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  1 / 55196 MEDLINE  
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[PMID]:29377926
[Au] Autor:Pan P; Zhao F; Ning J; Zhang L; Ouyang X; Zang H
[Ad] Endereço:College of Forestry, Jiangxi Agricultural University, Nanchang, China.
[Ti] Título:Impact of understory vegetation on soil carbon and nitrogen dynamic in aerially seeded Pinus massoniana plantations.
[So] Source:PLoS One;13(1):e0191952, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Understory vegetation plays a vital role in regulating soil carbon (C) and nitrogen (N) characteristics due to differences in plant functional traits. Different understory vegetation types have been reported following aerial seeding. While aerial seeding is common in areas with serious soil erosion, few studies have been conducted to investigate changes in soil C and N cycling as affected by understory vegetation in aerially seeded plantations. Here, we studied soil C and N characteristics under two naturally formed understory vegetation types (Dicranopteris and graminoid) in aerially seeded Pinus massoniana Lamb plantations. Across the two studied understory vegetation types, soil organic C was significantly correlated with all measured soil N variables, including total N, available N, microbial biomass N and water-soluble organic N, while microbial biomass C was correlated with all measured variables except soil organic C. Dicranopteris and graminoid differed in their effects on soil C and N process. Except water-soluble organic C, all the other C and N variables were higher in soils with graminoids. The higher levels of soil organic C, microbial biomass C, total N, available N, microbial biomass N and water-soluble organic N were consistent with the higher litter and root quality (C/N) of graminoid vegetation compared to Dicranopteris. Changes in soil C and N cycles might be impacted by understory vegetation types via differences in litter or root quality.
[Mh] Termos MeSH primário: Carbono/metabolismo
Nitrogênio/metabolismo
Pinus/metabolismo
Plantas/metabolismo
Solo/química
[Mh] Termos MeSH secundário: Biomassa
Carbono/química
Nitrogênio/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Soil); 7440-44-0 (Carbon); N762921K75 (Nitrogen)
[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:180130
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191952


  2 / 55196 MEDLINE  
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[PMID]:28987406
[Au] Autor:Szewczyk R; Kusmierska A; Bernat P
[Ad] Endereço:Department of Industrial Microbiology and Biotechnology, Institute of Microbiology, Biotechnology and Immunology, Faculty of Biology and Environmental Protection, University of Lódz, Banacha 12/16, 90-237 Lódz, Poland. Electronic address: rafal.szewczyk@biol.uni.lodz.pl.
[Ti] Título:Ametryn removal by Metarhizium brunneum: Biodegradation pathway proposal and metabolic background revealed.
[So] Source:Chemosphere;190:174-183, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ametryn is a representative of a class of s-triazine herbicides absorbed by plant roots and leaves and characterized as a photosynthesis inhibitor. It is still in use in some countries in the farming of pineapples, soybean, corn, cotton, sugar cane or bananas; however, due to the adverse effects of s-triazine herbicides on living organisms use of these pesticides in the European Union has been banned. In the current study, we characterized the biodegradation of ametryn (100 mg L ) by entomopathogenic fungal cosmopolite Metarhizium brunneum. Ametryn significantly inhibited the growth and glucose uptake in fungal cultures. The concentration of the xenobiotic drops to 87.75 mg L at the end of culturing and the biodegradation process leads to formation of four metabolites: 2-hydroxy atrazine, ethyl hydroxylated ametryn, S-demethylated ametryn and deethylametryn. Inhibited growth is reflected in the metabolomics data, where significant differences in concentrations of L-proline, gamma-aminobutyric acid, L-glutamine, 4-hydroxyproline, L-glutamic acid, ornithine and L-arginine were observed in the presence of the xenobiotic when compared to control cultures. The metabolomics data demonstrated that the presence of ametryn in the fungal culture induced oxidative stress and serious disruptions of the carbon and nitrogen metabolism. Our results provide deeper insights into the microorganism strategy for xenobiotic biodegradation which may result in future enhancements to ametryn removal by the tested strain.
[Mh] Termos MeSH primário: Herbicidas/isolamento & purificação
Metarhizium/metabolismo
Triazinas/metabolismo
[Mh] Termos MeSH secundário: Atrazina
Biodegradação Ambiental
Carbono/metabolismo
Ácido Glutâmico
Herbicidas/metabolismo
Herbicidas/farmacologia
Nitrogênio/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Prolina
Saccharum/metabolismo
Triazinas/isolamento & purificação
Triazinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Herbicides); 0 (Triazines); 1SPQ95183Y (ametryne); 3KX376GY7L (Glutamic Acid); 7440-44-0 (Carbon); 9DLQ4CIU6V (Proline); N762921K75 (Nitrogen); QJA9M5H4IM (Atrazine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171009
[St] Status:MEDLINE


  3 / 55196 MEDLINE  
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[PMID]:28278777
[Au] Autor:Lu YF; Ma LJ; Ma L; Shan B; Chang JJ
[Ad] Endereço:a School of Ecology and Environmental Science, Yunnan University , Kunming , People's Republic of China.
[Ti] Título:Improvement of start-up and nitrogen removal of the anammox process in reactors inoculated with conventional activated sludge using biofilm carrier materials.
[So] Source:Environ Technol;39(1):59-67, 2018 Jan.
[Is] ISSN:0959-3330
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The start-up of the anaerobic ammonium oxidation (anammox) process in three up-flow column reactors seeded with common mixed activated sludge and added with three materials, sponge (R1), sponge + volcanic rock (R2) and sponge + charcoal (R3), as carriers for biofilm formation were comparatively investigated in this study. The supplement of volcanic rock and charcoal could significantly shorten the start-up time of the anammox process, which primarily occurred in the activity-enhanced phase, with ammonium and nitrite removal efficiencies stabilized above 92.5% and 93.4% after an operation period of 145, 105 and 121 d for R1, R2 and R3, respectively. After the successful anammox start-up, R2 performed significantly better in TN removal (p < .05), achieving an average rate of 91.0% and 191.5 g N m d compared to R1 of 88.4% and 172.1 g N m d , and R3 of 89.9% and 180.1 g N m d in the steady running phase. The ratios of consumed [Formula: see text] and generated [Formula: see text]/consumed [Formula: see text] after anammox start-up were lower than the theoretical values, probably suggesting the simultaneous existences of anammox, denitrification as well as nitrification processes in the reactors. A reddish brown biofilm was wrapped on the carriers and morphological detection of biofilm displayed the presentations of thick and compact floc aggregates and some filamentous bacteria on the sponge, and spherical-, ovoid- and shortrod-shaped microorganisms on the volcanic rock and charcoal. Using porous material as carrier for biofilm development is an effective strategy for practical application of the anammox reactor.
[Mh] Termos MeSH primário: Biofilmes/crescimento & desenvolvimento
Nitrogênio/metabolismo
Eliminação de Resíduos Líquidos/métodos
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Compostos de Amônio
Reatores Biológicos/microbiologia
Carvão Vegetal
Crescimento Quimioautotrófico
Desnitrificação
Nitrificação
Nitritos
Nitrogênio/análise
Oxirredução
Esgotos/microbiologia
Poluentes Químicos da Água/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ammonium Compounds); 0 (Nitrites); 0 (Sewage); 0 (Water Pollutants, Chemical); 16291-96-6 (Charcoal); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170311
[St] Status:MEDLINE
[do] DOI:10.1080/09593330.2017.1294624


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[PMID]:28266229
[Au] Autor:Liu Y; Lei Y; Xi Y; Liao Z; Zhang X
[Ad] Endereço:a College of Environmental Science and Engineering, Fujian Key Laboratory of Pollution Control & Resource Reuse , Fujian Normal University , Fuzhou , People's Republic of China.
[Ti] Título:High-load domestic wastewater treatment using a combined anaerobic-aerobic bio-filter with coal cinder as medium.
[So] Source:Environ Technol;39(1):102-108, 2018 Jan.
[Is] ISSN:0959-3330
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A combined anaerobic-aerobic bio-filter technology was used for field treatment of high-organic-load domestic wastewater with coal cinder as the bio-filter medium. The effects of parameters, including hydraulic retention time (HRT) and backflow ratio, on the decrease in the chemical oxygen demand (COD), NH -N, total nitrogen (TN), total phosphorus (TP), and turbidity were investigated. The results showed the obvious influence of the HRT and ratio of backflow on wastewater treatment. Under the optimal HRT condition of 18 h, the removal efficiencies of COD, NH -N, TN, TP, and turbidity were 67.9%, 95.6%, 30.4%, 65.6%, and 83.8%, respectively. When the backflow ratio (2:1) was added to the treatment system, the TN removal obviously increased, and the removal efficiencies of COD, NH -N, TN, TP, and turbidity were 88.1%, 91.7%, 69.9%, 69.6%, and 97.5%, respectively. These results indicated that the combined technology has the potential as a treatment method for high-organic-load domestic wastewater.
[Mh] Termos MeSH primário: Filtração/métodos
Eliminação de Resíduos Líquidos/métodos
Águas Residuais/química
[Mh] Termos MeSH secundário: Anaerobiose
Carvão Mineral
Nitrogênio
Fósforo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coal); 0 (Waste Water); 27YLU75U4W (Phosphorus); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170308
[St] Status:MEDLINE
[do] DOI:10.1080/09593330.2017.1296496


  5 / 55196 MEDLINE  
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[PMID]:29231002
[Au] Autor:Xia ZY; Zhai XD; Liu BB; Zheng Z; Zhao LL; Mo YN
[Ad] Endereço:School of Forensic Medicine, Henan University of Science and Technology, Luoyang 471003, China.
[Ti] Título:[Relationship between Electrical Conductivity and Decomposition Rate of Rat Postmortem Skeletal Muscle].
[So] Source:Fa Yi Xue Za Zhi;33(1):17-20, 2017 Feb.
[Is] ISSN:1004-5619
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:OBJECTIVES: To analyze the relationship among electrical conductivity (EC), total volatile basic nitrogen (TVB-N), which is an index of decomposition rate for meat production, and postmortem interval (PMI). To explore the feasibility of EC as an index of cadaveric skeletal muscle decomposition rate and lay the foundation for PMI estimation. METHODS: Healthy Sprague-Dawley rats were sacrificed by cervical vertebrae dislocation and kept at 28 ℃. Muscle of rear limbs was removed at different PMI, homogenized in deionized water and then skeletal extraction liquid of mass concentration 0.1 g/mL was prepared. EC and TVB-N of extraction liquid were separately determined. The correlation between EC ( 1) and TVB-N ( 2) was analyzed, and their regression function was established. The relationship between PMI ( ) and these two parameters were studied, and their regression functions were separately established. RESULTS: The change trends of EC and TVB-N of skeletal extraction liquid at different PMI were almost the same, and there was a linear positive correlation between them. The regression equation was 2=0.14 1-164.91( ²=0.982). EC and TVB-N of skeletal muscle changed significantly with PMI, and the regression functions were =19.38 1³-370.68 1²+2 526.03 1-717.06( ²=0.994), and =2.56 2³-48.39 2²+330.60 2-255.04( ²=0.997), respectively. CONCLUSIONS: EC and TVB-N of rat postmortem skeletal muscle show similar change trends, which can be used as an index for decomposition rate of cadaveric skeletal muscle and provide a method for further study of late PMI estimation.
[Mh] Termos MeSH primário: Condutividade Elétrica
Patologia Legal
Músculo Esquelético/patologia
Mudanças Depois da Morte
[Mh] Termos MeSH secundário: Animais
Autopsia
Nitrogênio
Ratos
Ratos Sprague-Dawley
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE
[do] DOI:10.3969/j.issn.1004-5619.2017.01.004


  6 / 55196 MEDLINE  
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[PMID]:29335469
[Au] Autor:Aunkham A; Zahn M; Kesireddy A; Pothula KR; Schulte A; Baslé A; Kleinekathöfer U; Suginta W; van den Berg B
[Ad] Endereço:Biochemistry-Electrochemistry Research Unit, Institute of Science, Suranaree University of Technology, Nakhon Ratchasima, 30000, Thailand.
[Ti] Título:Structural basis for chitin acquisition by marine Vibrio species.
[So] Source:Nat Commun;9(1):220, 2018 01 15.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Chitin, an insoluble polymer of N-acetylglucosamine, is one of the most abundant biopolymers on Earth. By degrading chitin, chitinolytic bacteria such as Vibrio harveyi are critical for chitin recycling and maintenance of carbon and nitrogen cycles in the world's oceans. A decisive step in chitin degradation is the uptake of chito-oligosaccharides by an outer membrane protein channel named chitoporin (ChiP). Here, we report X-ray crystal structures of ChiP from V. harveyi in the presence and absence of chito-oligosaccharides. Structures without bound sugar reveal a trimeric assembly with an unprecedented closing of the transport pore by the N-terminus of a neighboring subunit. Substrate binding ejects the pore plug to open the transport channel. Together with molecular dynamics simulations, electrophysiology and in vitro transport assays our data provide an explanation for the exceptional affinity of ChiP for chito-oligosaccharides and point to an important role of the N-terminal gate in substrate transport.
[Mh] Termos MeSH primário: Carbono/metabolismo
Quitina/metabolismo
Nitrogênio/metabolismo
Vibrio/metabolismo
[Mh] Termos MeSH secundário: Acetilglucosamina/metabolismo
Proteínas da Membrana Bacteriana Externa/química
Proteínas da Membrana Bacteriana Externa/genética
Proteínas da Membrana Bacteriana Externa/metabolismo
Ciclo do Carbono
Cristalografia por Raios X
Modelos Moleculares
Ciclo do Nitrogênio
Oceanos e Mares
Oligossacarídeos/metabolismo
Porinas/química
Porinas/genética
Porinas/metabolismo
Conformação Proteica
Água do Mar/química
Água do Mar/microbiologia
Vibrio/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Bacterial Outer Membrane Proteins); 0 (Oligosaccharides); 0 (Porins); 1398-61-4 (Chitin); 7440-44-0 (Carbon); N762921K75 (Nitrogen); V956696549 (Acetylglucosamine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180117
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02523-y


  7 / 55196 MEDLINE  
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[PMID]:29362437
[Au] Autor:Otero XL; De La Peña-Lastra S; Pérez-Alberti A; Ferreira TO; Huerta-Diaz MA
[Ad] Endereço:Departamento de Edafoloxía e Química Agrícola, Campus Vida, Facultade de Bioloxía, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
[Ti] Título:Seabird colonies as important global drivers in the nitrogen and phosphorus cycles.
[So] Source:Nat Commun;9(1):246, 2018 01 23.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Seabirds drastically transform the environmental conditions of the sites where they establish their breeding colonies via soil, sediment, and water eutrophication (hereafter termed ornitheutrophication). Here, we report worldwide amounts of total nitrogen (N) and total phosphorus (P) excreted by seabirds using an inventory of global seabird populations applied to a bioenergetics model. We estimate these fluxes to be 591 Gg N y and 99 Gg P y , respectively, with the Antarctic and Southern coasts receiving the highest N and P inputs. We show that these inputs are of similar magnitude to others considered in global N and P cycles, with concentrations per unit of surface area in seabird colonies among the highest measured on the Earth's surface. Finally, an important fraction of the total excreted N (72.5 Gg y ) and P (21.8 Gg y ) can be readily solubilized, increasing their short-term bioavailability in continental and coastal waters located near the seabird colonies.
[Mh] Termos MeSH primário: Aves/fisiologia
Ecossistema
Nitrogênio/metabolismo
Fósforo/metabolismo
[Mh] Termos MeSH secundário: Migração Animal/fisiologia
Animais
Regiões Antárticas
Aves/classificação
Conservação dos Recursos Naturais
Água Doce
Geografia
Ciclo do Nitrogênio
Oceanos e Mares
Água do Mar
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
27YLU75U4W (Phosphorus); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180125
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02446-8


  8 / 55196 MEDLINE  
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[PMID]:28968514
[Au] Autor:Huang Y; Li P; Chen G; Peng L; Chen X
[Ad] Endereço:Shanghai Key Lab for Urban Ecological Processes and Eco-Restoration, School of Ecological and Environmental Sciences, East China Normal University, No.500 Dong Chuan Road, Shanghai 200241, PR China.
[Ti] Título:The production of cyanobacterial carbon under nitrogen-limited cultivation and its potential for nitrate removal.
[So] Source:Chemosphere;190:1-8, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Harmful cyanobacterial blooms (CyanoHABs) represent a serious threat to aquatic ecosystems. A beneficial use for these harmful microorganisms would be a promising resolution of this urgent issue. This study applied a simple method, nitrogen limitation, to cultivate cyanobacteria aimed at producing cyanobacterial carbon for denitrification. Under nitrogen-limited conditions, the common cyanobacterium, Microcystis, efficiently used nitrate, and had a higher intracellular C/N ratio. More importantly, organic carbons easily leached from its dry powder; these leachates were biodegradable and contained a larger amount of dissolved organic carbon (DOC) and carbohydrates, but a smaller amount of dissolved total nitrogen (DTN) and proteins. When applied to an anoxic system with a sediment-water interface, a significant increase of the specific NO -N removal rate was observed that was 14.2 times greater than that of the control. This study first suggests that nitrogen-limited cultivation is an efficient way to induce organic and carbohydrate accumulation in cyanobacteria, as well as a high C/N ratio, and that these cyanobacteria can act as a promising carbon source for denitrification. The results indicate that application as a carbon source is not only a new way to utilize cyanobacteria, but it also contributes to nitrogen removal in aquatic ecosystems, further limiting the proliferation of CyanoHABs.
[Mh] Termos MeSH primário: Biodegradação Ambiental
Carbono/metabolismo
Cianobactérias/metabolismo
Desnitrificação
Nitratos/isolamento & purificação
Nitrogênio/deficiência
[Mh] Termos MeSH secundário: Ecossistema
Microcystis/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Nitrates); 7440-44-0 (Carbon); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE


  9 / 55196 MEDLINE  
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[PMID]:28462789
[Au] Autor:Ren J; Sang Y; Lu J; Yao YF
[Ad] Endereço:Laboratory of Bacterial Pathogenesis, Department of Microbiology and Immunology, Institutes of Medical Sciences, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China.
[Ti] Título:Protein Acetylation and Its Role in Bacterial Virulence.
[So] Source:Trends Microbiol;25(9):768-779, 2017 Sep.
[Is] ISSN:1878-4380
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Protein acetylation is a universal post-translational modification which is found in both eukaryotes and prokaryotes. This process is achieved enzymatically by the protein acetyltransferase Pat, and nonenzymatically by metabolic intermediates (e.g., acetyl phosphate) in bacteria. Protein acetylation plays a role in bacterial chemotaxis, metabolism, DNA replication, and other cellular processes. Recently, accumulating evidence has suggested that protein acetylation might be involved in bacterial virulence because a number of bacterial virulence factors are acetylated. In this review, we summarize the progress in understanding bacterial protein acetylation and discuss how it mediates bacterial virulence.
[Mh] Termos MeSH primário: Acetiltransferases/metabolismo
Bactérias/metabolismo
Bactérias/patogenicidade
Proteínas/metabolismo
[Mh] Termos MeSH secundário: Acetilação
Bactérias/enzimologia
Proteínas de Bactérias/metabolismo
Carbono/metabolismo
Nitrogênio/metabolismo
Processamento de Proteína Pós-Traducional
Proteômica
Virulência
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Proteins); 7440-44-0 (Carbon); EC 2.3.1.- (Acetyltransferases); EC 2.3.1.- (protein acyltransferase); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE


  10 / 55196 MEDLINE  
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[PMID]:29291440
[Au] Autor:Vágvölgyi M; Martins A; Kulmány Á; Zupkó I; Gáti T; Simon A; Tóth G; Hunyadi A
[Ad] Endereço:Institute of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Szeged, Hungary.
[Ti] Título:Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam.
[So] Source:Eur J Med Chem;144:730-739, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Multidrug resistance is a widespread problem among various diseases and cancer is no exception. We had previously described the chemo-sensitizing activity of ecdysteroid derivatives with low polarity on drug susceptible and multi-drug resistant (MDR) cancer cells. We have also shown that these molecules have a marked selectivity towards the MDR cells. Recent studies on the oximation of various steroid derivatives indicated remarkable increase in their antitumor activity, but there is no related bioactivity data on ecdysteroid oximes. In our present study, 13 novel ecdysteroid derivatives (oximes, oxime ethers and a lactam) and one known compound were synthesized from 20-hydroxyecdysone 2,3;20,22-diacetonide and fully characterized by comprehensive NMR techniques revealing their complete H and C signal assignments. The compounds exerted moderate to strong in vitro antiproliferative activity on HeLa, SiHa, MCF-7 and MDA-MB-231 cell lines. Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. All compounds exerted potent chemo-sensitizing activity towards doxorubicin on a mouse lymphoma cell line and on its MDR counterpart, and, on the latter, the lactam was found the most active. Because of its MDR-selective chemo-sensitizing activity with no functional effect on P-gp, this lactam is of high potential interest as a new lead for further antitumor studies.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Ecdisteroides/farmacologia
Éteres/farmacologia
Lactamas/farmacologia
Neoplasias/tratamento farmacológico
Nitrogênio/farmacologia
Oximas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Resistência a Múltiplos Medicamentos/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Ecdisteroides/síntese química
Ecdisteroides/química
Éteres/síntese química
Éteres/química
Seres Humanos
Lactamas/síntese química
Lactamas/química
Estrutura Molecular
Neoplasias/patologia
Nitrogênio/química
Oximas/síntese química
Oximas/química
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Ecdysteroids); 0 (Ethers); 0 (Lactams); 0 (Oximes); N762921K75 (Nitrogen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180102
[St] Status:MEDLINE



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