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[PMID]:29431326
[Au] Autor:Khripach LV; Zheleznyak EV; Knyazeva TD; Koganova ZI; Salikhova DI; Grishin DA
[Ti] Título:[Method of colored model radicals for assessment of oxidative equilibrium in biologic samples].
[So] Source:Gig Sanit;95(9):884-90, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The most specific method of the recording of the rate offree radical reactions is the method of electron paramagnetic resonance (EPR) spectroscopy, but it is rarely used in applied biology due to expensive equipment and complexity of the execution of measurements. However chemists have found a number of colored organic radicals which lose the coloring under transition into diamagnetic form. In the given paper there are presented results of our studies on the development of methods for the assessment of oxidant equilibrium in biological media with a use of stable radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) and cation-radicals of N,N-diethyl-p-phenylenediamine (DEPPD). We have developed the new modification of DPPH test, replacing methanol-based incubation medium by non-ionic detergent solution, compatible with native blood serum. Modified DPPH test conserved typical biphasic kinetics of the origin variant, had the similar sensitivity to model antioxidants (IC values 49, 38 and 13 mkMfor ascorbate, a-tocopherol and quercetine, correspondingly) and was applied in experiments on laboratory animals treated with nano- and ionic silver, carbon nanotubes, microfine coal and electrolytic dust. We have tried also the assay of serum lipid hydroperoxides based on Fe-initiated DEPPD oxidation (Alberti et al., 2000). The comparison of kinetics of DEPPD oxidation in model (HO/Fe) and biologic (rat serum/Fe) systems, before and after Fe addition, seems to be an evidence that ceruloplasmin (CP) was involved in the resulting process, but failed to determine its polynomial kinetics, at least for the rat serum and DEPPD excess. The use of CP monoclonal antibodies seems to be the best way for the clarification of the mechanism of this reaction.
[Mh] Termos MeSH primário: Compostos de Bifenilo
Oxirredução
Fenilenodiaminas
Picratos
Plasma
[Mh] Termos MeSH secundário: Animais
Fenômenos Bioquímicos
Compostos de Bifenilo/análise
Compostos de Bifenilo/química
Compostos de Bifenilo/metabolismo
Corantes/análise
Corantes/química
Indicadores e Reagentes/análise
Indicadores e Reagentes/química
Modelos Químicos
Fenilenodiaminas/análise
Fenilenodiaminas/química
Fenilenodiaminas/metabolismo
Picratos/análise
Picratos/química
Picratos/metabolismo
Plasma/química
Plasma/metabolismo
Ratos
Kit de Reagentes para Diagnóstico
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Coloring Agents); 0 (Indicators and Reagents); 0 (Phenylenediamines); 0 (Picrates); 0 (Reagent Kits, Diagnostic); 93-05-0 (N,N-diethyl 4-phenylenediamine); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180213
[St] Status:MEDLINE


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[PMID]:29268129
[Au] Autor:Cen J; Guo H; Hong C; Lv J; Yang Y; Wang T; Fang D; Luo W; Wang C
[Ad] Endereço:Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China.
[Ti] Título:Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity.
[So] Source:Eur J Med Chem;144:128-136, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A novel series of tacrine-bifendate (THA-DDB) conjugates (7a-e) were synthesized and evaluated as potential anti-Alzheimer's agents. These compounds showed potent cholinesterase and self-induced ß-amyloid (Aß) aggregation inhibitory activities. A Lineweaver-Burk plot and molecular modeling study showed that these compounds can target both catalytic active site (CAS) and peripheral anionic site (PAS) of acetylcholinesterase (AChE). The cytotoxicity of the conjugate 7d against PC12 and HepG2 cells and hepatotoxicity against human hepatocyte cell line (HL-7702) were found to be considerably less compared to THA. Moreover, treatment with 7d did not exhibit significant hepatotoxicity in mice. Finally, in vivo studies confirmed that 7d significantly ameliorates the cognitive performances of scopolamine-treated ICR mice. Therefore, 7d has high potential for the treatment of Alzheimer's disease and warrants further investigation.
[Mh] Termos MeSH primário: Compostos de Bifenilo/química
Compostos de Bifenilo/farmacologia
Inibidores da Colinesterase/química
Inibidores da Colinesterase/farmacologia
Cognição/efeitos dos fármacos
Tacrina/análogos & derivados
Tacrina/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Doença de Alzheimer/tratamento farmacológico
Doença de Alzheimer/patologia
Animais
Compostos de Bifenilo/toxicidade
Linhagem Celular
Doença Hepática Induzida por Substâncias e Drogas/etiologia
Doença Hepática Induzida por Substâncias e Drogas/patologia
Inibidores da Colinesterase/toxicidade
Colinesterases/metabolismo
Desenho de Drogas
Células Hep G2
Seres Humanos
Fígado/efeitos dos fármacos
Fígado/patologia
Masculino
Camundongos Endogâmicos ICR
Células PC12
Ratos
Tacrina/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Cholinesterase Inhibitors); 0G32E321W1 (bifendate); 4VX7YNB537 (Tacrine); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Cholinesterases)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


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[PMID]:29216958
[Au] Autor:Guesmi F; Ben Hadj AS; Landoulsi A
[Ad] Endereço:Laboratory of Biochemistry and Molecular Biology, Faculty of Sciences of Bizerte, University of Carthage, Zarzouna 7021, Tunisia.
[Ti] Título:Investigation of Extracts from Tunisian Ethnomedicinal Plants as Antioxidants, Cytotoxins, and Antimicrobials.
[So] Source:Biomed Environ Sci;30(11):811-824, 2017 Nov.
[Is] ISSN:0895-3988
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To determine the medicinal potential of various plants and their parts extracted with different solvents. METHODS: The total phenolic content of acetonitrile/water (60%-40%) (ACN/W) and aqueous (W) extract fractions was determined by high-performance liquid chromatography (HPLC), and terpenic compounds were detected by gas chromatography/mass spectrometry (GC/MS). Antioxidant activity of the samples was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and ß-carotene bleaching method. Cell viability was investigated by thiazolyl blue tetrazolium bromide [3-(4,5-dimethylthiazol)-2-yl 2,5-diphenyltetrazolium bromide] (MTT) assay. The mechanisms involved in cytotoxic activity were investigated in a murine macrophage cell line (RAW 264.7) and cancer lines. RESULTS: Our findings show that 11 plant species exhibited biological activity. In addition, moderate antibacterial activity was reported against one or more of the tested bacterial strains at two concentrations: 300 µg and 3 mg/disc. Furthermore, our data reveal that among all plants investigated, some extract and hydrophobic fractions were potent scavengers of the DPPH radical (6.78 µg/mL < EC50 < 8.55 µg/mL). Taken together, our results show that Nerium oleander (NOACN/W) and Pituranthos tortuosus (PTACN/W) were highly cytotoxic against RAW 264.7 cells with IC80 values of 0.36, and 1.55 µg/mL, respectively. In contrast, murine macrophage cell lines had low growth and were significantly sensitive to water extracts of Thymus hirtus sp. algeriensis (THW), Lavandula multifida (LMW), and ACN/W extract of Erica multiflora (EMACN/W) at doses > 400, 47.20, and 116.74 µg/mL, respectively. The current work demonstrates that RAW 264.7 cell proliferation was inhibited by samples in a dose-dependent manner. CONCLUSION: Our findings, validated through free radical scavenging activity, agar diffusion assay, and cytotoxicity of essential oils towards cancer cells, show that ethnomedicinal plants used in this work have a novel application as a tumor suppressor.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antineoplásicos Fitogênicos/farmacologia
Citotoxinas/farmacologia
Extratos Vegetais/farmacologia
Plantas Medicinais/química
[Mh] Termos MeSH secundário: Animais
Antibacterianos/química
Antineoplásicos Fitogênicos/química
Bactérias/efeitos dos fármacos
Compostos de Bifenilo
Linhagem Celular
Citotoxinas/química
Etnobotânica
Camundongos
Estrutura Molecular
Fenóis/química
Fenóis/farmacologia
Picratos
Extratos Vegetais/química
Terpenos/química
Terpenos/farmacologia
Tunísia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents, Phytogenic); 0 (Biphenyl Compounds); 0 (Cytotoxins); 0 (Phenols); 0 (Picrates); 0 (Plant Extracts); 0 (Terpenes); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171209
[St] Status:MEDLINE
[do] DOI:10.3967/bes2017.109


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[PMID]:29184402
[Au] Autor:Wu X; Wang L; Qiu Y; Zhang B; Hu Z; Jin R
[Ad] Endereço:Department of Pediatrics, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan.
[Ti] Título:Cooperation of IRAK1/4 inhibitor and ABT-737 in nanoparticles for synergistic therapy of T cell acute lymphoblastic leukemia.
[So] Source:Int J Nanomedicine;12:8025-8034, 2017.
[Is] ISSN:1178-2013
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:T cell acute lymphoblastic leukemia (T-ALL) is caused by clonal expansion of variant T cell progenitors and is considered as a high risk leukemia. Contemporary single chemotherapy has a limited effect due to dynamic and versatile properties of T-ALL. Here IRAK1/4 inhibitor and ABT-737 were co-encapsulated into polyethylene glycol modified poly (lactic-co-glycolic acid) nanoparticles (IRAK/ABT-NP) to enhance synergistic therapy of T-ALL. The formulation was optimized to achieve high drug loading using Box-Behnken design and response surface methodology. The optimal parameter comprised 2.98% polymer in acetonitrile, a ratio of oil phase to water phase of 1:8.33, and 2.12% emulsifier concentration. High drug loading and uniform spherical shape was achieved. In vitro release study showed sustained release of IRAK1/4 inhibitor for 72 hours as well as sustained release of ABT-737 for more than 120 hours. Uptake efficiency of IRAK/ABT-NP and induced apoptotic T-ALL fraction by IRAK/ABT-NP were much higher than the IRAK1/4 and ABT-737 combined solution. IC of IRAK/ABT-NP was two-fold lower than free drug combination in Jurkat cells. Additionally, we conducted in vivo experiments in which IRAK/ABT-NP exhibited greater cytotoxicity toward T-ALL cells, the capacity to significantly restore white blood cell number in peripheral blood, and improved survival time of T-ALL mouse model compared to the IRAK1/4 and ABT-737 combined solution.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia
Quinases Associadas a Receptores de Interleucina-1/antagonistas & inibidores
Nanopartículas/química
Leucemia-Linfoma Linfoblástico de Células T Precursoras/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Compostos de Bifenilo/administração & dosagem
Compostos de Bifenilo/farmacologia
Liberação Controlada de Fármacos
Sinergismo Farmacológico
Feminino
Seres Humanos
Células Jurkat
Ácido Láctico/química
Camundongos
Nanopartículas/administração & dosagem
Nitrofenóis/administração & dosagem
Nitrofenóis/farmacologia
Piperazinas/administração & dosagem
Piperazinas/farmacologia
Ácido Poliglicólico/química
Sulfonamidas/administração & dosagem
Sulfonamidas/farmacologia
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-737); 0 (Biphenyl Compounds); 0 (Nitrophenols); 0 (Piperazines); 0 (Sulfonamides); 0 (polylactic acid-polyglycolic acid copolymer); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); EC 2.7.11.1 (IRAK1 protein, human); EC 2.7.11.1 (IRAK4 protein, human); EC 2.7.11.1 (Interleukin-1 Receptor-Associated Kinases)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171130
[St] Status:MEDLINE
[do] DOI:10.2147/IJN.S146875


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[PMID]:29353724
[Au] Autor:Jin K; Yin H; De Clercq E; Pannecouque C; Meng G; Chen F
[Ad] Endereço:Engineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China; Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs, Shanghai 200433, People's Republic of China.
[Ti] Título:Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
[So] Source:Eur J Med Chem;145:726-734, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A novel series of diarylpyrimidine (DAPY) derivatives bearing the biphenyl motif with multiple substituted groups was synthesized as human immunodeficiency virus (HIV)-1 non-nucleoside reverse transcriptase inhibitors. All of the target compounds were evaluated for their in vitro activity against HIV in MT-4 cells. Most of the compounds exhibited excellent activity with low nanomolar EC values against wild-type, single and double mutant HIV-1 strains. Compound 4b displayed an EC value of 1 nM against HIV-1 IIIB, 1.3 nM against L100I, 0.84 nM against K103 N, 1.5 nM against Y181C, 11 nM against Y188L, 2 nM against E138K, 10 nM against K103 N + Y181C, and almost 110 nM against F227L + V106. The improvement in the selectivity and potency of the target molecules against the wild-type and mutant HIV-1 strains validated our hypothesis. The biphenyl ring in the DAPY derivatives could strengthen the π-π stacking effect between the target molecule and the non-nucleoside inhibitor-binding pocket in the reverse transcriptase by extending the conjugating systems. This research represented a significant step toward the discovery of novel therapeutic DAPYs for treating acquired immunodeficiency syndrome in patients infected with HIV-1.
[Mh] Termos MeSH primário: Fármacos Anti-HIV/farmacologia
Compostos de Bifenilo/farmacologia
Transcriptase Reversa do HIV/antagonistas & inibidores
HIV-1/efeitos dos fármacos
Pirimidinas/farmacologia
Inibidores da Transcriptase Reversa/farmacologia
[Mh] Termos MeSH secundário: Fármacos Anti-HIV/síntese química
Fármacos Anti-HIV/química
Compostos de Bifenilo/química
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Descoberta de Drogas
Transcriptase Reversa do HIV/metabolismo
HIV-1/genética
Seres Humanos
Testes de Sensibilidade Microbiana
Simulação de Acoplamento Molecular
Estrutura Molecular
Mutação
Pirimidinas/síntese química
Pirimidinas/química
Inibidores da Transcriptase Reversa/síntese química
Inibidores da Transcriptase Reversa/química
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-HIV Agents); 0 (Biphenyl Compounds); 0 (Pyrimidines); 0 (Reverse Transcriptase Inhibitors); 2L9GJK6MGN (diphenyl); EC 2.7.7.49 (HIV Reverse Transcriptase)
[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]:29335204
[Au] Autor:Gu X; Jiang Y; Qu Y; Chen J; Feng D; Li C; Yin X
[Ad] Endereço:Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Jiangsu Center for the Collaboration and Innovation of Cancer Biotherapy, Xuzhou Medical University, Xuzhou 221004, People's Republic of China.
[Ti] Título:Synthesis and biological evaluation of bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potential P-glycoprotein and tumor metastasis inhibitors.
[So] Source:Eur J Med Chem;145:379-388, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:As a continuation of previous research, fifteen bifendate derivatives bearing 6,7-dihydro-dibenzo [c,e]azepine scaffold were synthesized and evaluated as P-gp-medicated multidrug resistance (MDR) reversal agents. Biological evaluation indicated that compounds 6k and 9c more potently reversed P-gp-mediated MDR than bifendate and verapamil (VRP) by blocking P-gp mediated drug efflux function and not by decreasing P-gp expression in K562/A02 MDR cells. Interestingly, wound-healing and chamber migration assay showed that 6k and 9c could significantly attenuate the migration of MDA-MB-231 cells. Notably, 6k and 9c could markedly suppress the invasive activity of MDA-MB-231 cells, thus displayed potential anti-metastasis activity. Preliminary mechanism studies indicated that the anti-metastasis activity of 6k and 9c was associated with their inhibitory effect on the activity and expression of MMP-2 and MMP-9. These results, together with the MDR reversal results indicated that compounds 6k and 9c might be promising leads for developing novel anti-cancer agents with P-gp and tumor metastasis inhibitory activities.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
Antineoplásicos/farmacologia
Azepinas/farmacologia
Compostos de Bifenilo/farmacologia
Neoplasias/tratamento farmacológico
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Antineoplásicos/síntese química
Antineoplásicos/química
Azepinas/química
Compostos de Bifenilo/síntese química
Compostos de Bifenilo/química
Linhagem Celular Tumoral
Relação Dose-Resposta a Droga
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Células K562
Estrutura Molecular
Neoplasias/metabolismo
Neoplasias/patologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Antineoplastic Agents); 0 (Azepines); 0 (Biphenyl Compounds); 0G32E321W1 (bifendate)
[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:180117
[St] Status:MEDLINE


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[PMID]:29355546
[Au] Autor:Shen P; Zhang Z; He Y; Gu C; Zhu K; Li S; Li Y; Lu X; Liu J; Zhang N; Cao Y
[Ad] Endereço:College of Veterinary Medicine, Jilin University, Changchun 130062, People's Republic of China.
[Ti] Título:Magnolol treatment attenuates dextran sulphate sodium-induced murine experimental colitis by regulating inflammation and mucosal damage.
[So] Source:Life Sci;196:69-76, 2018 Mar 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Magnolol, the main and active ingredient of the Magnolia officinalis, has been widely used in traditional prescription to the human disorders. Magnolol has been proved to have several pharmacological properties including anti-bacterial, anti-oxidant and anti-inflammatory activities. However, the effects of magnolol on ulcerative colitis (UC) have not been reported. The aim of this study was to investigate the protective effects and mechanisms of magnolol on dextran sulphate sodium (DSS)-induced colitis in mice. The results showed that magnolol significantly alleviated DSS-induced body weight loss, disease activities index (DAI), colon length shortening and colonic pathological damage. In addition, magnolol restrained the expression of TNF-α, IL-1ß and IL-12 via the regulation of nuclear factor-κB (NF-κB) and Peroxisome proliferator-activated receptor-γ (PPAR-γ) pathways. Magnolol also enhanced the expression of ZO-1 and occludin in DSS-induced mice colonic tissues. These results showed that magnolol played protective effects on DSS-induced colitis and may be an alternative therapeutic reagent for colitis treatment.
[Mh] Termos MeSH primário: Compostos de Bifenilo/uso terapêutico
Colite Ulcerativa/induzido quimicamente
Colite Ulcerativa/tratamento farmacológico
Sulfato de Dextrana
Fármacos Gastrointestinais/uso terapêutico
Mucosa Intestinal/efeitos dos fármacos
Lignanas/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Ceco/microbiologia
Colite Ulcerativa/patologia
Colo/patologia
Citocinas/biossíntese
Inflamação/fisiopatologia
Inflamação/prevenção & controle
Mediadores da Inflamação
Mucosa Intestinal/patologia
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Ocludina/antagonistas & inibidores
Ocludina/biossíntese
PPAR gama/efeitos dos fármacos
Perda de Peso/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Cytokines); 0 (Gastrointestinal Agents); 0 (Inflammation Mediators); 0 (Lignans); 0 (Occludin); 0 (PPAR gamma); 001E35HGVF (magnolol); 9042-14-2 (Dextran Sulfate)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180123
[St] Status:MEDLINE


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[PMID]:29381027
[Au] Autor:Lee CW; Hu SC; Yen FL; Hsu LF; Lee IT; Lin ZC; Tsai MH; Huang CL; Liang CJ; Chiang YC
[Ti] Título:Magnolol Nanoparticles Exhibit Improved Water Solubility and Suppress TNF-α-Induced VCAM-1 Expression in Endothelial Cells.
[So] Source:J Biomed Nanotechnol;13(3):255-68, 2017 Mar.
[Is] ISSN:1550-7033
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The expression of the adhesion molecule vascular cell adhesion molecule-1 (VCAM-1) on endothelial cells enables the attachment of leukocytes to the endothelium, which may lead to inflammation and the development of atherosclerosis. Magnolol is a major bioactive compound derived from the plant species Magnolia officinalis. In this study, we synthesized a novel nanoparticle formulation of magnolol to improve its water solubility and physicochemical properties, evaluated its effects on TNF-α-induced VCAM-1 expression in endothelial cells, and determined the signal transduction pathways involved. Our findings demonstrated that the magnolol nanoparticle system showed great improvements in physicochemical properties and water solubility owing to a reduction in particle size, transformation from a crystalline to amorphous structure, and the formation of hydrogen bonds with the nanoparticle carriers. In terms of its biological actions, magnolol nanoparticles attenuated TNF-α-induced VCAM-1 protein expression, promoter activity, and mRNA expression in endothelial cells in vitro. This was found to be mediated by the ERK, AKT, and NF-κB signaling pathways. In addition, magnolol nanoparticles inhibited TNF-α-induced leukocyte adhesion to endothelial cells, and suppressed TNF-α-induced VCAM-1 expression in the aortic endothelium of mice. In summary, since magnolol nanoparticles inhibit endothelial VCAM-1 expression and leukocyte adhesion to endothelial cells, this novel drug formulation may be a potentially useful therapeutic formulation to prevent the development of atherosclerosis and inflammatory diseases.
[Mh] Termos MeSH primário: Compostos de Bifenilo/administração & dosagem
Água Corporal/química
Células Endoteliais/efeitos dos fármacos
Células Endoteliais/metabolismo
Lignanas/administração & dosagem
Nanopartículas/administração & dosagem
Molécula 1 de Adesão de Célula Vascular/administração & dosagem
Molécula 1 de Adesão de Célula Vascular/metabolismo
[Mh] Termos MeSH secundário: Animais
Compostos de Bifenilo/química
Células Cultivadas
Regulação para Baixo/efeitos dos fármacos
Regulação para Baixo/fisiologia
Composição de Medicamentos/métodos
Seres Humanos
Lignanas/química
Camundongos
Camundongos Endogâmicos C57BL
Nanopartículas/química
Nanopartículas/ultraestrutura
Tamanho da Partícula
Solubilidade
Fator de Necrose Tumoral alfa
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Biphenyl Compounds); 0 (Lignans); 0 (Tumor Necrosis Factor-alpha); 0 (Vascular Cell Adhesion Molecule-1); 001E35HGVF (magnolol)
[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:180131
[St] Status:MEDLINE


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[PMID]:29372687
[Au] Autor:Stefaniková A; Klacanová K; Pilchová I; Hatok J; Racay P
[Ad] Endereço:1 Department of Medical Biochemistry Jessenius Faculty of Medicine in Martin, Comenius University in Bratislava, Martin, Slovakia. racay@jfmed.uniba.sk.
[Ti] Título:Cyclin-dependent kinase 2 inhibitor SU9516 increases sensitivity of colorectal carcinoma cells Caco-2 but not HT29 to BH3 mimetic ABT-737.
[So] Source:Gen Physiol Biophys;36(5):539-547, 2017 Dec.
[Is] ISSN:0231-5882
[Cp] País de publicação:Slovakia
[La] Idioma:eng
[Ab] Resumo:Colorectal carcinoma (CRC) that represents one of the major causes for cancer-related death in humans is often associated with over-expression of anti-apoptotic proteins of Bcl-2 family. The aim of presented study was to determine the effect of ABT-737 inhibitor of anti-apoptotic proteins Bcl-2, Bcl-XL and Bcl-w as well as cyclin-dependent kinase 2 (CDK2) inhibitor SU9516 alone and in combination with ABT-737 on survival of colorectal cell lines HT29 and Caco-2. We have shown that both Caco-2 and HT29 cells that are relatively resistant to ABT-737 are also partially sensitive to SU9516, which increased sensitivity of Caco-2 but not HT29 cells to ABT-737. Increased sensitivity of Caco-2 cells to ABT-737 after addition of SU9516 correlated well with SU9516-induced decrease of Mcl-1 expression while we have not observed downregulation of Mcl-1 after the treatment of HT29 cells with SU9516. Instead of this, we have shown that treatment of HT29 cells with SU9516 is associated with decreased expression of tumour suppressor protein p53. Our findings provide a rationale for clinical use of Bcl-2 family inhibitors in combination with CDK2 inhibitors for treatment of Mcl-1-dependent colorectal tumours associated with expression of Bcl-2, Bcl-XL and Bcl-w proteins. In addition, we have shown potential of CDK2 inhibitors for treatment of tumours expressing R273H mutant p53.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem
Compostos de Bifenilo/administração & dosagem
Neoplasias Colorretais/tratamento farmacológico
Neoplasias Colorretais/enzimologia
Quinase 2 Dependente de Ciclina/antagonistas & inibidores
Imidazóis/administração & dosagem
Indóis/administração & dosagem
Nitrofenóis/administração & dosagem
Sulfonamidas/administração & dosagem
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Proteína Agonista de Morte Celular de Domínio Interatuante com BH3/química
Compostos de Bifenilo/química
Células CACO-2
Sobrevivência Celular/efeitos dos fármacos
Neoplasias Colorretais/patologia
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Células HT29
Seres Humanos
Nitrofenóis/química
Piperazinas/administração & dosagem
Piperazinas/química
Sulfonamidas/química
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-737); 0 (BH3 Interacting Domain Death Agonist Protein); 0 (BID protein, human); 0 (Biphenyl Compounds); 0 (Imidazoles); 0 (Indoles); 0 (Nitrophenols); 0 (Piperazines); 0 (SU 9516); 0 (Sulfonamides); EC 2.7.11.22 (CDK2 protein, human); EC 2.7.11.22 (Cyclin-Dependent Kinase 2)
[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:180127
[St] Status:MEDLINE
[do] DOI:10.4149/gpb_2017030


  10 / 13832 MEDLINE  
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[PMID]:29394011
[Au] Autor:Saladino R; Chiocchini U; Botta G; Delfino M; Conigliaro R; Mosesso P
[Ti] Título:Free radical scavenging capacity and protective effect of natural substances in peloids from the thermal spring pool Bagnaccio (Viterbo, Italy).
[So] Source:J Cosmet Sci;67(2):71-92, 2016 Mar-Apr.
[Is] ISSN:1525-7886
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Natural peloids from sulfurous thermal springs are largely used in cosmetic and pelotherapy for the treatment of different dermatological conditions, including skin aging, dermatitis, and other eczemas. The beneficial effects are correlated to mineralogical and other thermal properties, as well as to the presence of natural substances with specific antioxidant activity. Few data are available for the comparison between natural peloids and synthetic (i.e., artificially maturated) muds. In this context, the natural substances and antioxidant activity of natural white mud (WM) and dark mud (DM) peloids from the sulfurous thermal spring pool Bagnaccio (Viterbo, Italy) have been studied in detail to evaluate possible relationships between physicochemical properties and therapeutic effect. A large panel of natural substances in WM and DM were characterized for the first time by ³¹P-nuclear magnetic resonance and gas chromatography associated to mass spectrometry analysis. Polar fractions of WM and DM peloids were characterized by the presence of several bioactive natural compounds, showing high antioxidant activity and DNA protective effect, as evaluated by 2,2-diphenyl-1-picrylhydrazyl assay, and hydrogen peroxide­induced DNA breakage in the alkaline comet assay. The antioxidant activity and DNA protective effect could be attributed to radical scavenging rather than a modulatory effect on the induced DNA repair, and are of order of intensity higher than that reported for synthetic muds.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Depuradores de Radicais Livres/farmacologia
Hidrocarbonetos Aromáticos/farmacologia
Fenóis/farmacologia
Terpenos/farmacologia
[Mh] Termos MeSH secundário: Alcaloides/química
Alcaloides/isolamento & purificação
Alcanos/química
Alcanos/isolamento & purificação
Alcanos/farmacologia
Alcenos/química
Alcenos/isolamento & purificação
Alcenos/farmacologia
Animais
Compostos de Bifenilo/antagonistas & inibidores
Compostos de Bifenilo/química
Células CHO
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Ensaio Cometa
Cricetulus
DNA/efeitos dos fármacos
Depuradores de Radicais Livres/química
Depuradores de Radicais Livres/isolamento & purificação
Fontes Termais
Seres Humanos
Hidrocarbonetos Aromáticos/química
Hidrocarbonetos Aromáticos/isolamento & purificação
Peróxido de Hidrogênio/antagonistas & inibidores
Peróxido de Hidrogênio/química
Itália
Espectroscopia de Ressonância Magnética
Camundongos
Terapia por Lama
Fenóis/química
Fenóis/isolamento & purificação
Picratos/antagonistas & inibidores
Picratos/química
Terpenos/química
Terpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Alkanes); 0 (Alkenes); 0 (Biphenyl Compounds); 0 (Free Radical Scavengers); 0 (Hydrocarbons, Aromatic); 0 (Phenols); 0 (Picrates); 0 (Terpenes); 9007-49-2 (DNA); BBX060AN9V (Hydrogen Peroxide); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180203
[St] Status:MEDLINE



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