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[PMID]: 29247858 [Au] Autor: Palace-Berl F; Pasqualoto KFM; Zingales B; Moraes CB; Bury M; Franco CH; da Silva Neto AL; Murayama JS; Nunes SL; Silva MN; Tavares LC [Ad] Endereço: Department of Biochemical and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, University of São Paulo, SP, Brazil. Electronic address: palaceberlf@usp.br. [Ti] Título: Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds. [So] Source: Eur J Med Chem;144:29-40, 2018 Jan 20. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: Chagas disease, caused by the protozoan Trypanosoma cruzi, is a neglected chronic tropical infection endemic in Latin America. New and effective treatments are urgently needed because the two available drugs - benznidazole (BZD) and nifurtimox (NFX) - have limited curative power in the chronic phase of the disease. We have previously reported the design and synthesis of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides that showed high trypanocidal activity against axenic epimastigote forms of three T. cruzi strains. Here we show that these compounds are also active against a BZD- and NFX-resistant strain. Herein, multivariate approaches (hierarchical cluster analysis and principal component analysis) were applied to a set of thirty-six formerly characterized compounds. Based on the findings from exploratory data analysis, novel compounds were designed and synthesized. These compounds showed two-to three-fold higher trypanocidal activity against epimastigote forms than the previous set and were 25-30-fold more active than BZD. Their activity was also evaluated against intracellular amastigotes by high content screening (HCS). The most active compounds (BSF-38 to BSF-40) showed a selective index (SI') greater than 200, in contrast to the SI' values of reference drugs (NFX, 16.45; BZD, > 3), and a 70-fold greater activity than BZD. These findings indicate that nitrofuran compounds designed based on the activity against epimastigote forms show promising trypanocidal activity against intracellular amastigotes, which correspond to the predominant parasite stage in the chronic phase of Chagas disease. [Mh] Termos MeSH primário: Nitrofuranos/química Nitrofuranos/farmacologia Tripanossomicidas/química Tripanossomicidas/farmacologia Trypanosoma cruzi/efeitos dos fármacos [Mh] Termos MeSH secundário: Linhagem Celular Doença de Chagas/tratamento farmacológico Desenho de Drogas Seres Humanos Modelos Moleculares Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Nitrofurans); 0 (Trypanocidal Agents) [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: 171217 [St] Status: MEDLINE

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[PMID]: 29291386 [Au] Autor: Said E; Zaitone SA; Eldosoky M; Elsherbiny NM [Ad] Endereço: Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt. [Ti] Título: Nifuroxazide, a STAT3 inhibitor, mitigates inflammatory burden and protects against diabetes-induced nephropathy in rats. [So] Source: Chem Biol Interact;281:111-120, 2018 Feb 01. [Is] ISSN: 1872-7786 [Cp] País de publicação: Ireland [La] Idioma: eng [Ab] Resumo: Diabetic nephropathy (DN) is a serious complication of diabetes mellitus. Moreover,it is amongst the most common causes of end-stage renal failure. Inflammation is a crucial player in both development and progression of DN. JAK2/STA3 is a pleotropic cascade reported to regulate diverse inflammatory events. Previous studies reported involvement of JAK2/STA3 signal transduction pathway in diabetes-associated renal injury. In the current study, the inhibitory effect of nifuroxazide (25 mg/kg/day, orally) against inflammatory condition associating diabetic kidney progression in rats was evaluated. The underlying hypothesis is mainly via the inhibitory effect of nifuroxazide on STAT3 signaling. Results revealed that nifuroxazide effectively inhibited STAT3 activation in diabetic male rats, improved glomerular filtration function, protected against diabetes-induced histopathological and ultramicroscopic structural alterations. Further, nifuroxazide treatment significantly reduced renal macrophage infiltration and fibrosis and decreased mRNA and protein levels of TNF-α and IL-18 in diabetic renal tissue. The current findings shed the light on nifuroxazide's efficacy as an alternative anti-inflammatory therapy to hinder the development and progression of DN in diabetic patients mainly via STAT3 inhibition. [Mh] Termos MeSH primário: Anti-Inflamatórios/uso terapêutico Diabetes Mellitus Experimental/complicações Nefropatias Diabéticas/prevenção & controle Hidroxibenzoatos/uso terapêutico Nitrofuranos/uso terapêutico Fator de Transcrição STAT3/antagonistas & inibidores [Mh] Termos MeSH secundário: Animais Anti-Inflamatórios/farmacologia Nitrogênio da Ureia Sanguínea Creatina/sangue Diabetes Mellitus Experimental/induzido quimicamente Diabetes Mellitus Experimental/patologia Nefropatias Diabéticas/etiologia Fibrose Hidroxibenzoatos/farmacologia Interleucina-18/genética Interleucina-18/metabolismo Janus Quinase 2/metabolismo Rim/efeitos dos fármacos Rim/metabolismo Rim/patologia Testes de Função Renal Macrófagos/citologia Macrófagos/imunologia Masculino Microscopia Eletrônica Nitrofuranos/farmacologia Ratos Fator de Transcrição STAT3/metabolismo Transdução de Sinais/efeitos dos fármacos Estreptozocina/toxicidade Fator de Necrose Tumoral alfa/genética Fator de Necrose Tumoral alfa/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Inflammatory Agents); 0 (Hydroxybenzoates); 0 (Interleukin-18); 0 (Nitrofurans); 0 (STAT3 Transcription Factor); 0 (Tumor Necrosis Factor-alpha); 5W494URQ81 (Streptozocin); EC 2.7.10.2 (Janus Kinase 2); MU72812GK0 (Creatine); PM5LI0P38J (nifuroxazide) [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: 180102 [St] Status: MEDLINE

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[PMID]: 28623772 [Au] Autor: Magotra A; Sharma A; Gupta AP; Wazir P; Sharma S; Singh PP; Tikoo MK; Vishwakarma RA; Singh G; Nandi U [Ad] Endereço: PK-PD, Toxicology and Formulation division, CSIR- Indian Institute of Integrative Medicine, Jammu 180 001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR- Indian Institute of Integrative Medicine, Jammu 180 001, India. [Ti] Título: Development and validation of a highly sensitive LC-ESI-MS/MS method for estimation of IIIM-MCD-211, a novel nitrofuranyl methyl piperazine derivative with potential activity against tuberculosis: Application to drug development. [So] Source: J Chromatogr B Analyt Technol Biomed Life Sci;1060:200-206, 2017 Aug 15. [Is] ISSN: 1873-376X [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: In the present study, a simple, sensitive, specific and rapid liquid chromatography (LC) tandem mass spectrometry (MS/MS) method was developed and validated according to the Food and Drug Administration (FDA) guidelines for estimation of IIIM-MCD-211 (a potent oral candidate with promising action against tuberculosis) in mice plasma using carbamazepine as internal standard (IS). Bioanalytical method consisted of one step protein precipitation for sample preparation followed by quantitation in LC-MS/MS using positive electrospray ionization technique (ESI) operating in multiple reaction monitoring (MRM) mode. Elution was achieved in gradient mode on High Resolution Chromolith RP-18e column with mobile phase comprised of acetonitrile and 0.1% (v/v) formic acid in water at the flow rate of 0.4mL/min. Precursor to product ion transitions (m/z 344.5/218.4 and m/z 237.3/194.2) were used to measure analyte and IS, respectively. All validation parameters were well within the limit of acceptance criteria. The method was successfully applied to assess the pharmacokinetics of the candidate in mice following oral (10mg/kg) and intravenous (IV; 2.5mg/kg) administration. It was also effectively used to quantitate metabolic stability of the compound in mouse liver microsomes (MLM) and human liver microsomes (HLM) followed by its in-vitro-in-vivo extrapolation. [Mh] Termos MeSH primário: Antituberculosos/análise Cromatografia Líquida/métodos Nitrofuranos/análise Piperazinas/análise Espectrometria de Massas em Tandem/métodos [Mh] Termos MeSH secundário: Animais Antituberculosos/química Antituberculosos/farmacocinética Antituberculosos/farmacologia Limite de Detecção Modelos Lineares Masculino Camundongos Microssomos Hepáticos/metabolismo Mycobacterium tuberculosis/efeitos dos fármacos Nitrofuranos/química Nitrofuranos/farmacocinética Nitrofuranos/farmacologia Piperazinas/química Piperazinas/farmacocinética Piperazinas/farmacologia Reprodutibilidade dos Testes Espectrometria de Massas por Ionização por Electrospray/métodos Tuberculose [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antitubercular Agents); 0 (Nitrofurans); 0 (Piperazines) [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: 170618 [St] Status: MEDLINE

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[PMID]: 28493683 [Au] Autor: Wang Y; Chan KKJ; Chan W [Ad] Endereço: Department of Chemistry, The Hong Kong University of Science and Technology , Clear Water Bay, Kowloon, Hong Kong. [Ti] Título: Plant Uptake and Metabolism of Nitrofuran Antibiotics in Spring Onion Grown in Nitrofuran-Contaminated Soil. [So] Source: J Agric Food Chem;65(21):4255-4261, 2017 May 31. [Is] ISSN: 1520-5118 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Environmental pollution caused by the discharge of mutagenic and carcinogenic nitrofurans to the aquatic and soil environment is an emerging public health concern because of the potential in producing drug-resistant microbes and being uptaken by food crops. Using liquid chromatography-tandem mass spectrometry analysis and with spring onion (Allium wakegi Araki) as the plant model, we investigated in this study the plant uptake and accumulation of nitrofuran from a contaminated environment. Our study revealed for the first time high uptake and accumulation rates of nitrofuran in the edible parts of the food crop. Furthermore, results indicated highly efficient plant metabolism of the absorbed nitrofuran within the plant, leading to the formation of genotoxic hydrazine-containing metabolites. The results from this study may disclose a previously unidentified human exposure pathway through contaminated food crops. [Mh] Termos MeSH primário: Antibacterianos/metabolismo Nitrofuranos/metabolismo Cebolas/metabolismo Poluentes do Solo/metabolismo [Mh] Termos MeSH secundário: Antibacterianos/análise Nitrofuranos/análise Cebolas/química Cebolas/crescimento & desenvolvimento Poluentes do Solo/análise [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Nitrofurans); 0 (Soil Pollutants) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 170608 [Lr] Data última revisão: 170608 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170512 [St] Status: MEDLINE [do] DOI: 10.1021/acs.jafc.7b01050

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[PMID]: 28476810 [Au] Autor: Gombodorj N; Yokobori T; Yoshiyama S; Kawabata-Iwakawa R; Rokudai S; Horikoshi I; Nishiyama M; Nakano T [Ad] Endereço: Department of Radiation Oncology, Gunma University Graduate School of Medicine, Gunma, Japan. [Ti] Título: Inhibition of Ubiquitin-conjugating Enzyme E2 May Activate the Degradation of Hypoxia-inducible Factors and, thus, Overcome Cellular Resistance to Radiation in Colorectal Cancer. [So] Source: Anticancer Res;37(5):2425-2436, 2017 05. [Is] ISSN: 1791-7530 [Cp] País de publicação: Greece [La] Idioma: eng [Ab] Resumo: BACKGROUND: NSC697923, a ubiquitin-conjugating enzyme E2 (UBE2) inhibitor, was suggested as an agent to degrade hypoxia-inducible factor 1 alpha subunit (HIF1α), a key factor in radiation resistance. We attempted to clarify whether NSC697923 could overcome radiation resistance. MATERIALS AND METHODS: Radiation resistance and expression of HIFs were evaluated in radiation-sensitive HCT116 and -resistant SW480 cells treated with or without NSC697923 and radiation under normoxia and hypoxia in vitro and in vivo. We examined NSC697923-regulated genes using RNA sequencing. RESULTS: HIF expression significantly increased under hypoxia with an increase of cellular radiation resistance in vitro and in vivo. The therapeutic activity of NSC697923 was higher in radiation-resistant SW480 than radiation-sensitive HCT116 in vivo. Next-generation RNA sequencing revealed that NSC697923 regulated the expression of cell migration-inducing protein, hyaluronan binding (CEMIP) and apelin (APLN) genes, that are related to HIF pathways. CONCLUSION: NSC697923 might effectively regulate HIF families, and be a promising partner with radiation to overcome resistance. [Mh] Termos MeSH primário: Fatores de Transcrição Hélice-Alça-Hélice Básicos/antagonistas & inibidores Subunidade alfa do Fator 1 Induzível por Hipóxia/antagonistas & inibidores Nitrofuranos/farmacologia Nitrofuranos/uso terapêutico Tolerância a Radiação/efeitos dos fármacos Sulfonas/farmacologia Sulfonas/uso terapêutico Enzimas de Conjugação de Ubiquitina/antagonistas & inibidores [Mh] Termos MeSH secundário: Animais Antineoplásicos/farmacologia Antineoplásicos/uso terapêutico Hipóxia Celular/efeitos dos fármacos Hipóxia Celular/genética Linhagem Celular Tumoral Sobrevivência Celular/efeitos dos fármacos Cisplatino/farmacologia Cisplatino/uso terapêutico Neoplasias Colorretais/tratamento farmacológico Neoplasias Colorretais/genética Neoplasias Colorretais/patologia Neoplasias Colorretais/radioterapia Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos Seres Humanos Masculino Camundongos Endogâmicos BALB C Camundongos Nus Carga Tumoral/efeitos da radiação [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (2-((4-methylphenyl)sulfonyl)-5-nitrofuran); 0 (Antineoplastic Agents); 0 (Basic Helix-Loop-Helix Transcription Factors); 0 (HIF1A protein, human); 0 (Hypoxia-Inducible Factor 1, alpha Subunit); 0 (Nitrofurans); 0 (Sulfones); 0 (endothelial PAS domain-containing protein 1); EC 2.3.2.23 (Ubiquitin-Conjugating Enzymes); Q20Q21Q62J (Cisplatin) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170814 [Lr] Data última revisão: 170814 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170507 [St] Status: MEDLINE

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[PMID]: 28214232 [Au] Autor: Krasavin M; Parchinsky V; Kantin G; Manicheva O; Dogonadze M; Vinogradova T; Karge B; Brönstrup M [Ad] Endereço: Institutes of Chemistry and Translational Biomedicine, Saint Petersburg State University, Saint Petersburg 199034, Russian Federation. Electronic address: m.krasavin@spbu.ru. [Ti] Título: New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis. [So] Source: Bioorg Med Chem;25(6):1867-1874, 2017 Mar 15. [Is] ISSN: 1464-3391 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A set of structurally diverse N-amino δ-lactams decorated with a 5-nitro-2-furyl moiety was synthesized using isocyanide-based multicomponent chemistry and evaluated for antibacterial activity. Three compounds displayed a selective and potent (MIC 22-33µM) inhibition of M. tuberculosis H Rv strain growth, while other Gram-positive (MRSA and E. faecium) or Gram-negative (E. coli, P. aeruginosa, A. baumannii, K. pneumoniae) pathogens were not affected. The compounds also displayed moderate-low cytotoxicity, as demonstrated in cell line viability assays. Several multidrug- and poly-resistant patient-derived M. tuberculosis strains were found to be susceptible to treatment with these compounds. The three most potent compounds share a significant structural similarity which provides a basis for further scaffold-hopping analog design. [Mh] Termos MeSH primário: Antituberculosos/farmacologia Cianetos/química Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos Mycobacterium tuberculosis/efeitos dos fármacos Nitrofuranos/farmacologia [Mh] Termos MeSH secundário: Antituberculosos/química Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 Seres Humanos Testes de Sensibilidade Microbiana Nitrofuranos/química Espectroscopia de Prótons por Ressonância Magnética [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antitubercular Agents); 0 (Cyanides); 0 (Nitrofurans) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171002 [Lr] Data última revisão: 171002 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170219 [St] Status: MEDLINE

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[PMID]: 28187378 [Au] Autor: Park MS; Kim KT; Kang JS [Ad] Endereço: College of Pharmacy Chungnam National University, Daejeon 34134, Republic of Korea; Ministry of Food and Drug Safety Korea, Cheongju-si 28159, Republic of Korea. [Ti] Título: Development of an analytical method for detecting nitrofurans in bee pollen by liquid chromatography-electrospray ionization tandem mass spectrometry. [So] Source: J Chromatogr B Analyt Technol Biomed Life Sci;1046:172-176, 2017 Mar 01. [Is] ISSN: 1873-376X [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Bee pollen collected by honeybees, which is in powdered form, is a good nutritional supplement. Nitrofuran antibiotics are assumed not to be present in bee pollen, which is important as the level of antibiotics in bee pollen is strongly regulated in many countries. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to detect nitrofurans in honey has been developed, but this method is not suitable for bee pollen because of it being in powdered form. During preparation of bee pollen samples, the dispersal of powder particles in an aqueous solution often makes them susceptible to forming an emulsion with solvent components such as hexane and ethyl acetate. This may reduce the reproducibility and sensitivity of analyses of nitrofuran levels in bee pollen. Therefore, we attempted to optimize the sample preparation conditions to detect nitrofurans in bee pollen by determining three nitrofuran residues, namely, 3-amino-2-oxazolidinone (AOZ), 3-amino-5-methyl-morpholino-2-oxazolidinone (AMOZ), and 1-aminohydantoin (AHD), using LC-MS/MS. The optimized method prevented the formation of powder-induced emulsion. To verify the reproducibility and sensitivity of this method, it was validated using nitrofuran-free bee pollen spiked with analytes with different side chains at 1.0, 2.0, and 5.0µgkg . The accuracy levels were 94.1%-104.0% and the coefficients of variation were less than 12%. The limits of detection for AOZ, AMOZ, and AHD were 0.18, 0.25, and 0.30µgkg , respectively, while their limits of quantitation were 0.59, 0.83, and 1.00µgkg . The LC-MS/MS method developed to analyze nitrofuran in bee pollen should contribute to the quality control of bee pollen and food safety. [Mh] Termos MeSH primário: Abelhas Nitrofuranos/análise Pólen/química [Mh] Termos MeSH secundário: Animais Cromatografia Líquida/métodos Limite de Detecção Modelos Lineares Reprodutibilidade dos Testes Espectrometria de Massas por Ionização por Electrospray/métodos Espectrometria de Massas em Tandem/métodos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Nitrofurans) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170522 [Lr] Data última revisão: 170522 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170211 [St] Status: MEDLINE

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[PMID]: 28055016 [Au] Autor: Ye TH; Yang FF; Zhu YX; Li YL; Lei Q; Song XJ; Xia Y; Xiong Y; Zhang LD; Wang NY; Zhao LF; Gou HF; Xie YM; Yang SY; Yu LT; Yang L; Wei YQ [Ad] Endereço: Department of Liver Surgery and Division of Digestive Diseases, State Key Laboratory of Biotherapy/Collaborative Innovation Center for Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, China. [Ti] Título: Inhibition of Stat3 signaling pathway by nifuroxazide improves antitumor immunity and impairs colorectal carcinoma metastasis. [So] Source: Cell Death Dis;8(1):e2534, 2017 Jan 05. [Is] ISSN: 2041-4889 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Colorectal carcinoma (CRC) is the one of the most common cancers with considerable metastatic potential, explaining the need for new drug candidates that inhibit tumor metastasis. The signal transducers and activators of the transcription 3 (Stat3) signaling pathway has an important role in CRC and has been validated as a promising anticancer target for CRC therapy. In the present study, we report our findings on nifuroxazide, an antidiarrheal agent identified as an inhibitor of Stat3. Our studies showed that nifuroxazide decreased the viability of three CRC cell lines and induced apoptosis of cancer cells in a concentration-dependent manner. Moreover, western blot analysis demonstrated that the occurrence of its apoptosis was correlated with the activation of Bax and cleaved caspase-3, and decreased the expression of Bcl-2. In addition, nifuroxazide markedly impaired CRC cell migration and invasion by downregulating phosphorylated-Stat3 , and also impaired the expression of matrix metalloproteinases (MMP-2 and MMP-9). Furthermore, our studies showed that nifuroxazide also significantly inhibited the tumor metastasis in lung and abdomen metastasis models of colon cancer. Meanwhile, nifuroxazide functionally reduced the proliferation index, induced tumor apoptosis and impaired metastasis. Notably, nifuroxazide reduced the number of myeloid-derived suppressor cells in the blood, spleens and tumors, accompanied by the increased infiltration of CD8 T cells in the tumors. Importantly, a marked decrease in the number of M2-type macrophages in tumor in the abdomen metastasis model was also observed. Taken together, our results indicated that nifuroxazide could effectively inhibit tumor metastasis by mediating Stat3 pathway and it might have a therapeutic potential for the treatment of CRC. [Mh] Termos MeSH primário: Apoptose/genética Neoplasias Colorretais/tratamento farmacológico Metástase Neoplásica/tratamento farmacológico Fator de Transcrição STAT3/genética [Mh] Termos MeSH secundário: Animais Linhagem Celular Tumoral Neoplasias Colorretais/genética Neoplasias Colorretais/patologia Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos Seres Humanos Hidroxibenzoatos/administração & dosagem Camundongos Metástase Neoplásica/genética Proteínas de Neoplasias/biossíntese Nitrofuranos/administração & dosagem Fator de Transcrição STAT3/antagonistas & inibidores Transdução de Sinais/efeitos dos fármacos Ensaios Antitumorais Modelo de Xenoenxerto [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Hydroxybenzoates); 0 (Neoplasm Proteins); 0 (Nitrofurans); 0 (STAT3 Transcription Factor); 0 (STAT3 protein, human); PM5LI0P38J (nifuroxazide) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171026 [Lr] Data última revisão: 171026 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170106 [St] Status: MEDLINE [do] DOI: 10.1038/cddis.2016.452

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[PMID]: 27979167 [Au] Autor: Li Z; Li Z; Xu D [Ad] Endereço: State Key Laboratory of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China. Electronic address: lizhonghui0106@gmail.com. [Ti] Título: Simultaneous detection of four nitrofuran metabolites in honey by using a visualized microarray screen assay. [So] Source: Food Chem;221:1813-1821, 2017 Apr 15. [Is] ISSN: 0308-8146 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A visualized microarray sensing technique has been developed and applied to the screening of honey samples for residues of banned nitrofuran antibiotics. Using a multiplexed approach, metabolites of four main nitrofuran antibiotics can be detected simultaneously. Individual antigens were spotted onto 96-well plates. An indirective competitive assay format, with visualized signal response, was employed. An extraction method, based on derivatization with 2-nitrobenzaldehyde and partition into ethyl acetate, was used for screening. The limits of detection were 0.10, 0.04, 0.04, and 0.10ngg for 3-amino-5-morpholino-2-oxazolidone (AMOZ), 3-amino-2-oxazolidinone (AOZ), semicarbazide (SEM), and 1-aminohydantoin (AHD), respectively. The recovery rate ranged from 78% to 93% for the four targets. In addition, this method was easy to operate with low detection cost and fast speed. This microarray method possesses the potential to be a fit-for-purpose screening technique in the arena of food safety monitoring. [Mh] Termos MeSH primário: Mel/análise Análise em Microsséries/métodos Nitrofuranos/química [Mh] Termos MeSH secundário: Acetatos/análise Antibacterianos/química Benzaldeídos/análise Análise de Alimentos Qualidade dos Alimentos Inocuidade dos Alimentos Hidantoínas/análise Limite de Detecção Oxazolidinonas/análise Reprodutibilidade dos Testes Semicarbazidas/análise [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (1-aminohydantoin); 0 (Acetates); 0 (Anti-Bacterial Agents); 0 (Benzaldehydes); 0 (Hydantoins); 0 (Nitrofurans); 0 (Oxazolidinones); 0 (Semicarbazides); 37QUC23K2X (carbamylhydrazine); 48B18Q9B8E (2-nitrobenzaldehyde); 76845O8NMZ (ethyl acetate); 80-65-9 (3-amino-2-oxazolidinone) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161217 [St] Status: MEDLINE

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[PMID]: 27810595 [Au] Autor: Arias DG; Herrera FE; Garay AS; Rodrigues D; Forastieri PS; Luna LE; Bürgi MD; Prieto C; Iglesias AA; Cravero RM; Guerrero SA [Ad] Endereço: Instituto de Agrobiotecnología del Litoral (CONICET-UNL), Argentina; Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral, Argentina. [Ti] Título: Rational design of nitrofuran derivatives: Synthesis and valuation as inhibitors of Trypanosoma cruzi trypanothione reductase. [So] Source: Eur J Med Chem;125:1088-1097, 2017 Jan 05. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: The rational design and synthesis of a series of 5-nitro-2-furoic acid analogues are presented. The trypanocidal activity against epimastigote forms of Trypanosoma cruzi and the toxic effects on human HeLa cells were tested. Between all synthetic compounds, three of thirteen had an IC value in the range of Nfx, but compound 13 exhibited an improved effect with an IC of 1.0 ± 0.1 µM and a selective index of 70 in its toxicity against HeLa cells. We analyzed the activity of compounds 8, 12 and 13 to interfere in the central redox metabolic pathway in trypanosomatids, which is dependent of reduced trypanothione as the major pivotal thiol. The three compounds behaved as better inhibitors of trypanothione reductase than Nfx (Ki values of 118 µM, 61 µM and 68 µM for 8, 12 and 13, respectively, compared with 245 µM for Nfx), all following an uncompetitive enzyme inhibition pattern. Docking analysis predicted a binding of inhibitors to the enzyme-substrate complex with binding energy calculated in-silico that supports such molecular interaction. [Mh] Termos MeSH primário: NADH NADPH Oxirredutases/antagonistas & inibidores Nitrofuranos/química Nitrofuranos/farmacologia Tripanossomicidas/química Tripanossomicidas/farmacologia Trypanosoma cruzi/enzimologia [Mh] Termos MeSH secundário: Doença de Chagas/tratamento farmacológico Doença de Chagas/parasitologia Desenho de Drogas Inibidores Enzimáticos/química Inibidores Enzimáticos/farmacologia Células HeLa Seres Humanos Simulação de Acoplamento Molecular NADH NADPH Oxirredutases/metabolismo Trypanosoma cruzi/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Enzyme Inhibitors); 0 (Nitrofurans); 0 (Trypanocidal Agents); EC 1.6.- (NADH, NADPH Oxidoreductases); EC 1.8.1.12 (trypanothione reductase) [Em] Mês de entrada: 1702 [Cu] Atualização por classe: 170217 [Lr] Data última revisão: 170217 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161105 [St] Status: MEDLINE

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