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[PMID]:29053748
[Au] Autor:Egarnes B; Blanchet MR; Gosselin J
[Ad] Endereço:Laboratory of Innate Immunology, Centre de recherche du CHU de Québec-Université Laval (CHUL) and Department of Molecular Medicine, Université Laval, Quebec, QC, Canada.
[Ti] Título:Treatment with the NR4A1 agonist cytosporone B controls influenza virus infection and improves pulmonary function in infected mice.
[So] Source:PLoS One;12(10):e0186639, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The transcription factor NR4A1 has emerged as a pivotal regulator of the inflammatory response and immune homeostasis. Although contribution of NR4A1 in the innate immune response has been demonstrated, its role in host defense against viral infection remains to be investigated. In the present study, we show that administration of cytosporone B (Csn-B), a specific agonist of NR4A1, to mice infected with influenza virus (IAV) reduces lung viral loads and improves pulmonary function. Our results demonstrate that administration of Csn-B to naive mice leads to a modest production of type 1 IFN. However, in IAV-infected mice, such production of IFNs is markedly increased following treatment with Csn-B. Our study also reveals that alveolar macrophages (AMs) appear to have a significant role in Csn-B effects, since selective depletion of AMs with clodronate liposome correlates with a marked reduction of IFN production, viral clearance and morbidity in IAV-infected mice. Furthermore, when reemergence of AMs is observed following clodronate liposome administration, an increased production of IFNs was detected in bronchoalveolar fluids of IAV-infected mice treated with Csn-B, supporting the contribution of AMs in Csn-B effects. While treatment of mice with Csn-B induces phosphorylation of transcriptional factors IRF3 and IRF7, the latter appears to be less indispensable since effects of Csn-B treatment on the synthesis of IFNs were slightly affected in IAV-infected mice lacking functional IRF7. Together, our results highlight the capacity of Csn-B and consequently of NR4A1 transcription factor in controlling IAV infection.
[Mh] Termos MeSH primário: Influenza Humana/prevenção & controle
Pulmão/fisiopatologia
Membro 1 do Grupo A da Subfamília 4 de Receptores Nucleares/agonistas
Fenilacetatos/farmacologia
[Mh] Termos MeSH secundário: Animais
Feminino
Seres Humanos
Influenza Humana/fisiopatologia
Interferon Tipo I/biossíntese
Camundongos
Camundongos Endogâmicos C57BL
Testes de Função Respiratória
Carga Viral
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Interferon Type I); 0 (Nr4a1 protein, mouse); 0 (Nuclear Receptor Subfamily 4, Group A, Member 1); 0 (Phenylacetates); 0 (cytosporone B)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171021
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0186639


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[PMID]:28835392
[Au] Autor:Xu Q; Langley M; Kanthasamy AG; Reddy MB
[Ad] Endereço:Departments of Food Science and Human Nutrition and.
[Ti] Título:Epigallocatechin Gallate Has a Neurorescue Effect in a Mouse Model of Parkinson Disease.
[So] Source:J Nutr;147(10):1926-1931, 2017 Oct.
[Is] ISSN:1541-6100
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Parkinson disease (PD) is a neurodegenerative disorder that has been associated with many factors, including oxidative stress, inflammation, and iron accumulation. The antioxidant, anti-inflammatory, and iron-chelating properties of epigallocatechin gallate (EGCG), a major polyphenol in green tea, may offer protection against PD. We sought to determine the neurorescue effects of EGCG and the role of iron in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD. We evaluated the neurorescue effect of EGCG (25 mg/kg, 7 d, oral administration) against MPTP-induced (20 mg/kg, 3 d, intraperitoneal injection) neurodegeneration in C57 male black mice. Thirty mice weighing ∼25 g were divided into 3 groups: control, MPTP, and MPTP + EGCG. The neurorescue effect of EGCG was assessed with the use of motor behavior tests, neurotransmitter analysis, oxidative stress indicators, and iron-related protein expression. Compared with the control group, MPTP treatment shortened the mice's latency to fall from the rotarod by 16% ( < 0.05), decreased the striatal dopamine concentration by 58% ( < 0.001) and dihydroxyphenylacetic acid by 35% ( < 0.05), and increased serum protein carbonyls by 71% ( = 0.07). However, EGCG rescued MPTP-induced neurotoxicity by increasing the rotational latency by 17% ( < 0.05) to a value similar to the control group. Striatal dopamine concentrations were 40% higher in the MPTP + EGCG group than in the MPTP group ( < 0.05), but the values were significantly lower than in the control group. Compared with the MPTP and control groups, mice in the MPTP + EGCG group had higher substantia nigra ferroportin expression (44% and 35%, respectively) ( < 0.05) but not hepcidin and divalent metal transporter 1 expression. Overall, our study demonstrated that EGCG regulated the iron-export protein ferroportin in substantia nigra, reduced oxidative stress, and exerted a neurorescue effect against MPTP-induced functional and neurochemical deficits in mice.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Catequina/análogos & derivados
Ferro/metabolismo
Fármacos Neuroprotetores/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Doença de Parkinson
Chá/química
[Mh] Termos MeSH secundário: 1-Metil-4-Fenil-1,2,3,6-Tetra-Hidropiridina
Animais
Antioxidantes/uso terapêutico
Comportamento Animal
Proteínas Sanguíneas/metabolismo
Catequina/farmacologia
Catequina/uso terapêutico
Proteínas de Transporte de Cátions/metabolismo
Modelos Animais de Doenças
Dopamina/metabolismo
Hepcidinas/metabolismo
Masculino
Camundongos Endogâmicos C57BL
Atividade Motora/efeitos dos fármacos
Fármacos Neuroprotetores/uso terapêutico
Doença de Parkinson/tratamento farmacológico
Doença de Parkinson/etiologia
Doença de Parkinson/fisiopatologia
Fenilacetatos/metabolismo
Fitoterapia
Extratos Vegetais/farmacologia
Extratos Vegetais/uso terapêutico
Carbonilação Proteica/efeitos dos fármacos
Substância Negra/efeitos dos fármacos
Substância Negra/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Blood Proteins); 0 (Cation Transport Proteins); 0 (Hepcidins); 0 (Neuroprotective Agents); 0 (Phenylacetates); 0 (Plant Extracts); 0 (Tea); 0 (metal transporting protein 1); 0 (solute carrier family 11- (proton-coupled divalent metal ion transporters), member 2); 8R1V1STN48 (Catechin); 9P21XSP91P (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine); BQM438CTEL (epigallocatechin gallate); E1UOL152H7 (Iron); ER5I1W795A (phenylacetic acid); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171012
[Lr] Data última revisão:
171012
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170825
[St] Status:MEDLINE
[do] DOI:10.3945/jn.117.255034


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[PMID]:28683548
[Au] Autor:Cao YY; Mao DJ; Wang WW; Du XH
[Ad] Endereço:Catalytic Hydrogenation Research Center, Zhejiang University of Technology , Zhejiang Key Laboratory of Green Pesticides and Cleaner Production Technology, Zhejiang Green Pesticide Collaborative Innovation Center, Hangzhou 310014, PR China.
[Ti] Título:Kresoxim-methyl Derivatives: Synthesis and Herbicidal Activities of (Pyridinylphenoxymethylene)phenyl Methoxyiminoacetates.
[So] Source:J Agric Food Chem;65(30):6114-6121, 2017 Aug 02.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A series of new kresoxim-methyl derivatives, (pyridinylphenoxymethylene)phenyl methoxyiminoacetates, were synthesized and their structures were confirmed by NMR and high-resolution mass spectrometry (HRMS). Although derived from a fungicide, the bioassays indicated that several new compounds had good herbicidal activities. At 37.5 g a.i./ha, compound 5c showed 100% inhibition against Abutilon theophrasti, Amaranthus retroflexus, and Eclipta prostrata, which was better than mesotrione. Compound 5e had a broad herbicidal spectrum against broadleaf weeds. The present work indicates that 5c and 5e may serve as new candidates for potential herbicides.
[Mh] Termos MeSH primário: Herbicidas/síntese química
Herbicidas/farmacologia
Fenilacetatos/química
[Mh] Termos MeSH secundário: Herbicidas/química
Metacrilatos/síntese química
Metacrilatos/química
Metacrilatos/farmacologia
Estrutura Molecular
Fenilacetatos/síntese química
Fenilacetatos/farmacologia
Plantas Daninhas/efeitos dos fármacos
Plantas Daninhas/crescimento & desenvolvimento
Estrobilurinas
Relação Estrutura-Atividade
Controle de Plantas Daninhas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Herbicides); 0 (Methacrylates); 0 (Phenylacetates); 0 (Strobilurins); 0LXZ062TTB (kresoxim-methyl)
[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:170708
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.7b02710


  4 / 5725 MEDLINE  
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[PMID]:28659358
[Au] Autor:Sweet RA; Nickerson KM; Cullen JL; Wang Y; Shlomchik MJ
[Ad] Endereço:Department of Immunobiology, Yale University School of Medicine, New Haven, CT 06519.
[Ti] Título:B Cell-Extrinsic and Negatively Regulate Autoreactive and Normal B Cell Immune Responses.
[So] Source:J Immunol;199(3):885-893, 2017 Aug 01.
[Is] ISSN:1550-6606
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:MyD88 and FcR common γ-chain (Fcer1g, FcRγ) elicit proinflammatory responses to exogenous Ags. Deletion of these receptors in autoimmune models has generally led to reduced overall disease. In B cells, is required for anti-DNA and anti-RNA autoantibody responses, whereas is not expressed in these cells. The roles of these receptors in myeloid cells during B cell autoimmune activation remain less clear. To investigate the roles of and in non-B cells, we transferred anti-self-IgG (rheumatoid factor) B cells and their physiologic target Ag, anti-chromatin Ab, into mice lacking , , or both and studied the extrafollicular plasmablast response. Surprisingly, we found a markedly higher and more prolonged response in the absence of either molecule; this effect was accentuated in doubly deficient recipients, with a 40-fold increase compared with wild-type recipients at day 10. This enhancement was dependent on CD40L, indicating that Myd88 and FcRγ, presumably on myeloid APCs, were required to downregulate T cell help for the extrafollicular response. To extend the generality, we then investigated a classic T cell-dependent response to (4-hydroxy-3-nitrophenyl)acetyl conjugated to chicken γ globulin and found a similar effect. Thus, these results reveal novel regulatory roles in the B cell response for receptors that are typically proinflammatory.
[Mh] Termos MeSH primário: Linfócitos B/imunologia
Fator 88 de Diferenciação Mieloide/metabolismo
Receptores Fc/imunologia
[Mh] Termos MeSH secundário: Animais
Anticorpos Antinucleares/imunologia
Autoimunidade
Linfócitos B/efeitos dos fármacos
Ligante de CD40/imunologia
Regulação da Expressão Gênica
Ativação Linfocitária
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Knockout
Fator 88 de Diferenciação Mieloide/deficiência
Fator 88 de Diferenciação Mieloide/genética
Fator 88 de Diferenciação Mieloide/imunologia
Nitrofenóis/farmacologia
Fenilacetatos/farmacologia
Receptores Fc/deficiência
Receptores Fc/genética
Transdução de Sinais
Linfócitos T/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Antinuclear); 0 (Myeloid Differentiation Factor 88); 0 (Nitrophenols); 0 (Phenylacetates); 0 (Receptors, Fc); 10463-20-4 (4-hydroxy-5-nitrophenyl acetic acid); 147205-72-9 (CD40 Ligand)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170630
[St] Status:MEDLINE
[do] DOI:10.4049/jimmunol.1600861


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[PMID]:28526370
[Au] Autor:Lee S; Kwon OS; Lee CS; Won M; Ban HS; Ra CS
[Ad] Endereço:School of Chemistry and Biochemistry, Yeungnam University, 280 Daehak-Ro, Gyeongsan-si, Gyeongbuk 38541, Republic of Korea.
[Ti] Título:Synthesis and biological evaluation of kresoxim-methyl analogues as novel inhibitors of hypoxia-inducible factor (HIF)-1 accumulation in cancer cells.
[So] Source:Bioorg Med Chem Lett;27(13):3026-3029, 2017 07 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We designed and synthesized strobilurin analogues as hypoxia-inducible factor (HIF) inhibitors based on the molecular structure of kresoxim-methyl. Biological evaluation in human colorectal cancer HCT116 cells showed that most of the synthesized kresoxim-methyl analogues possessed moderate to potent inhibitory activity against hypoxia-induced HIF-1 transcriptional activation. Three candidates, compounds 11b, 11c, and 11d were identified as potent inhibitors against HIF-1 activation with IC values of 0.60-0.94µM. Under hypoxic condition, compounds 11b, 11c, and 11d increased the intracellular oxygen contents, thereby attenuating the hypoxia-induced accumulation of HIF-1α protein.
[Mh] Termos MeSH primário: Subunidade alfa do Fator 1 Induzível por Hipóxia/antagonistas & inibidores
Fenilacetatos/farmacologia
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Células HCT116
Seres Humanos
Metacrilatos/síntese química
Metacrilatos/química
Metacrilatos/farmacologia
Estrutura Molecular
Fenilacetatos/síntese química
Fenilacetatos/química
Estrobilurinas
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Hypoxia-Inducible Factor 1, alpha Subunit); 0 (Methacrylates); 0 (Phenylacetates); 0 (Strobilurins); 0LXZ062TTB (kresoxim-methyl)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170521
[St] Status:MEDLINE


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[PMID]:28514527
[Au] Autor:Friton G; Thompson C; Karadzovska D; King S; King JN
[Ad] Endereço:Companion Animal Development, Elanco Animal Health Inc, Basel, Switzerland.
[Ti] Título:Efficacy and Safety of Injectable Robenacoxib for the Treatment of Pain Associated With Soft Tissue Surgery in Dogs.
[So] Source:J Vet Intern Med;31(3):832-841, 2017 May.
[Is] ISSN:1939-1676
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are used routinely to control pain and inflammation after surgery in dogs. Robenacoxib is a cyclooxygenase-2 selective NSAID. HYPOTHESIS/OBJECTIVE: Assess the clinical efficacy and safety of an injectable formulation of robenacoxib in dogs undergoing surgery. ANIMALS: Three hundred and seventeen client-owned dogs (N = 159 robenacoxib or N = 158 placebo). METHODS: In this prospective, multicenter, randomized, masked, placebo-controlled, parallel-group study, dogs received a SC injection of either robenacoxib, at a target dose of 2.0 mg/kg, or placebo once prior to surgery and for 2 additional days postoperatively. Pain assessments were performed using the short form of the Glasgow Composite Measure Pain Scale (CMPS-SF). The primary efficacy variable was treatment success/failure, with failure defined as the need for rescue therapy to control pain or withdrawal of the dog from the study due to an adverse event. RESULTS: Significantly (P = .006) more dogs administered robenacoxib were considered treatment successes (108 of 151, 73.7%) compared to dogs given placebo (85 of 152, 58.1%). Total pain scores (P < .01), pain at the surgery sites (response to touch, P < .01), and posture/activity (P < .05) were significantly improved at 3, 5, and 8 hours postextubation in dogs receiving robenacoxib versus placebo. CONCLUSIONS AND CLINICAL IMPORTANCE: Robenacoxib administered by SC injection prior to surgery and for 2 additional days postoperatively was effective and well tolerated in the control of postoperative pain and inflammation associated with soft tissue surgery in dogs.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/uso terapêutico
Difenilamina/análogos & derivados
Cães/cirurgia
Manejo da Dor/veterinária
Fenilacetatos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/efeitos adversos
Difenilamina/administração & dosagem
Difenilamina/efeitos adversos
Difenilamina/uso terapêutico
Feminino
Injeções Subcutâneas/veterinária
Masculino
Manejo da Dor/métodos
Medição da Dor/veterinária
Dor Pós-Operatória/prevenção & controle
Dor Pós-Operatória/veterinária
Fenilacetatos/administração & dosagem
Fenilacetatos/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Phenylacetates); 9N3CBB0BIQ (Diphenylamine); Z588009C7C (robenacoxib)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170518
[St] Status:MEDLINE
[do] DOI:10.1111/jvim.14698


  7 / 5725 MEDLINE  
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[PMID]:28493461
[Au] Autor:Margulis AV; Houben E; Hallas J; Overbeek JA; Pottegård A; Torp-Pedersen T; Perez-Gutthann S; Arana A
[Ad] Endereço:RTI Health Solutions, Barcelona, Spain.
[Ti] Título:Ophthalmic nepafenac use in the Netherlands and Denmark.
[So] Source:Acta Ophthalmol;95(5):509-517, 2017 Aug.
[Is] ISSN:1755-3768
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To describe nepafenac use in the Netherlands and Denmark with reference to its approved indications. For context, we also describe the use of ketorolac and diclofenac. METHODS: We identified users in the PHARMO Database Network (the Netherlands, 2008-2013) and the Danish national health registers (Denmark, 1994-2014). We described prevalence of cataract surgery and duration of use in patients with cataract surgery with and without diabetes. RESULTS: In the Netherlands, 9530 nepafenac users (mean age, 71 years; 60% women) contributed 12 691 therapy episodes, of which 21% had a recently recorded cataract surgery. Of 2266 episodes in adult non-diabetic patients with cataract surgery, 60% had one bottle dispensed (treatment duration ≤21 days). Of 441 episodes in adult diabetic patients with cataract surgery, 90% had up to two bottles dispensed (≤60 days). Denmark had 60 403 nepafenac users (mean age, 72 years; 58% women) and 73 648 episodes (41% had recorded cataract surgery). Of 26 649 nepafenac episodes in adult non-diabetic patients with cataract surgery, 92% had one bottle dispensed. Of 3801 episodes in adult diabetic patients with cataract surgery, 99.8% had up to two bottles dispensed. Use patterns of nepafenac, ketorolac and diclofenac were roughly similar in the Netherlands, but not in Denmark. CONCLUSION: Less than half of therapy episodes were related to cataract surgery; around 90% of episodes with surgery were within the approved duration. Underrecording of ophthalmic conditions and procedures was a challenge in this study.
[Mh] Termos MeSH primário: Benzenoacetamidas/farmacologia
Extração de Catarata/estatística & dados numéricos
Uso de Medicamentos/estatística & dados numéricos
Fenilacetatos/farmacologia
Complicações Pós-Operatórias/tratamento farmacológico
[Mh] Termos MeSH secundário: Idoso
Anti-Inflamatórios não Esteroides/farmacologia
Dinamarca/epidemiologia
Feminino
Seguimentos
Seres Humanos
Incidência
Masculino
Países Baixos/epidemiologia
Soluções Oftálmicas
Complicações Pós-Operatórias/epidemiologia
Estudos Retrospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Benzeneacetamides); 0 (Ophthalmic Solutions); 0 (Phenylacetates); 0J9L7J6V8C (nepafenac)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171004
[Lr] Data última revisão:
171004
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170512
[St] Status:MEDLINE
[do] DOI:10.1111/aos.13468


  8 / 5725 MEDLINE  
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[PMID]:28423022
[Au] Autor:Zhou K; Chen D; Li B; Zhang B; Miao F; Zhou L
[Ad] Endereço:College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi, People's Republic of China.
[Ti] Título:Bioactivity and structure-activity relationship of cinnamic acid esters and their derivatives as potential antifungal agents for plant protection.
[So] Source:PLoS One;12(4):e0176189, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A series of cinnamic acid esters and their derivatives were synthesized and evaluated for antifungal activities in vitro against four plant pathogenic fungi by using the mycelium growth rate method. Structure-activity relationship was derived also. Almost all of the compounds showed some inhibition activity on each of the fungi at 0.5 mM. Eight compounds showed the higher average activity with average EC50 values of 17.4-28.6 µg/mL for the fungi than kresoxim-methyl, a commercial fungicide standard, and ten compounds were much more active than commercial fungicide standards carbendazim against P. grisea or kresoxim-methyl against both P. grisea and Valsa mali. Compounds C1 and C2 showed the higher activity with average EC50 values of 17.4 and 18.5 µg/mL and great potential for development of new plant antifungal agents. The structure-activity relationship analysis showed that both the substitution pattern of the phenyl ring and the alkyl group in the alcohol moiety significantly influences the activity. There exists complexly comprehensive effect between the substituents on the phenyl ring and the alkyl group in the alcohol moiety on the activity. Thus, cinnamic acid esters showed great potential the development of new antifungal agents for plant protection due to high activity, natural compounds or natural compound framework, simple structure, easy preparation, low-cost and environmentally friendly.
[Mh] Termos MeSH primário: Cinamatos/síntese química
Ésteres/síntese química
Fungicidas Industriais/síntese química
Fusarium/efeitos dos fármacos
Pyricularia grisea/efeitos dos fármacos
Saccharomycetales/efeitos dos fármacos
[Mh] Termos MeSH secundário: Benzimidazóis/farmacologia
Carbamatos/farmacologia
Cinamatos/farmacologia
Desenho de Drogas
Ésteres/farmacologia
Fungicidas Industriais/farmacologia
Fusarium/crescimento & desenvolvimento
Metacrilatos/farmacologia
Testes de Sensibilidade Microbiana
Estrutura Molecular
Micélio/efeitos dos fármacos
Micélio/crescimento & desenvolvimento
Fenilacetatos/farmacologia
Pyricularia grisea/crescimento & desenvolvimento
Saccharomycetales/crescimento & desenvolvimento
Estrobilurinas
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Carbamates); 0 (Cinnamates); 0 (Esters); 0 (Fungicides, Industrial); 0 (Methacrylates); 0 (Phenylacetates); 0 (Strobilurins); 0LXZ062TTB (kresoxim-methyl); H75J14AA89 (carbendazim); U14A832J8D (cinnamic acid)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170420
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0176189


  9 / 5725 MEDLINE  
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[PMID]:28418095
[Au] Autor:Hedrick E; Lee SO; Safe S
[Ad] Endereço:Department of Veterinary Physiology and Pharmacology, Texas A&M University, College Station, Texas.
[Ti] Título:The nuclear orphan receptor NR4A1 regulates ß1-integrin expression in pancreatic and colon cancer cells and can be targeted by NR4A1 antagonists.
[So] Source:Mol Carcinog;56(9):2066-2075, 2017 Sep.
[Is] ISSN:1098-2744
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:ß1-Integrin is highly expressed and is a negative prognostic factor for colon and pancreatic cancer patients and the gene plays a functional role in cell migration and invasion. In this study, we demonstrate that ß1-integrin expression is regulated in pancreatic and colon cancer cells by the pro-oncogenic orphan nuclear receptor 4A1 (NR4A1, Nur77, TR3) and knockdown of this receptor by RNA interference decreases ß1-integrin protein and mRNA expression, α5-integrin, and also expression of ß1-integrin-dependent phosphorylation of FAK (pFak). Knockdown of NR4A1 also decreased migration and fibronectin-induced adhesion in pancreatic (Panc1, L3.6 pL, and MiaPaCa2) and colon (RKO and SW480) cancer cells. 1,1-Bis(3'-indolyl)-1-(p-substituted phenyl)methane (C-DIM) compounds containing p-hydroxy (DIM-C-pPhOH) and p-carbomethoxy (DIM-C-pPhCO Me) groups are NR4A1 ligands that act as antagonists for this receptor. Treatment of pancreatic and colon cancer cells with DIM-C-pPhOH or DIM-C-pPhCO Me mimics the effects of NR4A1 knockdown and decreases ß1-integrin expression, ß1-integrin regulated genes and responses including migration and adhesion. The results demonstrate a novel method for targeting ß1-integrin in colon and pancreatic cancer cells and indicate possible clinical applications for C-DIM/NR4A1 antagonists for pancreatic and colon cancer therapy.
[Mh] Termos MeSH primário: Neoplasias do Colo/metabolismo
Regulação Neoplásica da Expressão Gênica
Integrina beta1/genética
Membro 1 do Grupo A da Subfamília 4 de Receptores Nucleares/antagonistas & inibidores
Membro 1 do Grupo A da Subfamília 4 de Receptores Nucleares/metabolismo
Neoplasias Pancreáticas/metabolismo
[Mh] Termos MeSH secundário: Adesão Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Movimento Celular/efeitos dos fármacos
Técnicas de Silenciamento de Genes
Seres Humanos
Indóis/farmacologia
Fenóis/farmacologia
Fenilacetatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,1-bis(3'-indolyl)-1-(4-hydroxyphenyl)methane); 0 (Indoles); 0 (Integrin beta1); 0 (NR4A1 protein, human); 0 (Nuclear Receptor Subfamily 4, Group A, Member 1); 0 (Phenols); 0 (Phenylacetates); 0 (p-carboxymethylphenyl 1,1-bis(3'-indolyl)-1-(p-carboxymethylphenyl)methane)
[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:170419
[St] Status:MEDLINE
[do] DOI:10.1002/mc.22662


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[PMID]:28384525
[Au] Autor:Intaraudom C; Bunbamrung N; Dramae A; Boonyuen N; Kongsaeree P; Srichomthong K; Supothina S; Pittayakhajonwut P
[Ad] Endereço:National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency (NSTDA), Thailand Science Park, Paholyothin Road, Klong Luang, Pathumthani, 12120, Thailand.
[Ti] Título:Terphenyl derivatives and drimane - Phathalide/isoindolinones from Hypoxylon fendleri BCC32408.
[So] Source:Phytochemistry;139:8-17, 2017 Jul.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The genus Hypoxylon, a member of the family Xylariaceae, has been known to produce significant secondary metabolites in terms of chemical diversity. Moreover, the compounds isolated can also be used as chemotaxonomic characters for differentiation among the two sections, which are sect. Annulata and sect. Hypoxylon. In our continuing chemical screening programme for novel compounds, the crude extracts of H. fendleri BCC32408 gave significant chemical profiles in HPLC analyses. Thus, the chemical investigation of these crude extracts was then carried out. The investigation led to the isolation of ten previously undescribed compounds including three terphenylquinones (fendleryls A - C), one terphenyl (fendleryl D), and six novel drimane - phthalide-type lactone/isoindolinones derivatives (fendlerinines A - F) along with seven known compounds (2-O-methylatromentin, rickenyl E, atromentin, rickenyls C - D, (+)-ramulosin, and O-hydroxyphenyl acetic acid). The chemical structures were determined on the basis of spectroscopic analyses, including 1D, 2D NMR and high-resolution mass spectrometry, as well as chemical transformations. In addition, these isolated compounds were assessed for antimicrobial activity including antimalarial (against Plasmodium falciparum, K-1 strain), antifungal (against Candida albicans), antibacterial (against Bacillus cereus) activities. Cytotoxicity against both cancerous (KB, MCF-7, NCI-H187) and non-cancerous (Vero) cells of these compounds were also evaluated.
[Mh] Termos MeSH primário: Antifúngicos/isolamento & purificação
Antifúngicos/farmacologia
Antimaláricos/isolamento & purificação
Antimaláricos/farmacologia
Sesquiterpenos/isolamento & purificação
Compostos de Terfenil/isolamento & purificação
Compostos de Terfenil/farmacologia
Xylariales/química
[Mh] Termos MeSH secundário: Animais
Antibacterianos/química
Antifúngicos/química
Antimaláricos/química
Bacillus cereus/efeitos dos fármacos
Candida albicans/efeitos dos fármacos
Cromatografia Líquida de Alta Pressão
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Células KB
Lactonas/química
Testes de Sensibilidade Microbiana
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Fenilacetatos/química
Plasmodium falciparum/efeitos dos fármacos
Sesquiterpenos/química
Sesquiterpenos/farmacologia
Compostos de Terfenil/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Antimalarials); 0 (Lactones); 0 (Phenylacetates); 0 (Sesquiterpenes); 0 (Terphenyl Compounds); 0 (drimane); UK3R9Q59AV (2-hydroxyphenylacetic acid)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170804
[Lr] Data última revisão:
170804
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170407
[St] Status:MEDLINE



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