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Pesquisa : D03.383.725.150 [Categoria DeCS]
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[PMID]:29289881
[Au] Autor:Sathish M; Kavitha B; Nayak VL; Tangella Y; Ajitha A; Nekkanti S; Alarifi A; Shankaraiah N; Nagesh N; Kamal A
[Ad] Endereço:Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
[Ti] Título:Synthesis of podophyllotoxin linked ß-carboline congeners as potential anticancer agents and DNA topoisomerase II inhibitors.
[So] Source:Eur J Med Chem;144:557-571, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of new podophyllotoxin linked ß-carboline congeners have been synthesized by coupling various substituted ß-carboline acids with 4ß-aminopodophyllotoxin. Evaluation of their anticancer activity against a panel of human cancer cell lines such as lung cancer (A549), prostate cancer (DU-145), MDA MB-231 (breast cancer), HT-29 (colon cancer) and HeLa (cervical cancer) suggested that 7i and 7j are the most cytotoxic compounds with IC values of 1.07 ±â€¯0.07 µM and 1.14 ±â€¯0.16 respectively against DU-145 cell line. Further, detailed biological studies such as cell cycle analysis, topoisomerase II inhibition, Comet assay, DNA binding studies and docking studies have revealed that these congeners are DNA interacting topoisomerase II inhibitors.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carbolinas/farmacologia
DNA Topoisomerases Tipo II/metabolismo
Podofilotoxina/farmacologia
Inibidores da Topoisomerase II/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Carbolinas/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Podofilotoxina/química
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/síntese química
Inibidores da Topoisomerase II/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbolines); 0 (Topoisomerase II Inhibitors); 94HMA1I78O (norharman); EC 5.99.1.3 (DNA Topoisomerases, Type II); L36H50F353 (Podophyllotoxin)
[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:180101
[St] Status:MEDLINE


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[PMID]:29268246
[Au] Autor:Herraiz T; Flores A; Fernández L
[Ad] Endereço:Instituto de Ciencia y Tecnología de Alimentos y Nutrición (ICTAN), Spanish National Research Council (CSIC), Juan de la Cierva 3, 28006, Madrid, Spain. Electronic address: tomas.herraiz@csic.es.
[Ti] Título:Analysis of monoamine oxidase (MAO) enzymatic activity by high-performance liquid chromatography-diode array detection combined with an assay of oxidation with a peroxidase and its application to MAO inhibitors from foods and plants.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1073:136-144, 2018 Jan 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Monoamine oxidase (MAO) enzymes catalyze the oxidative deamination of biogenic amines and neurotransmitters and produce ammonia, aldehydes, and hydrogen peroxide which is involved in oxidative processes. Inhibitors of MAO-A and -B isozymes are useful as antidepressants and neuroprotectants. The assays of MAO usually measure amine oxidation products or hydrogen peroxide by spectrophotometric techniques. Those assays are often compromised by interfering compounds resulting in poor results. This research describes a new method that combines in the same assay the oxidative deamination of kynuramine to 4-hydroxyquinoline analyzed by HPLC-DAD with the oxidation of tetramethylbenzidine (TMB) (or Amplex Rex) by horseradish peroxidase (HRP) in presence of hydrogen peroxide. The new method was applied to study the inhibition of human MAO-A and -B by bioactive compounds including ß-carboline alkaloids and flavonoids occurring in foods and plants. As determined by HPLC-DAD, ß-carbolines, methylene blue, kaempferol and clorgyline inhibited MAO-A and methylene blue, 5-nitroindazole, norharman and deprenyl inhibited MAO-B, and all of them inhibited the oxidation of TMB in the same extent. The flavonoids catechin and cyanidin were not inhibitors of MAO by HPLC-DAD but highly inhibited the oxidation of TMB (or Amplex Red) by peroxidase whereas quercetin and resveratrol were moderate inhibitors of MAO-A by HPLC-DAD, but inhibited the peroxidase assay in a higher level. For some phenolic compounds, using the peroxidase-coupled assay to measure MAO activity led to mistaken results. The new method permits to discern between true inhibitors of MAO from those that are antioxidants and which interfere with peroxidase assays but do not inhibit MAO. For true inhibitors of MAO, inhibition as determined by HPLC-DAD correlated well with inhibition of the oxidation of TMB and this approach can be used to assess the in vitro antioxidant activity (less hydrogen peroxide production) resulting from MAO inhibition.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Inibidores da Monoaminoxidase/metabolismo
Monoaminoxidase/análise
Monoaminoxidase/metabolismo
Peroxidase/metabolismo
[Mh] Termos MeSH secundário: Antioxidantes/metabolismo
Carbolinas
Flavonoides
Seres Humanos
Cinuramina/análise
Cinuramina/metabolismo
Oxirredução
Extratos Vegetais/análise
Extratos Vegetais/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Carbolines); 0 (Flavonoids); 0 (Monoamine Oxidase Inhibitors); 0 (Plant Extracts); 363-36-0 (Kynuramine); EC 1.11.1.7 (Peroxidase); EC 1.4.3.4 (Monoamine Oxidase)
[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:171222
[St] Status:MEDLINE


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[PMID]:29288941
[Au] Autor:Ling Y; Guo J; Yang Q; Zhu P; Miao J; Gao W; Peng Y; Yang J; Xu K; Xiong B; Liu G; Tao J; Luo L; Zhu Q; Zhang Y
[Ad] Endereço:School of Pharmacy and Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong 226001, PR China; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, PR China.
[Ti] Título:Development of novel ß-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
[So] Source:Eur J Med Chem;144:398-409, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of novel ß-carboline-based hydroxamate derivatives 12a-k were designed and synthesized, and their biological activities in a series of in vitro assays were evaluated. Several of these ß-carboline derivatives not only showed excellent HDAC1/3/6 inhibitory effects, but also displayed significant antitumor activities against five human cancer cells. The most potent compound 12f demonstrated the highest anticancer potency against cancer cell lines with IC values of 0.53-1.56 µM, which was considerably more potent than harmine (IC = 46.7-55.3 µM) and also three-to ten-fold lower than that of SAHA (IC = 4.48-6.26 µM). Immunoblot analysis revealed that 12f dose-dependently inhibited histone H3 and α-tubulin acetylation, confirming its HDAC inhibitory effects. Moreover, 12f significantly arrested HepG2 cells at G2/M phase through inhibiting cell cycle related protein CDK1 and cyclin B in a concentration dependent manner. Interestingly, 12f also exerted strong anti-metastasis activity by simultaneously reducing the protein level of MMP2 and MMP9 and inhibiting MAPK signaling pathway.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carbolinas/farmacologia
Inibidores de Histona Desacetilases/farmacologia
Histona Desacetilases/metabolismo
Ácidos Hidroxâmicos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Carbolinas/química
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Inibidores de Histona Desacetilases/síntese química
Inibidores de Histona Desacetilases/química
Seres Humanos
Ácidos Hidroxâmicos/síntese química
Ácidos Hidroxâmicos/química
Estrutura Molecular
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbolines); 0 (Histone Deacetylase Inhibitors); 0 (Hydroxamic Acids); 94HMA1I78O (norharman); EC 3.5.1.98 (Histone Deacetylases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


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[PMID]:29173760
[Au] Autor:Foy V; Schenk MW; Baker K; Gomes F; Lallo A; Frese KK; Forster M; Dive C; Blackhall F
[Ad] Endereço:Clinical and Experimental Pharmacology Group, Cancer Research UK Manchester Institute, University of Manchester, UK.
[Ti] Título:Targeting DNA damage in SCLC.
[So] Source:Lung Cancer;114:12-22, 2017 Dec.
[Is] ISSN:1872-8332
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:SCLC accounts for 15% of lung cancer worldwide. Characterised by early dissemination and rapid development of chemo-resistant disease, less than 5% of patients survive 5 years. Despite 3 decades of clinical trials there has been no change to the standard platinum and etoposide regimen for first line treatment developed in the 1970's. The exceptionally high number of genomic aberrations observed in SCLC combined with the characteristic rapid cellular proliferation results in accumulation of DNA damage and genomic instability. To flourish in this precarious genomic context, SCLC cells are reliant on functional DNA damage repair pathways and cell cycle checkpoints. Current cytotoxic drugs and radiotherapy treatments for SCLC have long been known to act by induction of DNA damage and the response of cancer cells to such damage determines treatment efficacy. Recent years have witnessed improved understanding of strategies to exploit DNA damage and repair mechanisms in order to increase treatment efficacy. This review will summarise the rationale to target DNA damage response in SCLC, the progress made in evaluating novel DDR inhibitors and highlight various ongoing challenges for their clinical development in this disease.
[Mh] Termos MeSH primário: Dano ao DNA/genética
Neoplasias Pulmonares/tratamento farmacológico
Rad51 Recombinase/antagonistas & inibidores
Carcinoma de Pequenas Células do Pulmão/tratamento farmacológico
[Mh] Termos MeSH secundário: Aurora Quinases/uso terapêutico
Azepinas/uso terapêutico
Benzimidazóis/uso terapêutico
Carbolinas/uso terapêutico
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Pontos de Checagem do Ciclo Celular/genética
Proliferação Celular/efeitos dos fármacos
Proliferação Celular/genética
Citotoxinas/uso terapêutico
Dano ao DNA/efeitos dos fármacos
Reparo do DNA
Etoposídeo/uso terapêutico
Instabilidade Genômica/efeitos dos fármacos
Instabilidade Genômica/genética
Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico
Seres Humanos
Neoplasias Pulmonares/genética
Terapia de Alvo Molecular/métodos
Ftalazinas/uso terapêutico
Piperazinas/uso terapêutico
Inibidores de Poli(ADP-Ribose) Polimerases/uso terapêutico
Inibidores de Proteínas Quinases/uso terapêutico
Pirimidinas/uso terapêutico
Rad51 Recombinase/uso terapêutico
Carcinoma de Pequenas Células do Pulmão/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Azepines); 0 (Benzimidazoles); 0 (Carbolines); 0 (Cytotoxins); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (MLN 8237); 0 (PM 01183); 0 (Phthalazines); 0 (Piperazines); 0 (Poly(ADP-ribose) Polymerase Inhibitors); 0 (Protein Kinase Inhibitors); 0 (Pyrimidines); 01O4K0631N (veliparib); 6PLQ3CP4P3 (Etoposide); 9QHX048FRV (talazoparib); EC 2.7.11.1 (Aurora Kinases); EC 2.7.7.- (Rad51 Recombinase); WOH1JD9AR8 (olaparib)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180131
[Lr] Data última revisão:
180131
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:29050382
[Au] Autor:Schöll M; Ossenkoppele R; Strandberg O; Palmqvist S; Jögi J; Ohlsson T; Smith R; Hansson O; Swedish BioFINDER study
[Ad] Endereço:Clinical Memory Research Unit, Department of Clinical Sciences, Lund University, Malmö, Sweden.
[Ti] Título:Distinct 18F-AV-1451 tau PET retention patterns in early- and late-onset Alzheimer's disease.
[So] Source:Brain;140(9):2286-2294, 2017 Sep 01.
[Is] ISSN:1460-2156
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Patients with Alzheimer's disease can present with different clinical phenotypes. Individuals with late-onset Alzheimer's disease (>65 years) typically present with medial temporal lobe neurodegeneration and predominantly amnestic symptomatology, while patients with early-onset Alzheimer's disease (<65 years) exhibit greater neocortical involvement associated with a clinical presentation including dyspraxia, executive dysfunction, or visuospatial impairment. We recruited 20 patients with early-onset Alzheimer's disease, 21 with late-onset Alzheimer's disease, three with prodromal early-onset Alzheimer's disease and 13 with prodromal late-onset Alzheimer's disease, as well as 30 cognitively healthy elderly controls, that had undergone 18F-AV-1451 tau positron emission tomography and structural magnetic resonance imaging to explore whether early- and late-onset Alzheimer's disease exhibit differential regional tau pathology and atrophy patterns. Strong associations of lower age at symptom onset with higher 18F-AV-1451 uptake were observed in several neocortical regions, while higher age did not yield positive associations in neither patient group. Comparing patients with early-onset Alzheimer's disease with controls resulted in significantly higher 18F-AV-1451 retention throughout the neocortex, while comparing healthy controls with late-onset Alzheimer's disease patients yielded a distinct pattern of higher 18F-AV-1451 retention, predominantly confined to temporal lobe regions. When compared against each other, the early-onset Alzheimer's disease group exhibited greater uptake than the late-onset group in prefrontal and premotor, as well as in inferior parietal cortex. These preliminary findings indicate that age may constitute an important contributor to Alzheimer's disease heterogeneity highlighting the potential of tau positron emission tomography to capture phenotypic variation across patients with Alzheimer's disease.
[Mh] Termos MeSH primário: Doença de Alzheimer/metabolismo
Carbolinas/metabolismo
Sintomas Prodrômicos
Tauopatias/diagnóstico por imagem
Proteínas tau/metabolismo
[Mh] Termos MeSH secundário: Idade de Início
Idoso
Envelhecimento/metabolismo
Envelhecimento/patologia
Doença de Alzheimer/diagnóstico
Doença de Alzheimer/patologia
Atrofia/patologia
Estudos de Casos e Controles
Córtex Cerebral/metabolismo
Córtex Cerebral/patologia
Feminino
Seres Humanos
Imagem por Ressonância Magnética
Masculino
Meia-Idade
Neuroimagem
Tomografia por Emissão de Pósitrons
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole); 0 (Carbolines); 0 (tau Proteins)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171021
[St] Status:MEDLINE
[do] DOI:10.1093/brain/awx171


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[PMID]:28980714
[Au] Autor:Schonhaut DR; McMillan CT; Spina S; Dickerson BC; Siderowf A; Devous MD; Tsai R; Winer J; Russell DS; Litvan I; Roberson ED; Seeley WW; Grinberg LT; Kramer JH; Miller BL; Pressman P; Nasrallah I; Baker SL; Gomperts SN; Johnson KA; Grossman M; Jagust WJ; Boxer AL; Rabinovici GD
[Ad] Endereço:Memory and Aging Center, University of California, San Francisco, San Francisco, CA.
[Ti] Título: F-flortaucipir tau positron emission tomography distinguishes established progressive supranuclear palsy from controls and Parkinson disease: A multicenter study.
[So] Source:Ann Neurol;82(4):622-634, 2017 Oct.
[Is] ISSN:1531-8249
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: F-flortaucipir (formerly F-AV1451 or F-T807) binds to neurofibrillary tangles in Alzheimer disease, but tissue studies assessing binding to tau aggregates in progressive supranuclear palsy (PSP) have yielded mixed results. We compared in vivo F-flortaucipir uptake in patients meeting clinical research criteria for PSP (n = 33) to normal controls (n = 46) and patients meeting criteria for Parkinson disease (PD; n = 26). METHODS: Participants underwent magnetic resonance imaging and positron emission tomography for amyloid-ß ( C-PiB or F-florbetapir) and tau ( F-flortaucipir). F-flortaucipir standardized uptake value ratios were calculated (t = 80-100 minutes, cerebellum gray matter reference). Voxelwise and region-of-interest group comparisons were performed in template space, with receiver operating characteristic curve analyses to assess single-subject discrimination. Qualitative comparisons with postmortem tau are reported in 1 patient who died 9 months after F-flortaucipir. RESULTS: Clinical PSP patients showed bilaterally elevated F-flortaucipir uptake in globus pallidus, putamen, subthalamic nucleus, midbrain, and dentate nucleus relative to controls and PD patients (voxelwise p < 0.05 family wise error corrected). Globus pallidus binding best distinguished PSP patients from controls and PD (area under the curve [AUC] = 0.872 vs controls, AUC = 0.893 vs PD). PSP clinical severity did not correlate with F-flortaucipir in any region. A patient with clinical PSP and pathological diagnosis of corticobasal degeneration had severe tau pathology in PSP-related brain structures with good correspondence between in vivo F-flortaucipir and postmortem tau neuropathology. INTERPRETATION: F-flortaucipir uptake was elevated in PSP versus controls and PD patients in a pattern consistent with the expected distribution of tau pathology. Ann Neurol 2017;82:622-634.
[Mh] Termos MeSH primário: Encéfalo/diagnóstico por imagem
Carbolinas/farmacocinética
Doença de Parkinson/diagnóstico por imagem
Tomografia por Emissão de Pósitrons
Paralisia Supranuclear Progressiva/diagnóstico por imagem
Proteínas tau/metabolismo
[Mh] Termos MeSH secundário: Idoso
Compostos de Anilina/farmacocinética
Mapeamento Encefálico
Estudos de Casos e Controles
Transtornos Cognitivos/diagnóstico
Transtornos Cognitivos/etiologia
Diagnóstico
Feminino
Seres Humanos
Imagem por Ressonância Magnética
Masculino
Meia-Idade
Testes Neuropsicológicos
Doença de Parkinson/complicações
Índice de Gravidade de Doença
Paralisia Supranuclear Progressiva/complicações
Tiazóis/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY
[Nm] Nome de substância:
0 (2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole); 0 (7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole); 0 (Aniline Compounds); 0 (Carbolines); 0 (Thiazoles); 0 (tau Proteins)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171006
[St] Status:MEDLINE
[do] DOI:10.1002/ana.25060


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[PMID]:28962866
[Au] Autor:Miao X; You J; Wang J; Chen Y
[Ad] Endereço:Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan, Hubei 430062, China.
[Ti] Título:In vitro metabolism of 4, 5-dimethoxycanthin-6-one by human liver microsomes and its inhibition on human CYP1A2.
[So] Source:Life Sci;190:46-51, 2017 Dec 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: P. quassioides is a traditional Chinese medicine used for the treatment of gastroenteritis, snakebite, infection and hypertension in China. 4, 5-dimethoxycanthin-6-one is one of the main active canthinone alkaloid isolated from P. quassioides. The aim of this work was to identify the cytochrome P (CYP) 450 enzymes responsible for the metabolism of 4, 5-dimethoxycanthin-6-one (DCO) and to evaluate the inhibitory effect of DCO on CYP activity in human liver microsomes (HLM) in vitro. MATERIALS AND METHODS: the CYP isoforms responsible for DCO metabolism and the inhibitory effects of DCO on CYP activity was studied in HLM. KEY FINDINGS: The in vitro metabolic enzyme of DCO was CYP3A4 (mediated the formation of metabolites M1-M5), CYP2C9 (mediated the formation of metabolites M1-M3, M6 and M8) and CYP2D6 (mediated the formation of metabolite M3) in HLM. Furthermore, the present work found that DCO uncompetitively inhibited CYP1A2-mediated phenacetin O-deethylation with an IC value of 1.7µM and a Ki value of 2.6µM. SIGNIFICANCE: The results suggested that the metabolic interaction should be existed when the substrate drugs of CYP1A2 were co-administered with DCO or traditional Chinese medicine containing it, such as the extract of P. quassioides and Kumu injection.
[Mh] Termos MeSH primário: Carbolinas/administração & dosagem
Inibidores do Citocromo P-450 CYP1A2/administração & dosagem
Citocromo P-450 CYP1A2/efeitos dos fármacos
Microssomos Hepáticos/efeitos dos fármacos
Picrasma/química
[Mh] Termos MeSH secundário: Carbolinas/metabolismo
Carbolinas/farmacologia
Citocromo P-450 CYP1A2/metabolismo
Inibidores do Citocromo P-450 CYP1A2/metabolismo
Inibidores do Citocromo P-450 CYP1A2/farmacologia
Sistema Enzimático do Citocromo P-450/efeitos dos fármacos
Sistema Enzimático do Citocromo P-450/metabolismo
Seres Humanos
Técnicas In Vitro
Concentração Inibidora 50
Microssomos Hepáticos/enzimologia
Microssomos Hepáticos/metabolismo
Extratos Vegetais/administração & dosagem
Extratos Vegetais/metabolismo
Extratos Vegetais/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4,5-dimethoxycanthin-6-one); 0 (Carbolines); 0 (Cytochrome P-450 CYP1A2 Inhibitors); 0 (Plant Extracts); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 1.14.14.1 (CYP1A2 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A2)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171001
[St] Status:MEDLINE


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[PMID]:28923379
[Au] Autor:Chen J; Peng F; Zhang Y; Li B; She J; Jie X; Zou Z; Chen M; Chen L
[Ad] Endereço:Analysis Centre of Guangdong Medical University, Zhanjiang 524023, China; Guangdong Key Laboratory for Research and Development of Nature Drugs, Guangdong Medical University, Zhanjiang 524023, China.
[Ti] Título:Synthesis, characterization, cellular uptake and apoptosis-inducing properties of two highly cytotoxic cyclometalated ruthenium(II) ß-carboline complexes.
[So] Source:Eur J Med Chem;140:104-117, 2017 Nov 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Two new cyclometalated Ru(II) complexes of the general formula [Ru(N-N) (1-Ph-ßC)](PF ), where N-N = 4,4'-dimethyl-2,2'-bipyridine (dmb, Ru1), 2,2'-bipyridine (bpy, Ru2), and 1-Ph-ßC (1-phenyl-9H-pyrido[3,4-b]indole) is a ß-carboline alkaloids derivatives, have been synthesized and characterized. The in vitro cytotoxicities, cellular uptake and localization, cell cycle arrest and apoptosis-inducing mechanisms of these complexes have been extensively explored by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, inductively coupled plasma mass spectrometry (ICP-MS), flow cytometry, comet assay, inverted fluorescence microscope as well as western blotting experimental techniques. Notably, Ru1 and Ru2 exhibit potent antiproliferative activities against selected human cancer cell lines with IC values lower than those of cisplatin and other non-cyclometalated Ru(II) ß-carboline complexes. The cellular uptake and localization exhibit that these complexes can accumulate in the cell nuclei. Further antitumor mechanism studies show that Ru1 and Ru2 can cause cell cycle arrest in the G0/G1 phase by regulating cell cycle relative proteins and induce apoptosis through mitochondrial dysfunction, reactive oxygen species (ROS) accumulation and ROS-mediated DNA damage.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Carbolinas/farmacologia
Compostos Organometálicos/farmacologia
Rutênio/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Carbolinas/química
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Compostos Organometálicos/síntese química
Compostos Organometálicos/química
Rutênio/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbolines); 0 (Organometallic Compounds); 7UI0TKC3U5 (Ruthenium); 94HMA1I78O (norharman)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170920
[St] Status:MEDLINE


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[PMID]:28814462
[Au] Autor:Cho H; Baek MS; Choi JY; Lee SH; Kim JS; Ryu YH; Lee MS; Lyoo CH
[Ad] Endereço:From the Departments of Neurology (H.C., M.S.B., S.H.L., M.S.L., C.H.L.) and Nuclear Medicine (Y.H.R.), Gangnam Severance Hospital, Yonsei University College of Medicine; Division of RI-Convergence Research (J.Y.C.), Korea Institute Radiological and Medical Sciences; and Department of Neurology (J.S
[Ti] Título:F-AV-1451 binds to motor-related subcortical gray and white matter in corticobasal syndrome.
[So] Source:Neurology;89(11):1170-1178, 2017 Sep 12.
[Is] ISSN:1526-632X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To investigate tau distribution in patients with corticobasal syndrome (CBS) using F-AV-1451 PET. METHODS: Six consecutively recruited patients with CBS and 20 age-matched healthy controls underwent 2 PET scans with F-AV-1451 (for tau) and F-florbetaben (for ß-amyloid). We compared standardized uptake value ratio maps of the F-AV-1451 PET images between the patients with CBS and controls. RESULTS: Compared to controls, patients with CBS exhibited asymmetrically increased F-AV-1451 binding in the putamen, globus pallidus, and thalamus contralateral to the clinically more affected side and in the ipsilateral globus pallidus and dentate nucleus. Voxel-based comparison additionally showed asymmetrically increased F-AV-1451 binding in the focal regions of the precentral gray and white matter and in the midbrain, predominantly in the contralateral side. F-AV-1451 binding in the precentral white matter correlated with motor severity. CONCLUSIONS: F-AV-1451 asymmetrically binds to motor-related subcortical gray and white matter structures in patients with CBS. This pattern corresponds to tau pathology distribution in postmortem studies, and motor deficit in patients with CBS may be associated with tau accumulation predominantly in the subcortical white matter underlying the motor cortex, leading to disruptions in motor-related networks.
[Mh] Termos MeSH primário: Encéfalo/diagnóstico por imagem
Carbolinas
Transtornos Parkinsonianos/diagnóstico por imagem
Tomografia por Emissão de Pósitrons
Compostos Radiofarmacêuticos
Proteínas tau/metabolismo
[Mh] Termos MeSH secundário: Idoso
Amiloide/metabolismo
Compostos de Anilina
Encéfalo/metabolismo
Mapeamento Encefálico
Feminino
Substância Cinzenta/diagnóstico por imagem
Seres Humanos
Masculino
Meia-Idade
Atividade Motora/fisiologia
Transtornos Parkinsonianos/metabolismo
Índice de Gravidade de Doença
Estilbenos
Substância Branca/diagnóstico por imagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-(N-methylamino)-4'-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)stilbene); 0 (7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole); 0 (Amyloid); 0 (Aniline Compounds); 0 (Carbolines); 0 (MAPT protein, human); 0 (Radiopharmaceuticals); 0 (Stilbenes); 0 (tau Proteins)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170818
[St] Status:MEDLINE
[do] DOI:10.1212/WNL.0000000000004364


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[PMID]:28782526
[Au] Autor:Erba E; Romano M; Gobbi M; Zucchetti M; Ferrari M; Matteo C; Panini N; Colmegna B; Caratti G; Porcu L; Fruscio R; Perlangeli MV; Mezzanzanica D; Lorusso D; Raspagliesi F; D'Incalci M
[Ad] Endereço:Department of Oncology, IRCCS - Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, Milan, Italy.
[Ti] Título:Ascites interferes with the activity of lurbinectedin and trabectedin: Potential role of their binding to alpha 1-acid glycoprotein.
[So] Source:Biochem Pharmacol;144:52-62, 2017 Nov 15.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Trabectedin and its analogue lurbinectedin are effective drugs used in the treatment of ovarian cancer. Since the presence of ascites is a frequent event in advanced ovarian cancer we asked the question whether ascites could modify the activity of these compounds against ovarian cancer cells. The cytotoxicity induced by trabectedin or lurbinectedin against A2780, OVCAR-5 cell lines or primary culture of human ovarian cancer cells was compared by performing treatment in regular medium or in ascites taken from either nude mice or ovarian cancer patients. Ascites completely abolished the activity of lurbinectedin at up to 10nM (in regular medium corresponds to the IC90), strongly reduced that of trabectedin, inhibited the cellular uptake of lurbinectedin and, to a lesser extent, that of trabectedin. Since α1-acid glycoprotein (AGP) is present in ascites at relatively high concentrations, we tested if the binding of the drugs to this protein could be responsible for the reduction of their activity. Adding AGP to the medium at concentration range of those found in ascites, we reproduced the anticytotoxic effect of ascites. Erythromycin partially restored the activity of the drugs, presumably by displacing them from AGP. Equilibrium dialysis experiments showed that both drugs bind AGP, but the affinity of binding of lurbinectedin was much greater than that of trabectedin. KD values are 8±1.7 and 87±14nM for lurbinectedin and trabectedin, respectively. The studies intimate the possibility that AGP present in ascites might reduce the activity of lurbinectedin and to a lesser extent of trabectedin against ovarian cancer cells present in ascites. AGP plasma levels could influence the distribution of these drugs and thus they should be monitored in patients receiving these compounds.
[Mh] Termos MeSH primário: Ascite/metabolismo
Carbolinas/metabolismo
Dioxóis/metabolismo
Compostos Heterocíclicos de 4 ou mais Anéis/metabolismo
Orosomucoide/metabolismo
Neoplasias Ovarianas/metabolismo
Tetra-Hidroisoquinolinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Alquilantes/metabolismo
Antineoplásicos Alquilantes/farmacologia
Antineoplásicos Alquilantes/uso terapêutico
Carbolinas/farmacologia
Carbolinas/uso terapêutico
Linhagem Celular Tumoral
Dioxóis/farmacologia
Dioxóis/uso terapêutico
Relação Dose-Resposta a Droga
Feminino
Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia
Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico
Seres Humanos
Camundongos
Camundongos Nus
Neoplasias Ovarianas/tratamento farmacológico
Neoplasias Ovarianas/cirurgia
Ligação Proteica/fisiologia
Tetra-Hidroisoquinolinas/farmacologia
Tetra-Hidroisoquinolinas/uso terapêutico
Células Tumorais Cultivadas
Ensaios Antitumorais Modelo de Xenoenxerto/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Alkylating); 0 (Carbolines); 0 (Dioxoles); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (Orosomucoid); 0 (PM 01183); 0 (Tetrahydroisoquinolines); ID0YZQ2TCP (trabectedin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170808
[St] Status:MEDLINE



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