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Pesquisa : D02.241.081.251.140 [Categoria DeCS]
Referências encontradas : 168 [refinar]
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[PMID]:27402199
[Au] Autor:Kimura M; Mizukami S; Watanabe Y; Onda N; Yoshida T; Shibutani M
[Ad] Endereço:Laboratory of Veterinary Pathology, Tokyo University of Agriculture and Technology, 3-5-8 Saiwai-cho, Fuchu-shi, Tokyo 183-8509, Japan; Pathogenetic Veterinary Science, United Graduate School of Veterinary Sciences, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-1193, Japan.
[Ti] Título:Aberrant cell cycle regulation in rat liver cells induced by post-initiation treatment with hepatocarcinogens/hepatocarcinogenic tumor promoters.
[So] Source:Exp Toxicol Pathol;68(7):399-408, 2016 Aug.
[Is] ISSN:1618-1433
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The present study aimed to determine the onset time of hepatocarcinogen/hepatocarcinogenic tumor promoter-specific cell proliferation, apoptosis and aberrant cell cycle regulation after post-initiation treatment. Six-week-old rats were treated with the genotoxic hepatocarcinogen, carbadox (CRB), the marginally hepatocarcinogenic leucomalachite green (LMG), the tumor promoter, ß-naphthoflavone (BNF) or the non-carcinogenic hepatotoxicant, acetaminophen, for 2, 4 or 6 weeks during the post-initiation phase using a medium-term liver bioassay. Cell proliferation activity, expression of G2 to M phase- and spindle checkpoint-related molecules, and apoptosis were immunohistochemically analyzed at week 2 and 4, and tumor promotion activity was assessed at week 6. At week 2, hepatocarcinogen/tumor promoter-specific aberrant cell cycle regulation was not observed. At week 4, BNF and LMG increased cell proliferation together with hepatotoxicity, while CRB did not. Additionally, BNF and CRB reduced the number of cells expressing phosphorylated-histone H3 in both ubiquitin D (UBD)(+) cells and Ki-67(+) proliferating cells, suggesting development of spindle checkpoint dysfunction, regardless of cell proliferation activity. At week 6, examined hepatocarcinogens/tumor promoters increased preneoplastic hepatic foci expressing glutathione S-transferase placental form. These results suggest that some hepatocarcinogens/tumor promoters increase their toxicity after post-initiation treatment, causing regenerative cell proliferation. In contrast, some genotoxic hepatocarcinogens may disrupt the spindle checkpoint without facilitating cell proliferation at the early stage of tumor promotion. This suggests that facilitation of cell proliferation and disruption of spindle checkpoint function are induced by different mechanisms during hepatocarcinogenesis. Four weeks of post-initiation treatment may be sufficient to induce hepatocarcinogen/tumor promoter-specific cellular responses.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Carcinógenos/toxicidade
Proliferação Celular/efeitos dos fármacos
Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos
Fígado/efeitos dos fármacos
Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Acetaminofen/toxicidade
Animais
Carbadox/toxicidade
Cocarcinogênese
Dietilnitrosamina/toxicidade
Imuno-Histoquímica
Antígeno Ki-67/metabolismo
Fígado/metabolismo
Fígado/patologia
Masculino
Ratos Endogâmicos F344
Corantes de Rosanilina/toxicidade
Fatores de Tempo
beta-Naftoflavona/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carcinogens); 0 (Ki-67 Antigen); 0 (Rosaniline Dyes); 362O9ITL9D (Acetaminophen); 3IQ78TTX1A (Diethylnitrosamine); 6051-87-2 (beta-Naphthoflavone); 8U61G37Z20 (leucomalachite green); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170206
[Lr] Data última revisão:
170206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160713
[St] Status:MEDLINE


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[PMID]:26775945
[Au] Autor:Le T; Zhu L; Yu H
[Ad] Endereço:College of Life Science, Chongqing Normal University, Chongqing 401331, PR China. Electronic address: hnxylt@163.com.
[Ti] Título:Dual-label quantum dot-based immunoassay for simultaneous determination of Carbadox and Olaquindox metabolites in animal tissues.
[So] Source:Food Chem;199:70-4, 2016 May 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A novel and reliable dual-label direct competitive fluorescence-linked immunosorbent assay (dc-FLISA) based on quantum dots (QDs) was developed for the simultaneous determination of the major metabolites of Carbadox and Olaquindox residues in animal tissues, using anti-QCA monoclonal antibodies and anti-MQCA polyclonal antibodies labeled with QD520 and QD635, respectively. The limits of detection for QCA and MQCA were 0.05 and 0.07ng/ml, respectively. The method was used to analyze fortified samples and analyte recoveries ranged from 81.5% to 98.2% (QCA) and 84.2% to 95.7% (MQCA). Good correlations between the dc-FLISA method and HPLC were demonstrated for the determination of QCA and MQCA residues in swine tissue samples, confirming the reliability of the proposed method.
[Mh] Termos MeSH primário: Carbadox/metabolismo
Fluorimunoensaio/métodos
Pontos Quânticos
Quinoxalinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida de Alta Pressão/métodos
Reprodutibilidade dos Testes
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Quinoxalines); G3LAW9U88T (olaquindox); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160118
[Lr] Data última revisão:
160118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160119
[St] Status:MEDLINE


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[PMID]:26558467
[Au] Autor:Kimura M; Mizukami S; Watanabe Y; Hasegawa-Baba Y; Onda N; Yoshida T; Shibutani M
[Ad] Endereço:Laboratory of Veterinary Pathology, Tokyo University of Agriculture and Technology.
[Ti] Título:Disruption of spindle checkpoint function ahead of facilitation of cell proliferation by repeated administration of hepatocarcinogens in rats.
[So] Source:J Toxicol Sci;40(6):855-71, 2015 Dec.
[Is] ISSN:1880-3989
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:We aimed to clarify the hepatocarcinogen-specific disruption of cell cycle checkpoint functions and its time course after repeated administration of hepatocarcinogens. Thus, rats were repeatedly administered with hepatocarcinogens (methapyrilene, carbadox and thioacetamide), a marginal hepatocarcinogen (leucomalachite green), hepatocarcinogenic promoters (oxfendazole and ß-naphthoflavone) or non-carcinogenic hepatotoxicants (promethazine and acetaminophen) for 7, 28 or 90 days, and the temporal changes in cell proliferation, expression of G1/S and spindle checkpoint-related molecules, and apoptosis were examined using immunohistochemistry and/or real-time RT-PCR analysis. Hepatocarcinogens facilitating cell proliferation at day 28 of administration also facilitated cell proliferation and apoptosis at day 90. Hepatocarcinogen- or hepatocarcinogenic promoter-specific cellular responses were not detected by immunohistochemical single molecule analysis even after 90 days. Expression of Cdkn1a, Mad2l1, Chek1 and Rbl2 mRNA also lacked specificity to hepatocarcinogens or hepatocarcinogenic promoters. In contrast, all hepatocarcinogens and the marginally hepatocarcinogenic leucomalachite green induced Mdm2 upregulation or increase in the number of phosphorylated MDM2(+) cells from day 28, irrespective of the lack of cell proliferation facilitation by some compounds. However, different Tp53 expression levels suggest different mechanisms of induction or activation of MDM2 among hepatocarcinogens. On the other hand, hepatocarcinogenic methapyrilene and carbadox downregulated the number of both ubiquitin D(+) cells and proliferating cells remaining in M phase at day 28 and/or day 90, irrespective of the lack of cell proliferation facilitation in the latter. These results suggest that hepatocarcinogens disrupt spindle checkpoint function after 28 or 90 days of administration, which may be induced ahead of cell proliferation facilitation.
[Mh] Termos MeSH primário: Carbadox/toxicidade
Carcinógenos/administração & dosagem
Carcinógenos/toxicidade
Proliferação Celular/efeitos dos fármacos
Fígado/citologia
Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos
Metapirileno/toxicidade
Tioacetamida/toxicidade
[Mh] Termos MeSH secundário: Animais
Apoptose/efeitos dos fármacos
Apoptose/genética
Benzimidazóis/administração & dosagem
Benzimidazóis/toxicidade
Carbadox/administração & dosagem
Proliferação Celular/genética
Quinase do Ponto de Checagem 1
Inibidor de Quinase Dependente de Ciclina p21/genética
Inibidor de Quinase Dependente de Ciclina p21/metabolismo
Expressão Gênica/efeitos dos fármacos
Masculino
Metapirileno/administração & dosagem
Proteínas Quinases/genética
Proteínas Quinases/metabolismo
Ratos Endogâmicos F344
Corantes de Rosanilina/toxicidade
Fatores de Tempo
Ubiquitinas/genética
Ubiquitinas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Carcinogens); 0 (Cdkn1a protein, rat); 0 (Cyclin-Dependent Kinase Inhibitor p21); 0 (Rosaniline Dyes); 0 (UBD protein, human); 0 (Ubiquitins); 075T165X8M (Thioacetamide); 8U61G37Z20 (leucomalachite green); A01LX40298 (Methapyrilene); EC 2.7.- (Protein Kinases); EC 2.7.11.1 (CHEK1 protein, human); EC 2.7.11.1 (Checkpoint Kinase 1); EC 2.7.11.1 (Chek1 protein, rat); M2X04R2E2Y (Carbadox); OMP2H17F9E (oxfendazole)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151113
[St] Status:MEDLINE
[do] DOI:10.2131/jts.40.855


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[PMID]:26468892
[Au] Autor:Ferrey ML; Heiskary S; Grace R; Hamilton MC; Lueck A
[Ad] Endereço:Minnesota Pollution Control Agency, St. Paul, Minnesota, USA.
[Ti] Título:Pharmaceuticals and other anthropogenic tracers in surface water: a randomized survey of 50 Minnesota lakes.
[So] Source:Environ Toxicol Chem;34(11):2475-88, 2015 Nov.
[Is] ISSN:1552-8618
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Water from 50 randomly selected lakes across Minnesota, USA, was analyzed for pharmaceuticals, personal care products, hormones, and other commercial or industrial chemicals in conjunction with the US Environmental Protection Agency's 2012 National Lakes Assessment. Thirty-eight of the 125 chemicals analyzed were detected at least once, all at parts per trillion concentrations. The most widely detected was N,N-diethyl-m-toluamide, present in 48% of the lakes sampled. Amitriptyline, a widely used antidepressant, was found in 28% of the lakes. The endocrine active chemicals bisphenol A, androstenedione, and nonylphenol were found in 42%, 30%, and 10% of the lakes, respectively. Cocaine was found in 32% of the lakes, and its degradation product, benzoylecgonine, was detected at 28% of the locations. Carbadox, an antibiotic used solely in the production of swine, was also present in 28% of the lakes sampled. The means by which these and other chemicals were transported to several of the remote lakes is unclear but may involve atmospheric transport.
[Mh] Termos MeSH primário: Água Doce/análise
Lagos/química
Preparações Farmacêuticas/análise
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Amitriptilina/análise
Androstenodiona/análise
Animais
Antidepressivos/análise
Compostos Benzidrílicos/análise
Carbadox/análise
Cromatografia Líquida de Alta Pressão
Cocaína/análise
Cocaína/química
DEET/análise
Monitoramento Ambiental
Minnesota
Preparações Farmacêuticas/química
Fenóis/análise
Espectrometria de Massas por Ionização por Electrospray
Suínos
Estados Unidos
Poluentes Químicos da Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antidepressive Agents); 0 (Benzhydryl Compounds); 0 (Pharmaceutical Preparations); 0 (Phenols); 0 (Water Pollutants, Chemical); 134-62-3 (DEET); 1806D8D52K (Amitriptyline); 409J2J96VR (Androstenedione); 79F6A2ILP5 (nonylphenol); I5Y540LHVR (Cocaine); M2X04R2E2Y (Carbadox); MLT3645I99 (bisphenol A)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151016
[St] Status:MEDLINE
[do] DOI:10.1002/etc.3125


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[PMID]:26452885
[Au] Autor:Souza Dibai WL; de Alkimin Filho JF; da Silva Oliveira FA; Sampaio de Assis DC; Camargos Lara LJ; de Figueiredo TC; de Vasconcelos Cançado S
[Ad] Endereço:Laboratório Nacional Agropecuário (Lanagro-MG), Av. Rômulo Joviano, s/n -Pedro Leopoldo-MG, CEP 33.600-000, Brazil.
[Ti] Título:HPLC-MS/MS method validation for the detection of carbadox and olaquindox in poultry and swine feedingstuffs.
[So] Source:Talanta;144:740-4, 2015 Nov 01.
[Is] ISSN:1873-3573
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Carbadox (CBX) and olaquindox (OLA) were used in poultry and swine feed for growth promotion, to improve feed efficiency and increase the rate of weight gain. However, the use of these agents in feedingstuffs was prohibited because of concerns about their toxicity. Regulatory laboratories are required to have suitably validated analytical methods to ensure compliance with the ban. A quantitative and confirmatory method for determining the presence of CBX and OLA in poultry and swine feed by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was developed, optimized, and validated. The analytes extraction was performed with a mixture of water and acetonitrile (1:1v/v) and cleanup with hexane and C18 (dispersive phase). The method was evaluated by the following parameters: specificity, linearity, matrix effect, decision limits (CCα), detection capability (CCß), accuracy, precision, limits of detection (LoD), limits of quantification (LoQ) and measurement uncertainty. The validated method presented a broad linear study range and no significant matrix effect. The limit of detection (LoD) was defined at 9 µg kg(-1) for CBX and 80 µg kg(-1) for OLA, and the limit of quantification (LoQ) was defined at 12 µg kg(-1) and 110 µg kg(-1) for CBX and OLA, respectively. The accuracy of the method was adequate for CBX and OLA. The recovery values found in the repeatability conditions were 99.41% for CBX and 104.62% for OLA. Under intralaboratory reproducibility conditions, the values were 98.63% for CBX and 95.07% for OLA. It was concluded that the performance parameters demonstrated total method adequacy for the detection and quantification of CBX and OLA in poultry and swine feedingstuffs.
[Mh] Termos MeSH primário: Ração Animal/análise
Carbadox/análise
Análise de Alimentos/métodos
Contaminação de Alimentos/análise
Aves Domésticas
Quinoxalinas/análise
Suínos
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida de Alta Pressão
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Quinoxalines); G3LAW9U88T (olaquindox); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:151010
[Lr] Data última revisão:
151010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151011
[St] Status:MEDLINE


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[PMID]:26400201
[Au] Autor:Segato G; Biancotto G; Agnoletti F; Berto G; Montesissa C; Benetti C
[Ad] Endereço:a Food Safety Department - Chemistry Laboratory , Istituto Zooprofilattico Sperimentale delle Venezie , Legnaro , Italy.
[Ti] Título:In vivo studies to highlight possible illegal treatments of rabbits with carbadox and olaquindox.
[So] Source:Food Addit Contam Part A Chem Anal Control Expo Risk Assess;32(12):1976-91, 2015.
[Is] ISSN:1944-0057
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:For the treatment of rabbit dysentery and bacterial enteritis, veterinary practitioners often adopt veterinary medicinal products authorised for other food-producing species, but in some cases non-authorised drugs frequently used in the past, such as carbadox and olaquindox, might be illegally adopted. To verify the carbadox and olaquindox distribution and persistence in rabbit tissues, two independent in vivo studies were carried out. In the first study, 24 healthy rabbits received water medicated with carbadox at 100 mg l(-1) over a period 28 days, whereas in the second one, 24 healthy rabbits were administered water containing olaquindox at 100 mg l(-1). In each study rabbits were randomly assigned to four groups to be sacrificed respectively at 0, 5, 10 and 20 days from treatment withdrawal, for depletion studies. A control group of six animals was adopted for control and as a reservoir of blank tissues. Muscle and liver samples collected from each treated animal were stored at -20°C pending the analysis. Sensitive and robust liquid chromatography-tandem mass spectrometry analytical methods were set up for the parent compounds and their main metabolites quinoxaline-2-carboxylic acid, desoxycarbadox and 3-methylquinoxaline-2-carboxylic acid to verify their residual. Data collected demonstrate that the combination of liver as target matrix, quinoxaline-2-carboxylic acid and 3-methylquinoxaline-2-carboxylic acid as marker residue and enzymatic digestion is strategic to evidence carbadox and/or olaquindox illegal treatments in rabbits, even 20 days after treatment withdrawal at concentration levels higher than 0.5 µg kg(-1). This findings suggests that liver should be proposed as target matrix for official control in national monitoring plan.
[Mh] Termos MeSH primário: Anti-Infecciosos/isolamento & purificação
Carbadox/isolamento & purificação
Carcinógenos/isolamento & purificação
Fígado/química
Quinoxalinas/isolamento & purificação
Drogas Veterinárias/isolamento & purificação
[Mh] Termos MeSH secundário: Animais
Anti-Infecciosos/metabolismo
Anti-Infecciosos/farmacocinética
Biotransformação
Carbadox/metabolismo
Carbadox/farmacocinética
Carcinógenos/metabolismo
Carcinógenos/farmacocinética
Cromatografia Líquida
Resíduos de Drogas/isolamento & purificação
Resíduos de Drogas/metabolismo
Análise de Alimentos/métodos
Fígado/metabolismo
Masculino
Músculo Esquelético/química
Músculo Esquelético/metabolismo
Quinoxalinas/metabolismo
Quinoxalinas/farmacocinética
Coelhos
Espectrometria de Massas em Tandem
Drogas Veterinárias/metabolismo
Drogas Veterinárias/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (3-methylquinoxaline-2-carboxylic acid); 0 (Anti-Infective Agents); 0 (Carcinogens); 0 (Quinoxalines); 0 (Veterinary Drugs); G3LAW9U88T (olaquindox); M2X04R2E2Y (Carbadox); M5OE8SN42M (quinoxaline-2-carboxylic acid)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151127
[Lr] Data última revisão:
151127
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150925
[St] Status:MEDLINE
[do] DOI:10.1080/19440049.2015.1086822


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[PMID]:25267663
[Au] Autor:Kulakova L; Galkin A; Chen CZ; Southall N; Marugan JJ; Zheng W; Herzberg O
[Ad] Endereço:Institute for Bioscience and Biotechnology Research, University of Maryland, Rockville, Maryland, USA.
[Ti] Título:Discovery of novel antigiardiasis drug candidates.
[So] Source:Antimicrob Agents Chemother;58(12):7303-11, 2014 Dec.
[Is] ISSN:1098-6596
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Giardiasis is a severe intestinal parasitic disease caused by Giardia lamblia, which inflicts many people in poor regions and is the most common parasitic infection in the United States. Current standard care drugs are associated with undesirable side effects, treatment failures, and an increasing incidence of drug resistance. As follow-up to a high-throughput screening of an approved drug library, which identified compounds lethal to G. lamblia trophozoites, we have determined the minimum lethal concentrations of 28 drugs and advanced 10 of them to in vivo studies in mice. The results were compared to treatment with the standard care drug, metronidazole, in order to identify drugs with equal or better anti-Giardia activities. Three drugs, fumagillin, carbadox, and tioxidazole, were identified. These compounds were also potent against metronidazole-resistant human G. lamblia isolates (assemblages A and B), as determined in in vitro assays. Of these three compounds, fumagillin is currently an orphan drug used within the European Union to treat microsporidiosis in immunocompromised individuals, whereas carbadox and tioxidazole are used in veterinary medicine. A dose-dependent study of fumagillin in a giardiasis mouse model revealed that the effective dose of fumagillin was ∼ 100-fold lower than the metronidazole dose. Therefore, fumagillin may be advanced to further studies as an alternative treatment for giardiasis when metronidazole fails.
[Mh] Termos MeSH primário: Antiprotozoários/farmacologia
Cicloexanos/farmacologia
Descoberta de Drogas
Ácidos Graxos Insaturados/farmacologia
Giardia lamblia/efeitos dos fármacos
Giardíase/tratamento farmacológico
Trofozoítos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Aminopeptidases/antagonistas & inibidores
Aminopeptidases/química
Animais
Antiprotozoários/química
Cultura Axênica
Carbadox/química
Carbadox/farmacologia
Cicloexanos/química
Resistência a Medicamentos
Ácidos Graxos Insaturados/química
Giardia lamblia/crescimento & desenvolvimento
Giardíase/parasitologia
Glicoproteínas/antagonistas & inibidores
Glicoproteínas/química
Ensaios de Triagem em Larga Escala
Seres Humanos
Concentração Inibidora 50
Metronidazol/farmacologia
Camundongos
Testes de Sensibilidade Parasitária
Sesquiterpenos/química
Sesquiterpenos/farmacologia
Especificidade da Espécie
Relação Estrutura-Atividade
Tiazóis/química
Tiazóis/farmacologia
Trofozoítos/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, N.I.H., INTRAMURAL
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Cyclohexanes); 0 (Fatty Acids, Unsaturated); 0 (Glycoproteins); 0 (Sesquiterpenes); 0 (Thiazoles); 140QMO216E (Metronidazole); 7OW73204U1 (fumagillin); EC 3.4.11.- (Aminopeptidases); EC 3.4.11.18 (METAP2 protein, human); EC 3.4.11.18 (Metap2 protein, mouse); M2X04R2E2Y (Carbadox); NZW046NI85 (tioxidazole)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141001
[St] Status:MEDLINE
[do] DOI:10.1128/AAC.03834-14


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[PMID]:24291715
[Au] Autor:Sniegocki T; Gbylik-Sikorska M; Posyniak A; Zmudzki J
[Ad] Endereço:Department of Pharmacology and Toxicology, National Veterinary Research Institute, 24-100 Pulawy, Poland. Electronic address: sniego@piwet.pulawy.pl.
[Ti] Título:Determination of carbadox and olaquindox metabolites in swine muscle by liquid chromatography/mass spectrometry.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;944:25-9, 2014 Jan 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This paper presents LC-MS/MS method that was developed for the simultaneous determination and confirmation metabolites of carbadox (desoxycarbadox, quinoxaline-2-carboxylic) and olaquindox (3-methylquinoxaline-2-carboxylic acid) residues in pig muscle tissues at concentrations ≤3.0µgkg(-1). Pig muscle tissues were deproteinated with meta-phosphoric acid in methanol and then were extracted with ethyl acetate:dichloromethane (50:50, v/v). The whole extracts were evaporated to dryness in rotary evaporator at 45°C, and dry residues were re-dissolved in 0.5% isopropanol in 1% acetic acid. The LC separation was performed on a C8 column with a gradient system consisting of isopropanol/water/acetic acid and methanol as the mobile phase. Additionally SelexION™ technology to reduce matrix effect was used. The decision limit (CCα) ranged from 1.04µgkg(-1) to 2.11µgkg(-1) and the detection capability (CCß) ranged from 1.46µgkg(-1) to 2.89µgkg(-1). The total recoveries were from 99.8% to 101.2%. The results of validation fulfil the requirement of the confirmatory criteria according to the European Commission Decision 2002/657/EC.
[Mh] Termos MeSH primário: Carbadox/análise
Cromatografia Líquida/métodos
Quinoxalinas/análise
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Carbadox/química
Resíduos de Drogas/análise
Limite de Detecção
Músculos/química
Quinoxalinas/química
Reprodutibilidade dos Testes
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Quinoxalines); G3LAW9U88T (olaquindox); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1407
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131203
[St] Status:MEDLINE


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[PMID]:23957215
[Au] Autor:Chen Y; Zhang H
[Ad] Endereço:Department of Civil and Environmental Engineering, Temple University , Philadelphia, Pennsylvania 19122, United States.
[Ti] Título:Complexation facilitated reduction of aromatic N-oxides by aqueous Fe(II)-tiron complex: reaction kinetics and mechanisms.
[So] Source:Environ Sci Technol;47(19):11023-31, 2013 Oct 01.
[Is] ISSN:1520-5851
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Rapid reduction of carbadox (CDX), olaquindox and several other aromatic N-oxides were investigated in aqueous solution containing Fe(II) and tiron. Consistent with previous work, the 1:2 Fe(II)-tiron complex, FeL2(6-), is the dominant reactive species as its concentration linearly correlates with the observed rate constant kobs under various conditions. The N-oxides without any side chains were much less reactive, suggesting direct reduction of the N-oxides is slow. UV-vis spectra suggest FeL2(6-) likely forms 5- or 7-membered rings with CDX and olaquindox through the N and O atoms on the side chain. The formed inner-sphere complexes significantly facilitated electron transfer from FeL2(6-) to the N-oxides. Reduction products of the N-oxides were identified by HPLC/QToF-MS to be the deoxygenated analogs. QSAR analysis indicated neither the first electron transfer nor N-O bond cleavage is the rate-limiting step. Calculations of the atomic spin densities of the anionic N-oxides confirmed the extensive delocalization between the aromatic ring and the side chain, suggesting complex formation can significantly affect the reduction kinetics. Our results suggest the complexation facilitated N-oxide reduction by Fe(II)-tiron involves a free radical mechanism, and the subsequent deoxygenation might also benefit from the weak complexation of Fe(II) with the N-oxide O atom.
[Mh] Termos MeSH primário: Sal Dissódico do Ácido 1,2-Di-Hidroxibenzeno-3,5 Dissulfônico/química
Carbadox/química
Ferro/química
Óxidos/química
Quinoxalinas/química
Poluentes Químicos da Água/química
[Mh] Termos MeSH secundário: Oxirredução
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Oxides); 0 (Quinoxalines); 0 (Water Pollutants, Chemical); 4X87R5T106 (1,2-Dihydroxybenzene-3,5-Disulfonic Acid Disodium Salt); E1UOL152H7 (Iron); G3LAW9U88T (olaquindox); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1405
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130821
[St] Status:MEDLINE
[do] DOI:10.1021/es402655a


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[PMID]:23726999
[Au] Autor:Yang J; Liu Z; Li M; Qiu X
[Ad] Endereço:State Key Laboratory of Integrated Management of Pest Insects and Rodents, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China.
[Ti] Título:Hydroxylation of quinocetone and carbadox is mediated by CYP1As in the chicken (Gallus gallus).
[So] Source:Comp Biochem Physiol C Toxicol Pharmacol;158(2):84-90, 2013 Aug.
[Is] ISSN:1532-0456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Quinoxaline derivatives (quinoxalines) comprise a class of drugs that have been widely used as animal antimicrobial agents and feed additives. Although the metabolism of quinoxaline drugs has been mostly studied using chicken liver microsomes, the biochemical mechanism of biotransformation of these chemicals in the chicken has yet to be characterized. In this study, using bacteria produced enzymes, we demonstrated that both CYP1A4 and CYP1A5 participate in the oxidative metabolism of quinoxalines. For CYP1A5, three hydroxylated metabolites of quinocetone were generated. In addition, CYP1A5 is able to hydroxylate carbadox. For CYP1A4, only one hydroxylated product of quinocetone on the phenyl ring was identified. Neither CYP1A5 nor CYP1A4 showed hydroxylation activity towards mequindox and cyadox. Our results suggest that CYP1A4 and CYP1A5 have different and somewhat overlapping substrate specificity in quinoxaline metabolism, and CYP1A5 represents a crucial enzyme in hydroxylation of both quinocetone and carbadox.
[Mh] Termos MeSH primário: Hidrocarboneto de Aril Hidroxilases/metabolismo
Proteínas Aviárias/metabolismo
Carbadox/metabolismo
Quinoxalinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Galinhas
Hidroxilação
Microssomos Hepáticos/metabolismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Avian Proteins); 0 (Quinoxalines); 0 (quinocetone); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (CYP1A4 protein, Gallus gallus); EC 1.14.14.1 (cytochrome P-450 CYP1A5); M2X04R2E2Y (Carbadox)
[Em] Mês de entrada:1401
[Cu] Atualização por classe:130701
[Lr] Data última revisão:
130701
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130604
[St] Status:MEDLINE



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