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[PMID]: 29268129 [Au] Autor: Cen J; Guo H; Hong C; Lv J; Yang Y; Wang T; Fang D; Luo W; Wang C [Ad] Endereço: Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China. [Ti] Título: Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. [So] Source: Eur J Med Chem;144:128-136, 2018 Jan 20. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: A novel series of tacrine-bifendate (THA-DDB) conjugates (7a-e) were synthesized and evaluated as potential anti-Alzheimer's agents. These compounds showed potent cholinesterase and self-induced ß-amyloid (Aß) aggregation inhibitory activities. A Lineweaver-Burk plot and molecular modeling study showed that these compounds can target both catalytic active site (CAS) and peripheral anionic site (PAS) of acetylcholinesterase (AChE). The cytotoxicity of the conjugate 7d against PC12 and HepG2 cells and hepatotoxicity against human hepatocyte cell line (HL-7702) were found to be considerably less compared to THA. Moreover, treatment with 7d did not exhibit significant hepatotoxicity in mice. Finally, in vivo studies confirmed that 7d significantly ameliorates the cognitive performances of scopolamine-treated ICR mice. Therefore, 7d has high potential for the treatment of Alzheimer's disease and warrants further investigation. [Mh] Termos MeSH primário: Compostos de Bifenilo/química Compostos de Bifenilo/farmacologia Inibidores da Colinesterase/química Inibidores da Colinesterase/farmacologia Cognição/efeitos dos fármacos Tacrina/análogos & derivados Tacrina/farmacologia [Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo Doença de Alzheimer/tratamento farmacológico Doença de Alzheimer/patologia Animais Compostos de Bifenilo/toxicidade Linhagem Celular Doença Hepática Induzida por Substâncias e Drogas/etiologia Doença Hepática Induzida por Substâncias e Drogas/patologia Inibidores da Colinesterase/toxicidade Colinesterases/metabolismo Desenho de Drogas Células Hep G2 Seres Humanos Fígado/efeitos dos fármacos Fígado/patologia Masculino Camundongos Endogâmicos ICR Células PC12 Ratos Tacrina/toxicidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Biphenyl Compounds); 0 (Cholinesterase Inhibitors); 0G32E321W1 (bifendate); 4VX7YNB537 (Tacrine); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180309 [Lr] Data última revisão: 180309 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171222 [St] Status: MEDLINE

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[PMID]: 29188674 [Au] Autor: Ding BF; Shao L; Zhang RS; Liang C; Zhang YR [Ad] Endereço: College of Life and Environmental Sciences, Shanghai Normal University, Shanghai 200234, China. [Ti] Título: [Research Progress on Abused Drugs Metabolic in vivo]. [So] Source: Fa Yi Xue Za Zhi;32(4):290-295, 2016 Aug. [Is] ISSN: 1004-5619 [Cp] País de publicação: China [La] Idioma: chi [Ab] Resumo: Under the catalysis of a variety of metabolic enzymes , such as UDP-glucuronyl transferases, cytochrome P450, carboxylesterase, sulfotransferase, butyrylcholinesterase, catechol- -methyl transferase and 6-morphine dehydrogenase, the drugs perform glucuronidation, hydrolysis, oxidation, sulfonation and other reactions, then translate into active or inactive metabolites, which are excreted through urination, bile or the other pathways at last. Different drugs own their different metabolic pathways. This paper introduces the studies about the metabolism of drugs in human and animal in recent years, such as morphine-like drugs, amphetamine, ketamine, cannabis and cocaine, and reviews the research progress about the sites of metabolism, metabolic enzymes, metabolites and physiological activity of those drugs metabolic . [Mh] Termos MeSH primário: Colinesterases/metabolismo Sistema Enzimático do Citocromo P-450/metabolismo Glucuronosiltransferase/metabolismo Drogas Ilícitas/metabolismo [Mh] Termos MeSH secundário: Oxirredutases do Álcool/metabolismo Animais Carboxilesterase/metabolismo Catecol O-Metiltransferase/metabolismo Seres Humanos Oxirredução Sulfotransferases/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Street Drugs); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.1.218 (morphine 6-dehydrogenase); EC 2.1.1.6 (Catechol O-Methyltransferase); EC 2.4.1.17 (Glucuronosyltransferase); EC 2.8.2.- (Sulfotransferases); EC 3.1.1.1 (Carboxylesterase); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180215 [Lr] Data última revisão: 180215 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171201 [St] Status: MEDLINE [do] DOI: 10.3969/j.issn.1004-5619.2016.04.013

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[PMID]: 29304153 [Au] Autor: Barszcz M; Taciak M; Tusnio A; Skomial J [Ad] Endereço: Department of Animal Nutrition, The Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciences, Jablonna, Poland. [Ti] Título: Effects of dietary level of tannic acid and protein on internal organ weights and biochemical blood parameters of rats. [So] Source: PLoS One;13(1):e0190769, 2018. [Is] ISSN: 1932-6203 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Tannic acid (TA) is a polyphenolic compound with a health-promoting potential for humans. It is hypothesised that TA effects on the relative weight of internal organs and biochemical blood indices are modified by dietary protein level in rats. The study involved 72 rats divided into 12 groups fed diets with 10 or 18% of crude protein (CP) and supplemented with 0, 0.25, 0.5, 1, 1.5 or 2% of TA. After 3 weeks of feeding, the relative weight of the caecum was greater in rats fed TA diets, while feeding diets with 10% of CP increased the relative weight of the stomach, small intestine and caecum, but decreased that of kidneys and spleen. Albumin concentration was higher in rats fed 0.25% and 0.5% TA diets than in rats given the 2% TA diets. The 2% TA diets reduced creatine kinase (CK) activity compared to non-supplemented diets and those with 0.5, 1 and 1.5% of TA. Rats fed the 10% CP diets had a higher activity of alkaline phosphatase, amylase, and γ-glutamyltransferase as well as the concentration of iron and cholesterol, but lower that of urea and uric acid. The interaction affected only cholinesterase activity. In conclusion, TA induced caecal hypertrophy and could act as a cardioprotective agent, as demonstrated by reduced CK activity, but these effects were not modified by dietary protein level. [Mh] Termos MeSH primário: Dieta Proteínas na Dieta Taninos [Mh] Termos MeSH secundário: Animais Ceco/anatomia & histologia Colesterol/sangue Colinesterases/sangue Creatina Quinase/sangue Intestino Delgado/anatomia & histologia Rim/anatomia & histologia Masculino Tamanho do Órgão Ratos Endogâmicos WF Albumina Sérica Baço/anatomia & histologia Estômago/anatomia & histologia [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Dietary Proteins); 0 (Serum Albumin); 0 (Tannins); 97C5T2UQ7J (Cholesterol); EC 2.7.3.2 (Creatine Kinase); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180210 [Lr] Data última revisão: 180210 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180106 [St] Status: MEDLINE [do] DOI: 10.1371/journal.pone.0190769

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[PMID]: 28468728 [Au] Autor: Zhou H; Xiao Q; Tan W; Zhan Y; Pistolozzi M [Ad] Endereço: School of Bioscience & Bioengineering, South China University of Technology, Higher Education Mega Center, 510006, Guangzhou, People's Republic of China. [Ti] Título: Quantitative estimation of cholinesterase-specific drug metabolism of carbamate inhibitors provided by the analysis of the area under the inhibition-time curve. [So] Source: J Pharm Biomed Anal;144:167-174, 2017 Sep 10. [Is] ISSN: 1873-264X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Several molecules containing carbamate groups are metabolized by cholinesterases. This metabolism includes a time-dependent catalytic step which temporary inhibits the enzymes. In this paper we demonstrate that the analysis of the area under the inhibition versus time curve (AUIC) can be used to obtain a quantitative estimation of the amount of carbamate metabolized by the enzyme. (R)-bambuterol monocarbamate and plasma butyrylcholinesterase were used as model carbamate-cholinesterase system. The inhibition of different concentrations of the enzyme was monitored for 5h upon incubation with different concentrations of carbamate and the resulting AUICs were analyzed. The amount of carbamate metabolized could be estimated with <15% accuracy (RE%) and ≤23% precision (RSD%). Since the knowledge of the inhibition kinetics is not required for the analysis, this approach could be used to determine the amount of drug metabolized by cholinesterases in a selected compartment in which the cholinesterase is confined (e.g. in vitro solutions, tissues or body fluids), either in vitro or in vivo. [Mh] Termos MeSH primário: Inibidores da Colinesterase/farmacologia [Mh] Termos MeSH secundário: Biocatálise Carbamatos Colinesterases Cinética [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Carbamates); 0 (Cholinesterase Inhibitors); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180205 [Lr] Data última revisão: 180205 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170505 [St] Status: MEDLINE

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[PMID]: 28457693 [Au] Autor: Ahmad H; Ahmad S; Shah SAA; Latif A; Ali M; Khan FA; Tahir MN; Shaheen F; Wadood A; Ahmad M [Ad] Endereço: Department of Chemistry, University of Malakand, Chakdara, Dir (L) 18550, KP, Pakistan. [Ti] Título: Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum. [So] Source: Bioorg Med Chem;25(13):3368-3376, 2017 07 01. [Is] ISSN: 1464-3391 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Extensive chromatographic separations performed on the basic (pH=8-10) chloroform soluble fraction of Aconitum heterophyllum resulted in the isolation of three new diterpenoid alkaloids, 6ß-Methoxy, 9ß-dihydroxylheteratisine (1), 1α,11,13ß-trihydroxylhetisine (2), 6,15ß-dihydroxylhetisine (3), and the known compounds iso-atisine (4), heteratisine (5), hetisinone (6), 19-epi-isoatisine (7), and atidine (8). Structures of the isolated compounds were established by means of mass and NMR spectroscopy as well as single crystal X-ray crystallography. Compounds 1-8 were screened for their antioxidant and enzyme inhibition activities followed by in silico studies to find out the possible inhibitory mechanism of the tested compounds. This work is the first report demonstrating significant antioxidant and anticholinesterase potentials of diterpenoid alkaloids isolated from a natural source. [Mh] Termos MeSH primário: Aconitum/química Alcaloides/farmacologia Antioxidantes/farmacologia Inibidores da Colinesterase/farmacologia Colinesterases/metabolismo Diterpenos/farmacologia [Mh] Termos MeSH secundário: Alcaloides/química Alcaloides/isolamento & purificação Animais Antioxidantes/química Antioxidantes/isolamento & purificação Inibidores da Colinesterase/química Inibidores da Colinesterase/isolamento & purificação Cristalografia por Raios X Diterpenos/química Diterpenos/isolamento & purificação Relação Dose-Resposta a Droga Electrophorus Modelos Moleculares Estrutura Molecular Teoria Quântica Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Alkaloids); 0 (Antioxidants); 0 (Cholinesterase Inhibitors); 0 (Diterpenes); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 171208 [Lr] Data última revisão: 171208 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170502 [St] Status: MEDLINE

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[PMID]: 29048701 [Au] Autor: Food and Drug Administration, HHS [Ti] Título: Medical Devices; Clinical Chemistry and Clinical Toxicology Devices; Classification of the Organophosphate Test System. Final order. [So] Source: Fed Regist;82(200):48413-5, 2017 Oct 18. [Is] ISSN: 0097-6326 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: The Food and Drug Administration (FDA or we) is classifying the organophosphate test system into class II (special controls). The special controls that apply to the device type are identified in this order and will be part of the codified language for the organophosphate test system's classification. We are taking this action because we have determined that classifying the device into class II (special controls) will provide a reasonable assurance of safety and effectiveness of the device. We believe this action will also enhance patients' access to beneficial innovative devices, in part by reducing regulatory burdens. [Mh] Termos MeSH primário: Química Clínica/classificação Química Clínica/instrumentação Segurança de Equipamentos/classificação Organofosfatos/urina Toxicologia/classificação Toxicologia/instrumentação [Mh] Termos MeSH secundário: Colinesterases/envenenamento Aprovação de Equipamentos/legislação & jurisprudência Seres Humanos Estados Unidos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Organophosphates); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171031 [Lr] Data última revisão: 171031 [Sb] Subgrupo de revista: T [Da] Data de entrada para processamento: 171020 [St] Status: MEDLINE

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[PMID]: 28925729 [Au] Autor: Panek D; Wichur T; Godyn J; Pasieka A; Malawska B [Ad] Endereço: Department of Physicochemical Drug Analysis, Chair of Pharmaceutical Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, 30-688 Kraków, Medyczna 9, Poland. [Ti] Título: Advances toward multifunctional cholinesterase and ß-amyloid aggregation inhibitors. [So] Source: Future Med Chem;9(15):1835-1854, 2017 Oct. [Is] ISSN: 1756-8927 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: The emergence of a multitarget design approach in the development of new potential anti-Alzheimer's disease agents has resulted in the discovery of many multifunctional compounds focusing on various targets. Among them the largest group comprises inhibitors of both cholinesterases, with additional anti-ß-amyloid aggregation activity. This review describes recent advances in this research area and presents the most interesting compounds reported over a 2-year span (2015-2016). The majority of hybrids possess heterodimeric structures obtained by linking structurally active fragments interacting with different targets. Multipotent cholinesterase inhibitors with ß-amyloid antiaggregating activity may additionally possess antioxidative, neuroprotective or metal-chelating properties or less common features such as anti-ß-secretase or τ-antiaggregation activity. [Mh] Termos MeSH primário: Peptídeos beta-Amiloides/metabolismo Colinesterases/metabolismo [Mh] Termos MeSH secundário: Alcaloides/química Alcaloides/metabolismo Alcaloides/uso terapêutico Doença de Alzheimer/tratamento farmacológico Peptídeos beta-Amiloides/antagonistas & inibidores Inibidores da Colinesterase/química Inibidores da Colinesterase/metabolismo Inibidores da Colinesterase/uso terapêutico Colinesterases/química Seres Humanos Indanos/química Indanos/metabolismo Concentração Inibidora 50 Piperidinas/química Piperidinas/metabolismo Rivastigmina/química Rivastigmina/metabolismo Tacrina/química Tacrina/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Alkaloids); 0 (Amyloid beta-Peptides); 0 (Cholinesterase Inhibitors); 0 (Indans); 0 (Piperidines); 4VX7YNB537 (Tacrine); 8SSC91326P (donepezil); EC 3.1.1.8 (Cholinesterases); PKI06M3IW0 (Rivastigmine) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171025 [Lr] Data última revisão: 171025 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170920 [St] Status: MEDLINE [do] DOI: 10.4155/fmc-2017-0094

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[PMID]: 28880741 [Au] Autor: Ismail AA; Wang K; Olson JR; Bonner MR; Hendy O; Abdel Rasoul G; Rohlman DS [Ad] Endereço: a Department of Occupational and Environmental Health , College of Public Health, University of Iowa , Iowa City , IA , USA. [Ti] Título: The impact of repeated organophosphorus pesticide exposure on biomarkers and neurobehavioral outcomes among adolescent pesticide applicators. [So] Source: J Toxicol Environ Health A;80(10-12):542-555, 2017. [Is] ISSN: 1528-7394 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Egyptian adolescents are hired as seasonal workers to apply pesticides to the cotton crop and may perform this occupation for several years. However, few studies examined the effects of repeated pesticide exposure on health outcomes The goal of this study was to determine the impact of repeated pesticide exposure on neurobehavioral (NB) performance and biomarkers of exposure (urinary metabolite) and effect (cholinesterase activity). Eighty-four adolescents from two field stations in Menoufia, Egypt, were examined four times: before and during pesticide application season in 2010 and again before and during application season in 2011. At each of the four time points, participants completed a questionnaire, performed an NB test battery, and were assessed for urinary levels of the chlorpyrifos metabolite TCPy (3,5,6-trichloro-2-pyridinol) and blood cholinesterase activity. Following the study cohort over two consecutive pesticide application seasons revealed that TCPy levels significantly increased following exposure, and returned to baseline levels following the end of the application season. Blood butyryl cholinesterase activity exhibited a similar pattern. Although NB outcomes displayed learning and practice effects over time, deficits in performance were significantly associated with increased TCPy levels with reduction in the number of NB measures showing improvement over time. Biomarkers of exposure and effect demonstrated changes associated with pesticide application and recovery after application ended. Deficits in NB performance were correlated with elevated pesticide exposure. Data demonstrated that repeated pesticide exposure may exert a long-term adverse impact on human health. [Mh] Termos MeSH primário: Clorpirifos/urina Inseticidas/urina Exposição Ocupacional Piridonas/urina [Mh] Termos MeSH secundário: Adolescente Biomarcadores/urina Criança Colinesterases/sangue Egito Seres Humanos Estudos Longitudinais Testes Neuropsicológicos Adulto Jovem [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Biomarkers); 0 (Insecticides); 0 (Pyridones); 6515-38-4 (3,5,6-trichloro-2-pyridinol); EC 3.1.1.8 (Cholinesterases); JCS58I644W (Chlorpyrifos) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171021 [Lr] Data última revisão: 171021 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170908 [St] Status: MEDLINE [do] DOI: 10.1080/15287394.2017.1362612

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[PMID]: 28683335 [Au] Autor: Brodeur JC; Sanchez M; Castro L; Rojas DE; Cristos D; Damonte MJ; Poliserpi MB; D'Andrea MF; Andriulo AE [Ad] Endereço: Instituto de Recursos Biológicos, Centro de Investigaciones de Recursos Naturales (CIRN), Instituto Nacional de Tecnología Agropecuaria (INTA), Hurlingham, Buenos Aires, Argentina. Electronic address: brodeur.celine@inta.gob.ar. [Ti] Título: Accumulation of current-use pesticides, cholinesterase inhibition and reduced body condition in juvenile one-sided livebearer fish (Jenynsia multidentata) from the agricultural Pampa region of Argentina. [So] Source: Chemosphere;185:36-46, 2017 Oct. [Is] ISSN: 1879-1298 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: The aim of this study was to characterize the level and nature of the pesticide contamination received by one-sided livebearer fish (Jenynsia multidentata) from a watercourse situated within the main agricultural region of Argentina, and to assess the effects of this contamination on fish health. Juvenile one-sided livebearer fish (Jenynsia multidentata) were collected in December 2011 and March 2012 from three sites along the Pergamino River. Pesticide contamination was characterized by extracting whole fish and analytically determining thirty different pesticide molecules. The biomarkers catalase, glutathione-S-transferase, and cholinesterases were assessed. Body condition was calculated as an estimate of the amount of energy reserves possessed by the fish. Seventeen different pesticides were detected in fish tissues with 81% of captured animals containing at least one pesticide molecule. The pyrethroid insecticides fenvalerate and bifenthrin were most frequently detected, being respectively found in 41.8 and 36.4% of samples tested. Highly toxic dichlorvos and pirimiphos-methyl were detected. Differential levels of contamination could not be established amongst sites but were observed within sites amongst the two sampling dates. The months when pesticide residues were most abundant from in Site A and B corresponded to the months when body condition was at its lowest in the two sites. The inhibition of Che activity in March when body condition was reduced also points to a role of insecticide contamination in the reduction of body condition. These findings provide strong new evidence that current-used agricultural pesticides can accumulate in wild fish and impact their health and energetics. [Mh] Termos MeSH primário: Inibidores da Colinesterase/metabolismo Colinesterases/metabolismo Ciprinodontiformes/metabolismo Praguicidas/metabolismo [Mh] Termos MeSH secundário: Agricultura Animais Argentina Biomarcadores Inibidores da Colinesterase/toxicidade Ciprinodontiformes/fisiologia Monitoramento Ambiental Inseticidas/toxicidade Nitrilos Resíduos de Praguicidas Praguicidas/análise Praguicidas/toxicidade Piretrinas/metabolismo Piretrinas/toxicidade Rios Poluentes Químicos da Água/análise [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Biomarkers); 0 (Cholinesterase Inhibitors); 0 (Insecticides); 0 (Nitriles); 0 (Pesticide Residues); 0 (Pesticides); 0 (Pyrethrins); 0 (Water Pollutants, Chemical); 6B66JED0KN (bifenthrin); EC 3.1.1.8 (Cholinesterases); Z6MXZ39302 (fenvalerate) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171102 [Lr] Data última revisão: 171102 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170707 [St] Status: MEDLINE

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[PMID]: 28655305 [Au] Autor: Amri Z; Ghorbel A; Turki M; Akrout FM; Ayadi F; Elfeki A; Hammami M [Ad] Endereço: Biochemistry Laboratory, LR12ES05 "Nutrition- Functional Foods and vascular Health", Faculty of Medicine, University of Monastir, 5019, Monastir, Tunisia. zahraamri23@yahoo.fr. [Ti] Título: Effect of pomegranate extracts on brain antioxidant markers and cholinesterase activity in high fat-high fructose diet induced obesity in rat model. [So] Source: BMC Complement Altern Med;17(1):339, 2017 Jun 27. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: To investigate beneficial effects of Pomegranate seeds oil (PSO), leaves (PL), juice (PJ) and (PP) on brain cholinesterase activity, brain oxidative stress and lipid profile in high-fat-high fructose diet (HFD) induced-obese rat. METHODS: In vitro and in vivo cholinesterase activity, brain oxidative status, body and brain weight and plasma lipid profile were measured in control rats, HFD-fed rats and HFD-fed rats treated by PSO, PL, PJ and PP. RESULTS: In vitro study showed that PSO, PL, PP, PJ inhibited cholinesterase activity in dose dependant manner. PL extract displayed the highest inhibitory activity by IC50 of 151.85 mg/ml. For in vivo study, HFD regime induced a significant increase of cholinesterase activity in brain by 17.4% as compared to normal rats. However, the administration of PSO, PL, PJ and PP to HDF-rats decreased cholinesterase activity in brain respectively by 15.48%, 6.4%, 20% and 18.7% as compared to untreated HFD-rats. Moreover, HFD regime caused significant increase in brain stress, brain and body weight, and lipid profile disorders in blood. Furthermore, PSO, PL, PJ and PP modulated lipid profile in blood and prevented accumulation of lipid in brain and body evidenced by the decrease of their weights as compared to untreated HFD-rats. In addition administration of these extract protected brain from stress oxidant, evidenced by the decrease of malondialdehyde (MDA) and Protein carbonylation (PC) levels and the increase in superoxide dismutase (SOD) and glutathione peroxidase (GPx) levels. CONCLUSION: These findings highlight the neuroprotective effects of pomegranate extracts and one of mechanisms is the inhibition of cholinesterase and the stimulation of antioxidant capacity. [Mh] Termos MeSH primário: Antioxidantes/metabolismo Encéfalo/efeitos dos fármacos Colinesterases/metabolismo Dieta Hiperlipídica/efeitos adversos Frutose/efeitos adversos Obesidade/tratamento farmacológico Extratos Vegetais/administração & dosagem Punicaceae/química [Mh] Termos MeSH secundário: Animais Encéfalo/enzimologia Encéfalo/metabolismo Modelos Animais de Doenças Glutationa Peroxidase/metabolismo Seres Humanos Masculino Malondialdeído/metabolismo Obesidade/enzimologia Obesidade/metabolismo Estresse Oxidativo/efeitos dos fármacos Ratos Ratos Wistar Superóxido Dismutase/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antioxidants); 0 (Plant Extracts); 30237-26-4 (Fructose); 4Y8F71G49Q (Malondialdehyde); EC 1.11.1.9 (Glutathione Peroxidase); EC 1.15.1.1 (Superoxide Dismutase); EC 3.1.1.8 (Cholinesterases) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170817 [Lr] Data última revisão: 170817 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170629 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-017-1842-9

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2	and or and not		PalavrasDescritor de assuntoDescritor de assunto primárioLimitesAutorPalavras do títuloPalavras do resumoIdiomaPaís de publicaçãoNome de substânciaNome de pessoa como assuntoRevistaAssunto de RevistaISSNTipo de publicaçãoIdentificador únicoMês de entradaAno de publicaçãoTexto completoAtualização por classeCategoria DeCSCategoria DeCS explodidaCategoria CID-10SubSetsPais de AfiliaçãoAfiliaçãoAfiliação 2
3	and or and not		PalavrasDescritor de assuntoDescritor de assunto primárioLimitesAutorPalavras do títuloPalavras do resumoIdiomaPaís de publicaçãoNome de substânciaNome de pessoa como assuntoRevistaAssunto de RevistaISSNTipo de publicaçãoIdentificador únicoMês de entradaAno de publicaçãoTexto completoAtualização por classeCategoria DeCSCategoria DeCS explodidaCategoria CID-10SubSetsPais de AfiliaçãoAfiliaçãoAfiliação 2

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