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  1 / 17 MEDLINE  
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[PMID]:28259840
[Au] Autor:Mohd Siddique MU; McCann GJ; Sonawane VR; Horley N; Gatchie L; Joshi P; Bharate SB; Jayaprakash V; Sinha BN; Chaudhuri B
[Ad] Endereço:Department of Pharmaceutical Sciences & Technology, Birla Institute of Technology, Mesra, Ranchi, 835215, India.
[Ti] Título:Quinazoline derivatives as selective CYP1B1 inhibitors.
[So] Source:Eur J Med Chem;130:320-327, 2017 Apr 21.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:CYP1B1 is implicated to have a role in the development of breast, ovarian, renal, skin and lung carcinomas. It has been suggested that identification of potent and specific CYP1B1 inhibitors can lead to a novel treatment of cancer. Flavonoids have a compact rigid skeleton which fit precisely within the binding cavity of CYP1B1. Systematic isosteric replacement of flavonoid 'O' atom with 'N' atom led to the prediction that a 'quinazoline' scaffold could be the basis for designing potential CYP1B1 inhibitors. A total of 20 quinazoline analogs were synthesized and screened for CYP1B1 and CYP1A1 inhibition in Sacchrosomes™. IC determinations of six compounds with capability of inhibiting CYP1B1 identified quinazolines 5c and 5h as the best candidates for CYP1B1 inhibition, with IC values in the nM range. Further selectivity studies with homologous CYPs, belonging to the CYP1, CYP2 and CYP3 family of enzymes, showed that the compounds are likely to be free from critical drug-drug interaction liability. Molecular modelling studies were performed to rationalize the observed enzymatic inhibitions. Further biological studies in live yeast and human cells, harboring CYP1A1 and CYP1B1 enzymes, have illustrated the most potent compounds' cellular permeability and capability of potently inhibiting CYP1B1 enzyme expressed within live cells.
[Mh] Termos MeSH primário: Antineoplásicos/química
Citocromo P-450 CYP1B1/antagonistas & inibidores
Quinazolinas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/farmacocinética
Antineoplásicos/farmacologia
Permeabilidade da Membrana Celular
Células Cultivadas
Citocromo P-450 CYP1A1
Família 2 do Citocromo P450/efeitos dos fármacos
Família 3 do Citocromo P450/efeitos dos fármacos
Inibidores Enzimáticos/química
Inibidores Enzimáticos/farmacocinética
Seres Humanos
Modelos Moleculares
Quinazolinas/química
Quinazolinas/farmacocinética
Leveduras/citologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Enzyme Inhibitors); 0 (Quinazolines); EC 1.14.14.1 (CYP1A1 protein, human); EC 1.14.14.1 (CYP1B1 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A1); EC 1.14.14.1 (Cytochrome P-450 CYP1B1); EC 1.14.14.1 (Cytochrome P450 Family 2); EC 1.14.14.1 (Cytochrome P450 Family 3)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170322
[Lr] Data última revisão:
170322
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170306
[St] Status:MEDLINE


  2 / 17 MEDLINE  
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[PMID]:27498925
[Au] Autor:Toselli F; Dodd PR; Gillam EM
[Ad] Endereço:a Department of Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit , AstraZeneca , Mölndal , Sweden ;
[Ti] Título:Emerging roles for brain drug-metabolizing cytochrome P450 enzymes in neuropsychiatric conditions and responses to drugs.
[So] Source:Drug Metab Rev;48(3):379-404, 2016 Aug.
[Is] ISSN:1097-9883
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:P450s in the human brain were originally considered unlikely to contribute significantly to the clearance of drugs and other xenobiotic chemicals, since their overall expression was a small fraction of that found in the liver. However, it is now recognized that P450s play substantial roles in the metabolism of both exogenous and endogenous chemicals in the brain, but in a highly cell type- and region-specific manner, in line with the greater functional heterogeneity of the brain compared to the liver. Studies of brain P450 expression and the characterization of the catalytic activity of specific forms expressed as recombinant enzymes have suggested possible roles for xenobiotic-metabolizing P450s in the brain. It is now possible to confirm these roles through the use of intracerebroventricular administration of selective P450 inhibitors in animal models, coupled with brain sampling techniques to measure drug concentrations in vivo, and modern neuroimaging techniques. The purpose of this review is to discuss the evidence behind the functional importance of P450s from the "xenobiotic-metabolizing" families, CYP1, CYP2 and CYP3 in the brain. Approaches used to define the quantitative and qualitative significance of these P450s in determining tissue-specific levels of xenobiotics in brain will be considered. Finally, the possible roles of these enzymes in brain biochemistry will be examined in light of the demonstrated activity of these enzymes in vitro and the association of particular P450 forms with disease states.
[Mh] Termos MeSH primário: Encéfalo/enzimologia
Família 1 do Citocromo P450/metabolismo
Família 2 do Citocromo P450/metabolismo
Família 3 do Citocromo P450/metabolismo
Transtornos Mentais/enzimologia
Xenobióticos/metabolismo
[Mh] Termos MeSH secundário: Animais
Encéfalo/fisiologia
Inibidores das Enzimas do Citocromo P-450/farmacologia
Família 1 do Citocromo P450/fisiologia
Família 2 do Citocromo P450/fisiologia
Família 3 do Citocromo P450/fisiologia
Seres Humanos
Fígado/metabolismo
Transtornos Mentais/fisiopatologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Xenobiotics); EC 1.14.14.1 (Cytochrome P450 Family 1); EC 1.14.14.1 (Cytochrome P450 Family 2); EC 1.14.14.1 (Cytochrome P450 Family 3)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160809
[St] Status:MEDLINE
[do] DOI:10.1080/03602532.2016.1221960


  3 / 17 MEDLINE  
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[PMID]:27118859
[Au] Autor:Guo M; Dai X; Hu D; Zhang Y; Sun Y; Ren W; Wang L
[Ad] Endereço:Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Nanjing Agricultural University, Nanjing, Jiangsu Province, 210095, PR China Center for Safety Evaluation of Drugs, Science and Technology Division, Nanjing University of Traditional Chinese Medicine, Nanjing 21002
[Ti] Título:Potential pharmacokinetic effect of rifampicin on enrofloxacin in broilers: Roles of P-glycoprotein and BCRP induction by rifampicin.
[So] Source:Poult Sci;95(9):2129-35, 2016 Sep 01.
[Is] ISSN:1525-3171
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:P-glycoprotein ( P-GP: , encoding gene Abcb1) and Breast Cancer Resistance Protein ( BCRP: , encoding gene Abcg2) are transport proteins that play a major role in modulating the bioavailability of oral drugs in humans and rodents. It has been shown that rifampicin is the typical inducer of P-gp in rodents by activating the nuclear receptor. However, its effect on Abcb1, Abcg2, CYP3A, and chicken xenobiotic-sensing orphan nuclear receptor ( CXR: ) mRNA expression in broilers is poorly understood. This study explored the effect of rifampicin on mRNA expression of Abcb1, Abcg2, CYP3A37, CXR as well as its effect on the pharmacokinetics of enrofloxacin in broilers. The mRNA levels of Abcb1, Abcg2, CYP3A37, and CXR were significantly increased in the liver (except Abcg2), kidney, jejunum, and ileum (P < 0.05) but not significantly changed in the duodenum (P > 0.05) after treated with rifampicin. Further analysis revealed that the variation tendencies of Abcb1, Abcg2, and CYP3A37 expression levels were significantly correlated with CXR mRNA expression levels in liver, kidney, jejunum, and ileum. Coadministration of rifampicin significantly changed the pharmacokinetic behavior of enrofloxacin orally administered by showing clearly lower AUC0-∞, AUC0-t, and Cmax as well as longer Tmax. The bioavailability of orally administered enrofloxacin was decreased from 72.5% to 24.8% by rifampicin. However, rifampicin did not significantly change the pharmacokinetics of enrofloxacin following intravenous administration. Our study shows that rifampicin up-regulated the small intestinal level of P-gp and BCRP and suggests that P-gp and BCRP are key factors that affected pharmacokinetic behavior of orally administered enrofloxacin by limiting its absorption from the intestine in broilers.
[Mh] Termos MeSH primário: Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/genética
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética
Proteínas Aviárias/genética
Galinhas/genética
Galinhas/metabolismo
Rifampina/farmacocinética
[Mh] Termos MeSH secundário: Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Animais
Antibacterianos/metabolismo
Antibacterianos/farmacocinética
Hidrocarboneto de Aril Hidroxilases/genética
Hidrocarboneto de Aril Hidroxilases/metabolismo
Proteínas Aviárias/metabolismo
Disponibilidade Biológica
Família 3 do Citocromo P450/genética
Família 3 do Citocromo P450/metabolismo
Feminino
Fluoroquinolonas/metabolismo
Expressão Gênica
Masculino
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Distribuição Aleatória
Receptores Citoplasmáticos e Nucleares/genética
Receptores Citoplasmáticos e Nucleares/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP Binding Cassette Transporter, Sub-Family G, Member 2); 0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Anti-Bacterial Agents); 0 (Avian Proteins); 0 (CXR protein, chicken); 0 (Fluoroquinolones); 0 (RNA, Messenger); 0 (Receptors, Cytoplasmic and Nuclear); 3DX3XEK1BN (enrofloxacin); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken)); VJT6J7R4TR (Rifampin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160428
[St] Status:MEDLINE
[do] DOI:10.3382/ps/pew148


  4 / 17 MEDLINE  
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[PMID]:24498193
[Au] Autor:Guo M; Sun Y; Zhang Y; Bughio S; Dai X; Ren W; Wang L
[Ad] Endereço:Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Nanjing Agricultural University, Nanjing, Jiangsu Province, PR China.
[Ti] Título:E. coli infection modulates the pharmacokinetics of oral enrofloxacin by targeting P-glycoprotein in small intestine and CYP450 3A in liver and kidney of broilers.
[So] Source:PLoS One;9(1):e87781, 2014.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:P-glycoprotein (P-gp) expression determines the absorption, distribution, metabolism and excretion of many drugs in the body. Also, up-regulation of P-gp acts as a defense mechanism against acute inflammation. This study examined expression levels of abcb1 mRNA and localization of P-gp protein in the liver, kidney, duodenum, jejunum and ileum in healthy and E. coli infected broilers by real time RT-PCR and immunohistochemistry. Meanwhile, pharmacokinetics of orally administered enrofloxacin was also investigated in healthy and infected broilers by HPLC. The results indicated that E. coli infection up-regulated expression of abcb1 mRNA levels significantly in the kidney, jejunum and ileum (P<0.05), but not significantly in the liver and duodenum (P>0.05). However, the expression level of CYP 3A37 mRNA were observed significantly decreased only in liver and kidney of E. coli infected broilers (P<0.05) compared with healthy birds. Furthermore, the infection reduced absorption of orally administered enrofloxacin, significantly decreased Cmax (0.34 vs 0.98 µg mL(-1), P = 0.000) and AUC0-12h (4.37 vs 8.88 µg mL(-1) h, P = 0.042) of enrofloxacin, but increased Tmax (8.32 vs 3.28 h, P = 0.040), T1/2a(2.66 vs 1.64 h(-1), P = 0.050) and V/F (26.7 vs 5.2 L, P = 0.040). Treatment with verapamil, an inhibitor of P-gp, significantly improved the absorption of enrofloxacin in both healthy and infected broilers. The results suggest that the E. coli infection induces intestine P-gp expression, altering the absorption of orally administered enrofloxacin in broilers.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Antineoplásicos/farmacologia
Hidrocarboneto de Aril Hidroxilases/metabolismo
Proteínas Aviárias/metabolismo
Infecções por Escherichia coli
Fluoroquinolonas/farmacologia
Enteropatias
Intestinos/metabolismo
Rim/metabolismo
Fígado/metabolismo
Doenças das Aves Domésticas
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
Animais
Proteínas Aviárias/antagonistas & inibidores
Galinhas
Família 3 do Citocromo P450
Infecções por Escherichia coli/tratamento farmacológico
Infecções por Escherichia coli/metabolismo
Infecções por Escherichia coli/patologia
Feminino
Enteropatias/tratamento farmacológico
Enteropatias/metabolismo
Enteropatias/patologia
Intestinos/patologia
Rim/patologia
Fígado/patologia
Masculino
Doenças das Aves Domésticas/tratamento farmacológico
Doenças das Aves Domésticas/metabolismo
Doenças das Aves Domésticas/patologia
Verapamil/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Antineoplastic Agents); 0 (Avian Proteins); 0 (Fluoroquinolones); 3DX3XEK1BN (enrofloxacin); CJ0O37KU29 (Verapamil); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken))
[Em] Mês de entrada:1410
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140206
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0087781


  5 / 17 MEDLINE  
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[PMID]:24090734
[Au] Autor:Yuan Y; Zhou X; Yang J; 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:T-2 toxin is hydroxylated by chicken CYP3A37.
[So] Source:Food Chem Toxicol;62:622-7, 2013 Dec.
[Is] ISSN:1873-6351
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:T-2 toxin (T-2) is an acute toxic trichothecene mycotoxin produced mainly by Fusarium species, detected in many crops including oats, wheat and barley, in animal feed and food. It is important to know the metabolic pathway and kinetics of T-2 in food animals given that T-2 can cause serious adverse effects on human health. In this study, we investigated the metabolic capacity of chicken CYP3A37 in the metabolism of T-2 using reconstituted bacteria produced enzymes. Our results showed that chicken CYP3A37 is able to convert T-2 to 3'-OH T-2 with an apparent Km of 15.29 µM, and T-2 hydroxylation activity of CYP3A37 is strongly inhibited by ketoconazole (IC50=0.11 µM). We also observed that chicken CYP3A37 can catalyze erythromycin N-demethylation, another CYP3A-specific activity. These findings imply that chicken CYP3A37 may have a broad substrate spectrum, similar to its human homologue CYP3A4.
[Mh] Termos MeSH primário: Hidrocarboneto de Aril Hidroxilases/metabolismo
Toxina T-2/metabolismo
[Mh] Termos MeSH secundário: Animais
Hidrocarboneto de Aril Hidroxilases/antagonistas & inibidores
Hidrocarboneto de Aril Hidroxilases/genética
Galinhas
Citocromo P-450 CYP3A/metabolismo
Família 3 do Citocromo P450
Citocromos b5/genética
Escherichia coli/genética
Hidroxilação
Cetoconazol/farmacologia
Proteínas Recombinantes/genética
Proteínas Recombinantes/metabolismo
Toxina T-2/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Recombinant Proteins); 9035-39-6 (Cytochromes b5); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P-450 CYP3A); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken)); I3FL5NM3MO (T-2 Toxin); R9400W927I (Ketoconazole)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:161128
[Lr] Data última revisão:
161128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131005
[St] Status:MEDLINE


  6 / 17 MEDLINE  
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[PMID]:23330986
[Au] Autor:Osselaere A; De Bock L; Eeckhaut V; De Backer P; Van Bocxlaer J; Boussery K; Croubels S
[Ad] Endereço:Department of Pharmacology, Toxicology and Biochemistry, Faculty of Veterinary Medicine, Ghent University, Merelbeke, Belgium.
[Ti] Título:Hepatic and intestinal CYP3A expression and activity in broilers.
[So] Source:J Vet Pharmacol Ther;36(6):588-93, 2013 Dec.
[Is] ISSN:1365-2885
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Cytochrome P450 is involved in drug metabolism. Subfamily CYP3A shows a degree of similarity across different animal species. However, little information is available about its expression and activity in broiler chickens. A RT-PCR method was developed for the quantification of CYP3A37 expression in the liver and small intestine of broilers. A higher expression in the jejunum was observed compared with that in the ileum. In the liver, a significantly lower expression compared with that in the jejunum was noticed. Thus, the role of the small bowel in drug metabolism cannot be neglected in broilers. CYP3A activity was studied in vitro using midazolam as a substrate. Two protocols for the preparation of intestinal microsomes were compared. Mincing of the tissues before ultracentrifugation seemed to be more appropriate than a protocol based on ethylenediaminetetra-acetic acid separation. CYP3A activity revealed to be the highest in the duodenum with a decreasing trend towards the ileum. Activity in liver was comparable to duodenal activity.
[Mh] Termos MeSH primário: Hidrocarboneto de Aril Hidroxilases/metabolismo
Galinhas
Regulação Enzimológica da Expressão Gênica/fisiologia
Intestinos/enzimologia
Fígado/enzimologia
[Mh] Termos MeSH secundário: Animais
Hidrocarboneto de Aril Hidroxilases/genética
Família 3 do Citocromo P450
Feminino
Intestinos/metabolismo
Fígado/metabolismo
Masculino
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (RNA, Messenger); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken))
[Em] Mês de entrada:1407
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130122
[St] Status:MEDLINE
[do] DOI:10.1111/jvp.12034


  7 / 17 MEDLINE  
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[PMID]:22302310
[Au] Autor:Cassone CG; Vongphachan V; Chiu S; Williams KL; Letcher RJ; Pelletier E; Crump D; Kennedy SW
[Ad] Endereço:Environment Canada, National Wildlife Research Centre, Ottawa, Ontario, Canada K1A 0H3.
[Ti] Título:In ovo effects of perfluorohexane sulfonate and perfluorohexanoate on pipping success, development, mRNA expression, and thyroid hormone levels in chicken embryos.
[So] Source:Toxicol Sci;127(1):216-24, 2012 May.
[Is] ISSN:1096-0929
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Perfluoroalkyl acids (PFAAs), specifically perfluorinated sulfonates and carboxylates, are synthetic substances known for their chemical stability, resistance to degradation, and potential to biomagnify in food chains. The toxicological and biological effects of PFAAs in avian species are not well characterized, although there is some evidence to suggest that they can impact neurodevelopment and hatching success. Our laboratory recently reported significant effects of perfluorohexane sulfonate (PFHxS) and perfluorohexanoate (PFHxA) on messenger RNA (mRNA) levels of thyroid hormone (TH)-responsive genes in chicken embryonic neuronal cells. In this study, we determined in ovo effects of PFHxS and PFHxA exposure (maximum dose = 38,000 and 9700 ng/g egg, respectively) on embryonic death, developmental endpoints, tissue accumulation, mRNA expression in liver and cerebral cortex, and plasma TH levels. Pipping success was reduced to 63% at the highest dose of PFHxS; no effects were observed for PFHxA. PFHxS exposure (38,000 ng/g) decreased tarsus length and embryo mass. PFHxS and PFHxA accumulated in the three tissue compartments analyzed as follows: yolk sac > liver > cerebral cortex. Type II and type III 5'-deiodinases (D2 and D3) and cytochrome P450 3A37 mRNA levels were induced in liver tissue of chicken embryos exposed to PFHxS, whereas D2, neurogranin (RC3), and octamer motif binding factor 1 mRNA levels were upregulated in cerebral cortex. Plasma TH levels were reduced in a concentration-dependent manner following PFHxS exposure; PFHxA had no effect. This in ovo study successfully validated previous in vitro results concerning the modulation of TH-responsive genes and identified adverse effects associated with TH homeostasis in response to PFHxS treatment.
[Mh] Termos MeSH primário: Caproatos/toxicidade
Embrião de Galinha/efeitos dos fármacos
Desenvolvimento Embrionário/efeitos dos fármacos
Fluorcarbonetos/toxicidade
Regulação da Expressão Gênica no Desenvolvimento/efeitos dos fármacos
Fígado/efeitos dos fármacos
Ácidos Sulfônicos/toxicidade
Tiroxina/sangue
[Mh] Termos MeSH secundário: Animais
Hidrocarboneto de Aril Hidroxilases/genética
Hidrocarboneto de Aril Hidroxilases/metabolismo
Biomarcadores/metabolismo
Caproatos/farmacocinética
Córtex Cerebral/efeitos dos fármacos
Córtex Cerebral/embriologia
Família 3 do Citocromo P450
Perda do Embrião/induzido quimicamente
Fluorcarbonetos/farmacocinética
Iodeto Peroxidase/genética
Iodeto Peroxidase/metabolismo
Fígado/embriologia
RNA Mensageiro/metabolismo
Ácidos Sulfônicos/farmacocinética
Saco Vitelino/efeitos dos fármacos
Saco Vitelino/embriologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Biomarkers); 0 (Caproates); 0 (Fluorocarbons); 0 (RNA, Messenger); 0 (Sulfonic Acids); 355-46-4 (perfluorohexanesulfonic acid); EC 1.11.1.8 (Iodide Peroxidase); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken)); Q51BO43MG4 (Thyroxine); ZP34Q2220R (perfluorohexanoic acid)
[Em] Mês de entrada:1208
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120204
[St] Status:MEDLINE
[do] DOI:10.1093/toxsci/kfs072


  8 / 17 MEDLINE  
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[PMID]:21893176
[Au] Autor:Egloff C; Crump D; Chiu S; Manning G; McLaren KK; Cassone CG; Letcher RJ; Gauthier LT; Kennedy SW
[Ad] Endereço:Centre for Advanced Research in Environmental Genomics, Department of Biology, University of Ottawa, 20 Marie Curie Street, Ottawa, Ontario, Canada K1N6N5.
[Ti] Título:In vitro and in ovo effects of four brominated flame retardants on toxicity and hepatic mRNA expression in chicken embryos.
[So] Source:Toxicol Lett;207(1):25-33, 2011 Nov 10.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Some currently used brominated flame retardants (BFRs), such as hexachlorocyclopentadienyl-dibromocyclooctane (HCDBCO), bis(2-ethylhexyl)tetrabromophthalate (BEHTBP), 1,2-bis(2,4,6-tribromophenoxy)ethane (BTBPE) and decabromodiphenylethane (DBDPE), are persistent organic contaminants detected in various environmental matrices, including wild birds. Data on potential toxicological and molecular responses to exposure of these BFRs are lacking for avian species. A combined in vitro/in ovo approach was used to determine the concentration-dependent effects of these BFRs on overt toxicity and hepatic messenger RNA (mRNA) expression levels of 11 transcripts in (1) primary cultures of chicken embryonic hepatocytes (CEH; all four BFRs) and (2) chicken embryos (HCDBCO and BTBPE only). Neither hepatocyte viability nor embryonic pipping success were affected by the BFRs at any of the administered concentrations (CEH: 0.001-30 µM, egg injection: 0.1-10 µg/g nominal dose). In CEH, 10 µM HCDBCO induced cytochrome P450 2H1 (CYP2H1) and CYP3A37, while CYP1A4/5 were down-regulated at all tested concentrations. In contrast, only transthyretin was down-regulated by HCDBCO in embryonic liver. There was concordance between the BTBPE-induced transcriptional responses in vitro and in ovo for CYP1A4/5 (up-regulated) and type III iodothyronine 5'-deiodinase (DIO3; down-regulated). DBDPE induced CYP1A4/5 29- and 59-fold at 0.2 µM in CEH and increased DIO1. None of the gene targets were responsive to BEHTBP exposure in CEH. The multi-tiered in vitro/in ovo screening approach was effective for assessing toxicological and molecular biological effects of these BFRs in an avian species.
[Mh] Termos MeSH primário: Retardadores de Chama/toxicidade
Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos
Fígado/efeitos dos fármacos
Bifenil Polibromatos/toxicidade
RNA Mensageiro/biossíntese
[Mh] Termos MeSH secundário: Animais
Hidrocarboneto de Aril Hidroxilases/biossíntese
Hidrocarboneto de Aril Hidroxilases/genética
Sobrevivência Celular/efeitos dos fármacos
Embrião de Galinha
Família 3 do Citocromo P450
Perfilação da Expressão Gênica
Hepatócitos/efeitos dos fármacos
Hepatócitos/metabolismo
Iodeto Peroxidase/biossíntese
Iodeto Peroxidase/genética
Fígado/citologia
Fígado/embriologia
Fígado/enzimologia
RNA Mensageiro/genética
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Estatísticas não Paramétricas
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Flame Retardants); 0 (Polybrominated Biphenyls); 0 (RNA, Messenger); EC 1.11.1.- (iodothyronine deiodinase type I); EC 1.11.1.8 (Iodide Peroxidase); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken))
[Em] Mês de entrada:1201
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110907
[St] Status:MEDLINE
[do] DOI:10.1016/j.toxlet.2011.08.015


  9 / 17 MEDLINE  
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[PMID]:21616088
[Au] Autor:Rawal S; Coulombe RA
[Ad] Endereço:Graduate Toxicology Program, and Department of Veterinary Sciences, School of Veterinary Medicine, Utah State University, Logan, UT 84322, USA.
[Ti] Título:Metabolism of aflatoxin B1 in turkey liver microsomes: the relative roles of cytochromes P450 1A5 and 3A37.
[So] Source:Toxicol Appl Pharmacol;254(3):349-54, 2011 Aug 01.
[Is] ISSN:1096-0333
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The extreme sensitivity of turkeys to aflatoxin B(1) (AFB(1)) is associated with efficient epoxidation by hepatic cytochromes P450 (P450) 1A5 and 3A37 to exo-aflatoxin B(1)-8,9-epoxide (exo-AFBO). The combined presence of 1A5 and 3A37, which obey different kinetic models, both of which metabolize AFB(1) to the exo-AFBO and to detoxification products aflatoxin M(1) (AFM(1)) and aflatoxin Q(1) (AFQ(1)), respectively, complicates the kinetic analysis of AFB(1) in turkey liver microsomes (TLMs). Antisera directed against 1A5 and 3A37, thereby individually removing the catalytic contribution of these enzymes, were used to identify the P450 responsible for epoxidating AFB(1) in TLMs. In control TLMs, AFB(1) was converted to exo-AFBO in addition to AFM(1) and AFQ(1) confirming the presence of functional 1A5 and 3A37. Pretreatment with anti-1A5 inhibited exo-AFBO formation, especially at low, submicromolar (~0.1µM), while anti-3A37, resulted in inhibition of exo-AFBO formation, but at higher (>50µM) AFB(1) concentrations. Metabolism in immunoinhibited TLMs resembled that of individual enzymes: 1A5 produced exo-AFBO and AFM(1), conforming to Michaelis-Menten, while 3A37 produced exo-AFBO and AFQ(1) following the kinetic Hill equation. At 0.1µM AFB(1), close to concentrations in livers of exposed animals, 1A5 contributed to 98% of the total exo-AFBO formation. At this concentration, 1A5 accounted for a higher activation:detoxification (50:1, exo-AFBO: AFM(1)) compared to 3A37 (0.15: 1, exo-AFBO: AFQ(1)), suggesting that 1A5 is high, while 3A4 is the low affinity enzyme in turkey liver. The data support the conclusion that P450 1A5 is the dominant enzyme responsible for AFB(1) bioactivation and metabolism at environmentally-relevant AFB(1) concentrations in turkey liver.
[Mh] Termos MeSH primário: Aflatoxina B1/metabolismo
Hidrocarboneto de Aril Hidroxilases/fisiologia
Microssomos Hepáticos/metabolismo
[Mh] Termos MeSH secundário: Animais
Família 3 do Citocromo P450
Microssomos Hepáticos/enzimologia
Perus
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
9N2N2Y55MH (Aflatoxin B1); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP1A5); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken))
[Em] Mês de entrada:1109
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110528
[St] Status:MEDLINE
[do] DOI:10.1016/j.taap.2011.05.010


  10 / 17 MEDLINE  
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[PMID]:19617698
[Au] Autor:Rawal S; Mendoza KM; Reed KM; Coulombe RA
[Ad] Endereço:Graduate Toxicology Program and Department of Veterinary Sciences, Utah State University, Logan, Utah 84322, USA.
[Ti] Título:Structure, genetic mapping, and function of the cytochrome P450 3A37 gene in the turkey (Meleagris gallopavo).
[So] Source:Cytogenet Genome Res;125(1):67-73, 2009.
[Is] ISSN:1424-859X
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Cytochromes P450 (P450 for protein; CYP for gene) are a superfamily of membrane-bound hemoproteins that oxidize a large number of endogenous and exogenous compounds. Through oxidation reactions, these enzymes are often responsible for the toxic and carcinogenic effects of natural food-borne toxicants, such as the mycotoxin aflatoxin B1 (AFB1). Previous studies in our laboratory have shown that the extreme sensitivity of turkeys to AFB1 is in part explained by efficient hepatic P450-mediated epoxidation to the toxic and reactive metabolite the exo-AFB1-8,9-epoxide (AFBO). Using 3'-5'-rapid amplification of cDNA ends (RACE), we amplified CYP3A37 from turkey liver RNA, the E. coli-expressed protein which efficiently epoxidates AFB(1). Turkey CYP3A37 has an ORF of 1512 bp, and the protein is predicted to be 504 amino acids with 97% homology to chicken CYP3A37. The turkey gene is organized into 13 exons and 12 introns. A single nucleotide polymorphism in the 11th intron was used to assign CYP3A37 to turkey linkage group 10 (corresponding to chicken chromosome 14, GGA14). Because of the important role of P450s in the extreme sensitivity of turkeys to the toxic effects of AFB(1), this study will contribute to the identifying allelic variants of this important gene in poultry.
[Mh] Termos MeSH primário: Hidrocarboneto de Aril Hidroxilases/genética
Perus/genética
[Mh] Termos MeSH secundário: Aflatoxina B1/farmacocinética
Aflatoxina B1/toxicidade
Sequência de Aminoácidos
Animais
Hidrocarboneto de Aril Hidroxilases/metabolismo
Sequência de Bases
Galinhas/genética
Mapeamento Cromossômico
Família 3 do Citocromo P450
Primers do DNA/genética
DNA Complementar/genética
Fígado/metabolismo
Dados de Sequência Molecular
Proteínas Recombinantes/genética
Proteínas Recombinantes/metabolismo
Homologia de Sequência de Aminoácidos
Homologia de Sequência do Ácido Nucleico
Especificidade da Espécie
Perus/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (DNA Primers); 0 (DNA, Complementary); 0 (Recombinant Proteins); 9N2N2Y55MH (Aflatoxin B1); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (Cytochrome P450 Family 3); EC 1.14.14.1 (cytochrome P-450 CYP3A37 (chicken))
[Em] Mês de entrada:0907
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090721
[St] Status:MEDLINE
[do] DOI:10.1159/000218748



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