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[PMID]:29353726
[Au] Autor:Czarnecka K; Chufarova N; Halczuk K; Maciejewska K; Girek M; Skibinski R; Jonczyk J; Bajda M; Kabzinski J; Majsterek I; Szymanski P
[Ad] Endereço:Department of Pharmaceutical Chemistry, Drug Analyses and Radiopharmacy, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland. Electronic address: kamila.czarnecka@umed.lodz.pl.
[Ti] Título:Tetrahydroacridine derivatives with dichloronicotinic acid moiety as attractive, multipotent agents for Alzheimer's disease treatment.
[So] Source:Eur J Med Chem;145:760-769, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A novel series of 9-amino-1,2,3,4-tetrahydroacridine and 5,6-dichloronicotinic acid moiety were conjugated with different linkers. Afterwards new derivatives were evaluated as potential multifunctional acetylcholinesterase inhibitors (AChEIs), anti-Alzheimer's disease (AD) drug candidates. All the compounds were synthesized and tested for capacity for the inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. Specifically, the most promising derivative 3b (IC = 1.02 nM) had higher inhibitory potency compared to the reference drug, tacrine. Consequently, kinetic studies of 3b compound showed a mixed-type inhibition of both AChE and BuChE. Afterwards the best potent AChE inhibitor has been examined on amyloid ß (Aß) self-induced aggregation. Furthermore, 3b compound was tested in various concentrations and had moderate activity against Aß aggregation. Inhibition of Aß aggregation was 46.63% and 19.41% at 50 µM and 5  µM concentrations, respectively. Moreover, no cytotoxicity was observed for the mentioned concentrations. Therefore, 3b compound is a promising multipotent agent for the treatment of AD.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Acridinas/farmacologia
Doença de Alzheimer/tratamento farmacológico
Butirilcolinesterase/metabolismo
Inibidores da Colinesterase/farmacologia
Ácidos Nicotínicos/farmacologia
[Mh] Termos MeSH secundário: Acridinas/química
Doença de Alzheimer/metabolismo
Peptídeos beta-Amiloides/antagonistas & inibidores
Peptídeos beta-Amiloides/metabolismo
Animais
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Electrophorus
Cavalos
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Ácidos Nicotínicos/química
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5,6-dichloronicotinic acid); 0 (Acridines); 0 (Amyloid beta-Peptides); 0 (Cholinesterase Inhibitors); 0 (Nicotinic Acids); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180123
[St] Status:MEDLINE


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[PMID]:29318581
[Au] Autor:Vietto V; Franco JV; Saenz V; Cytryn D; Chas J; Ciapponi A
[Ad] Endereço:Family and Community Medicine Service, Hospital Italiano de Buenos Aires, Buenos Aires, Argentina.
[Ti] Título:Prostanoids for critical limb ischaemia.
[So] Source:Cochrane Database Syst Rev;1:CD006544, 2018 01 10.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Peripheral arterial occlusive disease (PAOD) is a common cause of morbidity and mortality due to cardiovascular disease in the general population. Although numerous treatments have been adopted for patients at different disease stages, no option other than amputation is available for patients presenting with critical limb ischaemia (CLI) unsuitable for rescue or reconstructive intervention. In this regard, prostanoids have been proposed as a therapeutic alternative, with the aim of increasing blood supply to the limb with occluded arteries through their vasodilatory, antithrombotic, and anti-inflammatory effects. This is an update of a review first published in 2010. OBJECTIVES: To determine the effectiveness and safety of prostanoids in patients with CLI unsuitable for rescue or reconstructive intervention. SEARCH METHODS: For this update, the Cochrane Vascular Information Specialist searched the Specialised Register (January 2017) and the Cochrane Central Register of Controlled Trials (CENTRAL; 2017, Issue 1). In addition, we searched trials registries (January 2017) and contacted pharmaceutical manufacturers, in our efforts to identify unpublished data and ongoing trials. SELECTION CRITERIA: Randomised controlled trials describing the efficacy and safety of prostanoids compared with placebo or other pharmacological control treatments for patients presenting with CLI without chance of rescue or reconstructive intervention. DATA COLLECTION AND ANALYSIS: Two review authors independently selected trials, assessed trials for eligibility and methodological quality, and extracted data. We resolved disagreements by consensus or by consultation with a third review author. MAIN RESULTS: For this update, 15 additional studies fulfilled selection criteria. We included in this review 33 randomised controlled trials with 4477 participants; 21 compared different prostanoids versus placebo, seven compared prostanoids versus other agents, and five conducted head-to-head comparisons using two different prostanoids.We found low-quality evidence that suggests no clear difference in the incidence of cardiovascular mortality between patients receiving prostanoids and those given placebo (risk ratio (RR) 0.81, 95% confidence interval (CI) 0.41 to 1.58). We found high-quality evidence showing that prostanoids have no effect on the incidence of total amputations when compared with placebo (RR 0.97, 95% CI 0.86 to 1.09). Adverse events were more frequent with prostanoids than with placebo (RR 2.11, 95% CI 1.79 to 2.50; moderate-quality evidence). The most commonly reported adverse events were headache, nausea, vomiting, diarrhoea, flushing, and hypotension. We found moderate-quality evidence showing that prostanoids reduced rest-pain (RR 1.30, 95% CI 1.06 to 1.59) and promoted ulcer healing (RR 1.24, 95% CI 1.04 to 1.48) when compared with placebo, although these small beneficial effects were diluted when we performed a sensitivity analysis that excluded studies at high risk of bias. Additionally, we found evidence of low to very low quality suggesting the effects of prostanoids versus other active agents or versus other prostanoids because studies conducting these comparisons were few and we judged them to be at high risk of bias. None of the included studies assessed quality of life. AUTHORS' CONCLUSIONS: We found high-quality evidence showing that prostanoids have no effect on the incidence of total amputations when compared against placebo. Moderate-quality evidence showed small beneficial effects of prostanoids for rest-pain relief and ulcer healing when compared with placebo. Additionally, moderate-quality evidence showed a greater incidence of adverse effects with the use of prostanoids, and low-quality evidence suggests that prostanoids have no effect on cardiovascular mortality when compared with placebo. None of the included studies reported quality of life measurements. The balance between benefits and harms associated with use of prostanoids in patients with critical limb ischaemia with no chance of reconstructive intervention is uncertain; therefore careful assessment of therapeutic alternatives should be considered. Main reasons for downgrading the quality of evidence were high risk of attrition bias and imprecision of effect estimates.
[Mh] Termos MeSH primário: Isquemia/tratamento farmacológico
Perna (Membro)/irrigação sanguínea
Doenças Vasculares Periféricas/tratamento farmacológico
Prostaglandinas/uso terapêutico
[Mh] Termos MeSH secundário: Alprostadil/uso terapêutico
Amputação/estatística & dados numéricos
Epoprostenol/uso terapêutico
Seres Humanos
Iloprosta/uso terapêutico
Isquemia/mortalidade
Perna (Membro)/cirurgia
Úlcera da Perna/tratamento farmacológico
Nafronil/uso terapêutico
Ácidos Nicotínicos/uso terapêutico
Pentoxifilina/uso terapêutico
Prostaglandinas/efeitos adversos
Ensaios Clínicos Controlados Aleatórios como Assunto
Vasodilatadores/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Nicotinic Acids); 0 (Prostaglandins); 0 (Vasodilator Agents); 42H8PQ0NMJ (Nafronyl); A99MK953KZ (Inositol Niacinate); DCR9Z582X0 (Epoprostenol); F5TD010360 (Alprostadil); JED5K35YGL (Iloprost); SD6QCT3TSU (Pentoxifylline)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD006544.pub3


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[PMID]:27771381
[Au] Autor:Montserrat-de la Paz S; Naranjo MC; Lopez S; Abia R; Muriana FJG; Bermudez B
[Ad] Endereço:Laboratory of Cellular and Molecular Nutrition, Instituto de la Grasa, CSIC, Seville, Spain.
[Ti] Título:Niacin and its metabolites as master regulators of macrophage activation.
[So] Source:J Nutr Biochem;39:40-47, 2017 Jan.
[Is] ISSN:1873-4847
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Niacin is a broad-spectrum lipid-regulating drug used for clinical therapy of chronic high-grade inflammatory diseases. However, the mechanisms by which either niacin or the byproducts of its catabolism ameliorate these inflammatory diseases are not clear yet. Human circulating monocytes and mature macrophages were used to analyze the effects of niacin and its metabolites (NAM, NUA and 2-Pyr) on oxidative stress, plasticity and inflammatory response by using biochemical, flow cytometry, quantitative real-time PCR and Western blot technologies. Niacin, NAM and 2-Pyr significantly decreased ROS, NO and NOS2 expression in LPS-treated human mature macrophages. Niacin and NAM skewed macrophage polarization toward antiinflammatory M2 macrophage whereas a trend toward proinflammatory M1 macrophage was noted following treatment with NUA. Niacin and NAM also reduced the inflammatory competence of LPS-treated human mature macrophages and promoted bias toward antiinflammatory CD14 CD16 nonclassical human primary monocytes. This study reveals for the first time that niacin and its metabolites possess antioxidant, reprogramming and antiinflammatory properties on human primary monocytes and monocyte-derived macrophages. Our findings imply a new understanding of the mechanisms by which niacin and its metabolites favor a continuous and gradual plasticity process in the human monocyte/macrophage system.
[Mh] Termos MeSH primário: Ativação de Macrófagos/efeitos dos fármacos
Niacina/farmacologia
Niacinamida/farmacologia
Ácidos Nicotínicos/farmacologia
Piridonas/farmacologia
[Mh] Termos MeSH secundário: Anti-Inflamatórios/farmacologia
Antioxidantes/farmacologia
Diferenciação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Seres Humanos
Monócitos/efeitos dos fármacos
Óxido Nítrico Sintase Tipo II/genética
Óxido Nítrico Sintase Tipo II/metabolismo
Estresse Oxidativo
Espécies Reativas de Oxigênio/metabolismo
Reação em Cadeia da Polimerase em Tempo Real
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antioxidants); 0 (N-methyl-2-pyridone-5-carboxamide); 0 (Nicotinic Acids); 0 (Pyridones); 0 (Reactive Oxygen Species); 25X51I8RD4 (Niacinamide); 2679MF687A (Niacin); 77V5315PIU (nicotinuric acid); EC 1.14.13.39 (NOS2 protein, human); EC 1.14.13.39 (Nitric Oxide Synthase Type II)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180117
[Lr] Data última revisão:
180117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE


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[PMID]:28649735
[Au] Autor:Lawal IO; Ankrah AO; Mokgoro NP; Vorster M; Maes A; Sathekge MM
[Ad] Endereço:Department of Nuclear Medicine, University of Pretoria and Steve Biko Academic Hospital, Pretoria, South Africa.
[Ti] Título:Diagnostic sensitivity of Tc-99m HYNIC PSMA SPECT/CT in prostate carcinoma: A comparative analysis with Ga-68 PSMA PET/CT.
[So] Source:Prostate;77(11):1205-1212, 2017 Aug.
[Is] ISSN:1097-0045
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Emerging data from published studies are demonstrating the superiority of Ga-68 PSMA PET/CT imaging in prostate cancer. However, the low yield of the Ge-68/Ga-68 from which Gallium-68 is obtained and fewer installed PET/CT systems compared to the SPECT imaging systems may limit its availability. We, therefore, evaluated in a head-to-head comparison, the diagnostic sensitivity of Ga-68 PSMA PET/CT and Tc-99m PSMA SPECT/CT in patients with prostate cancer. METHODS: A total of 14 patients with histologically confirmed prostate cancer were prospectively recruited to undergo Ga-68 PSMA PET/CT and Tc-99m HYNIC PSMA SPECT/CT. The mean age of patients was 67.21 ± 8.15 years and the median PSA level was 45.18 ng/mL (range = 1.51-687 ng/mL). SUVmax of all lesions and the size of lymph nodes with PSMA avidity on Ga-68 PSMA PET/CT were determined. Proportions of these lesions detected on Tc-99m HYNIC PSMA SPECT/CT read independent of PET/CT findings were determined. RESULTS: A total of 46 lesions were seen on Ga-68 PSMA PET/CT localized to the prostate (n = 10), lymph nodes (n = 24), and bones (n = 12). Of these, Tc-99m HYNIC PSMA SPECT/CT detected 36 lesions: Prostate = 10/10 (100%), lymph nodes = 15/24 (62.5%), and bones = 11/12 (91.7%) with an overall sensitivity of 78.3%. Lesions detected on Tc-99m HYNIC PSMA SPECT/CT were bigger in size (P < 0.001) and had higher SUVmax (P < 0.001) as measured on Ga-68 PSMA PET/CT compared to those lesions that were not detected. All lymph nodes greater than 10 mm in size were detected while only 28% of nodes less than 10 mm were detected by Tc-99m HYNIC PSMA SPECT/CT. In a univariate analysis, Lymph node size (P = 0.033) and the SUVmax of all lesions (P = 0.007) were significant predictors of lesion detection on Tc-99m HYNIC PSMA SPECT/CT. CONCLUSION: Tc-99m HYNIC PSMA may be a useful in imaging of prostate cancer although with a lower sensitivity for lesion detection compared to Ga-68 PSMA PET/CT. Its use is recommended when Ga-68 PSMA is not readily available, in planning radio-guided surgery or the patient is being considered for radio-ligand therapy with Lu-177 PSMA. It performs poorly in detecting small-sized lesions hence its use is not recommended in patients with small volume disease.
[Mh] Termos MeSH primário: Radioisótopos de Gálio/normas
Glutamato Carboxipeptidase II/normas
Hidrazinas/normas
Ácidos Nicotínicos/normas
Tomografia Computadorizada com Tomografia por Emissão de Pósitrons/normas
Neoplasias da Próstata/diagnóstico por imagem
Tomografia Computadorizada com Tomografia Computadorizada de Emissão de Fóton Único/normas
Tecnécio/normas
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Antígenos de Superfície/administração & dosagem
Radioisótopos de Gálio/administração & dosagem
Glutamato Carboxipeptidase II/administração & dosagem
Seres Humanos
Hidrazinas/administração & dosagem
Masculino
Meia-Idade
Ácidos Nicotínicos/administração & dosagem
Tomografia Computadorizada com Tomografia por Emissão de Pósitrons/métodos
Estudos Prospectivos
Neoplasias da Próstata/metabolismo
Tomografia Computadorizada com Tomografia Computadorizada de Emissão de Fóton Único/métodos
Tecnécio/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (6-hydrazinopyridine-3-carboxylic acid); 0 (Antigens, Surface); 0 (Gallium Radioisotopes); 0 (Hydrazines); 0 (Nicotinic Acids); 7440-26-8 (Technetium); EC 3.4.17.21 (Glutamate Carboxypeptidase II); EC 3.4.17.21 (glutamate carboxypeptidase II, human)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170627
[St] Status:MEDLINE
[do] DOI:10.1002/pros.23379


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[PMID]:28475923
[Au] Autor:Pérez-Iglesias JM; Ruiz de Arcaute C; Natale GS; Soloneski S; Larramendy ML
[Ad] Endereço:Cátedra de Citología, Facultad de Ciencias Naturales y Museo, Universidad Nacional de La Plata, Calle 64 No 3, B1904AMA La Plata, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Argentina.
[Ti] Título:Evaluation of imazethapyr-induced DNA oxidative damage by alkaline Endo III- and Fpg-modified single-cell gel electrophoresis assay in Hypsiboas pulchellus tadpoles (Anura, Hylidae).
[So] Source:Ecotoxicol Environ Saf;142:503-508, 2017 Aug.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Imazethapyr (IMZT) is a selective postemergent herbicide with residual action. Available data analyzing its effects in aquatic vertebrates are scarce. In previous studies, we demonstrated that IMZT induces lesions into the DNA of Hypsiboas pulchellus tadpoles using the single-cell gel electrophoresis (SCGE) assay as a biomarker for genotoxicity. Currently, this assay can be modified by including incubation with lesion-specific endonucleases, e.g., endonuclease III (Endo III) and formamidopyrimidine-DNA glycosylase (Fpg), which detect oxidized pyrimidine and purine bases, respectively. The aim of this study was to evaluate the role of oxidative stress in the genotoxic damage in circulating blood cells of H. pulchellus tadpoles exposed to the IMZT-based Pivot H formulation (10.59% IMZT) at a concentration equivalent to 25% of the LC (96h) value (0.39mg/L IMZT) during 48 and 96h. Our results demonstrate that the herbicide induces oxidative DNA damage on H. pulchellus tadpoles at purines bases but not at pyrimidines. Our findings represent the first evidence of oxidative damage caused by IMZT on anuran DNA using the alkaline restriction enzyme-modified SCGE assay.
[Mh] Termos MeSH primário: Dano ao DNA
Herbicidas/toxicidade
Mutagênicos/toxicidade
Ácidos Nicotínicos/toxicidade
Estresse Oxidativo/efeitos dos fármacos
Poluentes Químicos da Água/toxicidade
[Mh] Termos MeSH secundário: Animais
Anuros
Ensaio Cometa
DNA-Formamidopirimidina Glicosilase/química
Desoxirribonuclease (Dímero de Pirimidina)/química
Proteínas de Escherichia coli/química
Larva/efeitos dos fármacos
Oxirredução
Estresse Oxidativo/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Escherichia coli Proteins); 0 (Herbicides); 0 (Mutagens); 0 (Nicotinic Acids); 0 (Water Pollutants, Chemical); 72T2IN94I4 (imazethapyr); EC 3.1.25.1 (Deoxyribonuclease (Pyrimidine Dimer)); EC 3.1.25.1 (NTH protein, E coli); EC 3.2.2.23 (DNA-Formamidopyrimidine Glycosylase)
[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:170506
[St] Status:MEDLINE


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[PMID]:28358906
[Au] Autor:Zötterman J; Mirdell R; Horsten S; Farnebo S; Tesselaar E
[Ad] Endereço:Department of Hand Surgery, Plastic Surgery and Burns and Department of Clinical and Experimental Medicine, Linköping University, Linköping, Sweden.
[Ti] Título:Methodological concerns with laser speckle contrast imaging in clinical evaluation of microcirculation.
[So] Source:PLoS One;12(3):e0174703, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Laser Speckle Contrast Imaging (LSCI) is a non-invasive and fast technique for measuring microvascular blood flow that recently has found clinical use for burn assessment and evaluation of flaps. Tissue motion caused by for example breathing or patient movements may however affect the measurements in these clinical applications, as may distance between the camera and the skin and tissue curvature. Therefore, the aims of this study were to investigate the effect of frame rate, number of frames/image, movement of the tissue, measuring distance and tissue curvature on the measured perfusion. METHODS: Methyl nicotinate-induced vasodilation in the forearm skin was measured using LSCI during controlled motion at different speeds, using different combinations of frame rate and number of frames/image, and at varying camera angles and distances. Experiments were made on healthy volunteers and on a cloth soaked in a colloidal suspension of polystyrene microspheres. RESULTS: Measured perfusion increased with tissue motion speed. The relation was independent of the absolute perfusion in the skin and of frame rate and number of frames/image. The measured perfusion decreased with increasing angles (16% at 60°, p = 0.01). Measured perfusion did not vary significantly between measurement distances from 15 to 40 cm (p = 0.77, %CV 0.9%). CONCLUSION: Tissue motion increases and measurement angles beyond 45° decrease the measured perfusion in LSCI. These findings have to be taken into account when LSCI is used to assess moving or curved tissue surfaces, which is common in clinical applications.
[Mh] Termos MeSH primário: Antebraço/diagnóstico por imagem
Fluxometria por Laser-Doppler/métodos
Microcirculação/fisiologia
Imagem de Perfusão/métodos
[Mh] Termos MeSH secundário: Adulto
Velocidade do Fluxo Sanguíneo
Feminino
Antebraço/fisiologia
Seres Humanos
Masculino
Ácidos Nicotínicos/administração & dosagem
Fluxo Sanguíneo Regional
Vasodilatação/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Nicotinic Acids); 7B1AVU9DJN (methyl nicotinate)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170331
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0174703


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[PMID]:28301614
[Au] Autor:Sugarman JL; Gold LS; Lebwohl MG; Pariser DM; Alexander BJ; Pillai R
[Ti] Título:A Phase 2, Multicenter, Double-Blind, Randomized, Vehicle Controlled Clinical Study to Assess the Safety and Efficacy of a Halobetasol/Tazarotene Fixed Combination in the Treatment of Plaque Psoriasis.
[So] Source:J Drugs Dermatol;16(3):197-204, 2017 Mar 01.
[Is] ISSN:1545-9616
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:

BACKGROUND: Psoriasis is a chronic, immune-mediated disease that varies widely in its clinical expression. Treatment options focus on relieving symptoms, reducing inflammation, induration, and scaling, and controlling the extent of the disease. Topical corticosteroids are the mainstay of treatment, however long-term safety remains a concern, particularly with the more potent formulations. Combination therapy with a corticosteroid and tazarotene may improve psoriasis signs at a lower corticosteroid concentration providing a superior safety profile. OBJECTIVE: To investigate the efficacy and safety of a once-daily application of a fixed combination halobetasol propionate 0.01% and tazarotene 0.045% (HP/TAZ) lotion in comparison with its monads and vehicle in subjects with moderate-to-severe plaque psoriasis. METHODS: Multicenter, randomized, double-blind, vehicle-controlled Phase 2 study in moderate or severe psoriasis (N=212). Subjects randomized (2:2:2:1 ratio) to receive HP/TAZ, individual monads, or vehicle, once-daily for 8 weeks. Efficacy assessments included treatment success (defined as at least a 2-grade improvement from baseline in the IGA score and a score of 'Clear' or 'Almost Clear'), and impact on individual signs of psoriasis (erythema, plaque elevation, and scaling) at the target lesion. Safety and treatment emergent adverse events (TEAEs) were evaluated throughout. RESULTS: HP/TAZ lotion demonstrated statistically significant superiority over vehicle as early as 2 weeks. At week 8, 52.5% of subjects had treatment success compared with 33.3%, 18.6%, and 9.7% in the HP (P=0.033), TAZ (P less than 0.001), and vehicle (P less than 0.001) groups, respectively. HP/TAZ lotion was superior to its monads and vehicle in reducing the psoriasis signs of erythema, plaque elevation, and scaling at the target lesion. At week 8, a 2-grade improvement in IGA was achieved by 54.2% of subjects for erythema, 67.8% for plaque elevation, and 64.4% for scaling. Most frequently reported TEAEs were application site reactions, and were more likely associated with the tazarotene component. Side effects such as skin atrophy were rare. CONCLUSIONS: HP/TAZ lotion was consistently more effective than its monads or vehicle in achieving treatment success and reducing psoriasis signs of erythema, plaque elevation, and scaling at the target lesion. Safety data were consistent with the known safety profile of halobetasol propionate and tazarotene, and did not reveal any new safety concerns with the combination product.

J Drugs Dermatol. 2017;16(3):197-204.

.
[Mh] Termos MeSH primário: Clobetasol/análogos & derivados
Fármacos Dermatológicos/uso terapêutico
Glucocorticoides/uso terapêutico
Ácidos Nicotínicos/uso terapêutico
Psoríase/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Cutânea
Clobetasol/administração & dosagem
Clobetasol/efeitos adversos
Clobetasol/uso terapêutico
Fármacos Dermatológicos/administração & dosagem
Fármacos Dermatológicos/efeitos adversos
Método Duplo-Cego
Combinação de Medicamentos
Feminino
Glucocorticoides/administração & dosagem
Glucocorticoides/efeitos adversos
Seres Humanos
Masculino
Ácidos Nicotínicos/administração & dosagem
Ácidos Nicotínicos/efeitos adversos
Veículos Farmacêuticos/administração & dosagem
Índice de Gravidade de Doença
Creme para a Pele
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE II; COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Dermatologic Agents); 0 (Drug Combinations); 0 (Glucocorticoids); 0 (Nicotinic Acids); 0 (Pharmaceutical Vehicles); 81BDR9Y8PS (tazarotene); 9P6159HM7T (halobetasol); ADN79D536H (Clobetasol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170914
[Lr] Data última revisão:
170914
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170317
[St] Status:MEDLINE


  8 / 6031 MEDLINE  
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[PMID]:28272993
[Au] Autor:Kumar V; Singh A; Das TK; Sarkar DJ; Singh SB; Dhaka R; Kumar A
[Ad] Endereço:a Division of Agricultural Chemicals , ICAR-Indian Agricultural Research Institute , New Delhi , India.
[Ti] Título:Release behavior and bioefficacy of imazethapyr formulations based on biopolymeric hydrogels.
[So] Source:J Environ Sci Health B;52(6):402-409, 2017 Jun 03.
[Is] ISSN:1532-4109
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Controlled release formulations of imazethapyr herbicide have been developed employing guar gum-g-cl-polyacrylate/bentonite clay hydrogel composite (GG-HG) and guar gum-g-cl-PNIPAm nano hydrogel (GG-NHG) as carriers, to assess the suitability of biopolymeric hydrogels as controlled herbicide release devices. The kinetics of imazethapyr release from the developed formulations was studied in water and it revealed that the developed formulations of imazethapyr behaved as slow release formulations as compared to commercial formulation. The calculated diffusion exponent (n) values showed that Fickian diffusion was the predominant mechanism of imazethapyr release from the developed formulations. Time for release of half of the loaded imazethapyr (t ) ranged between 0.06 and 4.8 days in case of GG-NHG and 4.4 and 12.6 days for the GG-HG formulations. Weed control index (WCI) of GG-HG and GG-NHG formulations was similar to that of the commercial formulation and the herbicidal effect was observed for relatively longer period. Guar gum-based biopolymeric hydrogels in both macro and nano particle size range can serve as potential carriers in developing slow release herbicide formulations.
[Mh] Termos MeSH primário: Herbicidas/farmacocinética
Hidrogéis/química
Ácidos Nicotínicos/farmacocinética
[Mh] Termos MeSH secundário: Resinas Acrílicas
Silicatos de Alumínio/química
Bentonita/química
Difusão
Galactanos/química
Herbicidas/química
Índia
Cinética
Mananas/química
Nanocompostos/química
Ácidos Nicotínicos/química
Tamanho da Partícula
Gomas Vegetais/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylic Resins); 0 (Aluminum Silicates); 0 (Galactans); 0 (Herbicides); 0 (Hydrogels); 0 (Mannans); 0 (Nicotinic Acids); 0 (Plant Gums); 1302-78-9 (Bentonite); 1302-87-0 (clay); 25189-55-3 (poly-N-isopropylacrylamide); 72T2IN94I4 (imazethapyr); E89I1637KE (guar gum)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE
[do] DOI:10.1080/03601234.2017.1293446


  9 / 6031 MEDLINE  
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[PMID]:28271350
[Au] Autor:Soloneski S; Ruiz de Arcaute C; Nikoloff N; Larramendy ML
[Ad] Endereço:Cátedra de Citología, Facultad de Ciencias Naturales y Museo, Universidad Nacional de La Plata, Calle 64 Nro. 3 (esq. 120), B1904AMA, La Plata, Argentina.
[Ti] Título:Genotoxicity of the herbicide imazethapyr in mammalian cells by oxidative DNA damage evaluation using the Endo III and FPG alkaline comet assays.
[So] Source:Environ Sci Pollut Res Int;24(11):10292-10300, 2017 Apr.
[Is] ISSN:1614-7499
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:We evaluated the role of oxidative stress in the genotoxic damage induced by imazethapyr (IMZT) and its formulation Pivot® in mammalian CHO-K1 cell line. Using the alkaline comet assay, we observed that a concentration of 0.1 µg/mL of IMZT or Pivot® was able to induce DNA damage by increasing the frequency of damaged nucleoids. To test whether the DNA lesions were caused by oxidative stress, the DNA repair enzymes endonuclease III (Endo III) and formamidopyrimidine-DNA glycosylase (Fpg), which convert base damage to strand breaks, were used. Our results demonstrate that after treatment of CHO-K1 cells with the pure active ingredient as well as the commercial formulation Pivot®, an increase in DNA strand breaks was observed after incubation of both Endo III and Fpg enzymes, indicating that both compounds induce DNA damage involving both pyrimidine and purine-based oxidations, at least in CHO-K1 cells. Our findings confirm the genotoxic potential of IMZT and suggest that this herbicide formulation must be employed with great caution, especially not only for exposed occupational workers but also for other living species.
[Mh] Termos MeSH primário: Ensaio Cometa
Dano ao DNA
Herbicidas/toxicidade
Ácidos Nicotínicos/toxicidade
[Mh] Termos MeSH secundário: Animais
Desoxirribonuclease (Dímero de Pirimidina)
Proteínas de Escherichia coli
Estresse Oxidativo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Escherichia coli Proteins); 0 (Herbicides); 0 (Nicotinic Acids); 72T2IN94I4 (imazethapyr); EC 3.1.25.1 (Deoxyribonuclease (Pyrimidine Dimer)); EC 3.1.25.1 (NTH protein, E coli)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE
[do] DOI:10.1007/s11356-017-8666-5


  10 / 6031 MEDLINE  
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[PMID]:28270518
[Au] Autor:Li Y; Zheng X; Yi X; Liu C; Kong D; Zhang J; Gong M
[Ad] Endereço:Tianjin Neurological Institute, Tianjin Medical University General Hospital, Tianjin Medical University, Tianjin, China.
[Ti] Título:Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist.
[So] Source:FASEB J;31(6):2603-2611, 2017 Jun.
[Is] ISSN:1530-6860
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The physiologic properties of glucagon-like peptide 1 (GLP-1) make it a potent candidate drug target in the treatment of type 2 diabetes mellitus (T2DM). GLP-1 is capable of regulating the blood glucose level by insulin secretion after administration of oral glucose. The advantages of GLP-1 for the avoidance of hypoglycemia and the control of body weight are attractive despite its poor stability. The clinical efficacies of long-acting GLP-1 derivatives strongly support discovery pursuits aimed at identifying and developing orally active, small-molecule GLP-1 receptor (GLP-1R) agonists. The purpose of this study was to identify and characterize a novel oral agonist of GLP-1R ( , myricetin). The insulinotropic characterization of myricetin was performed in isolated islets and in Wistar rats. Long-term oral administration of myricetin demonstrated glucoregulatory activity. The data in this study suggest that myricetin might be a potential drug candidate for the treatment of T2DM as a GLP-1R agonist. Further structural modifications on myricetin might improve its pharmacology and pharmacokinetics.-Li, Y., Zheng, X., Yi, X., Liu, C., Kong, D., Zhang, J., Gong, M. Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist.
[Mh] Termos MeSH primário: Diabetes Mellitus Experimental/tratamento farmacológico
Diabetes Mellitus Tipo 2/tratamento farmacológico
Flavonoides/farmacologia
Receptor do Peptídeo Semelhante ao Glucagon 1/agonistas
Insulina/metabolismo
Ilhotas Pancreáticas/efeitos dos fármacos
[Mh] Termos MeSH secundário: Aminoácidos
Animais
Glicemia/metabolismo
Cromo
Seres Humanos
Ilhotas Pancreáticas/metabolismo
Masculino
Camundongos
Camundongos Knockout
Ácidos Nicotínicos
Ratos Wistar
Ratos Zucker
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acids); 0 (Blood Glucose); 0 (Flavonoids); 0 (Glucagon-Like Peptide-1 Receptor); 0 (Insulin); 0 (Nicotinic Acids); 0 (glucose tolerance factor); 0R0008Q3JB (Chromium); 76XC01FTOJ (myricetin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171118
[Lr] Data última revisão:
171118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE
[do] DOI:10.1096/fj.201601339R



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