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[PMID]:28452903
[Au] Autor:Maschio M; Dinapoli L; Zarabla A; Maialetti A; Giannarelli D; Fabi A; Vidiri A; Cantelmi T
[Ad] Endereço:*Center for Tumor-Related Epilepsy, UOSD Neurology, †Biostatistic Unit, Departments of ‡Oncology, §Radiology, and ∥Service of Psychiatry, Regina Elena National Cancer Institute, Rome, Italy.
[Ti] Título:Zonisamide in Brain Tumor-Related Epilepsy: An Observational Pilot Study.
[So] Source:Clin Neuropharmacol;40(3):113-119, 2017 May/Jun.
[Is] ISSN:1537-162X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Epilepsy heavily affects the quality of life (QoL) of patients with brain tumor because in addition to taking treatments for the oncological illness, patients are required to live with the long-term taking of antiepileptic drugs (AEDs). The AEDs' adverse effects are common in these patients and can negatively influence their perceptions of their QoL.We conducted an observational pilot study in patients with brain tumor-related epilepsy to verify efficacy, tolerability, and impact on QoL and global neurocognitive performances of zonisamide (ZNS) in add-on. MATERIALS AND METHODS: We recruited 13 patients (5 females, 8 males; mean age, 49.6 years) presenting uncontrolled seizures. At first visit and at final follow-up at 6 months, patients underwent neurological examination, evaluation of adverse events, and cognitive and QoL tests. A seizure diary was given. RESULTS: Eight patients underwent chemotherapy, 3 underwent radiotherapy, and 5 had disease progression. Mean dosage of ZNS at final follow-up was 300 mg/d.Of 9 patients who reached the sixth month follow-up, the mean weekly seizure number before ZNS had been 3.2 ± 5.0, and at final follow-up, the mean weekly seizure number was 0.18 ± 0.41 (P = 0.05).Compared with baseline, we observed stability in all cognitive domains, except for verbal fluency that significantly worsened.Results on QoL tests showed that QoL remained unchanged over time, which could indicate that ZNS did not influence the patients' perceived QoL. CONCLUSIONS: Zonisamide as add-on in our patients seems to be well tolerated and efficacious in controlling seizures. Despite having limitations represented by the fact that our study is observational, with a small study population and a short follow-up period, our results confirm that when choosing an AED, in addition to efficacy, the drug's effect on patients' QoL also needs to be considered, especially for patients facing many psychosocial challenges, such as those with brain tumor-related epilepsy.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Neoplasias Encefálicas/fisiopatologia
Disfunção Cognitiva/prevenção & controle
Epilepsia/tratamento farmacológico
Isoxazóis/uso terapêutico
Nootrópicos/uso terapêutico
Qualidade de Vida
[Mh] Termos MeSH secundário: Antineoplásicos/efeitos adversos
Antineoplásicos/uso terapêutico
Neoplasias Encefálicas/tratamento farmacológico
Neoplasias Encefálicas/radioterapia
Disfunção Cognitiva/induzido quimicamente
Disfunção Cognitiva/etiologia
Disfunção Cognitiva/fisiopatologia
Terapia Combinada/efeitos adversos
Resistência a Medicamentos
Quimioterapia Combinada/efeitos adversos
Epilepsia/induzido quimicamente
Epilepsia/etiologia
Epilepsia/fisiopatologia
Feminino
Seguimentos
Seres Humanos
Itália
Transtornos da Linguagem/induzido quimicamente
Transtornos da Linguagem/etiologia
Transtornos da Linguagem/fisiopatologia
Transtornos da Linguagem/prevenção & controle
Masculino
Meia-Idade
Projetos Piloto
Radioterapia/efeitos adversos
Índice de Gravidade de Doença
Comportamento Verbal/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Antineoplastic Agents); 0 (Isoxazoles); 0 (Nootropic Agents); 459384H98V (zonisamide)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.1097/WNF.0000000000000218


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[PMID]:28460477
[Au] Autor:Park E; Kim D; Lee SM; Jun HS
[Ad] Endereço:Lee Gil Ya Cancer and Diabetes Institute, Gachon University, Incheon, Republic of Korea.
[Ti] Título:Inhibition of lysophosphatidic acid receptor ameliorates Sjögren's syndrome in NOD mice.
[So] Source:Oncotarget;8(16):27240-27251, 2017 Apr 18.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Lysophosphatidic acid (LPA), a bioactive lysophospholipid, is involved in the pathogenesis of chronic inflammatory and autoimmune diseases. In this study, we investigated the role of LPA/LPA receptor (LPAR) signaling in the pathogenesis of Sjögren's syndrome (SS). We found that autotaxin, an LPA producing enzyme, and LPAR1 and LPAR3 mRNA, and IL-17 mRNA were highly expressed in the exocrine glands of 20-week-old nonobese diabetic (NOD) mice, which show SS symptoms at this age, as compared with non-symptomatic 8-week-old NOD mice. In an adoptive transfer model using NOD lymphocytes, treatment with Ki16425, an LPAR1/3 antagonist, restored tear and saliva secretion and decreased symptoms of SS compared with the vehicle-treated group. IL-17 levels in serum and lacrimal glands were also significantly reduced by Ki16425 in recipient mice. In addition, Ki16425 treatment of 20-week-old NOD mice, which spontaneously developed SS, restored saliva volume. Treatment of NOD splenocytes with LPA induced the expression of IL-17 in a dose-dependent manner, and Ki16425 inhibited this increase. LPA stimulated the activation of ROCK2 and p38 MAPK; and inhibition of ROCK2 or p38 MAPK suppressed LPA-induced IL-17 expression. Our data suggest that LPAR signaling stimulates SS development by induction of IL-17 production via ROCK and p38 MAPK pathways. Thus, LPAR inhibition could be a possible therapeutic strategy for SS.
[Mh] Termos MeSH primário: Receptores de Ácidos Lisofosfatídicos/antagonistas & inibidores
Receptores de Ácidos Lisofosfatídicos/metabolismo
Síndrome de Sjogren/metabolismo
[Mh] Termos MeSH secundário: Animais
Autoanticorpos/sangue
Autoanticorpos/imunologia
Citocinas/genética
Citocinas/metabolismo
Modelos Animais de Doenças
Feminino
Expressão Gênica
Imunoterapia Adotiva
Mediadores da Inflamação/metabolismo
Interleucina-17/sangue
Interleucina-17/metabolismo
Isoxazóis/farmacologia
Aparelho Lacrimal/imunologia
Aparelho Lacrimal/metabolismo
Aparelho Lacrimal/patologia
Masculino
Camundongos
Camundongos Endogâmicos NOD
Diester Fosfórico Hidrolases/genética
Diester Fosfórico Hidrolases/metabolismo
Propionatos/farmacologia
Receptores de Ácidos Lisofosfatídicos/genética
Saliva/metabolismo
Transdução de Sinais/efeitos dos fármacos
Síndrome de Sjogren/genética
Síndrome de Sjogren/imunologia
Síndrome de Sjogren/terapia
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
Quinases Associadas a rho/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl amino)-3-methyl-5-isoxazolyl) benzylsulfanyl) propanoic acid); 0 (Autoantibodies); 0 (Cytokines); 0 (Inflammation Mediators); 0 (Interleukin-17); 0 (Isoxazoles); 0 (Propionates); 0 (Receptors, Lysophosphatidic Acid); EC 2.7.11.1 (Rock2 protein, mouse); EC 2.7.11.1 (rho-Associated Kinases); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); EC 3.1.4.- (Phosphoric Diester Hydrolases); EC 3.1.4.39 (alkylglycerophosphoethanolamine phosphodiesterase)
[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:170503
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.15916


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[PMID]:29357281
[Au] Autor:Zhang C; Chu M
[Ad] Endereço:Department of Urology, The Second Affiliated Hospital, Harbin Medical University, 246 Xuefu St., Nan Gang District, Harbin, China.
[Ti] Título:Leflunomide: A promising drug with good antitumor potential.
[So] Source:Biochem Biophys Res Commun;496(2):726-730, 2018 02 05.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Leflunomide, an inhibitor of dihydroorotase dehydrogenase and thereby pyrimidine synthesis, was approved for treatment of rheumatoid arthritis in 1998. During the following years, leflunomide was used in various preclinical studies as a potential cancer treatment; at the same time, more mechanisms underlying the anticancer effect of leflunomide were identified. Thus, leflunomide has been identified as a potent anticancer drug. This article summarizes the mechanisms as well as results of leflunomide in the evolving field of cancer therapy.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Isoxazóis/uso terapêutico
Neoplasias/tratamento farmacológico
[Mh] Termos MeSH secundário: Inibidores da Angiogênese/farmacologia
Inibidores da Angiogênese/uso terapêutico
Animais
Anti-Inflamatórios não Esteroides/farmacologia
Anti-Inflamatórios não Esteroides/uso terapêutico
Antineoplásicos/farmacologia
Inibidores Enzimáticos/farmacologia
Inibidores Enzimáticos/uso terapêutico
Seres Humanos
Fatores Imunológicos/farmacologia
Fatores Imunológicos/uso terapêutico
Isoxazóis/farmacologia
Neoplasias/patologia
Células-Tronco Neoplásicas/efeitos dos fármacos
Células-Tronco Neoplásicas/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Angiogenesis Inhibitors); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 0 (Enzyme Inhibitors); 0 (Immunologic Factors); 0 (Isoxazoles); G162GK9U4W (leflunomide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180123
[St] Status:MEDLINE


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[PMID]:28923341
[Au] Autor:Jia ZQ; Liu D; Sheng CW; Casida JE; Wang C; Song PP; Chen YM; Han ZJ; Zhao CQ
[Ad] Endereço:Education Ministry Key Laboratory of Integrated Management of Crop Diseases and Pests, College of Plant Protection, Nanjing Agricultural University, Nanjing, 210095, China.
[Ti] Título:Acute toxicity, bioconcentration, elimination and antioxidant effects of fluralaner in zebrafish, Danio rerio.
[So] Source:Environ Pollut;232:183-190, 2018 Jan.
[Is] ISSN:1873-6424
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Fluralaner is a novel isoxazoline insecticide which shows high insecticidal activity against parasitic, sanitary and agricultural pests, but there is little information about the effect of fluralaner on non-target organisms. This study reports the acute toxicity, bioconcentration, elimination and antioxidant response of fluralaner in zebrafish. All LC values of fluralaner to zebrafish were higher than 10 mg L at 24, 48, 72 and 96 h. To study the bioconcentration and elimination, the zebrafish were exposed to sub-lethal concentrations of fluralaner (2.00 and 0.20 mg L ) for 15 d and then held 6 d in clean water. The results showed medium BCF of fluralaner with values of 12.06 (48 h) and 21.34 (144 h) after exposure to 2.00 and 0.20 mg L fluralaner, respectively. In the elimination process, a concentration of only 0.113 mg kg was found in zebrafish on the 6th day after removal to clean water. After exposure in 2.00 mg L fluralaner, the enzyme activities of SOD, CAT, and GST, GSH-PX, CarE and content of MDA were measured. Only CAT and CarE activities were significantly regulated and the others stayed at a stable level compared to the control group. Meanwhile, transcriptional expression of CYP1C2, CYP1D1, CYP11A were significantly down-regulated at 12 h exposed to 2.00 mg L of fluralaner. Except CYP1D1, others CYPs were up-regulated at different time during exposure periods. Fluralaner and its formulated product (BRAVECTO ) are of low toxicity to zebrafish and are rapidly concentrated in zebrafish and eliminated after exposure in clean water. Antioxidant defense and metabolic systems were involved in the fluralaner-induced toxicity. Among them, the activities of CAT and CarE, and most mRNA expression level of CYPs showed fast response to the sub-lethal concentration of fluralaner, which could be used as a biomarker relevant to the toxicity.
[Mh] Termos MeSH primário: Inseticidas/toxicidade
Isoxazóis/toxicidade
Poluentes Químicos da Água/toxicidade
Peixe-Zebra/fisiologia
[Mh] Termos MeSH secundário: Animais
Antioxidantes/metabolismo
Biomarcadores/metabolismo
Catalase/metabolismo
Sistema Enzimático do Citocromo P-450/metabolismo
Glutationa Transferase/metabolismo
Superóxido Dismutase/metabolismo
Testes de Toxicidade Aguda
Peixe-Zebra/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (A1443 compound); 0 (Antioxidants); 0 (Biomarkers); 0 (Insecticides); 0 (Isoxazoles); 0 (Water Pollutants, Chemical); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 1.11.1.6 (Catalase); EC 1.15.1.1 (Superoxide Dismutase); EC 2.5.1.18 (Glutathione Transferase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180209
[Lr] Data última revisão:
180209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170920
[St] Status:MEDLINE


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[PMID]:29322271
[Au] Autor:Stenert C; de Mello ÍCMF; Pires MM; Knauth DS; Katayama N; Maltchik L
[Ad] Endereço:Laboratory of Ecology and Conservation of Aquatic Ecosystems, UNISINOS, Unisinos Avenue, 950, São Leopoldo, RS, 93.022-750, Brazil. cstenert@unisinos.br.
[Ti] Título:Responses of macroinvertebrate communities to pesticide application in irrigated rice fields.
[So] Source:Environ Monit Assess;190(2):74, 2018 Jan 10.
[Is] ISSN:1573-2959
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The ability to recover to original states after disturbances makes macroinvertebrates useful tools for assessing the impacts of pesticides. Many studies showed that direct exposure to pesticides decreases macroinvertebrate richness and alters their composition. The main objective of this study was to assess recovery patterns in macroinvertebrate communities after pesticide application in irrigated rice fields. We analyzed short-term temporal dynamics of macroinvertebrate communities after application of the herbicides bispyribac-sodium and clomazone and the insecticide chlorantraniliprole, over the rice-growing season in southern Brazil. We selected three conventional rice fields and the recovery of macroinvertebrate communities was also compared with three adjacent natural ponds. The study was developed from November 2011 to February 2012 (rice-growing season). Five macroinvertebrate collections were carried out 3, 7, 14, 38, and 60 days after pesticide application (November 25). Rice fields showed lower richness and abundance than ponds in the period immediately after pesticide application, and recovery rates in the richness of macroinvertebrate communities were more conspicuous as pesticide residuals dissipated from the fields. Macroinvertebrate community structure in rice fields also became more similar to natural ponds as pesticide traces were scarcer. However, macroinvertebrate abundance patterns were not related to pesticide concentrations in the fields. Our results supported the general hypothesis on the negative effects of pesticide application on macroinvertebrate community in irrigated rice fields, although other environmental features (e.g., length of the flooded period) also contributed to explain temporal dynamics in the macroinvertebrate communities from irrigated rice fields.
[Mh] Termos MeSH primário: Irrigação Agrícola
Herbicidas/toxicidade
Inseticidas/toxicidade
Invertebrados/efeitos dos fármacos
Oryza
[Mh] Termos MeSH secundário: Animais
Benzoatos/análise
Benzoatos/toxicidade
Monitoramento Ambiental/métodos
Herbicidas/análise
Inseticidas/análise
Isoxazóis/análise
Isoxazóis/toxicidade
Oxazolidinonas/análise
Oxazolidinonas/toxicidade
Pirimidinas/análise
Pirimidinas/toxicidade
ortoaminobenzoatos/análise
ortoaminobenzoatos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Herbicides); 0 (Insecticides); 0 (Isoxazoles); 0 (Oxazolidinones); 0 (Pyrimidines); 0 (ortho-Aminobenzoates); 570RAC03NF (clomazone); 622AK9DH9G (chlorantranilipole); 9W20BD966G (bispyribac)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180129
[Lr] Data última revisão:
180129
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1007/s10661-017-6425-1


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[PMID]:29207341
[Au] Autor:Varrica MG; Zagni C; Mineo PG; Floresta G; Monciino G; Pistarà V; Abbadessa A; Nicosia A; Castilho RM; Amata E; Rescifina A
[Ad] Endereço:Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125, Catania, Italy.
[Ti] Título:DNA intercalators based on (1,10-phenanthrolin-2-yl)isoxazolidin-5-yl core with better growth inhibition and selectivity than cisplatin upon head and neck squamous cells carcinoma.
[So] Source:Eur J Med Chem;143:583-590, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:((3RS,5SR)- and ((3RS,5RS)-2-(2-methoxybenzyl)-3-(1,10-phenanthrolin-2-yl)isoxazolidin-5-yl)methanol have been synthesized, according to 1,3-dipolar cycloaddition methodology, as DNA intercalating agents and evaluated for their anticancer activity against human cervical carcinoma HeLa and head and neck squamous cells carcinoma cell lines. The synthesized compounds exhibited good cytotoxic activity with IC better than cisplatin, used as the main and effective treatment for HNSCC, and a 24.3-72.0-fold selectivity respect to the 184B5 non-cancerous immortalized breast epithelial cell lines. Unwinding assay, circular dichroism data, and Uv-vis melting experiments confirmed that these compounds act as DNA intercalators with a binding constant in the order of 10 M . Docking studies showed that both compounds can interact as intercalating agent with both poly-d(AT) and poly-d(GC) , preferring an entrance by the minor groove of the poly-d(AT) .
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carcinoma de Células Escamosas/tratamento farmacológico
Cisplatino/farmacologia
DNA de Neoplasias/efeitos dos fármacos
Neoplasias de Cabeça e Pescoço/tratamento farmacológico
Substâncias Intercalantes/farmacologia
Isoxazóis/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Carcinoma de Células Escamosas/patologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Cisplatino/química
DNA de Neoplasias/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Neoplasias de Cabeça e Pescoço/patologia
Seres Humanos
Substâncias Intercalantes/síntese química
Substâncias Intercalantes/química
Isoxazóis/síntese química
Isoxazóis/química
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(2-methoxybenzyl)-3-(1,10-phenanthrolin-2-yl)isoxazolidin-5-yl)methanol); 0 (Antineoplastic Agents); 0 (DNA, Neoplasm); 0 (Intercalating Agents); 0 (Isoxazoles); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180110
[Lr] Data última revisão:
180110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171206
[St] Status:MEDLINE


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[PMID]:29227929
[Au] Autor:Sowmya DV; Lakshmi Teja G; Padmaja A; Kamala Prasad V; Padmavathi V
[Ad] Endereço:Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.
[Ti] Título:Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity.
[So] Source:Eur J Med Chem;143:891-898, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A variety of N-((1,3-diphenyl-5-aryl-1H-pyrazol-4-yl)sulfonyl)thiophene-2-carboxamides (7) and N-((5-aryl-3-phenylisoxazol-4-yl)sulfonyl)thiophene-2-carboxamides (8) were prepared from (E)-N-(arylethenesulfonyl)thiophene-2-carboxamides (4) adopting 1,3-dipolar cycloaddition of nitrile imines and nitrile oxides generated from araldehyde phenylhydrazones and araldoximes in the presence of iodosobenzene and CTAB followed by oxidation with I in DMSO. The compounds 4f, 7e, 7f, 8e and 8f showed potential antibacterial activity against B. subtilis whereas 8e and 8f exhibited potential antifungal activity against A. niger.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antifúngicos/farmacologia
Aspergillus niger/efeitos dos fármacos
Bacillus subtilis/efeitos dos fármacos
Isoxazóis/farmacologia
Pirazóis/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antifúngicos/síntese química
Antifúngicos/química
Reação de Cicloadição
Relação Dose-Resposta a Droga
Isoxazóis/química
Testes de Sensibilidade Microbiana
Estrutura Molecular
Pirazóis/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Isoxazoles); 0 (Pyrazoles)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE


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[PMID]:29050931
[Au] Autor:Jiang L; Zhang W; Li W; Ling C; Jiang M
[Ad] Endereço:Department of Respiratory Diseases, The First Affiliated Hospital of Soochow University, 215006, China.
[Ti] Título:Anti-inflammatory drug, leflunomide and its metabolite teriflunomide inhibit NSCLC proliferation in vivo and in vitro.
[So] Source:Toxicol Lett;282:154-165, 2018 Jan 05.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Lung cancer causes more than 150000 deaths annually in the United States alone, of which non-small cell lung cancer (NSCLC) accounts for 80%. Our studies demonstrated that NSCLC cells were sensitive to leflunomide and its metabolite teriflunomide, a FDA approved drug, which was a well-known immunomodulatory drug for relapsing multiple sclerosis (MS). In the present studies, we found first time that they displayed anti-tumor activity of NSCLC in vitro and in vivo. Potent anti-cancer effects in NSCLC in vitro, including inhibiting NSCLC cells viability, arresting cell cycle at the G0/G1 phase, inducing cell apoptosis, delaying and suppressing NSCLC cells colony-forming ability and cell motility, could be achieved with this agent. Meanwhile, we provided evidence that these effects were applicable in vivo by using H460 cells xenograft model in nude mice. In addition, to comprehensively clarify the mechanisms of teriflunomide in NSCLC, we explored a genome-wide transcriptomic analysis, and found that teriflunomide was involved in multiple signaling pathways and cellular processes, such as cell cycle, apoptosis, MAPK and p53 signaling pathway. Taken together, the results of our studies provided insights into a novel anti-cancer effect of leflunomide and teriflunomide on NSCLC and might open new therapeutic avenues for the treatment of NSCLC.
[Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia
Antineoplásicos/farmacologia
Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico
Proliferação Celular/efeitos dos fármacos
Crotonatos/farmacologia
Isoxazóis/farmacologia
Toluidinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Apoptose/efeitos dos fármacos
Carcinoma Pulmonar de Células não Pequenas/patologia
Linhagem Celular Tumoral
Movimento Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Feminino
Seres Humanos
Camundongos Nus
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antineoplastic Agents); 0 (Crotonates); 0 (Isoxazoles); 0 (Toluidines); 1C058IKG3B (teriflunomide); G162GK9U4W (leflunomide)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171201
[Lr] Data última revisão:
171201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171021
[St] Status:MEDLINE


  9 / 7381 MEDLINE  
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[PMID]:28466558
[Au] Autor:Matricoti I; Maina E
[Ad] Endereço:Servizi Dermatologici Veterinari, Bologna, 40125, Italy.
[Ti] Título:The use of oral fluralaner for the treatment of feline generalised demodicosis: a case report.
[So] Source:J Small Anim Pract;58(8):476-479, 2017 Aug.
[Is] ISSN:1748-5827
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:There is little agreement on the most effective and safest treatment for feline demodicosis. Protocols generally consist of long-lasting therapy courses based on rinses, subcutaneous injections, oral drug administration or repeated spot-on formulation and the efficacy of most of these is poorly documented. Many of these products have also been associated with adverse effects and may be difficult to administer in cats, leading to poor owner compliance and treatment failure. This case report describes the successful use of fluralaner in treating a generalised form of demodicosis caused by Demodex cati in an adult cat that was probably triggered by chronic glucocorticoid administration. After a single oral dose of 28 mg/kg fluralaner, negative skin scrapings were obtained within one month and clinical cure within two months. No side effects were observed. Larger studies are needed to evaluate the efficacy of fluralaner in treating feline generalised demodicosis.
[Mh] Termos MeSH primário: Antiparasitários/uso terapêutico
Doenças do Gato/tratamento farmacológico
Isoxazóis/uso terapêutico
Infestações por Ácaros/veterinária
[Mh] Termos MeSH secundário: Administração Oral
Animais
Gatos
Feminino
Infestações por Ácaros/tratamento farmacológico
Ácaros/efeitos dos fármacos
[Pt] Tipo de publicação:CASE REPORTS
[Nm] Nome de substância:
0 (A1443 compound); 0 (Antiparasitic Agents); 0 (Isoxazoles)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE
[do] DOI:10.1111/jsap.12682


  10 / 7381 MEDLINE  
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[PMID]:28982310
[Au] Autor:Kim SH; Kang JG; Kim CS; Ihm SH; Choi MG; Yoo HJ; Lee SJ
[Ad] Endereço:Division of Endocrinology and Metabolism, Department of Internal Medicine, College of Medicine, Hallym University, Chuncheon, Republic of Korea.
[Ti] Título:The dipeptidyl peptidase-IV inhibitor gemigliptin alone or in combination with NVP-AUY922 has a cytotoxic activity in thyroid carcinoma cells.
[So] Source:Tumour Biol;39(10):1010428317722068, 2017 Oct.
[Is] ISSN:1423-0380
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The effect of the dipeptidyl peptidase-IV inhibitor gemigliptin alone or in combination with the heat shock protein 90 inhibitor NVP-AUY922 (AUY922) on survival of thyroid carcinoma cells was elucidated. The SW1736 and TPC-1 human thyroid carcinoma cells were used. Cell viability, the percentage of viable cells, cytotoxic activity, the percentage of apoptotic cells, and mitochondrial membrane potential were measured. To evaluate the combined effect of gemigliptin with AUY922, the interactions were estimated by calculating combination index. Gemigliptin led to cell death in conjunction with overexpression of the phosphorylated protein levels of Akt, extracellular signal-regulated kinase 1/2, and adenosine monophosphate-activated protein kinase. In gemigliptin-treated cells, wortmannin augmented cell death, whereas AZD6244 and compound C did not affect cell survival. Wortmannin decreased phosphorylated adenosine monophosphate-activated protein kinase protein levels, and AZD6244 increased phosphorylated Akt protein levels. Meanwhile, cotreatment of both gemigliptin and AUY922, compared with treatment of AUY922 alone, potentiated cell death. All the combination index values were lower than 1.0, suggesting synergistic cytotoxicity of gemigliptin with AUY922. In treatment of both gemigliptin and AUY922, compared with AUY922 alone, the protein levels of total and phosphorylated Akt, phosphorylated extracellular signal-regulated kinase 1/2, and phosphorylated adenosine monophosphate-activated protein kinase increased without alteration in those of total extracellular signal-regulated kinase 1/2 and total adenosine monophosphate-activated protein kinase. The percentage of apoptotic cells increased. The protein levels of Bax and cleaved poly (ADP-ribose) polymerase increased, whereas Bcl2 protein levels were unchanged, resulting in increment of Bax/Bcl2 ratio. Transfection of Bax small interfering RNA did not cause any variation in cell viability, the percentage of viable cells and cytotoxic activity. Our results demonstrate that gemigliptin exerts a cytotoxic activity with concomitant alterations in expression of Akt, extracellular signal-regulated kinase 1/2, and adenosine monophosphate-activated protein kinase in thyroid carcinoma cells. Furthermore, gemigliptin synergizes with AUY922 in induction of cytotoxicity via regulation of Akt, extracellular signal-regulated kinase 1/2, and adenosine monophosphate-activated protein kinase as well as involvement of Bcl2 family proteins in thyroid carcinoma cells.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carcinoma/patologia
Isoxazóis/farmacologia
Piperidonas/farmacologia
Pirimidinas/farmacologia
Resorcinóis/farmacologia
Neoplasias da Glândula Tireoide/patologia
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Western Blotting
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Inibidores da Dipeptidil Peptidase IV/farmacologia
Sinergismo Farmacológico
Citometria de Fluxo
Seres Humanos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5-(2,4-dihydroxy-5-isopropylphenyl)-4-(4-morpholin-4-ylmethylphenyl)isoxazole-3-carboxylic acid ethylamide); 0 (Antineoplastic Agents); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Isoxazoles); 0 (LC15-0444); 0 (Piperidones); 0 (Pyrimidines); 0 (Resorcinols)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171017
[Lr] Data última revisão:
171017
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171007
[St] Status:MEDLINE
[do] DOI:10.1177/1010428317722068



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