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[PMID]:27770709
[Au] Autor:Wang B; Chen Q; Shen L; Zhao S; Pang W; Zhang J
[Ad] Endereço:MOE-Shanghai Key Laboratory of Children's Environmental Health, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China.
[Ti] Título:Perfluoroalkyl and polyfluoroalkyl substances in cord blood of newborns in Shanghai, China: Implications for risk assessment.
[So] Source:Environ Int;97:7-14, 2016 12.
[Is] ISSN:1873-6750
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Perfluoroalkyl and polyfluoroalkyl substances (PFASs) are commonly used in industrial applications and consumer products, and their potential health impacts are of concern, especially for vulnerable population like fetuses. However, in utero exposure to PFASs and health implications are far from fully characterized in China. To fill in the gap, we analyzed 10 PFASs in cord plasma samples (N=687) collected in Shanghai between 2011 and 2012, one of the regions widely polluted with PFASs in China. A questionnaire survey on maternal and diet-related factors was conducted. Except for perfluoroheptanoic acid (PFHpA) and perfluorooctane sulfonamide (PFOSA), all other PFASs were detected in ˃90% of the samples. Perfluorooctanoic acid (PFOA) was the most predominant PFAS (median value: 6.96ng/mL), followed by perfluorooctane sulfonate (PFOS) (2.48ng/mL). PFOA and PFOS combined contributed to 80% of the total PFASs. The final multiple regression models showed that maternal factors including maternal age, body mass index, gestational age, economic status and educational level as well as consumption of fish and wheat were significantly related with concentrations of PFASs in cord blood. The risk assessment using the hazard quotients (HQs) approach on the basis of plasma PFAS levels indicated no potential concern for developmental toxicity in the local newborns. The results demonstrate the unique profiles of local prenatal exposure to PFASs, suggesting that PFOA has been the primary human exposure due to its widespread use and pollution. Special attention to high PFOA exposure and confirmation of potential determinants should be taken as a priority in the future plan for risk management and actions in this area.
[Mh] Termos MeSH primário: Poluentes Ambientais/sangue
Sangue Fetal/química
Hidrocarbonetos Fluorados/sangue
[Mh] Termos MeSH secundário: Animais
China
Feminino
Peixes
Alimentos
Seres Humanos
Gravidez
Medição de Risco
Sulfonamidas/sangue
Ácidos Sulfônicos/sangue
Inquéritos e Questionários
Triticum
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Environmental Pollutants); 0 (Hydrocarbons, Fluorinated); 0 (Sulfonamides); 0 (Sulfonic Acids)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:180311
[Lr] Data última revisão:
180311
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161023
[St] Status:MEDLINE


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[PMID]:29295712
[Au] Autor:Ovais M; Ayaz M; Khalil AT; Shah SA; Jan MS; Raza A; Shahid M; Shinwari ZK
[Ad] Endereço:Department of Biotechnology, Quaid-i-Azam University, Islamabad, 44000, Pakistan.
[Ti] Título:HPLC-DAD finger printing, antioxidant, cholinesterase, and α-glucosidase inhibitory potentials of a novel plant Olax nana.
[So] Source:BMC Complement Altern Med;18(1):1, 2018 Jan 03.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The medicinal importance of a novel plant Olax nana Wall. ex Benth. (family: Olacaceae) was revealed for the first time via HPLC-DAD finger printing, qualitative phytochemical analysis, antioxidant, cholinesterase, and α-glucosidase inhibitory assays. METHODS: The crude methanolic extract of O. nana (ON-Cr) was subjected to qualitative phytochemical analysis and HPLC-DAD finger printing. The antioxidant potential of ON-Cr was assessed via 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H O ) free radical scavenging assays. Furthermore, acetylcholinesterase (AChE) & butyrylcholinesterase (BChE) inhibitory activities were performed using Ellman's assay, while α- glucosidase inhibitory assay was carried out using a standard protocol. RESULTS: The qualitative phytochemical analysis of ON-Cr revealed the presence of secondary metabolites like alkaloids, flavonoids, tannins, sterols, saponins and terpenoids. The HPLC-DAD finger printing revealed the presence of 40 potential compounds in ON-Cr. Considerable anti-radical activities was revealed by ON-Cr in the DPPH, ABTS and H O free radical scavenging assays with IC values of 71.46, 72.55 and 92.33 µg/mL, respectively. Furthermore, ON-Cr showed potent AChE and BChE inhibitory potentials as indicated by their IC values of 33.2 and 55.36 µg/mL, respectively. In the α-glucosidase inhibition assay, ON-Cr exhibited moderate inhibitory propensity with an IC value of 639.89 µg/mL. CONCLUSIONS: This study investigated Olax nana for the first time for detailed qualitative phytochemical tests, HPLC-DAD finger printing analysis, antioxidant, anticholinesterase and α-glucosidase inhibition assays. The antioxidant and cholinesterase inhibitory results were considerable and can provide scientific basis for further studies on the neuroprotective and anti-Alzheimer's potentials of this plant. ON-Cr may further be subjected to fractionation and polarity guided fractionation to narrow down the search for isolation of bioactive compounds.
[Mh] Termos MeSH primário: Antioxidantes/análise
Inibidores da Colinesterase/análise
Cromatografia Líquida de Alta Pressão/métodos
Inibidores de Glicosídeo Hidrolases/análise
Olacaceae/química
Extratos Vegetais/análise
[Mh] Termos MeSH secundário: Antioxidantes/química
Antioxidantes/metabolismo
Benzotiazóis/análise
Benzotiazóis/metabolismo
Compostos de Bifenilo/análise
Compostos de Bifenilo/metabolismo
Inibidores da Colinesterase/química
Inibidores da Colinesterase/metabolismo
Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/metabolismo
Peróxido de Hidrogênio/análise
Peróxido de Hidrogênio/metabolismo
Picratos/análise
Picratos/metabolismo
Extratos Vegetais/química
Extratos Vegetais/metabolismo
Ácidos Sulfônicos/análise
Ácidos Sulfônicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Benzothiazoles); 0 (Biphenyl Compounds); 0 (Cholinesterase Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Picrates); 0 (Plant Extracts); 0 (Sulfonic Acids); 28752-68-3 (2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid); BBX060AN9V (Hydrogen Peroxide); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[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:180104
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-017-2057-9


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[PMID]:29390901
[Au] Autor:Iqbal J; El-Gamal MI; Ejaz SA; Lecka J; Sévigny J; Oh CH
[Ad] Endereço:a Centre for Advanced Drug Research , COMSATS Institute of Information Technology , Abbottabad , Pakistan.
[Ti] Título:Tricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies.
[So] Source:J Enzyme Inhib Med Chem;33(1):479-484, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tissue-nonspecific alkaline phosphatase (TNAP) is an important isozyme of alkaline phosphatases, which plays different pivotal roles within the human body. Most importantly, it is responsible for maintaining the balanced ratio of phosphate and inorganic pyrophosphate, thus regulates the extracellular matrix calcification during bone formation and growth. The elevated level of TNAP has been linked to vascular calcification and end-stage renal diseases. Consequently, there is a need to search for highly potent and selective inhibitors of alkaline phosphatases (APs) for treatment of disorders associated with the over-expression of APs. Herein, a series of tricyclic coumarin sulphonate 1a-za with known antiproliferative activity, was evaluated for AP inhibition against human tissue nonspecific alkaline phosphatase (h-TNAP) and human intestinal alkaline phosphatase (h-IAP). The methylbenzenesulphonate derivative 1f (IC = 0.38 ± 0.01 µM) was found to be the most active h-TNAP inhibitor. Another 4-fluorobenzenesulphonate derivative 1i (IC = 0.45 ± 0.02 µM) was found as the strongest inhibitor of h-IAP. Some of the derivatives were also identified as highly selective inhibitors of APs. Detailed structure-activity relationship (SAR) was investigated to identify the functional groups responsible for the effective inhibition of AP isozymes. The study was also supported by the docking studies to rationalise the most possible binding site interactions of the identified inhibitors with the targeted enzymes.
[Mh] Termos MeSH primário: Fosfatase Alcalina/antagonistas & inibidores
Cumarínicos/farmacologia
Inibidores Enzimáticos/farmacologia
Simulação de Acoplamento Molecular
Ácidos Sulfônicos/farmacologia
[Mh] Termos MeSH secundário: Fosfatase Alcalina/metabolismo
Cumarínicos/síntese química
Cumarínicos/química
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Proteínas Ligadas por GPI/antagonistas & inibidores
Proteínas Ligadas por GPI/metabolismo
Seres Humanos
Estrutura Molecular
Relação Estrutura-Atividade
Ácidos Sulfônicos/síntese química
Ácidos Sulfônicos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coumarins); 0 (Enzyme Inhibitors); 0 (GPI-Linked Proteins); 0 (Sulfonic Acids); EC 3.1.3.1 (ALPI protein, human); EC 3.1.3.1 (ALPL protein, human); EC 3.1.3.1 (Alkaline Phosphatase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180203
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1428193


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[PMID]:28749778
[Au] Autor:Grandjean P; Heilmann C; Weihe P; Nielsen F; Mogensen UB; Budtz-Jørgensen E
[Ad] Endereço:Department of Environmental Medicine, University of Southern Denmark, Odense, Denmark
[Ti] Título:Serum Vaccine Antibody Concentrations in Adolescents Exposed to Perfluorinated Compounds.
[So] Source:Environ Health Perspect;125(7):077018, 2017 07 26.
[Is] ISSN:1552-9924
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Postnatal exposure to perfluorinated alkylate substances (PFASs) is associated with lower serum concentrations of specific antibodies against certain childhood vaccines at 7 y. OBJECTIVES: We prospectively followed a Faroese birth cohort to determine these associations at 13 y. METHODS: In 516 subjects (79% of eligible cohort members) who were 13 years old, serum concentrations of PFASs and of antibodies against diphtheria and tetanus were measured and were compared with data from the previous examination at 7 y. Multiple regression analyses and structural equation models were applied to determine the association between postnatal PFAS exposures and antibody concentrations. RESULTS: Serum concentrations of PFASs and antibodies generally declined from 7 y to 13 y. However, 68 subjects had visited the emergency room and had likely received a vaccination booster, and a total of 202 children showed higher vaccine antibody concentrations at 13 y than at 7 y. Therefore, separate analyses were conducted after exclusion of these two subgroups. Diphtheria antibody concentrations decreased at elevated PFAS concentrations at 13 y and 7 y; the associations were statistically significant for perfluorodecanoate (PFDA) at 7 y and for perfluorooctanoate (PFOA) at 13 y, both suggesting a decrease by ∼25% for each doubling of exposure. Structural equation models showed that a doubling in PFAS exposure at 7 y was associated with losses in diphtheria antibody concentrations at 13 y of 10­30% for the five PFASs. Few associations were observed for anti-tetanus concentrations. CONCLUSIONS: These results are in accord with previous findings of PFAS immunotoxicity at current exposure levels. https://doi.org/10.1289/EHP275.
[Mh] Termos MeSH primário: Anticorpos Antibacterianos/sangue
Toxoide Diftérico/imunologia
Exposição Ambiental
Poluentes Ambientais/sangue
Fluorcarbonetos/sangue
Ácidos Sulfônicos/sangue
Toxoide Tetânico/imunologia
[Mh] Termos MeSH secundário: Adolescente
Criança
Dinamarca
Toxoide Diftérico/administração & dosagem
Monitoramento Ambiental
Feminino
Seres Humanos
Masculino
Estudos Prospectivos
Toxoide Tetânico/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antibodies, Bacterial); 0 (Diphtheria Toxoid); 0 (Environmental Pollutants); 0 (Fluorocarbons); 0 (Sulfonic Acids); 0 (Tetanus Toxoid)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:180206
[Lr] Data última revisão:
180206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE
[do] DOI:10.1289/EHP275


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[PMID]:29248446
[Au] Autor:Sanchez Garcia D; Sjödin M; Hellstrandh M; Norinder U; Nikiforova V; Lindberg J; Wincent E; Bergman Å; Cotgreave I; Munic Kos V
[Ad] Endereço:Swetox, Karolinska Institutet, Unit of Toxicology Sciences, Forskargatan 20, SE-151 36 Södertälje, Sweden.
[Ti] Título:Cellular accumulation and lipid binding of perfluorinated alkylated substances (PFASs) - A comparison with lysosomotropic drugs.
[So] Source:Chem Biol Interact;281:1-10, 2018 Feb 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Many chemicals accumulate in organisms through a variety of different mechanisms. Cationic amphiphilic drugs (CADs) accumulate in lysosomes and bind to membranes causing phospholipidosis, whereas many lipophilic chemicals target adipose tissue. Perfluoroalkyl substances (PFASs) are widely used as surfactants, but many of them are highly bioaccumulating and persistent in the environment, making them notorious environmental toxicants. Understanding the mechanisms of their bioaccumulation is, therefore, important for their regulation and substitution with new, less harmful chemicals. We compared the highly bioaccumulative perfluorooctanesulfonic acid PFOS to its three less bioaccumulative alternatives perfluorooctanoic acid (PFOA), perfluorohexanoic acid (PFHxA) and perfluorobutane sulfonic acid (PFBS), in their ability to accumulate and remain in lung epithelial cells (NCI-H292) and adipocytes (3T3-L1K) in vitro. As a reference point we tested a set of cationic amphiphilic drugs (CADs), known to highly accumulate in cells and strongly bind to phospholipids, together with their respective non-CAD controls. Finally, all compounds were examined for their ability to bind to neutral lipids and phospholipids in cell-free systems. Cellular accumulation and retention of the test compounds were highly correlated between the lung epithelial cells and adipocytes. Interestingly, although an anion itself, intensities of PFOS accumulation and retention in cells were comparable to those of CAD compounds, but PFOS failed to induce phospholipidosis or alter lysosomal volume. Compared to other lipophilicity measures, phospholipophilicity shows the highest correlation (Rˆ2 = 0.75) to cellular accumulation data in both cell types and best distinguishes between high and low accumulating compounds. This indicates that binding to phospholipids may be the most important component in driving high cellular accumulation in lung epithelial cells, as well as in adipocytes, and for both CADs and bioaccumulating PFASs. Obtained continuous PLS models based on compound's affinity for phospholipids and neutral lipids can be used as good prediction models of cellular accumulation and retention of PFASs and CADs.
[Mh] Termos MeSH primário: Ácidos Alcanossulfônicos/metabolismo
Fluorcarbonetos/metabolismo
Lisossomos/metabolismo
Preparações Farmacêuticas/metabolismo
Fosfolipídeos/metabolismo
[Mh] Termos MeSH secundário: Adipócitos/citologia
Adipócitos/metabolismo
Ácidos Alcanossulfônicos/química
Animais
Azitromicina/química
Azitromicina/metabolismo
Caproatos/química
Caproatos/metabolismo
Caprilatos/química
Caprilatos/metabolismo
Cátions/química
Linhagem Celular
Sobrevivência Celular
Células Epiteliais/citologia
Células Epiteliais/metabolismo
Fluorcarbonetos/química
Seres Humanos
Análise dos Mínimos Quadrados
Modelos Lineares
Lipídeos/química
Camundongos
Preparações Farmacêuticas/química
Fosfolipídeos/química
Ácidos Sulfônicos/química
Ácidos Sulfônicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkanesulfonic Acids); 0 (Caproates); 0 (Caprylates); 0 (Cations); 0 (Fluorocarbons); 0 (Lipids); 0 (Pharmaceutical Preparations); 0 (Phospholipids); 0 (Sulfonic Acids); 0 (perfluorobutanesulfonic acid); 83905-01-5 (Azithromycin); 947VD76D3L (perfluorooctanoic acid); 9H2MAI21CL (perfluorooctane sulfonic acid); ZP34Q2220R (perfluorohexanoic acid)
[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:171218
[St] Status:MEDLINE


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[PMID]:28742246
[Au] Autor:Shi H; Fan Z; Hong B; Pera-Titus M
[Ad] Endereço:Eco-Efficient Products and Processes Laboratory (E2P2L), UMI 3464 CNRS-Solvay, Shanghai, 201108, China.
[Ti] Título:Aquivion Perfluorosulfonic Superacid as an Efficient Pickering Interfacial Catalyst for the Hydrolysis of Triglycerides.
[So] Source:ChemSusChem;10(17):3363-3367, 2017 09 11.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Rational design of the surface properties of heterogeneous catalysts can boost the interfacial activity in biphasic reactions through the generation of Pickering emulsions. This concept, termed Pickering interfacial catalysis (PIC), has shown promising credentials in acid-catalyzed transesterification, ester hydrolysis, acetalization, etherification, and alkylation reactions. PIC has now been applied to the efficient, solvent-free hydrolysis of the triglyceride glyceryl trilaurate to lauric acid, catalyzed by Aquivion perfluorosulfonic superacid at mild conditions (100 °C and ambient pressure).
[Mh] Termos MeSH primário: Ácidos Sulfônicos/química
Triglicerídeos/química
[Mh] Termos MeSH secundário: Catálise
Hidrólise
Modelos Moleculares
Conformação Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Sulfonic Acids); 0 (Triglycerides)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:180118
[Lr] Data última revisão:
180118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170726
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700663


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[PMID]:27778249
[Au] Autor:Campochiaro PA; Peters KG
[Ad] Endereço:Department of Ophthalmology, Johns Hopkins University School of Medicine, Baltimore, MD, USA. pcampo@jhmi.edu.
[Ti] Título:Targeting Tie2 for Treatment of Diabetic Retinopathy and Diabetic Macular Edema.
[So] Source:Curr Diab Rep;16(12):126, 2016 12.
[Is] ISSN:1539-0829
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Tie2 is a tyrosine kinase receptor located predominantly on vascular endothelial cells that plays a central role in vascular stability. Angiopoietin-1 (Angpt1), produced by perivascular cells, binds, clusters, and activates Tie2, leading to Tie2 autophosphorylation and downstream signaling. Activated Tie2 increases endothelial cell survival, adhesion, and cell junction integrity, thereby stabilizing the vasculature. Angiopoietin-2 (Angpt2) and vascular endothelial-protein tyrosine phosphatase (VE-PTP) are negative regulators increased by hypoxia; they inactivate Tie2, destabilizing the vasculature and increasing responsiveness to vascular endothelial growth factor (VEGF) and other inflammatory cytokines that stimulate vascular leakage and neovascularization. AKB-9778 is a small-molecule antagonist of VE-PTP which increases phosphorylation of Tie2 even in the presence of high Angpt2 levels. In preclinical studies, AKB-9778 reduced VEGF-induced leakage and ocular neovascularization (NV) and showed additive benefit when combined with VEGF suppression. In two clinical trials in diabetic macular edema (DME) patients, subcutaneous injections of AKB-9778 were safe and provided added benefit to VEGF suppression. Preliminary data suggest that AKB-9778 monotherapy improves diabetic retinopathy. These data suggest that Tie2 activation may be a valuable strategy to treat or prevent diabetic retinopathy.
[Mh] Termos MeSH primário: Compostos de Anilina/uso terapêutico
Retinopatia Diabética/tratamento farmacológico
Edema Macular/tratamento farmacológico
Receptor TIE-2/antagonistas & inibidores
Ácidos Sulfônicos/uso terapêutico
[Mh] Termos MeSH secundário: Angiopoietina-1/fisiologia
Angiopoietina-2/fisiologia
Seres Humanos
Receptor TIE-2/fisiologia
Proteínas Tirosina Fosfatases Classe 3 Semelhantes a Receptores/fisiologia
Transdução de Sinais
Fator A de Crescimento do Endotélio Vascular/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (AKB-9778); 0 (Angiopoietin-1); 0 (Angiopoietin-2); 0 (Aniline Compounds); 0 (Sulfonic Acids); 0 (Vascular Endothelial Growth Factor A); EC 2.7.10.1 (Receptor, TIE-2); EC 3.1.3.48 (Receptor-Like Protein Tyrosine Phosphatases, Class 3)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171210
[Lr] Data última revisão:
171210
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE


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[PMID]:28905987
[Au] Autor:Bryant JL; Gieling RG; Meredith SL; Allen TJ; Walker L; Telfer BA; Supuran CT; Williams KJ; White A
[Ad] Endereço:Division of Diabetes, Endocrinology & Gastroenterology, University of Manchester, Manchester, United Kingdom.
[Ti] Título:Novel carbonic anhydrase IX-targeted therapy enhances the anti-tumour effects of cisplatin in small cell lung cancer.
[So] Source:Int J Cancer;142(1):191-201, 2018 Jan 01.
[Is] ISSN:1097-0215
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Small cell lung cancer (SCLC) has an extremely poor prognosis and methods of improving chemotherapeutic intervention are much sought after. A promising approach lies in inhibiting the tumour-associated enzyme, carbonic anhydrase IX (CA IX), which supports tumour cell survival. The aim of this study was to assess the potential of CA IX inhibition using 4-(3'-(3″,5″-dimethylphenyl)ureido)phenyl sulfamate (S4), for the treatment of human SCLC alone and in combination with cisplatin chemotherapy. Treating SCLC cell lines (DMS 79 and COR-L24) with 100 µM S4 reduced viability in vitro and enhanced cell death when combined with 7 µM cisplatin, most prominently under hypoxic conditions (0.1% O ). When either cell line was grown as a xenograft tumour in nude mice, intraperitoneal injection of 50 mg/kg S4 alone and in combination with 3 mg/kg cisplatin led to significantly reduced tumour growth. Combination therapy was superior to single agents and response was greatly accentuated when administering repeated doses of cisplatin in DMS 79 tumours. The mechanism of therapeutic response was investigated in vitro, where S4 treatment increased apoptosis under hypoxic conditions in both DMS 79 and COR-L24 cells. DMS 79 tumours receiving S4 in vivo also displayed increased apoptosis and necrosis. Combining S4 with cisplatin reduced both the area of hypoxia and CA IX-positive cells within tumours and increased necrosis, suggesting hypoxia-specific targeting. This study presents a novel, targeted approach to improving current SCLC therapy via inhibition of CA IX, which enhances apoptosis and significantly inhibits xenograft tumour growth when administered alone and in combination with cisplatin chemotherapy.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Anidrase Carbônica IX/antagonistas & inibidores
Inibidores Enzimáticos/farmacologia
Neoplasias Pulmonares/tratamento farmacológico
Compostos de Fenilureia/farmacologia
Carcinoma de Pequenas Células do Pulmão/tratamento farmacológico
Ácidos Sulfônicos/farmacologia
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Cisplatino/farmacologia
Sinergismo Farmacológico
Seres Humanos
Camundongos
Camundongos Nus
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-(3'-(3'',5''-dimethylphenyl)ureido)phenyl sulfamate); 0 (Antineoplastic Agents); 0 (Enzyme Inhibitors); 0 (Phenylurea Compounds); 0 (Sulfonic Acids); 9NFU33906Q (sulfamic acid); EC 4.2.1.1 (Carbonic Anhydrase IX); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170915
[St] Status:MEDLINE
[do] DOI:10.1002/ijc.31042


  9 / 6625 MEDLINE  
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[PMID]:29020076
[Au] Autor:Callejón S; Sendra R; Ferrer S; Pardo I
[Ad] Endereço:ENOLAB-Estructura de Recerca Interdisciplinar BioTecMed and Departament de Microbiologia i Ecologia. Universitat de València, c/ Dr. Moliner 50, Burjassot, Spain.
[Ti] Título:Recombinant laccase from Pediococcus acidilactici CECT 5930 with ability to degrade tyramine.
[So] Source:PLoS One;12(10):e0186019, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Biogenic amines degradation by bacterial laccases is little known, so we have cloned and heterologously expressed, in E. coli, a new laccase from Pediococcus acidilactici CECT 5930 (Lpa5930), a lactic acid bacterium commonly found in foods able to degrade tyramine. The recombinant enzyme has been characterized by physical and biochemical assays. Here we report the optimization of expression and purification procedures of this laccase. DNA encoding sequence of laccase from P. acidilactici was amplified by PCR and cloned into the expression plasmid pET28a for induction by isopropyl-ß-D-thiogalactoipyranoside. Protein expression was performed in E. coli BL21(DE3) harboring pGro7 plasmid expressing a chaperone folding assistant induced by arabinose. Purification was performed by column metal-chelating chromatography on Ni-NTA-agarose. The laccase enzyme obtained has an apparent molecular mass of ∼60 kDa, an optimum temperature activity toward 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) of 28°C, and was quickly inactivated at temperatures higher than 70°C. The apparent Km value for ABTS was 1.7 mM and the Vmax obtained was 24 U/mg. In addition to ABTS, recombinant Lpa5930 laccase degraded the biogenic amine tyramine at pH 9.5 and pH 4.0 with or without ABTS as a mediator. Tyramine degradation by laccases could solve the problems generated in food due to the presence of this toxic compound.
[Mh] Termos MeSH primário: Lacase/metabolismo
Pediococcus acidilactici/enzimologia
Proteínas Recombinantes/isolamento & purificação
Tiramina/metabolismo
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Proteínas de Bactérias/química
Sequência de Bases
Benzotiazóis/metabolismo
Clonagem Molecular
Eletroforese em Gel de Poliacrilamida
Concentração de Íons de Hidrogênio
Oxirredução
Proteínas Recombinantes/metabolismo
Análise de Sequência de DNA
Espectrofotometria Ultravioleta
Especificidade por Substrato
Ácidos Sulfônicos/metabolismo
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Benzothiazoles); 0 (Recombinant Proteins); 0 (Sulfonic Acids); 28752-68-3 (2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid); EC 1.10.3.2 (Laccase); X8ZC7V0OX3 (Tyramine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171012
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0186019


  10 / 6625 MEDLINE  
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[PMID]:28903003
[Au] Autor:Yao C; Tu Y; Ding L; Li C; Wang J; Fang H; Huang Y; Zhang K; Lu Q; Wu M; Wang Y
[Ad] Endereço:Institute of Nano-chemistry and Nano-biology, Shanghai University , Shanghai 200444, P.R. China.
[Ti] Título:Tumor Cell-Specific Nuclear Targeting of Functionalized Graphene Quantum Dots In Vivo.
[So] Source:Bioconjug Chem;28(10):2608-2619, 2017 Oct 18.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Specific targeting of tumor tissues is essential for tumor imaging and therapeutics but remains challenging. Here, we report an unprecedented method using synthetic sulfonic-graphene quantum dots (sulfonic-GQDs) to exactly target the cancer cell nuclei in vivo without any bio- ligand modification, with no intervention in cells of normal tissues. The key factor for such selectivity is the high interstitial fluid pressure (IFP) in tumor tissues, which allows the penetration of sulfonic-GQDs into the plasma membrane of tumor cells. In vitro, the sulfonic-GQDs are repelled out of the cell membrane because of the repulsive force between negatively charged sulfonic-GQDs and the cell membranes which contributes to the low distribution in normal tissues in vivo. However, the plasma membrane-crossing process can be activated by incubating cells in ultrathin film culture medium because of the attachment of sulfonic-GQDs on cell memebranes. Molecular dynamics simulations demonstrated that, once transported across the plasma membrane, the negatively charged functional groups of these GQDs will leave the membrane with a self-cleaning function retaining a small enough size to achieve penetration through the nuclear membrane into the nucleus. Our study showed that IFP is a previously unrecognized mechanism for specific targeting of tumor cell nuclei and suggested that sulfonic-GQDs may be developed into novel tools for tumor-specific imaging and therapeutics.
[Mh] Termos MeSH primário: Núcleo Celular/metabolismo
Grafite/química
Grafite/metabolismo
Pontos Quânticos/química
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Membrana Celular/metabolismo
Líquido Extracelular/metabolismo
Grafite/farmacocinética
Seres Humanos
Camundongos
Conformação Molecular
Simulação de Dinâmica Molecular
Ácidos Sulfônicos/química
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sulfonic Acids); 7782-42-5 (Graphite)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171107
[Lr] Data última revisão:
171107
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170914
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.7b00466



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