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[PMID]:29339253
[Au] Autor:Xiao X; Zhang XX; Zhan MM; Cheng K; Li S; Xie Z; Liao C
[Ad] Endereço:School of Biological and Medical Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
[Ti] Título:Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
[So] Source:Eur J Med Chem;145:588-593, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Parkinson's disease (PD) is associated with elevated levels of hMAO-B in the brain, and MAO-B has been recognized a successful target for developing anti-PD drugs. Herein we report rasagiline derivatives as novel potent and selective hMAO-B inhibitors. They were designed by employing fragment-based drug design strategy to link rasagiline and hydrophobic fragments, which may target a hydrophobic pocket in the entrance cavity of hMAO-B. Different linkers such as -OCH -, -SCH -, -OCH CH -, -OCH CH O-, -OCH CH CH O- were tried. A promising selective hMAO-B inhibitor D14 with similar inhibitory activity as rasagiline and improved isoform selectivity was yielded. The selectivity profile of compounds reported herein suggests that we can further develop more potent hMAO-B inhibitors with high isoform selectivity through this strategy.
[Mh] Termos MeSH primário: Aminas/farmacologia
Desenho de Drogas
Indanos/farmacologia
Indenos/farmacologia
Inibidores da Monoaminoxidase/farmacologia
Monoaminoxidase/metabolismo
[Mh] Termos MeSH secundário: Aminas/síntese química
Aminas/química
Cristalografia por Raios X
Relação Dose-Resposta a Droga
Seres Humanos
Indanos/química
Indenos/síntese química
Indenos/química
Modelos Moleculares
Estrutura Molecular
Inibidores da Monoaminoxidase/síntese química
Inibidores da Monoaminoxidase/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Indans); 0 (Indenes); 0 (Monoamine Oxidase Inhibitors); 003N66TS6T (rasagiline); 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:180118
[St] Status:MEDLINE


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[PMID]:28821607
[Au] Autor:Tripathi SK; Xu T; Feng Q; Avula B; Shi X; Pan X; Mask MM; Baerson SR; Jacob MR; Ravu RR; Khan SI; Li XC; Khan IA; Clark AM; Agarwal AK
[Ad] Endereço:From the National Center for Natural Products Research.
[Ti] Título:Two plant-derived aporphinoid alkaloids exert their antifungal activity by disrupting mitochondrial iron-sulfur cluster biosynthesis.
[So] Source:J Biol Chem;292(40):16578-16593, 2017 Oct 06.
[Is] ISSN:1083-351X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Eupolauridine and liriodenine are plant-derived aporphinoid alkaloids that exhibit potent inhibitory activity against the opportunistic fungal pathogens and However, the molecular mechanism of this antifungal activity is unknown. In this study, we show that eupolauridine 9591 (E9591), a synthetic analog of eupolauridine, and liriodenine methiodide (LMT), a methiodide salt of liriodenine, mediate their antifungal activities by disrupting mitochondrial iron-sulfur (Fe-S) cluster synthesis. Several lines of evidence supported this conclusion. First, both E9591 and LMT elicited a transcriptional response indicative of iron imbalance, causing the induction of genes that are required for iron uptake and for the maintenance of cellular iron homeostasis. Second, a genome-wide fitness profile analysis showed that yeast mutants with deletions in iron homeostasis-related genes were hypersensitive to E9591 and LMT. Third, treatment of wild-type yeast cells with E9591 or LMT generated cellular defects that mimicked deficiencies in mitochondrial Fe-S cluster synthesis including an increase in mitochondrial iron levels, a decrease in the activities of Fe-S cluster enzymes, a decrease in respiratory function, and an increase in oxidative stress. Collectively, our results demonstrate that E9591 and LMT perturb mitochondrial Fe-S cluster biosynthesis; thus, these two compounds target a cellular pathway that is distinct from the pathways commonly targeted by clinically used antifungal drugs. Therefore, the identification of this pathway as a target for antifungal compounds has potential applications in the development of new antifungal therapies.
[Mh] Termos MeSH primário: Antifúngicos/farmacologia
Aporfinas/farmacologia
Candida albicans
Proteínas Fúngicas
Indenos/farmacologia
Proteínas com Ferro-Enxofre
Proteínas Mitocondriais
Naftiridinas/farmacologia
[Mh] Termos MeSH secundário: Antifúngicos/química
Aporfinas/química
Candida albicans/genética
Candida albicans/crescimento & desenvolvimento
Cryptococcus neoformans/genética
Cryptococcus neoformans/crescimento & desenvolvimento
Proteínas Fúngicas/genética
Proteínas Fúngicas/metabolismo
Estudo de Associação Genômica Ampla
Indenos/química
Proteínas com Ferro-Enxofre/genética
Proteínas com Ferro-Enxofre/metabolismo
Proteínas Mitocondriais/genética
Proteínas Mitocondriais/metabolismo
Naftiridinas/química
Estresse Oxidativo/efeitos dos fármacos
Estresse Oxidativo/genética
Consumo de Oxigênio/efeitos dos fármacos
Consumo de Oxigênio/genética
Saccharomyces cerevisiae
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Aporphines); 0 (Fungal Proteins); 0 (Indenes); 0 (Iron-Sulfur Proteins); 0 (Mitochondrial Proteins); 0 (Naphthyridines); 58786-39-3 (eupolauridine); E134R7X4O9 (liriodenine)
[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:170820
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M117.781773


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[PMID]:28646757
[Au] Autor:Kadayat TM; Banskota S; Gurung P; Bist G; Thapa Magar TB; Shrestha A; Kim JA; Lee ES
[Ad] Endereço:College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
[Ti] Título:Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease.
[So] Source:Eur J Med Chem;137:575-597, 2017 Sep 08.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:To develop effective therapeutics for inflammatory bowel disease (IBD), 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives, were designed and synthesized and their structure-activity relationships (SAR) were investigated. Compounds 7, 25, 26, 32, 39, 41, 52, 54, and 55 showed potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to IBD. Such inhibitory activity of the compounds correlated with their suppressive activities against the TNF-α-induced production of ROS; ICAM-1 and MCP-1 expression, critical molecules involved in monocyte-epithelial adhesion; and NF-κB transcriptional activity. In addition, compounds 41 and 55 significantly suppressed the lipopolysaccharide (LPS)-induced expression of the TNF-α gene, with compound 55 showing better efficacy. This inhibition of TNF-α expression by compounds 41 and 55 corresponded to their additional inhibitory activity against AP-1 transcriptional activity, which is another transcription factor required for high level TNF-α expression. The strong inhibitory activity of compound 55 against an in vivo colitis model was confirmed by its dose-dependent inhibitory activity in a rat model of 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis, demonstrating compound 55 as a new potential candidate for the development of therapeutics against IBD.
[Mh] Termos MeSH primário: Benzofuranos/farmacologia
Descoberta de Drogas
Indenos/farmacologia
Doenças Inflamatórias Intestinais/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Benzofuranos/síntese química
Benzofuranos/química
Colite/induzido quimicamente
Colite/tratamento farmacológico
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Feminino
Células HT29
Seres Humanos
Indenos/síntese química
Indenos/química
Doenças Inflamatórias Intestinais/genética
Estrutura Molecular
Ratos
Ratos Sprague-Dawley
Relação Estrutura-Atividade
Fator de Transcrição AP-1/antagonistas & inibidores
Fator de Transcrição AP-1/genética
Ácido Trinitrobenzenossulfônico
Células Tumorais Cultivadas
Fator de Necrose Tumoral alfa/antagonistas & inibidores
Fator de Necrose Tumoral alfa/genética
Células U937
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzofurans); 0 (Indenes); 0 (Transcription Factor AP-1); 0 (Tumor Necrosis Factor-alpha); 8T3HQG2ZC4 (Trinitrobenzenesulfonic Acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170625
[St] Status:MEDLINE


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[PMID]:28558967
[Au] Autor:Egbewande FA; Nilsson N; White JM; Coster MJ; Davis RA
[Ad] Endereço:Griffith Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
[Ti] Título:The design, synthesis, and anti-inflammatory evaluation of a drug-like library based on the natural product valerenic acid.
[So] Source:Bioorg Med Chem Lett;27(14):3185-3189, 2017 07 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The plant natural product, valerenic acid (1) was chosen as a desirable scaffold for the generation of a novel screening library due to its drug-like physicochemical parameters (such as LogP, hydrogen bond donor/acceptor counts, and molecular weight). An 11-membered amide library (2-12) was subsequently generated using parallel solution-phase synthesis and Ghosez's reagent. The chemical structures of all semi-synthetic analogues (2-12) were elucidated following analysis of the NMR, MS, UV and IR data. The structures of compounds 8 and 11 were also confirmed by X-ray crystallographic analysis. All library members were evaluated for their ability to inhibit the release of IL-8 and TNF-α. Six analogues showed moderate activity in the IL-8 assay with IC values of 2.8-8.3µM, while none of the tested compounds showed any significant effect on inhibiting TNF-α release.
[Mh] Termos MeSH primário: Anti-Inflamatórios/síntese química
Produtos Biológicos/química
Desenho de Drogas
Indenos/química
Sesquiterpenos/química
Bibliotecas de Moléculas Pequenas/síntese química
[Mh] Termos MeSH secundário: Anti-Inflamatórios/química
Anti-Inflamatórios/farmacologia
Linhagem Celular
Cristalografia por Raios X
Seres Humanos
Interleucina-8/metabolismo
Queratinócitos/citologia
Queratinócitos/efeitos dos fármacos
Queratinócitos/metabolismo
Espectrometria de Massas
Conformação Molecular
Bibliotecas de Moléculas Pequenas/química
Bibliotecas de Moléculas Pequenas/farmacologia
Espectrofotometria Ultravioleta
Fator de Necrose Tumoral alfa/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Biological Products); 0 (Indenes); 0 (Interleukin-8); 0 (Sesquiterpenes); 0 (Small Molecule Libraries); 0 (Tumor Necrosis Factor-alpha); 34NDB285PM (valerenic acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170601
[St] Status:MEDLINE


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[PMID]:28382516
[Au] Autor:Osanai K; Kobayashi Y; Otsu M; Izawa T; Sakai K; Iwashita M
[Ad] Endereço:Department of Obstetrics and Gynecology, Kyorin University School of Medicine, 6-20-2 Shinkawa, Mitaka, Tokyo, 181-8611, Japan.
[Ti] Título:Ramelteon, a selective MT1/MT2 receptor agonist, suppresses the proliferation and invasiveness of endometrial cancer cells.
[So] Source:Hum Cell;30(3):209-215, 2017 Jul.
[Is] ISSN:1749-0774
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The incidence of endometrial cancer is increasing, making it the fifth most common cancer worldwide. To date, however, there is no standard therapy for patients with recurrent endometrial cancer. Melatonin, a hormone secreted by the pineal gland, has been shown to have anti-tumor effects in various tumor types. Although melatonin is available as a supplement, it has not been approved for cancer treatment. Ramelteon, a selective melatonin receptor type 1 and 2 (MT1/MT2) receptor agonist, has been approved to treat sleep disorders, suggesting that ramelteon may be effective in the treatment of endometrial cancer. To determine whether this agent may be effective in the treatment of endometrial cancer, this study investigated the ability of ramelteon to suppress the proliferation and invasiveness of HHUA cells, an estrogen receptor-positive endometrial cancer cell line. Ramelteon at 10 M maximally suppressed the proliferation of HHUA cells, reducing the percentage of Ki-67 positive proliferating cells. This effect was completely blocked by luzindole, a MT1/MT2 receptor antagonist. Furthermore, ramelteon inhibited HHUA cell invasion and reduced the expression of the MMP-2 and MMP-9 genes. These results suggested that ramelteon may be a candidate for the treatment of recurrent endometrial cancer, with activity similar to that of melatonin.
[Mh] Termos MeSH primário: Proliferação Celular/efeitos dos fármacos
Neoplasias do Endométrio/patologia
Indenos/farmacologia
Invasividade Neoplásica
Receptor MT1 de Melatonina/agonistas
Receptor MT2 de Melatonina/agonistas
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Depressão Química
Feminino
Expressão Gênica
Seres Humanos
Metaloproteinase 2 da Matriz/genética
Metaloproteinase 9 da Matriz/genética
Invasividade Neoplásica/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indenes); 0 (Receptor, Melatonin, MT1); 0 (Receptor, Melatonin, MT2); 901AS54I69 (ramelteon); EC 3.4.24.24 (MMP2 protein, human); EC 3.4.24.24 (Matrix Metalloproteinase 2); EC 3.4.24.35 (MMP9 protein, human); EC 3.4.24.35 (Matrix Metalloproteinase 9)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171112
[Lr] Data última revisão:
171112
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170407
[St] Status:MEDLINE
[do] DOI:10.1007/s13577-017-0169-7


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[PMID]:28270270
[Au] Autor:Edmonds C; Swanoski M
[Ti] Título:A Review of Suvorexant, Doxepin, Ramelteon, and Tasimelteon for the Treatment of Insomnia in Geriatric Patients.
[So] Source:Consult Pharm;32(3):156-160, 2017 Mar 01.
[Is] ISSN:0888-5109
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Geriatric patients often experience insomnia because of physiological and neurological changes that occur during the aging process. Use of benzodiazepines, nonbenzodiazepine hypnotics, and diphenhydramine for the treatment of insomnia pose an increased risk of cognitive impairment, falls, and fractures in this patient population. Therapeutic alternatives approved by the Food and Drug Administration include suvorexant, doxepin, ramelteon, and tasimelteon, which have shown efficacy and safety in various studies. This paper explores and outlines the available safety and efficacy data associated with these medications and reviews their potential place in therapy in treating insomnia in the geriatric population.
[Mh] Termos MeSH primário: Hipnóticos e Sedativos/farmacologia
Hipnóticos e Sedativos/uso terapêutico
Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Azepinas/farmacologia
Azepinas/uso terapêutico
Benzofuranos/farmacologia
Benzofuranos/uso terapêutico
Ciclopropanos/farmacologia
Ciclopropanos/uso terapêutico
Doxepina/farmacologia
Doxepina/uso terapêutico
Seres Humanos
Hipnóticos e Sedativos/administração & dosagem
Hipnóticos e Sedativos/efeitos adversos
Indenos/farmacologia
Indenos/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Triazóis/farmacologia
Triazóis/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Azepines); 0 (Benzofurans); 0 (Cyclopropanes); 0 (Hypnotics and Sedatives); 0 (Indenes); 0 (Triazoles); 081L192FO9 (suvorexant); 1668-19-5 (Doxepin); 901AS54I69 (ramelteon); SHS4PU80D9 (tasimelteon)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE
[do] DOI:10.4140/TCP.n.2017.156


  7 / 2706 MEDLINE  
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[PMID]:28115120
[Au] Autor:González-Delgado AM; Shukla MK; Ashigh J; Perkins R
[Ad] Endereço:Plant and Environmental Sciences Department, New Mexico State University, Las Cruces, NM 88003-8003, USA. Electronic address: amgonz4@nmsu.edu.
[Ti] Título:Effect of application rate and irrigation on the movement and dissipation of indaziflam.
[So] Source:J Environ Sci (China);51:111-119, 2017 Jan.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Indaziflam is a new preemergence herbicide for the control of annual grass and broadleaf weeds in various cropping systems including pecan orchards. The objectives of this study were to (1) determine the mobility and dissipation of indaziflam and (2) evaluate herbicide efficacy in a flood-irrigated pecan orchard in southern New Mexico, USA. Indaziflam was applied at 0, 36.5, and 73.1g/ha in areas with (impacted) and without (unimpacted) tree injury symptoms. Soil samples were collected at 0-15, 15-30, and 30-46cm depths 26, 63, 90, and 126days after the first herbicide application. Additional soil samples were collected 4, 30, and 56days after the second application. Indaziflam was detected in soil samples collected at each depth, suggesting movement with irrigation water. Indaziflam concentrations decreased with increasing soil depth and time. Indaziflam mass recoveries were greater in the unimpacted area than in the impacted area after the first and second applications. Dissipation half-lives of indaziflam in the soil ranged from 30 to 86days for total indaziflam recovered from the entire soil profile after the first and second applications in both areas. The percent weed control was similar in the impacted and unimpacted areas for both rates of indaziflam on 26 and 63days after application; however, on 90days after the application, percent weed control was lower in the impacted than unimpacted area.
[Mh] Termos MeSH primário: Herbicidas/análise
Indenos/análise
Poluentes do Solo/análise
Triazinas/análise
[Mh] Termos MeSH secundário: Irrigação Agrícola/métodos
Monitoramento Ambiental
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Herbicides); 0 (Indenes); 0 (N-(2,3-dihydro-2,6-dimethyl-1H-inden-1-yl)-6-(1-fluoroethyl)-1,3,5-triazine-2,4-diamine); 0 (Soil Pollutants); 0 (Triazines)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170209
[Lr] Data última revisão:
170209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170125
[St] Status:MEDLINE


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[PMID]:28009436
[Au] Autor:Ward SE; Beswick P; Calcinaghi N; Dawson LA; Gartlon J; Graziani F; Jones DN; Lacroix L; Selina Mok MH; Oliosi B; Pardoe J; Starr K; Woolley ML; Harries MH
[Ad] Endereço:University of Sussex, Brighton, UK.
[Ti] Título:Pharmacological characterization of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2, 3-dihydro-1H-inden-2-yl]-2-propanesulfonamide: a novel, clinical AMPA receptor positive allosteric modulator.
[So] Source:Br J Pharmacol;174(5):370-385, 2017 Mar.
[Is] ISSN:1476-5381
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND PURPOSE: AMPA receptor positive allosteric modulators represent a potential therapeutic strategy to improve cognition in people with schizophrenia. These studies collectively constitute the preclinical pharmacology data package used to build confidence in the pharmacology of this molecule and enable a clinical trial application. EXPERIMENTAL APPROACH: [N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro 1H-inden-2-yl]-2-propanesulfonamide] (UoS12258) was profiled in a number of in vitro and in vivo studies to highlight its suitability as a novel therapeutic agent. KEY RESULTS: We demonstrated that UoS12258 is a selective, positive allosteric modulator of the AMPA receptor. At rat native hetero-oligomeric AMPA receptors, UoS12258 displayed a minimum effective concentration of approximately 10 nM in vitro and enhanced AMPA receptor-mediated synaptic transmission at an estimated free brain concentration of approximately 15 nM in vivo. UoS12258 reversed a delay-induced deficit in novel object recognition in rats after both acute and sub-chronic dosing. Sub-chronic dosing reduced the minimum effective dose from 0.3 to 0.03 mg·kg . UoS12258 was also effective at improving performance in two other cognition models, passive avoidance in scopolamine-impaired rats and water maze learning and retention in aged rats. In side-effect profiling studies, UoS12258 did not produce significant changes in the maximal electroshock threshold test at doses below 10 mg·kg . CONCLUSION AND IMPLICATIONS: We conclude that UoS12258 is a potent and selective AMPA receptor modulator exhibiting cognition enhancing properties in several rat behavioural models superior to other molecules that have previously entered clinical evaluation.
[Mh] Termos MeSH primário: Comportamento Animal/efeitos dos fármacos
Indenos/farmacologia
Nootrópicos/farmacologia
Receptores de AMPA/efeitos dos fármacos
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos
Animais
Aprendizagem da Esquiva/efeitos dos fármacos
Cognição/efeitos dos fármacos
Relação Dose-Resposta a Droga
Eletrochoque
Seres Humanos
Indenos/administração & dosagem
Indenos/toxicidade
Masculino
Aprendizagem em Labirinto/efeitos dos fármacos
Nootrópicos/administração & dosagem
Nootrópicos/toxicidade
Ratos
Ratos Sprague-Dawley
Ratos Wistar
Receptores de AMPA/metabolismo
Recognição (Psicologia)/efeitos dos fármacos
Hidrobrometo de Escopolamina/toxicidade
Sulfonamidas/administração & dosagem
Sulfonamidas/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indenes); 0 (N-(5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl)-2-propanesulfonamide); 0 (Nootropic Agents); 0 (Receptors, AMPA); 0 (Sulfonamides); 451IFR0GXB (Scopolamine Hydrobromide)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170728
[Lr] Data última revisão:
170728
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161224
[St] Status:MEDLINE
[do] DOI:10.1111/bph.13696


  9 / 2706 MEDLINE  
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[PMID]:27868343
[Au] Autor:Yamada K
[Ad] Endereço:Department of Psychiatry, Tokyo Women's Medical University Medical Center East, Tokyo, Japan.
[Ti] Título:Effectiveness of ramelteon for residual sleep disturbances (hypersomnia) in a patient with premenstrual dysphoric disorder.
[So] Source:Psychiatry Clin Neurosci;71(2):147, 2017 Feb.
[Is] ISSN:1440-1819
[Cp] País de publicação:Australia
[La] Idioma:eng
[Mh] Termos MeSH primário: Distúrbios do Sono por Sonolência Excessiva/tratamento farmacológico
Indenos/uso terapêutico
Transtorno Disfórico Pré-Menstrual/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Feminino
Seres Humanos
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; LETTER
[Nm] Nome de substância:
0 (Indenes); 901AS54I69 (ramelteon)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170323
[Lr] Data última revisão:
170323
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161122
[St] Status:MEDLINE
[do] DOI:10.1111/pcn.12484


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[PMID]:27853836
[Au] Autor:Vaccaro MC; Mariaevelina A; Malafronte N; De Tommasi N; Leone A
[Ad] Endereço:Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 134D, 80084, Fisciano, Italy.
[Ti] Título:Increasing the synthesis of bioactive abietane diterpenes in Salvia sclarea hairy roots by elicited transcriptional reprogramming.
[So] Source:Plant Cell Rep;36(2):375-386, 2017 Feb.
[Is] ISSN:1432-203X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:KEY MESSAGE: Transcriptional activation of genes belonging to the plastidial MEP-derived isoprenoid pathway by elicitation with methyl jasmonate and coronatine enhanced the content of bioactive abietane diterpenes in Salvia sclarea hairy roots. We have shown that aethiopinone, an abietane diterpene synthesized in Salvia sclarea roots is cytotoxic and induces apoptosis in human melanoma cells. To develop a production platform for this compound and other abietane diterpenes, hairy root technology was combined with the elicitation of methyl jasmonate (MeJA) or the phytotoxin coronatine (Cor). Both MeJA and Cor induced a significant accumulation of aethiopinone, but prolonged exposure to MeJA irremediably caused inhibition of hairy root growth, which was unaffected by Cor treatment. Considering together the fold increase in aethiopinone content and the final hairy root biomass, the best combination was a Cor treatment for 28 days, which allowed to obtain up to 105.34 ± 2.30 mg L of this compound to be obtained, corresponding to a 24-fold increase above the basal content in untreated hairy roots. MeJA or Cor elicitation also enhanced the synthesis of other bioactive abietane-quinone diterpenes. The elicitor-dependent steering effect was due to a coordinated transcriptional activation of several biosynthetic genes belonging to the plastidial MEP-derived isoprenoid pathway. High correlations between aethiopinone content and MeJA or Cor-elicited level of gene transcripts were found for DXS2 (r  = 0.99), DXR (r  = 0.99), and GGPPS (r  = 0.98), encoding enzymes acting upstream of GGPP, the common precursor of diterpenes and other plastidial-derived terpenes, as well as CPPS (r  = 0.99), encoding the enzyme involved in the first cyclization steps leading to copalyl-diphosphate, the precursor of abietane-like diterpenes. These results point to these genes as possible targets of metabolic engineering approaches to establish a more efficient production platform for such promising anti-proliferative plant-derived compounds.
[Mh] Termos MeSH primário: Diterpenos Abietanos/biossíntese
Raízes de Plantas/genética
Raízes de Plantas/metabolismo
Salvia/genética
Salvia/metabolismo
Transcrição Genética
[Mh] Termos MeSH secundário: Acetatos/farmacologia
Aminoácidos/farmacologia
Biomassa
Ciclopentanos/farmacologia
Perfilação da Expressão Gênica
Regulação da Expressão Gênica de Plantas/efeitos dos fármacos
Indenos/farmacologia
Naftoquinonas/metabolismo
Oxilipinas/farmacologia
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Salvia/efeitos dos fármacos
Transcrição Genética/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetates); 0 (Amino Acids); 0 (Cyclopentanes); 0 (Diterpenes, Abietane); 0 (Indenes); 0 (Naphthoquinones); 0 (Oxylipins); 0 (RNA, Messenger); 62251-96-1 (coronatine); 79491-58-0 (aethiopinone); 900N171A0F (methyl jasmonate)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171004
[Lr] Data última revisão:
171004
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161118
[St] Status:MEDLINE
[do] DOI:10.1007/s00299-016-2076-x



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