a Discipline of Ophthalmology , University of Sydney , Sydney , Australia.
[Ti] Título:Brimonidine and brinzolamide for treating glaucoma and ocular hypertension; a safety evaluation.
[So] Source:Expert Opin Drug Saf;16(9):1071-1078, 2017 Sep.
[Is] ISSN:1744-764X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Brimonidine tartrate and brinzolamide eye drops are often used as third and fourth line treatment options to reduce intraocular pressure (IOP) in the management of glaucoma and ocular hypertension. Better tolerated, more effective topical agents requiring once daily instillation including prostaglandin analogues and beta-blockers usually are preferred as initial therapy, unless there are contraindications. Brimonidine and brinzolamide are often required owing to progressive glaucoma or intolerances to or ineffectiveness of front-line agents. Areas covered: We review the safety of formulations containing brimonidine tartrate and/or brinzolamide. Safety considerations for these agents in higher risk populations are highlighted. Expert opinion: Each class of ocular hypotensive eye drop has a unique set of possible side effects. Brimonidine might have neuro-protective capabilities and offer reasonable IOP control, but its use is limited by a relatively high rate of ocular allergy, hyperemia and discomfort. Brinzolamide is generally well tolerated, but often lacks efficacy. The introduction of brimonidine/brinzolamide fixed combination suspension improves adherence (by simplifying the medical regimen) and reduces preservative load on the ocular surface. New drug delivery systems incorporating brimonidine and brinzolamide are in development and promise to improve the safety profiles of both drugs.
[Mh] Termos MeSH primário: Tartarato de Brimonidina/efeitos adversos
Glaucoma
Sulfonamidas/efeitos adversos
Tiazinas/efeitos adversos
[Mh] Termos MeSH secundário: Administração Oftálmica
Animais
Anti-Hipertensivos/administração & dosagem
Anti-Hipertensivos/efeitos adversos
Tartarato de Brimonidina/administração & dosagem
Inibidores da Anidrase Carbônica/administração & dosagem
Inibidores da Anidrase Carbônica/efeitos adversos
Sistemas de Liberação de Medicamentos
Glaucoma/tratamento farmacológico
Seres Humanos
Hipertensão Ocular/tratamento farmacológico
Sulfonamidas/administração & dosagem
Tiazinas/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Carbonic Anhydrase Inhibitors); 0 (Sulfonamides); 0 (Thiazines); 4S9CL2DY2H (Brimonidine Tartrate); 9451Z89515 (brinzolamide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170904
[Lr] Data última revisão:
170904
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170629
[St] Status:MEDLINE
[do] DOI:10.1080/14740338.2017.1346083



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