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Pesquisa : D02.065.884.725 [Categoria DeCS]
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[PMID]:29217384
[Au] Autor:Markowicz-Piasecka M; Huttunen KM; Mikiciuk-Olasik E; Sikora J
[Ad] Endereço:Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszynskiego1, 90-151 Lodz, Poland. Electronic address: magdalena.markowicz@umed.lodz.pl.
[Ti] Título:Biocompatible sulfenamide and sulfonamide derivatives of metformin can exert beneficial effects on plasma haemostasis.
[So] Source:Chem Biol Interact;280:15-27, 2018 Jan 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:As the pharmacokinetic properties of metformin are unfavourable, several analogues and prodrugs have been synthesised to improve its bioavailability. The aim of this study was to assess the plasma stability of sulfenamide and sulfonamide derivatives of metformin and establish their effects on plasma haemostasis and integrity of red blood cells (RBCs). The overall haemostasis potential was evaluated spectrophotometrically by clot formation and lysis test (CL-test). PT (Prothrombin Time) and APTT (Activated Partial Tromboplastin Time) were used to evaluate the effects if the compounds on the extrinsic and intrinsic coagulation pathway. Haemolysis assay, microscopy and flow cytometry studies were conducted to determine the effect of the compounds on RBCs. Two sulfonamide and one sulfenamide derivatives of metformin were associated with a statistically significant decrease in the overall potential of clot formation and fibrinolysis (↓ CL ), suggesting that these compounds may exert beneficial effects regarding plasma haemostasis, which is frequently impaired in diabetic patients. p- and o-Nitrobenzene sulfonamides contributed to the beneficial change in kinetic parameters of clot formation and fibrinolysis. o-Nitrobenzene sulfonamide significantly increased thrombin generation time (↑ TGt) and was also found to prolong both APTT and PT. All compounds did not exert any effects on the integrity of RBCs over the concentration range 0.006-0.6 µmol/mL which constitutes the expected therapeutic concentration. In conclusion, sulfonamide derivatives of metformin present potentially beneficial properties in terms of plasma haemostasis which is frequently impaired in T2DM patients. Therefore, metformin sulfonamides may become a prototype for further design and synthesis of novel metformin analogues and prodrugs with improved pharmacokinetic properties.
[Mh] Termos MeSH primário: Materiais Biocompatíveis/química
Hemólise/efeitos dos fármacos
Metformina/análogos & derivados
Sulfamerazina/química
Sulfanilamidas/química
[Mh] Termos MeSH secundário: Materiais Biocompatíveis/metabolismo
Materiais Biocompatíveis/farmacologia
Estabilidade de Medicamentos
Eritrócitos/citologia
Eritrócitos/efeitos dos fármacos
Eritrócitos/metabolismo
Fibrinólise/efeitos dos fármacos
Metformina/metabolismo
Metformina/farmacologia
Microscopia de Contraste de Fase
Tempo de Tromboplastina Parcial
Tempo de Protrombina
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biocompatible Materials); 0 (Sulfanilamides); 0 (sulfenamide); 21240MF57M (sulfanilamide); 9100L32L2N (Metformin); UR1SAB295F (Sulfamerazine)
[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:171209
[St] Status:MEDLINE


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[PMID]:29289291
[Au] Autor:Bennett KA; Kelly SD; Tang X; Reid BJ
[Ad] Endereço:School of Environmental Sciences, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK.
[Ti] Título:Potential for natural and enhanced attenuation of sulphanilamide in a contaminated chalk aquifer.
[So] Source:J Environ Sci (China);62:39-48, 2017 Dec.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Understanding antibiotic biodegradation is important to the appreciation of their fate and removal from the environment. In this research an Isotope Ratio Mass Spectrometry (IRMS) method was developed to evaluate the extent of biodegradation of the antibiotic, sulphanilamide, in contaminated groundwater. Results indicted an enrichment in δ C of 8.44‰ from -26.56 (at the contaminant source) to -18.12‰ (300m downfield of the source). These results confirm reductions in sulphanilamide concentrations (from 650 to 10mg/L) across the contaminant plume to be attributable to biodegradation (56%) vs. other natural attenuation processes, such as dilution or dispersion (42%). To understand the controls on sulphanilamide degradation ex-situ microcosms assessed the influence of sulphanilamide concentration, redox conditions and an alternative carbon source. Results indicated, high levels of anaerobic capacity (~50% mineralisation) to degrade sulphanilamide under high (263mg/L), moderate (10mg/L) and low (0.02mg/L) substrate concentrations. The addition of electron acceptors; nitrate and sulphate, did not significantly enhance the capacity of the groundwater to anaerobically biodegrade sulphanilamide. Interestingly, where alternative carbon sources were present, the addition of nitrate and sulphate inhibited sulphanilamide biodegradation. These results suggest, under in-situ conditions, when a preferential carbon source was available for biodegradation, sulphanilamide could be acting as a nitrogen and/or sulphur source. These findings are important as they highlight sulphanilamide being used as a carbon and a putative nitrogen and sulphur source, under prevailing iron reducing conditions.
[Mh] Termos MeSH primário: Água Subterrânea/química
Sulfanilamidas/análise
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Biodegradação Ambiental
Carbonato de Cálcio
Microbiologia da Água
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sulfanilamides); 0 (Water Pollutants, Chemical); 21240MF57M (sulfanilamide); H0G9379FGK (Calcium Carbonate)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180103
[Lr] Data última revisão:
180103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180101
[St] Status:MEDLINE


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[PMID]:28611469
[Au] Autor:Angius F; Piras E; Uda S; Madeddu C; Serpe R; Bigi R; Chen W; Dittmer DP; Pompei R; Ingianni A
[Ad] Endereço:Department of Biomedical Sciences, University of Cagliari, Cagliari, Italy.
[Ti] Título:Antimicrobial sulfonamides clear latent Kaposi sarcoma herpesvirus infection and impair MDM2-p53 complex formation.
[So] Source:J Antibiot (Tokyo);70(9):962-966, 2017 Aug.
[Is] ISSN:0021-8820
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Kaposi sarcoma herpesvirus (KSHV), also known as human herpesvirus 8, is the causative agent of Kaposi sarcoma; this malignant angiosarcoma is usually treated with conventional antitumor agents that can control disease evolution, but do not clear the latent KSHV episome that binds to cellular DNA. Some commercial antibacterial sulfonamides were tested for the ability to suppress latent KSHV. Quantitative PCR (qPCR) and cytofluorometry assays were used for detecting both viral DNA and the latency factor LANA (latency-associated nuclear antigen) in BC3 cells, respectively. The capacity of sulfonamides to impair MDM2-p53 complex formation was detected by an enzyme-linked immunosorbent assay method. The analysis of variance was performed according to one-way analysis of variance with Fisher as a post hoc test. Here we show that sulfonamide antibiotics are able to suppress the KSHV latent state in permanently infected BC3 lymphoma cells and interfere with the formation of the MDM2-p53 complex that KSHV seemingly needs to support latency and to trigger tumor cell transformation. These findings detected a new molecular target for the activity of sulfonamides and offer a new potential perspective for treating KSHV-induced lymphoproliferative diseases.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antivirais/farmacologia
Herpesvirus Humano 8/efeitos dos fármacos
Proteínas Proto-Oncogênicas c-mdm2/antagonistas & inibidores
Sulfonamidas/farmacologia
Proteína Supressora de Tumor p53/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antibacterianos/efeitos adversos
Antígenos Virais/metabolismo
Antivirais/efeitos adversos
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Transformação Celular Neoplásica/efeitos dos fármacos
Transformação Celular Viral/efeitos dos fármacos
Células Cultivadas
DNA Viral/metabolismo
Herpesvirus Humano 8/crescimento & desenvolvimento
Herpesvirus Humano 8/metabolismo
Células Endoteliais da Veia Umbilical Humana/citologia
Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos
Células Endoteliais da Veia Umbilical Humana/metabolismo
Células Endoteliais da Veia Umbilical Humana/virologia
Seres Humanos
Concentração Inibidora 50
Proteínas Nucleares/metabolismo
Multimerização Proteica/efeitos dos fármacos
Proteínas Proto-Oncogênicas c-mdm2/química
Proteínas Proto-Oncogênicas c-mdm2/genética
Proteínas Proto-Oncogênicas c-mdm2/metabolismo
Proteínas Recombinantes de Fusão/química
Proteínas Recombinantes de Fusão/metabolismo
Sulfaguanidina/efeitos adversos
Sulfaguanidina/farmacologia
Sulfametoxazol/efeitos adversos
Sulfametoxazol/farmacologia
Sulfanilamidas/efeitos adversos
Sulfanilamidas/farmacologia
Sulfatiazóis/efeitos adversos
Sulfatiazóis/farmacologia
Sulfonamidas/efeitos adversos
Proteína Supressora de Tumor p53/química
Proteína Supressora de Tumor p53/genética
Proteína Supressora de Tumor p53/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antigens, Viral); 0 (Antiviral Agents); 0 (DNA, Viral); 0 (Nuclear Proteins); 0 (Recombinant Fusion Proteins); 0 (Sulfanilamides); 0 (Sulfathiazoles); 0 (Sulfonamides); 0 (TP53 protein, human); 0 (Tumor Suppressor Protein p53); 0 (latency-associated nuclear antigen); 15XQ8043FN (Sulfaguanidine); 21240MF57M (sulfanilamide); EC 2.3.2.27 (MDM2 protein, human); EC 2.3.2.27 (Proto-Oncogene Proteins c-mdm2); JE42381TNV (Sulfamethoxazole); Y7FKS2XWQH (sulfathiazole)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170907
[Lr] Data última revisão:
170907
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170615
[St] Status:MEDLINE
[do] DOI:10.1038/ja.2017.67


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[PMID]:28431390
[Au] Autor:García-Muñoz P; Pliego G; Zazo JA; Bahamonde A; Casas JA
[Ad] Endereço:Sección departamental de Ingeniería Química, Facultad de Ciencias, Universidad Autónoma de Madrid, 28049 Madrid, Spain. Electronic address: patricia.garciam@uam.es.
[Ti] Título:Sulfonamides photoassisted oxidation treatments catalyzed by ilmenite.
[So] Source:Chemosphere;180:523-530, 2017 Aug.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This work assesses the feasibility of several advanced oxidation processes (CWPO Catalytic Wet Peroxide Oxidation), Photocatalysis and their combination (CWPO-Photoassisted process) for sulfonamide antibiotic degradation. Raw ilmenite was used as catalyst in both processes, because of the presence of iron and titanium in its structure. Despite both treatments allowed reaching a total starting antibiotic depletion working at pH = 3 and T = 30 °C within 30 min reaction time, significant differences were observed in terms of mineralization. Thus, whereas photocatalytic process just reduced 35% of initial TOC after 120 min, a 85% of mineralization was reached in the presence of H O (CWPO-Photoassisted process) which was related to the oxidation pathway. Only a 35% of mineralization was reached in case of CWPO. In this sense, the degradation route under CWPO-Photoassisted process displayed a mechanism based on the hydroxylation that led to lower molecular weight intermediates. On the contrary, under photocatalysis conditions, the appearance of higher molecular weight intermediates due to organic radical recombination indicates the prevailing of a condensation mechanism.
[Mh] Termos MeSH primário: Ferro/química
Modelos Químicos
Processos Fotoquímicos
Sulfonamidas/química
Titânio/química
[Mh] Termos MeSH secundário: Catálise
Peróxido de Hidrogênio/química
Oxirredução
Peróxidos/química
Sulfanilamidas
Eliminação de Resíduos Líquidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Peroxides); 0 (Sulfanilamides); 0 (Sulfonamides); 12168-52-4 (ilmenite); 21240MF57M (sulfanilamide); BBX060AN9V (Hydrogen Peroxide); D1JT611TNE (Titanium); E1UOL152H7 (Iron)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170724
[Lr] Data última revisão:
170724
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170422
[St] Status:MEDLINE


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[PMID]:28319782
[Au] Autor:Devender N; Gunjan S; Tripathi R; Tripathi RP
[Ad] Endereço:Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
[Ti] Título:Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores.
[So] Source:Eur J Med Chem;131:171-184, 2017 May 05.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC of 1.87, 1.93, 2.00, 2.17 µM against CQ sensitive Pf3D7 strain and 1.69, 2.12, 1.60, 2.19 µM against CQ resistant PfK1 strain, respectively.
[Mh] Termos MeSH primário: Antimaláricos/farmacologia
Plasmodium falciparum/efeitos dos fármacos
Sulfanilamidas/farmacologia
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Antimaláricos/síntese química
Antimaláricos/química
Cercopithecus aethiops
Relação Dose-Resposta a Droga
Indóis/síntese química
Indóis/química
Indóis/farmacologia
Estrutura Molecular
Testes de Sensibilidade Parasitária
Relação Estrutura-Atividade
Sulfanilamidas/química
Triazóis/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Indoles); 0 (Sulfanilamides); 0 (Triazoles); 21240MF57M (sulfanilamide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170512
[Lr] Data última revisão:
170512
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170321
[St] Status:MEDLINE


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[PMID]:28318023
[Au] Autor:Paine MF
[Ad] Endereço:College of Pharmacy, Washington State University, Spokane, Washington, USA.
[Ti] Título:Therapeutic disasters that hastened safety testing of new drugs.
[So] Source:Clin Pharmacol Ther;101(4):430-434, 2017 Apr.
[Is] ISSN:1532-6535
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:New drugs were not required to undergo premarket safety testing in the United States until 1938, when a therapeutic disaster-the Elixir Sulfanilamide tragedy-prompted Congress to pass a bill mandating this now-routine process. History repeated itself nearly 25 years later, when another therapeutic disaster-the thalidomide tragedy-led to passage of new amendments in 1962 to ensure drug efficacy and greater drug safety. As is typical with historical events, critical information was gained that led to novel approaches for understanding, predicting, diagnosing, and managing drug-induced toxicities. Continued refinement of current, along with development of new, approaches will mitigate future drug-related catastrophes, with the goal of avoiding them entirely.
[Mh] Termos MeSH primário: Aprovação de Drogas/história
Aprovação de Drogas/legislação & jurisprudência
Legislação de Medicamentos/história
United States Food and Drug Administration/história
[Mh] Termos MeSH secundário: Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/história
História do Século XX
Seres Humanos
Segurança
Sulfanilamidas/efeitos adversos
Sulfanilamidas/história
Estados Unidos
[Pt] Tipo de publicação:EDITORIAL; HISTORICAL ARTICLE
[Nm] Nome de substância:
0 (Sulfanilamides); 21240MF57M (sulfanilamide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170516
[Lr] Data última revisão:
170516
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170321
[St] Status:MEDLINE
[do] DOI:10.1002/cpt.613


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[PMID]:28292723
[Au] Autor:Spielmeyer A; Höper H; Hamscher G
[Ad] Endereço:Justus Liebig University, Institute for Food Chemistry and Food Biotechnology, Heinrich-Buff-Ring 17, D-35392 Giessen, Germany. Electronic address: astrid.spielmeyer@lcb.chemie.uni-giessen.de.
[Ti] Título:Long-term monitoring of sulfonamide leaching from manure amended soil into groundwater.
[So] Source:Chemosphere;177:232-238, 2017 Jun.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Veterinary antibiotics such as sulfonamides are frequently applied in livestock farming worldwide. Due to poor absorption in the animal gut and/or reversible metabolization sulfonamides are excreted in considerable amounts and can subsequently be detected in liquid manure. As manure is utilized for soil fertilization, sulfonamides can enter the environment via this pathway. Water samples taken below an agriculture field in Lower Saxony revealed the permanent entrance of sulfamethazine into groundwater and concentrations up to 100 ng L were determined. During a long-term lysimeter study, nine sulfonamides were applied to two different soil types by using fortified liquid manure. Divert mobilities were found with sulfamethazine und sulfamethoxazole showing the highest detection frequency in water samples taken below both bedrock and sandy soil. Four years after the last application of fortified manure, sulfonamides were still detectable in the leachate. Based on analyses of manure and fermentation residue samples, a permanent input of sulfonamides to the soil can be excluded. Thus, the positive findings must be caused by the antibiotics once applied. Soils fertilized with manure contaminated with sulfonamides can consequently be a long-time source for the transfer of antibiotics into groundwater.
[Mh] Termos MeSH primário: Monitoramento Ambiental
Água Subterrânea/análise
Esterco/análise
Poluentes do Solo/análise
Solo/química
Sulfonamidas/análise
[Mh] Termos MeSH secundário: Agricultura
Animais
Antibacterianos/análise
Fertilizantes/análise
Sulfametazina/análise
Sulfametoxazol/análise
Sulfanilamidas/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Fertilizers); 0 (Manure); 0 (Soil); 0 (Soil Pollutants); 0 (Sulfanilamides); 0 (Sulfonamides); 21240MF57M (sulfanilamide); 48U51W007F (Sulfamethazine); JE42381TNV (Sulfamethoxazole)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170316
[St] Status:MEDLINE


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[PMID]:28272358
[Au] Autor:Vullo D; Del Prete S; Di Fonzo P; Carginale V; Donald WA; Supuran CT; Capasso C
[Ad] Endereço:Laboratorio di Chimica Bioinorganica, Dipartimento Di Chimica, Università degli Studi di Firenze, Polo Scientifico, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy. daniela.vullo@unifi.it.
[Ti] Título:Comparison of the Sulfonamide Inhibition Profiles of the ß- and γ-Carbonic Anhydrases from the Pathogenic Bacterium Burkholderia pseudomallei.
[So] Source:Molecules;22(3), 2017 Mar 07.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:We have cloned, purified, and characterized a ß-carbonic anhydrase (CA, EC 4.2.1.1), BpsCAß, from the pathogenic bacterium , responsible for the tropical disease melioidosis. The enzyme showed high catalytic activity for the physiologic CO2 hydration reaction to bicarbonate and protons, with the following kinetic parameters: k of 1.6 × 105 s and k /K of 3.4 × 107 M s . An inhibition study with a panel of 38 sulfonamides and one sulfamate-including 15 compounds that are used clinically-revealed an interesting structure-activity relationship for the interaction of this enzyme with these inhibitors. Many simple sulfonamides and clinically used agents such as topiramate, sulpiride, celecoxib, valdecoxib, and sulthiame were ineffective BpsCAß inhibitors (K > 50 µM). Other drugs, such as ethoxzolamide, dorzolamide, brinzolamide, zonisamide, indisulam, and hydrochlorothiazide were moderately potent micromolar inhibitors. The best inhibition was observed with benzene-1,3-disulfonamides-benzolamide and its analogs acetazolamide and methazolamide-which showed K in the range of 185-745 nM. The inhibition profile of BpsCAß is very different from that of the γ-class enzyme from the same pathogen, BpsCAγ. Thus, identifying compounds that would effectively interact with both enzymes is relatively challenging. However, benzolamide was one of the best inhibitors of both of these CAs with K of 653 and 185 nM, respectively, making it an interesting lead compound for the design of more effective agents, which may be useful tools for understanding the pathogenicity of this bacterium.
[Mh] Termos MeSH primário: Burkholderia pseudomallei/efeitos dos fármacos
Burkholderia pseudomallei/enzimologia
Inibidores da Anidrase Carbônica/farmacologia
Sulfanilamidas/farmacologia
[Mh] Termos MeSH secundário: Burkholderia pseudomallei/genética
Ativação Enzimática/efeitos dos fármacos
Cinese
Estrutura Molecular
Proteínas Recombinantes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Recombinant Proteins); 0 (Sulfanilamides); 21240MF57M (sulfanilamide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170518
[Lr] Data última revisão:
170518
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE


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[PMID]:27871381
[Au] Autor:Bourais I; Maliki S; Mohammadi H; Amine A
[Ad] Endereço:Laboratoire Analyses Chimiques et Biocapteurs, Faculté des Sciences et Techniques, Hassan II University of Casablanca, B.P.146, Mohammedia, Morocco.
[Ti] Título:Investigation of sulfonamides inhibition of carbonic anhydrase enzyme using multiphotometric and electrochemical techniques.
[So] Source:Enzyme Microb Technol;96:23-29, 2017 Jan.
[Is] ISSN:1879-0909
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two approaches for sulfonamides (SA's) determination, based on carbonic anhydrase enzyme inhibition have been investigated in this work. In the first method, nine different SA's have been screened using simultaneous multiphotometric measurement in multiwell plates. The sulfanilamide (SAD) showed significant inhibition compared to other sulfonamides. The carbonic anhydrase (CA) kinetic interactions reveal noncompetitive binding of SAD. Interferences from other inhibitors with enzyme were studied and the results showed very good selectivity toward SAD. In the second approach, an electrochemical enzyme inhibition biosensor, based on CA entrapped in a carbon paste electrode using carbon black nanoparticles and solid paraffin, was successfully applied to SAD measurements. Results from the quantitative analysis of SAD are discussed in terms of detection limit, linear range and sensitivity using multiphotometric and biosensor-based methods The biosensor developed was successfully applied to the determination of SAD at submicromolar levels and it is recommended for application for in situ analysis.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/farmacologia
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Técnicas Biossensoriais/métodos
Inibidores da Anidrase Carbônica/análise
Anidrases Carbônicas/metabolismo
Técnicas Eletroquímicas/métodos
Estabilidade Enzimática
Seres Humanos
Concentração de Íons de Hidrogênio
Fotometria/métodos
Fuligem
Sulfanilamidas/análise
Sulfanilamidas/farmacologia
Sulfonamidas/análise
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Soot); 0 (Sulfanilamides); 0 (Sulfonamides); 21240MF57M (sulfanilamide); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170530
[Lr] Data última revisão:
170530
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161123
[St] Status:MEDLINE


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[PMID]:27864640
[Au] Autor:Zhang Q; Qu Y; Wang Q; Song P; Wang P; Jia Q; Guo J
[Ad] Endereço:College of Life Sciences, State Key Laboratory of Crop Genetics and Germplasm Enhancement, Nanjing Agricultural University, Nanjing, 210095, People's Republic of China. zhangqun@njau.edu.cn.
[Ti] Título:Arabidopsis phospholipase D alpha 1-derived phosphatidic acid regulates microtubule organization and cell development under microtubule-interacting drugs treatment.
[So] Source:J Plant Res;130(1):193-202, 2017 Jan.
[Is] ISSN:1618-0860
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Phospholipase D (PLD) and its product phosphatidic acid (PA) are emerging as essential regulators of cytoskeleton organization in plants. However, the underlying molecular mechanisms of PA-mediated microtubule reorganization in plants remain largely unknown. In this study, we used pharmacological and genetic approaches to analyze the function of Arabidopsis thaliana PLDα1 in the regulation of microtubule organization and cell development in response to microtubule-affecting drugs. Treatment with the microtubule-stabilizing drug paclitaxel resulted in less growth inhibition and decreased rightward slant of roots, longitudinal alignment of microtubules, and enhanced length of hypocotyl epidermal cells in the pldα1 mutant, the phenotype of which was rescued by exogenous application of PA. Moreover, the pldα1 mutant was sensitive to the microtubule-disrupting drugs oryzalin and propyzamide in terms of seedling survival ratio, left-skewing angle of roots and microtubule organization. In addition, both disruption and stabilization of microtubules induced by drugs activated PLDα1 activity. Our findings demonstrate that in A. thaliana, PLDα1/PA might regulate cell development by modulating microtubule organization in an activity-dependent manner.
[Mh] Termos MeSH primário: Proteínas de Arabidopsis/metabolismo
Arabidopsis/enzimologia
Dinitrobenzenos/farmacologia
Microtúbulos/efeitos dos fármacos
Paclitaxel/farmacologia
Ácidos Fosfatídicos/metabolismo
Fosfolipase D/metabolismo
Sulfanilamidas/farmacologia
[Mh] Termos MeSH secundário: Arabidopsis/efeitos dos fármacos
Arabidopsis/genética
Arabidopsis/crescimento & desenvolvimento
Proteínas de Arabidopsis/genética
Técnicas de Inativação de Genes
Microtúbulos/ultraestrutura
Mutação
Fosfolipase D/genética
Raízes de Plantas/efeitos dos fármacos
Raízes de Plantas/enzimologia
Raízes de Plantas/genética
Raízes de Plantas/crescimento & desenvolvimento
Plântulas/efeitos dos fármacos
Plântulas/enzimologia
Plântulas/genética
Plântulas/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Arabidopsis Proteins); 0 (Dinitrobenzenes); 0 (Phosphatidic Acids); 0 (Sulfanilamides); 662E385DWH (oryzalin); EC 3.1.4.4 (PLDalpha1 protein, Arabidopsis); EC 3.1.4.4 (Phospholipase D); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171014
[Lr] Data última revisão:
171014
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161120
[St] Status:MEDLINE
[do] DOI:10.1007/s10265-016-0870-8



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