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Pesquisa : D02.078.370 [Categoria DeCS]
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[PMID]:29478637
[Au] Autor:Gurtowski LA; Griggs CS; Gude VG; Shukla MK
[Ad] Endereço:Environmental Laboratory, Engineer Research and Development Center, Vicksburg, MS 39180, USA.
[Ti] Título:An integrated theoretical and experimental investigation of insensitive munition compounds adsorption on cellulose, cellulose triacetate, chitin and chitosan surfaces.
[So] Source:J Environ Sci (China);64:174-180, 2018 Feb.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This manuscript reports results of combined computational chemistry and batch adsorption investigation of insensitive munition compounds, 2,4-dinitroanisole (DNAN), triaminotrinitrobenzene (TATB), 1,1-diamino-2,2-dinitroethene (FOX-7) and nitroguanidine (NQ), and traditional munition compound 2,4,6-trinitrotoluene (TNT) on the surfaces of cellulose, cellulose triacetate, chitin and chitosan biopolymers. Cellulose, cellulose triacetate, chitin and chitosan were modeled as trimeric form of the linear chain of C chair conformation of ß-d-glucopyranos, its triacetate form, ß-N-acetylglucosamine and D-glucosamine, respectively, in the 1âž”4 linkage. Geometries were optimized at the M062X functional level of the density functional theory (DFT) using the 6-31G(d,p) basis set in the gas phase and in the bulk water solution using the conductor-like polarizable continuum model (CPCM) approach. The nature of potential energy surfaces of the optimized geometries were ascertained through the harmonic vibrational frequency analysis. The basis set superposition error (BSSE) corrected interaction energies were obtained using the 6-311G(d,p) basis set at the same theoretical level. The computed BSSE in the gas phase was used to correct interaction energy in the bulk water solution. Computed and experimental results regarding the ability of considered surfaces in adsorbing the insensitive munitions compounds are discussed.
[Mh] Termos MeSH primário: Substâncias Explosivas/química
Modelos Químicos
[Mh] Termos MeSH secundário: Adsorção
Anisóis/química
Celulose/análogos & derivados
Celulose/química
Quitina/química
Quitosana/química
Guanidinas/química
Nitrocompostos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,1-diamino-2,2-dinitroethene); 0 (Anisoles); 0 (Explosive Agents); 0 (Guanidines); 0 (Nitro Compounds); 1398-61-4 (Chitin); 1L0OD70295 (2,4-dinitroanisole); 9004-34-6 (Cellulose); 9012-09-3 (cellulose triacetate); 9012-76-4 (Chitosan); NAY6KWL67F (nitroguanidine)
[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:180227
[St] Status:MEDLINE


  2 / 17479 MEDLINE  
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[PMID]:29324342
[Au] Autor:Wang PC; Chiu DC; Jan JT; Huang WI; Tseng YC; Li TT; Cheng TJ; Tsai KC; Fang JM
[Ad] Endereço:Department of Chemistry, National Taiwan University, Taipei 106, Taiwan.
[Ti] Título:Peramivir conjugates as orally available agents against influenza H275Y mutant.
[So] Source:Eur J Med Chem;145:224-234, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Peramivir is an efficacious neuraminidase (NA) inhibitor for treatment of influenza by intravenous administration. However, the efficacy of peramivir toward the H275Y mutant is appreciably reduced. To address this drawback, conjugation of peramivir with caffeic acid is devised in this study to enhance the binding affinity with neuraminidases. The C2-OH group of peramivir is elaborated to link with caffeate derivatives, giving the desired conjugates 8 and 9 that possess potent NA inhibitory activity against both wild-type and H275Y viruses with the IC values in nanomolar range. The molecular modeling reveals that the caffeate moiety of conjugate 9 prefers to reside in the 295-cavity of H275Y neuraminidase, thus providing additional hydrogen bonds and hydrophobic interactions to compensate the reduced binding affinity of the peramivir moiety due to Glu-276 dislocation in H275Y mutant. In comparison with peramivir, the lipophilicity of conjugates 8 and 9 also increases by incorporation of the caffeate moiety. Thus, conjugates 8 and 9 offer better effect to protect MDCK cells from infection of H275Y virus with low EC value (∼17 nM). Administration of conjugates 8 or 9 by oral gavage is effective in treatment of mice that are infected by lethal dose of wild-type or H275Y influenza viruses. Considering drug metabolism, since the ester linkage in conjugate 8 is susceptible to hydrolysis in plasma, conjugate 9 with robust amide linkage may be a better candidate for development into orally available anti-influenza drug that is also active to mutant viruses.
[Mh] Termos MeSH primário: Antivirais/farmacologia
Ciclopentanos/farmacologia
Guanidinas/farmacologia
Vírus da Influenza A/efeitos dos fármacos
[Mh] Termos MeSH secundário: Administração Oral
Animais
Antivirais/administração & dosagem
Antivirais/química
Ciclopentanos/administração & dosagem
Ciclopentanos/química
Cães
Relação Dose-Resposta a Droga
Guanidinas/administração & dosagem
Guanidinas/química
Células HEK293
Seres Humanos
Vírus da Influenza A/genética
Masculino
Camundongos
Camundongos Endogâmicos BALB C
Testes de Sensibilidade Microbiana
Modelos Moleculares
Estrutura Molecular
Mutação
Coelhos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Cyclopentanes); 0 (Guanidines); QW7Y7ZR15U (peramivir)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE


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[PMID]:29174818
[Au] Autor:Pei Z; Deng Q; Babcock SA; He EY; Ren J; Zhang Y
[Ad] Endereço:The Second Department of Cardiology, The Third Hospital of Nanchang, Nanchang, Jiangxi 330009, China.
[Ti] Título:Inhibition of advanced glycation endproduct (AGE) rescues against streptozotocin-induced diabetic cardiomyopathy: Role of autophagy and ER stress.
[So] Source:Toxicol Lett;284:10-20, 2018 Mar 01.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Diabetes mellitus leads to oxidative stress and contractile dysfunction in the heart. Although several rationales have been speculated, the precise mechanism behind diabetic cardiomyopathy remains elusive. This study was designed to assess the role of inhibition of advanced glycation endproducts (AGE) in streptozotocin (STZ)-induced diabetic cardiac dysfunction. Cardiac contractile function was assessed in normal C57BL/6 and STZ (200mg/kg, single injection and maintained for 2 wks)-induced diabetic mice treated with or without the AGE inhibitor aminoguanidine (50mg/kg/d in drinking water) for 2 weeks using echocardiography and IonOptix MyoCam techniques. Diabetes compromised cardiac contractile function shown as reduced fractional shortening and ejection fraction, enlarged left ventricular end systolic/diastolic diameters, decreased peak shortening, maximal velocity of shortening/relengthening, prolonged shortening and relengthening duration as well as impaired intracellular Ca homeostasis, the effects of which were alleviated or reversed by aminoguanidine treatment. Diabetes also inhibited autophagy, increased ER stress and phosphorylation of pro-hypertrophic signaling molecules Akt and mTOR, the effect of which was reversed by aminoguanidine. In vitro study revealed that methylglyoxal-derived AGE (MG-AGE) incubation in isolated cardiomyocytes promoted oxidation of sarco(endo)plasmic reticulum Ca -ATPase (SERCA2a) and production of superoxide, the effects of which were negated by the autophagy inducer rapamycin, the ER stress chaperone TUDCA or the antioxidant N-acetylcysteine. Taken together, these data revealed that inhibition of AGE formation rescues against experimental diabetes-induced cardiac remodeling and contractile dysfunction possible through regulation of autophagy and ER stress.
[Mh] Termos MeSH primário: Autofagia/efeitos dos fármacos
Diabetes Mellitus Experimental/metabolismo
Cardiomiopatias Diabéticas/prevenção & controle
Estresse do Retículo Endoplasmático/efeitos dos fármacos
Produtos Finais de Glicação Avançada/antagonistas & inibidores
Guanidinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Cálcio/metabolismo
Diabetes Mellitus Experimental/patologia
Cardiomiopatias Diabéticas/metabolismo
Cardiomiopatias Diabéticas/patologia
Ecocardiografia
Masculino
Camundongos Endogâmicos C57BL
Contração Miocárdica/efeitos dos fármacos
Miócitos Cardíacos/efeitos dos fármacos
Estreptozocina
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycation End Products, Advanced); 0 (Guanidines); 5W494URQ81 (Streptozocin); SCQ4EZQ113 (pimagedine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:29309811
[Au] Autor:Park EJ; Park SJ; Kim S; Lee K; Chang J
[Ad] Endereço:Graduate school of East-West Medical Science, Kyung Hee University, Yongin-si, Gyeonggi-do, 17104, Republic of Korea. Electronic address: pejtoxic@hanmail.net.
[Ti] Título:Lung fibroblasts may play an important role in clearing apoptotic bodies of bronchial epithelial cells generated by exposure to PHMG-P-containing solution.
[So] Source:Toxicol Lett;286:108-119, 2018 Apr.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Polyhexamethylene guanidine (PHMG) has been widely used in the industry owing to its excellent biocidal, anti-corrosive, and anti-biofouling properties. In Korea, consumers exposed to PHMG-phosphate (PHMG-P)-containing humidifier disinfectant have begun to suffer from fibrotic lung injury-related symptoms for unknown reasons. However, no appropriate treatment has yet been found because the detail toxic mechanism has not been identified. Herein, we first studied the toxic mechanism of PHMG-P-containing solution using human normal bronchial epithelial cells (BEAS-2B cells). When exposed for 24 h, PHMG-P-containing solution rapidly decreased cell viability from around 6 h after exposure and significantly increased of the phosphatidylserine exposure and the LDH release. At 6 h of exposure, the material contained in the solution was found to be bound to the cell membrane and the inner wall of vacuoles, and damaged the cell membrane and organelles. In addition, a significant increase of IFN-γ was observed among cytokines, the expression of apoptosis-, autophagy-, and membrane and DNA damage-related proteins was also enhanced. Meanwhile, the level of intracellular ROS and the secretion of IL-8 and CXCL-1, which are chemokines for professional phagocytes, decreased. Thus, we treated dead BEAS-2B cells to lung fibroblasts (HFL-1), non-professional phagocytes, and then we observed that the dead cells rapidly attached to HFL-1 cells and were taken up. Additionally, increased secretion of IL-8 and CXCL-1 was observed in the cells. Based on these results, we suggest that pulmonary exposure to PHMG-P induces apoptosis of bronchial epithelial cells and lung fibroblasts might play an important role in the clearance of the apoptotic debris.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Brônquios/efeitos dos fármacos
Citofagocitose
Desinfetantes/toxicidade
Células Epiteliais/efeitos dos fármacos
Fibroblastos/metabolismo
Guanidinas/toxicidade
[Mh] Termos MeSH secundário: Brônquios/metabolismo
Brônquios/ultraestrutura
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Quimiocina CXCL1/metabolismo
Relação Dose-Resposta a Droga
Células Epiteliais/metabolismo
Células Epiteliais/ultraestrutura
Fibroblastos/ultraestrutura
Seres Humanos
Interferon gama/metabolismo
Interleucina-8/metabolismo
L-Lactato Desidrogenase/metabolismo
Fosfatidilserinas/metabolismo
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (CXCL1 protein, human); 0 (Chemokine CXCL1); 0 (Disinfectants); 0 (Guanidines); 0 (IFNG protein, human); 0 (IL8 protein, human); 0 (Interleukin-8); 0 (Phosphatidylserines); 31961-54-3 (polyhexamethyleneguanidine); 82115-62-6 (Interferon-gamma); EC 1.1.1.27 (L-Lactate Dehydrogenase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180109
[St] Status:MEDLINE


  5 / 17479 MEDLINE  
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[PMID]:29262703
[Au] Autor:Gyori J; Farkas A; Stolyar O; Székács A; Mörtl M; Vehovszky Á
[Ad] Endereço:1 Department of Experimental Zoology, MTA Centre for Ecological Research, Balaton Limnological Institute , H-8237 Tihany, POB 35 , Hungary.
[Ti] Título:Inhibitory effects of four neonicotinoid active ingredients on acetylcholine esterase activity.
[So] Source:Acta Biol Hung;68(4):345-357, 2017 Dec.
[Is] ISSN:0236-5383
[Cp] País de publicação:Hungary
[La] Idioma:eng
[Ab] Resumo:There is a great concern about the decline of pollinators, and neonicotinoids emerging bee disorders are assumed to play a significant role. Since changes in learning ability has been observed in honey bees exposed to some acetylcholine esterase (AChE) inhibitors, we therefore, tested in vitro the effect of four neonicotinoids on purified eel AChE. AChE activity was inhibited in a concentration-dependent manner, and calculated IC values for thiamethoxam (IC = 414 µM) and clothianidin (IC = 160 µM) were found to be much higher compared to acetamiprid (IC = 75.2 µM) and thiacloprid (IC = 87.8 µM). The Lineweaver-Burk reciprocal plots for acetamiprid shows unchanged V and increased K values with inhibitor concentrations, while analysis of Michaelis-Menten plots shows predominantly competitive mechanism. The inhibition constant value (K = 24.3 µM) indicates strong binding of the acetamiprid complex to AChE. Finally, the four tested neonicotinoids are not a uniform group regarding their blocking ability. Our results suggest a previously not established, direct AChE blocking mechanism of neonicotinoids tested, thus the neuronal AChE enzyme is likely among the direct targets of the neonicotinoid insecticides. We conclude, that these AChE inhibitory effects may also contribute to toxic effects on the whole exposed animal.
[Mh] Termos MeSH primário: Acetilcolinesterase/química
Inibidores da Colinesterase/química
Electrophorus
Proteínas de Peixes
Guanidinas/química
Neonicotinoides/química
Nitrocompostos/química
Oxazinas/química
Tiazóis/química
[Mh] Termos MeSH secundário: Animais
Proteínas de Peixes/antagonistas & inibidores
Proteínas de Peixes/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Fish Proteins); 0 (Guanidines); 0 (Neonicotinoids); 0 (Nitro Compounds); 0 (Oxazines); 0 (Thiazoles); 2V9906ABKQ (clothianidin); 5HL5N372P0 (acetamiprid); 747IC8B487 (thiamethoxam); EC 3.1.1.7 (Acetylcholinesterase)
[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:171222
[St] Status:MEDLINE
[do] DOI:10.1556/018.68.2017.4.1


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[PMID]:29175483
[Au] Autor:White DP; Baumgarner BL; Watanabe WO; Alam MS; Kinsey ST
[Ad] Endereço:Department of Biology and Marine Biology, University of North Carolina Wilmington, Wilmington, NC 28403-5915, United States. Electronic address: dpwhite4@illinois.edu.
[Ti] Título:The effects of dietary ß-guanidinopropionic acid on growth and muscle fiber development in juvenile red porgy, Pagrus pagrus.
[So] Source:Comp Biochem Physiol B Biochem Mol Biol;216:48-58, 2018 Feb.
[Is] ISSN:1879-1107
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:ß-guanidinopropionic acid (ß-GPA) has been used in mammalian models to reduce intracellular phosphocreatine (PCr) concentration, which in turn lowers the energetic state of cells. This leads to changes in signaling pathways that attempt to re-establish energetic homeostasis. Changes in those pathways elicit effects similar to those of exercise such as changes in body and muscle growth, metabolism, endurance and health. Generally, exercise effects are beneficial to fish health and aquaculture, but inducing exercise in fishes can be impractical. Therefore, this study evaluated the potential use of supplemental ß-GPA to induce exercise-like effects in a rapidly growing juvenile teleost, the red porgy (Pagrus pagrus). We demonstrate for the first time that ß-GPA can be transported into teleost muscle fibers and is phosphorylated, and that this perturbs the intracellular energetic state of the cells, although to a lesser degree than typically seen in mammals. ß-GPA did not affect whole animal growth, nor did it influence skeletal muscle fiber size or myonuclear recruitment. There was, however, an increase in mitochondrial volume within myofibers in treated fish. GC/MS metabolomic analysis revealed shifts in amino acid composition of the musculature, putatively reflecting increases in connective tissue and decreases in protein synthesis that are associated with ß-GPA treatment. These results suggest that ß-GPA modestly affects fish muscle in a manner similar to that observed in mammals, and that ß-GPA may have application to aquaculture by providing a more practical means of generating some of the beneficial effects of exercise in fishes.
[Mh] Termos MeSH primário: Suplementos Nutricionais
Guanidinas/farmacologia
Fibras Musculares Esqueléticas/metabolismo
Propionatos/farmacologia
Dourada/crescimento & desenvolvimento
[Mh] Termos MeSH secundário: Animais
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Guanidines); 0 (Propionates); UL1984YRKA (guanidinopropionic acid)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180210
[Lr] Data última revisão:
180210
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


  7 / 17479 MEDLINE  
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[PMID]:29323846
[Au] Autor:Nosik NN; Nosik DN; Chizhov AI
[Ti] Título:A comparative analysis of virucidal efficiency of biocide agents.
[So] Source:Vopr Virusol;62(1):41-5, 2017.
[Is] ISSN:0507-4088
[Cp] País de publicação:Russia (Federation)
[La] Idioma:eng
[Ab] Resumo:The main groups of biocide agents used for inactivation of bacteria and viruses were studied for their virucidal activity against enveloped (HIV, viral hepatitis C, influenza virus A) and non-enveloped viruses (poliovirus, adenovirus). Their efficiency was analyzed. Quarterly ammonium compounds (QAC) themselves are not able to properly inactivate non-enveloped viruses. However, they can be successfully applied in combination with other biocides (guanidines, aldehydes). Effective composition of QAC with amines and guanidines provided inactivation of viruses (4.0 lgTCID50) in concentrations of 0.166-0.280% for non-enveloped viruses and 0.080-00.185% for enveloped viruses. The combination of QAC with aldehydes is especially effective (0.04-0.64% for non-enveloped viruses). The virucidal efficiency does not directly depend on the QAC concentration in the chemical disinfectants.
[Mh] Termos MeSH primário: Aldeídos/farmacologia
Desinfetantes/farmacologia
Guanidinas/farmacologia
Compostos de Amônio Quaternário/farmacologia
Inativação de Vírus
[Mh] Termos MeSH secundário: Adenoviridae/efeitos dos fármacos
Adenoviridae/fisiologia
Aldeídos/química
Desinfetantes/química
Guanidinas/química
HIV/efeitos dos fármacos
HIV/fisiologia
Hepacivirus/efeitos dos fármacos
Hepacivirus/fisiologia
Vírus da Influenza A/efeitos dos fármacos
Vírus da Influenza A/fisiologia
Poliovirus/efeitos dos fármacos
Poliovirus/fisiologia
Compostos de Amônio Quaternário/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aldehydes); 0 (Disinfectants); 0 (Guanidines); 0 (Quaternary Ammonium Compounds)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180208
[Lr] Data última revisão:
180208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE


  8 / 17479 MEDLINE  
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[PMID]:29208359
[Au] Autor:Dantas N; de Aquino TM; de Araújo-Júnior JX; da Silva-Júnior E; Gomes EA; Gomes AAS; Siqueira-Júnior JP; Mendonça Junior FJB
[Ad] Endereço:Laboratório de Genética de Microorganismo, Departamento de Biologia Molecular/CCEN/Universidade Federal da Paraíba-UFPB, 58051-970 João Pessoa, PB, Brazil.
[Ti] Título:Aminoguanidine hydrazones (AGH's) as modulators of norfloxacin resistance in Staphylococcus aureus that overexpress NorA efflux pump.
[So] Source:Chem Biol Interact;280:8-14, 2018 Jan 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:One of the promising fields for improving the effectiveness of antimicrobial agents is their combination with efflux pump inhibitors (EPIs), which besides expanding the use of existing antibiotics. The goal of this research was to evaluate a series of aminoguanidine hydrazones (AGH's, 1-19) as antibacterial agents and NorA efflux pump inhibitors in Staphylococcus aureus strain SA-1199B. Molecular modeling and docking studies were also performed in order to explain at the molecular level the interactions of the compounds with the generated NorA efflux pump model. The MICs of the antibiotic and ethidium bromide were determined by microdilution assay in absence or presence of a subinhibitory concentration of aminoguanidine hydrazones and macrophages viability was determined through MTT assay. Bioinformatic software Swiss-Model and AutoDock 4.2 were used to perform modeling and docking studies, respectively. As results, all AGH's were able to potentiate the action for the antibiotic norfloxacin, causing MIC's reduction of 16-fold and 32-fold to ethidium bromide. In the cell viability test, the concentration of 10 µg/mL showed better results than 90% and the concentration of 1000 µg/mL showed the lowest viability, reaching a maximum of 50% for the analyzed aminoguanidine hydrazones. Molecular docking studies showed that both norfloxacin and derivative 13 were recognized by the same binding site of NorA pump, suggesting a competitive mechanism. The present work demonstrated for the first time that AGH derivatives have potential to be putative inhibitors of NorA efflux pump, showing a promising activity as an antibacterial drug development.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Proteínas de Bactérias/metabolismo
Farmacorresistência Bacteriana/efeitos dos fármacos
Inibidores Enzimáticos/farmacologia
Hidrazonas/química
Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo
Staphylococcus aureus/metabolismo
[Mh] Termos MeSH secundário: Animais
Proteínas de Bactérias/antagonistas & inibidores
Sítios de Ligação
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Inibidores Enzimáticos/química
Inibidores Enzimáticos/toxicidade
Guanidinas/química
Hidrazonas/síntese química
Hidrazonas/farmacologia
Camundongos
Testes de Sensibilidade Microbiana
Simulação de Acoplamento Molecular
Proteínas Associadas à Resistência a Múltiplos Medicamentos/antagonistas & inibidores
Norfloxacino/farmacologia
Estrutura Terciária de Proteína
Staphylococcus aureus/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Bacterial Proteins); 0 (Enzyme Inhibitors); 0 (Guanidines); 0 (Hydrazones); 0 (Multidrug Resistance-Associated Proteins); N0F8P22L1P (Norfloxacin); SCQ4EZQ113 (pimagedine)
[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:171207
[St] Status:MEDLINE


  9 / 17479 MEDLINE  
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[PMID]:29175452
[Au] Autor:Kim MS; Kim SH; Jeon D; Kim HY; Lee K
[Ad] Endereço:National Center for Efficacy Evaluation of Respiratory Disease Product, Korea Institute of Toxicology, Jeongeup-si, Jeollabuk-do, 56212, Republic of Korea.
[Ti] Título:Changes in expression of cytokines in polyhexamethylene guanidine-induced lung fibrosis in mice: Comparison of bleomycin-induced lung fibrosis.
[So] Source:Toxicology;393:185-192, 2018 01 15.
[Is] ISSN:1879-3185
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Inhalation of polyhexamethylene guanidine (PHMG) causes irreversible pulmonary injury, such as pulmonary fibrosis. However, the mechanism underlying PHMG-induced lung injury is unclear. In this study, we compared the difference in time-dependent lung injury between PHMG- and bleomycin (BLM)-treated mice and determined cytokines involved in inducing lung injury by performing cytokine antibody array analysis. Mice were treated once with 1.8mg/kg BLM or 1.2mg/kg PHMG through intratracheal instillation and were sacrificed on days 7 and 28. Bronchoalveolar lavage fluid (BALF) analysis showed that the number of neutrophils was significantly higher in PHMG-treated mice than in BLM-treated mice on day 7. Histopathological analysis showed inflammatory cell infiltration and fibrosis mainly in the terminal bronchioles and alveoli in the lungs of PHMG- and BLM-treated mice. However, continuous macrophage infiltration in the alveolar space and bronchioloalveolar epithelial hyperplasia (BEH) were only observed in PHMG-treated mice. Cytokine antibody array analysis showed that 15 and eight cytokines were upregulated in PHMG- and BLM-treated mice, respectively, on day 7. On day 28, 13 and five cytokines were upregulated in PHMG and BLM-treated mice, respectively. In addition, the expressed cytokines between days 7 and 28 in BLM-treated mice were clearly different, but were similar in PHMG-treated mice. Consequently, between PHMG- and BLM-treated mice, we observed differences in the expression patterns and types of cytokines. These differences are considered to be a result of the inflammatory processes induced by both substances, which may mainly involve macrophage infiltration. Therefore, continuous induction of the inflammatory response by PHMG may play an important role in the development of pulmonary fibrosis.
[Mh] Termos MeSH primário: Bleomicina
Citocinas/imunologia
Guanidinas
Fibrose Pulmonar/induzido quimicamente
Fibrose Pulmonar/imunologia
[Mh] Termos MeSH secundário: Animais
Líquido da Lavagem Broncoalveolar/citologia
Contagem de Células
Pulmão/efeitos dos fármacos
Pulmão/imunologia
Pulmão/patologia
Macrófagos/efeitos dos fármacos
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Neutrófilos/efeitos dos fármacos
Fibrose Pulmonar/patologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cytokines); 0 (Guanidines); 11056-06-7 (Bleomycin); 31961-54-3 (polyhexamethyleneguanidine)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:180122
[Lr] Data última revisão:
180122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:29252986
[Au] Autor:Ngufor C; Fongnikin A; Rowland M; N'Guessan R
[Ad] Endereço:London School of Hygiene and Tropical Medicine (LSHTM), London, United Kingdom.
[Ti] Título:Indoor residual spraying with a mixture of clothianidin (a neonicotinoid insecticide) and deltamethrin provides improved control and long residual activity against pyrethroid resistant Anopheles gambiae sl in Southern Benin.
[So] Source:PLoS One;12(12):e0189575, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: There is an urgent need for new insecticides for indoor residual spraying (IRS) which can provide improved and prolonged control of malaria vectors that have developed resistance to existing insecticides. The neonicotinoid, clothianidin represents a class of chemistry new to public health. Clothianidin acts as an agonist on nicotinic acetyl choline receptors. IRS with a mixture of Clothianidin and another WHO approved insecticide such as deltamethrin could provide improved control of insecticide resistant malaria vector populations and serve as a tool for insecticide resistance management. METHODS: The efficacy and residual activity of a novel IRS mixture of deltamethrin and clothianidin was evaluated against wild pyrethroid resistant An. gambiae sl in experimental huts in Cove, Benin. Two application rates of the mixture were tested and comparison was made with clothianidin and deltamethrin applied alone. To assess the residual efficacy of the treatments on different local wall substrates, the inner walls of the experimental huts were covered with either cement, mud or plywood. RESULTS: Clothianidin demonstrated a clear delayed expression in mortality of wild pyrethroid resistant An. gambiae sl in the experimental huts which reached its full effect 120 hours after exposure. Overall mortality over the 12-month hut trial was 15% in the control hut and 24-29% in the deltamethrin-treated huts. The mixture of clothianidin 200mg/m2 and deltamethrin 25mg/m2 induced high overall hut mortality rates (87% on mud walls, 82% on cement walls and 61% on wooden walls) largely due to the clothianidin component and high hut exiting rates (67-76%) mostly due to the deltamethrin component. Mortality rates remained >80% for 8-9 months on mud and cement walls. The residual activity trend was confirmed by results from monthly in situ cone bioassays with laboratory susceptible An. gambiae Kisumu strain. CONCLUSION: IRS campaigns with the mixture of clothianidin plus deltamethrin have the potential to provide prolonged control of malaria transmitted by pyrethroid resistant mosquito populations.
[Mh] Termos MeSH primário: Anopheles
Culex
Guanidinas
Resistência a Inseticidas
Inseticidas
Controle de Mosquitos/métodos
Neonicotinoides
Piretrinas
Tiazóis
[Mh] Termos MeSH secundário: Animais
Benin
Habitação
Seres Humanos
Malária/prevenção & controle
Organização Mundial da Saúde
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Guanidines); 0 (Insecticides); 0 (Neonicotinoids); 0 (Pyrethrins); 0 (Thiazoles); 2V9906ABKQ (clothianidin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180108
[Lr] Data última revisão:
180108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171219
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0189575



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