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  1 / 459 MEDLINE  
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[PMID]:25868474
[Au] Autor:Maher S; Rasool S; Mehmood R; Perveen S; Tareen RB
[Ad] Endereço:a H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi , Karachi 75270 , Pakistan.
[Ti] Título:Trichosides A and B, new withanolide glucosides from Tricholepis eburnea.
[So] Source:Nat Prod Res;32(1):1-6, 2018 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Trichosides A (1) and B (2), new withanolide glucosides, have been isolated from the n-butanolic fraction of the 75% methanolic extract of aerial parts of Tricholepis eburnea. Their structures were elucidated through spectroscopic analysis including ESI-MS, 2D NMR and acid hydrolysis.
[Mh] Termos MeSH primário: Asteraceae/química
Glucosídeos/química
Vitanolídeos/química
[Mh] Termos MeSH secundário: Hidrólise
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glucosides); 0 (Withanolides)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150415
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2015.1030340


  2 / 459 MEDLINE  
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[PMID]:28923386
[Au] Autor:Llanos GG; Araujo LM; Jiménez IA; Moujir LM; Rodríguez J; Jiménez C; Bazzocchi IL
[Ad] Endereço:Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Instituto Canario de Investigación del Cáncer, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain.
[Ti] Título:Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers.
[So] Source:Eur J Med Chem;140:52-64, 2017 Nov 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Apoptosis inducers represent an attractive approach for the discovery and development of anticancer agents. Herein, we report on the development by molecular fine tuning of a withaferin A-based library of 63 compounds (2-64), 53 of them reported for the first time. Their antiproliferative evaluation on HeLa, A-549 and MCF-7 human tumor cell lines identified fifteen analogues displaying higher activity (IC values ranging 0.3-4.8 µM) than the lead (IC values ranging 1.3-10.1 µM) either in lag or log growth phases. SAR analysis revealed that acylation enhances cytotoxicity, suggesting the hydrophobic moiety contributes to the activity, presumably by increasing affinity and/or cell membrane permeability. Further investigation clearly indicated that compounds 3, 11, 12, and 18 induce apoptosis evidenced by chromatin condensation, phosphatidylserine externalization, and caspase-3 activation effects on HeLa cells. The potent capacity to induce apoptosis with concomitant cell loss in G2/M highlights the potential of 27-benzyl analogue (18) as an apoptotic inducer drug candidate.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia
Apoptose/efeitos dos fármacos
Desenho de Drogas
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/síntese química
Antineoplásicos Fitogênicos/química
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Células Cultivadas
Cercopithecus aethiops
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Folhas de Planta/química
Relação Estrutura-Atividade
Células Vero
Withania/química
Vitanolídeos/síntese química
Vitanolídeos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Withanolides); L6DO3QW4K5 (withaferin A)
[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


  3 / 459 MEDLINE  
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[PMID]:28774732
[Au] Autor:Ma T; Zhang Y; Zhang C; Luo JG; Kong LY
[Ad] Endereço:State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
[Ti] Título:Downregulation of TIGAR sensitizes the antitumor effect of physapubenolide through increasing intracellular ROS levels to trigger apoptosis and autophagosome formation in human breast carcinoma cells.
[So] Source:Biochem Pharmacol;143:90-106, 2017 Nov 01.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Physapubenolide (PB) is a cytotoxic withanolide isolated from Physalis angulata that was used as a traditional Chinese medicine. In this study, we investigated the role of TIGAR and ROS in PB-induced apoptosis and autophagosome formation in human breast carcinoma MDA-MB-231 and MCF-7 cells. PB induced apoptosis by decreasing mitochondrial membrane potential and elevating the Bax/Bcl-2 protein expression ratio in MDA-MB-231 and MCF-7 cells. Caspase inhibitor Z-VAD-FMK treatment partly blocked PB induced cytotoxicity, suggesting that apoptosis serves as an important role in the anti-proliferative effect of PB. Meanwhile, PB induced autophagosome formation, as characterized by increased acridine orange-stained positive cells, accumulation of punctate LC3B fluorescence and a greater number of autophagic vacuoles under electron microscopy. Furthermore, PB inhibited autophagic flux as reflected by the overlapping of mCherry and GFP fluorescence when MDA-MB-231 cells were transfected with GFP-mCherry-LC3 plasmid. Depletion of LC3B, ATG5 or ATG7 reduced PB-induced cytotoxicity, indicating that autophagosome associated cell death participated in the anti-cancer effect of PB. Moreover, PB-induced apoptosis and autophagosome formation were linked to the generation of intracellular ROS, and pre-treatment with the antioxidant NAC obviously mitigated the effects. Interestingly, PB treatment slightly increased TIGAR expression at low concentrations but decreased TIGAR expression drastically at high concentrations. Downregulation of TIGAR by small interfering RNA augmented low concentrations of PB-induced apoptosis and autophagosome formation, which contributed to the observed anti-cancer effect of PB and were reversed by NAC pre-treatment. Consistently, in MDA-MB-231 or MCF-7 xenograft mouse model, PB suppressed tumor growth through ROS induced apoptosis and autophagosome associated cell death accompanied with the downregulation of TIGAR. Taken together, these results indicate that downregulation of TIGAR increased PB-induced apoptosis and autophagosomes associated cell death through promoting ROS generation in MDA-MB-231 and MCF-7 cells.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia
Apoptose/efeitos dos fármacos
Autofagossomos/efeitos dos fármacos
Peptídeos e Proteínas de Sinalização Intracelular/genética
Espécies Reativas de Oxigênio/metabolismo
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/isolamento & purificação
Autofagia/efeitos dos fármacos
Neoplasias da Mama/metabolismo
Neoplasias da Mama/patologia
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Regulação para Baixo
Feminino
Citometria de Fluxo
Seres Humanos
Células MCF-7
Camundongos Endogâmicos BALB C
Camundongos Nus
Physalis/química
RNA Interferente Pequeno/genética
Ensaio Tumoral de Célula-Tronco
Vitanolídeos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (C12orf5 protein, human); 0 (Intracellular Signaling Peptides and Proteins); 0 (RNA, Small Interfering); 0 (Reactive Oxygen Species); 0 (Withanolides); 0 (physapubenolide)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170805
[St] Status:MEDLINE


  4 / 459 MEDLINE  
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[PMID]:28678390
[Au] Autor:Sheremet M; Kapoor S; Schröder P; Kumar K; Ziegler S; Waldmann H
[Ad] Endereço:Department of Chemical Biology, Max-Planck-Institut für Molekulare Physiologie, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
[Ti] Título:Small Molecules Inspired by the Natural Product Withanolides as Potent Inhibitors of Wnt Signaling.
[So] Source:Chembiochem;18(18):1797-1806, 2017 Sep 19.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Wnt signaling is a fundamental pathway that drives embryonic development and is essential for stem cell maintenance and tissue homeostasis. Dysregulation of Wnt signaling is linked to various diseases, and a constitutively active Wnt pathway drives tumorigenesis. Thus, disruption of the Wnt response is deemed a promising strategy for cancer drug discovery. However, only few clinical drug candidates that target Wnt signaling are available so far, and new small-molecule modulators of Wnt-related processes are in high demand. Here we describe the synthesis of small molecules inspired by withanolide natural products by using a pregnenolone-derived ß-lactone as the key intermediate that was transformed into a δ-lactone appended to the D-ring of the steroidal scaffold. This natural-product-inspired compound library contained potent inhibitors of Wnt signaling that act upstream of the destruction complex to stabilize Axin in a tankyrase-independent manner.
[Mh] Termos MeSH primário: Bibliotecas de Moléculas Pequenas/farmacologia
Vitanolídeos/química
Via de Sinalização Wnt/efeitos dos fármacos
[Mh] Termos MeSH secundário: Produtos Biológicos/química
Sobrevivência Celular/efeitos dos fármacos
Células HCT116
Células HEK293
Seres Humanos
Concentração Inibidora 50
Bibliotecas de Moléculas Pequenas/síntese química
Bibliotecas de Moléculas Pequenas/química
Relação Estrutura-Atividade
Vitanolídeos/síntese química
Vitanolídeos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biological Products); 0 (Small Molecule Libraries); 0 (Withanolides)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170706
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700260


  5 / 459 MEDLINE  
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[PMID]:28648460
[Au] Autor:Huang CY; Ahmed AF; Su JH; Sung PJ; Hwang TL; Chiang PL; Dai CF; Liaw CC; Sheu JH
[Ad] Endereço:Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 804, Taiwan.
[Ti] Título:Bioactive new withanolides from the cultured soft coral Sinularia brassica.
[So] Source:Bioorg Med Chem Lett;27(15):3267-3271, 2017 08 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Continuing study of the ethyl acetate (EtOAc) extract of the cultured soft coral Sinularia brassica afforded five new withanolides, sinubrasolides H-L (1-5). The structures of the new compounds were elucidated on the basis of spectroscopic analysis. The cytotoxicities of new compounds 1-5 and a known compound sinubrasolide A (6) against the proliferation of a limited panel of cancer cell lines were assayed. The anti-inflammatory activities of compounds 1-6 were evaluated by measuring their ability to suppress N-formyl-methionyl-leucyl-phenyl-alanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release in human neutrophils.
[Mh] Termos MeSH primário: Antozoários/química
Anti-Inflamatórios/química
Anti-Inflamatórios/farmacologia
Antineoplásicos/química
Antineoplásicos/farmacologia
Vitanolídeos/química
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/isolamento & purificação
Antineoplásicos/isolamento & purificação
Linhagem Celular Tumoral
Citocalasina B/imunologia
Seres Humanos
Modelos Moleculares
Neoplasias/tratamento farmacológico
Neutrófilos/efeitos dos fármacos
Elastase Pancreática/imunologia
Superóxidos/imunologia
Vitanolídeos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antineoplastic Agents); 0 (Withanolides); 11062-77-4 (Superoxides); 3CHI920QS7 (Cytochalasin B); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170627
[St] Status:MEDLINE


  6 / 459 MEDLINE  
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[PMID]:28617942
[Au] Autor:Su Y; Wang Q; Yang B; Wu L; Cheng G; Kuang H
[Ad] Endereço:Key Laboratory of Chinese Material Medica, Department of Pharmacology, Heilongjiang University of Chinese Medicine, Harbin, China.
[Ti] Título:Withasteroid B from D. metel L. regulates immune responses by modulating the JAK/STAT pathway and the IL-17 RORγt /IL-10 FoxP3 ratio.
[So] Source:Clin Exp Immunol;190(1):40-53, 2017 Oct.
[Is] ISSN:1365-2249
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Datura metel L. is a medicinal herb that contains withasteroids and has a wide range of biological activities. We isolated seven withasteroids from the flowers of D. metel L and examined their ability to inhibit immune responses in vitro and in vivo. Among the withasteroids, withasteroid B2 exhibited the strongest inhibitory effect on immune responses comparing B2 with other isolated compounds from D. metel L., including suppressing the differentiation of CD4 T cells by inhibiting the expression and production of T cell lineage-specific master regulators and cytokines and directly suppressing the cytokine-induced Janus kinase/signal transducer and activator of transcription (JAK/STAT) signalling pathways. In the interleukin (IL)-23-induced mouse ear model of skin disease, B2 repressed disease development by inhibiting the expression of proinflammatory mediators in murine ear skin. Moreover, B2 affected the maturation of dendritic cells (DCs) in vitro which, in turn, induced T cell differentiation with an increased regulatory T cell (T ) phenotype and decreased T helper type 17 (Th17) phenotype. This study provides new evidence that B2 might ameliorate chronic inflammatory skin diseases by suppressing pathogenic CD4 T cell differentiation and the IL-17 retinoic-acid-receptor-related orphan receptor gamma t (RORγt) /IL-10 forkhead box protein 3 (FoxP3) ratio. These findings suggest that B2 might mediate the therapeutic effects observed in psoriasis patients following treatment with D. metel L.
[Mh] Termos MeSH primário: Imunossupressores/uso terapêutico
Psoríase/tratamento farmacológico
Pele/efeitos dos fármacos
Linfócitos T Reguladores/efeitos dos fármacos
Células Th17/efeitos dos fármacos
Vitanolídeos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Diferenciação Celular
Células Cultivadas
Datura metel/imunologia
Modelos Animais de Doenças
Fatores de Transcrição Forkhead/metabolismo
Seres Humanos
Imunomodulação
Interleucina-10/metabolismo
Interleucina-17/metabolismo
Interleucina-23/imunologia
Janus Quinases/metabolismo
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Endogâmicos C57BL
Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares/metabolismo
Psoríase/imunologia
Fatores de Transcrição STAT/metabolismo
Transdução de Sinais/efeitos dos fármacos
Pele/patologia
Linfócitos T Reguladores/imunologia
Células Th17/imunologia
Vitanolídeos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Forkhead Transcription Factors); 0 (Foxp3 protein, mouse); 0 (Immunosuppressive Agents); 0 (Interleukin-17); 0 (Interleukin-23); 0 (Nuclear Receptor Subfamily 1, Group F, Member 3); 0 (STAT Transcription Factors); 0 (Withanolides); 0 (withasteroid B); 130068-27-8 (Interleukin-10); EC 2.7.10.2 (Janus Kinases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170616
[St] Status:MEDLINE
[do] DOI:10.1111/cei.12998


  7 / 459 MEDLINE  
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[PMID]:28617598
[Au] Autor:Xu YM; Wijeratne EMK; Babyak AL; Marks HR; Brooks AD; Tewary P; Xuan LJ; Wang WQ; Sayers TJ; Gunatilaka AAL
[Ad] Endereço:Natural Products Center, School of Natural Resources and the Environment, College of Agriculture and Life Sciences, University of Arizona , 250 E. Valencia Road, Tucson, Arizona 85706, United States.
[Ti] Título:Withanolides from Aeroponically Grown Physalis peruviana and Their Selective Cytotoxicity to Prostate Cancer and Renal Carcinoma Cells.
[So] Source:J Nat Prod;80(7):1981-1991, 2017 Jul 28.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Investigation of aeroponically grown Physalis peruviana resulted in the isolation of 11 new withanolides, including perulactones I-L (1-4), 17-deoxy-23ß-hydroxywithanolide E (5), 23ß-hydroxywithanolide E (6), 4-deoxyphyperunolide A (7), 7ß-hydroxywithanolide F (8), 7ß-hydroxy-17-epi-withanolide K (9), 24,25-dihydro-23ß,28-dihydroxywithanolide G (10), and 24,25-dihydrowithanolide E (11), together with 14 known withanolides (12-25). The structures of 1-11 were elucidated by the analysis of their spectroscopic data, and 12-25 were identified by comparison of their spectroscopic data with those reported. All withanolides were evaluated for their cytotoxic activity against a panel of tumor cell lines including LNCaP (androgen-sensitive human prostate adenocarcinoma), 22Rv1 (androgen-resistant human prostate adenocarcinoma), ACHN (human renal adenocarcinoma), M14 (human melanoma), SK-MEL-28 (human melanoma), and normal human foreskin fibroblast cells. Of these, the 17ß-hydroxywithanolides (17-BHWs) 6, 8, 9, 11-13, 15, and 19-22 showed selective cytotoxic activity against the two prostate cancer cell lines LNCaP and 22Rv1, whereas 13 and 20 exhibited selective toxicity for the ACHN renal carcinoma cell line. These cytotoxicity data provide additional structure-activity relationship information for the 17-BHWs.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/farmacologia
Neoplasias Renais/tratamento farmacológico
Physalis/química
Neoplasias da Próstata/tratamento farmacológico
Vitanolídeos/isolamento & purificação
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Masculino
Melanoma/tratamento farmacológico
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Physalis/crescimento & desenvolvimento
Relação Estrutura-Atividade
Vitanolídeos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Withanolides)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170616
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b01129


  8 / 459 MEDLINE  
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[PMID]:28573248
[Au] Autor:Hou WC; Miao XH; Ma LJ; Bai XX; Liu Q; Song L
[Ad] Endereço:Department of Neurology, The First Hospital of Jilin University, Changchun 130021, China.
[Ti] Título:WITHAFERIN A INDUCES APOPTOSIS IN RAT C6 GLIOMA CELLS THROUGH REGULATING NF-KB NUCLEAR TRANSLOCATION AND ACTIVATION OF CASPASE CASCADE.
[So] Source:Afr J Tradit Complement Altern Med;14(2):319-324, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The demand for the chemopreventive drug from the plant source is increasing in recent times, owing to its various biological activities without any adverse effect. The intention of this current study was to examine the anti-glioma effect of Withaferin A (WFA) on C6 glioma cell line model. MATERIALS AND METHODS: C6 glioma cells were administrated with different concentration of WFA (50, 100, 200 and 500 µg/mL) and DMSO (control) group to examine its anti-proliferative, anti-inflammatory and pro-apoptotic activities. RESULTS: Treatment with WFA showed a significant decline in the glioma cell count in a dose-dependent manner and thus proving its anti-proliferative effect. Similarly, inflammatory markers were also substantially lowered upon treatment with different concentration of WFA. However, DNA fragmentation and apoptotic markers like Caspase-3 and 9 were concomitantly enhanced after co-cultured with different concentration of WFA and thus exhibiting its cytotoxicity efficacy. Furthermore, the protein expression of Bcl2 and Bax were markedly downregulated and upregulated respectively; upon treatment with WFA on C6 glioma cells. CONCLUSION: The outcome of this study evidently demonstrates that C6 glioma cells co-cultured with increased concentration of WFA, showed an anti-proliferative, anti-inflammatory and pro-apoptotic effect in a dose-dependent fashion.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/uso terapêutico
Apoptose
Caspases/metabolismo
Glioma/tratamento farmacológico
NF-kappa B/metabolismo
Fitoterapia
Vitanolídeos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/farmacologia
Transporte Biológico
Linhagem Celular Tumoral
Proliferação Celular
Fragmentação do DNA/efeitos dos fármacos
Ativação Enzimática
Glioma/metabolismo
Inflamação/etiologia
Inflamação/prevenção & controle
Extratos Vegetais/farmacologia
Extratos Vegetais/uso terapêutico
Proteínas Proto-Oncogênicas c-bcl-2/metabolismo
Ratos
Withania/química
Vitanolídeos/farmacologia
Proteína X Associada a bcl-2/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Bax protein, rat); 0 (Bcl2 protein, rat); 0 (NF-kappa B); 0 (Plant Extracts); 0 (Proto-Oncogene Proteins c-bcl-2); 0 (Withanolides); 0 (bcl-2-Associated X Protein); EC 3.4.22.- (Caspases); L6DO3QW4K5 (withaferin A)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170816
[Lr] Data última revisão:
170816
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i2.33


  9 / 459 MEDLINE  
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[PMID]:28476645
[Au] Autor:Falkenberg KD; Jakobs A; Matern JC; Dörner W; Uttarkar S; Trentmann A; Steinmann S; Coulibaly A; Schomburg C; Mootz HD; Schmidt TJ; Klempnauer KH
[Ad] Endereço:Institute for Biochemistry, Westfälische-Wilhelms-Universität, D-48149 Münster, Germany.
[Ti] Título:Withaferin A, a natural compound with anti-tumor activity, is a potent inhibitor of transcription factor C/EBPß.
[So] Source:Biochim Biophys Acta;1864(7):1349-1358, 2017 07.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Recent work has shown that deregulation of the transcription factor Myb contributes to the development of leukemia and several other human cancers, making Myb and its cooperation partners attractive targets for drug development. By employing a myeloid Myb-reporter cell line we have identified Withaferin A (WFA), a natural compound that exhibits anti-tumor activities, as an inhibitor of Myb-dependent transcription. Analysis of the inhibitory mechanism of WFA showed that WFA is a significantly more potent inhibitor of C/EBPß, a transcription factor cooperating with Myb in myeloid cells, than of Myb itself. We show that WFA covalently modifies specific cysteine residues of C/EBPß, resulting in the disruption of the interaction of C/EBPß with the co-activator p300. Our work identifies C/EBPß as a novel direct target of WFA and highlights the role of p300 as a crucial co-activator of C/EBPß. The finding that WFA is a potent inhibitor of C/EBPß suggests that inhibition of C/EBPß might contribute to the biological activities of WFA.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Proteína beta Intensificadora de Ligação a CCAAT/antagonistas & inibidores
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Células 3T3
Animais
Sítios de Ligação
Proteína beta Intensificadora de Ligação a CCAAT/química
Linhagem Celular Tumoral
Seres Humanos
Camundongos
Ligação Proteica
Fatores de Transcrição de p300-CBP/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (CCAAT-Enhancer-Binding Protein-beta); 0 (Withanolides); EC 2.3.1.48 (p300-CBP Transcription Factors); L6DO3QW4K5 (withaferin A)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170507
[St] Status:MEDLINE


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[PMID]:28445002
[Au] Autor:Kunimasa K; Nagano T; Shimono Y; Dokuni R; Kiriu T; Tokunaga S; Tamura D; Yamamoto M; Tachihara M; Kobayashi K; Satouchi M; Nishimura Y
[Ad] Endereço:Division of Respiratory Medicine, Kobe University Graduate School of Medicine, Kobe, Japan.
[Ti] Título:Glucose metabolism-targeted therapy and withaferin A are effective for epidermal growth factor receptor tyrosine kinase inhibitor-induced drug-tolerant persisters.
[So] Source:Cancer Sci;108(7):1368-1377, 2017 Jul.
[Is] ISSN:1349-7006
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In pathway-targeted cancer drug therapies, the relatively rapid emergence of drug-tolerant persisters (DTPs) substantially limits the overall therapeutic benefit. However, little is known about the roles of DTPs in drug resistance. In this study, we investigated the features of epidermal growth factor receptor-tyrosine kinase inhibitor-induced DTPs and explored a new treatment strategy to overcome the emergence of these DTPs. We used two EGFR-mutated lung adenocarcinoma cell lines, PC9 and II-18. They were treated with 2 µM gefitinib for 6, 12, or 24 days or 6 months. We analyzed the mRNA expression of the stem cell-related markers by quantitative RT-PCR and the expression of the cellular senescence-associated proteins. Then we sorted DTPs according to the expression pattern of CD133 and analyzed the features of sorted cells. Finally, we tried to ablate DTPs by glucose metabolism targeting therapies and a stem-like cell targeting drug, withaferin A. Drug-tolerant persisters were composed of at least two types of cells, one with the properties of cancer stem-like cells (CSCs) and the other with the properties of therapy-induced senescent (TIS) cells. The CD133 cell population had CSC properties and the CD133 cell population had TIS properties. The CD133 cell population containing TIS cells showed a senescence-associated secretory phenotype that supported the emergence of the CD133 cell population containing CSCs. Glucose metabolism inhibitors effectively eliminated the CD133 cell population. Withaferin A effectively eliminated the CD133 cell population. The combination of phloretin and withaferin A effectively suppressed gefitinib-resistant tumor growth.
[Mh] Termos MeSH primário: Resistência a Medicamentos Antineoplásicos/fisiologia
Células-Tronco Neoplásicas/efeitos dos fármacos
Floretina/farmacologia
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Adenocarcinoma
Animais
Western Blotting
Carcinoma Pulmonar de Células não Pequenas
Linhagem Celular Tumoral
Senescência Celular/efeitos dos fármacos
Citometria de Fluxo
Glucose/metabolismo
Seres Humanos
Neoplasias Pulmonares
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Terapia de Alvo Molecular/métodos
Células-Tronco Neoplásicas/patologia
Reação em Cadeia da Polimerase
Inibidores de Proteínas Quinases/farmacologia
Quinazolinas/farmacologia
Receptor do Fator de Crescimento Epidérmico/antagonistas & inibidores
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Protein Kinase Inhibitors); 0 (Quinazolines); 0 (Withanolides); EC 2.7.10.1 (EGFR protein, human); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); IY9XDZ35W2 (Glucose); L6DO3QW4K5 (withaferin A); S5J5OE47MK (Phloretin); S65743JHBS (gefitinib)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170427
[St] Status:MEDLINE
[do] DOI:10.1111/cas.13266



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