Base de dados : MEDLINE
Pesquisa : D02.078 [Categoria DeCS]
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[PMID]:29406027
[Au] Autor:Wu Y; Guo H; Bu J; Tan Y; Zhong J; Zhao Q
[Ad] Endereço:Department of Forensic Science and Technology, Chongqing Police College, Chongqing 401331, China.
[Ti] Título:Rapid and sensitive determination of formamidines and metabolites with HPLC-MS/MS using core-shell columns.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1076:22-28, 2018 Feb 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A number of poisoning and suicide cases involving formamidine pesticides have been reported, thus developing a rapid and low cost determination method is crucial. In this work, a rapid, sensitive and low-cost method for the simultaneous determination of formamidine pesticides (amitraz, chlordimeform, formetanate) and their main metabolites, N-(2,4-dimethylphenyl)-N-methyl-formamidine, 2,4-dimethylformamidine, 2,4-dimethylaniline, 4-chloro-2-methylaniline and 3-hydroxyacetanilide in human blood by high-performance liquid chromatography with tandem mass spectrometry is developed. The application of columns with core-shell particles significantly reduced the analysis time. Very low LODs (0.01-0.04 µg L ) were obtained for formamidine pesticides and their metabolites. The method was successfully applied to the analysis of human blood samples from a real forensic case. The significantly reduced analysis time, high sensitivity and low cost are the primary advantages of the developed method. This methodology provides important value for sensitive and rapid determination of residue pesticides and metabolites, study of residue pesticides behavior in human body, as well as application in real forensic cases.
[Mh] Termos MeSH primário: Amidinas/sangue
Cromatografia Líquida de Alta Pressão/métodos
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Adulto
Amidinas/envenenamento
Criança
Feminino
Seres Humanos
Limite de Detecção
Modelos Lineares
Masculino
Resíduos de Praguicidas/sangue
Reprodutibilidade dos Testes
Cloreto de Sódio
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Pesticide Residues); 451W47IQ8X (Sodium Chloride); 463-52-5 (formamidine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180307
[Lr] Data última revisão:
180307
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180207
[St] Status:MEDLINE


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[PMID]:27779493
[Au] Autor:Sales AJ; Hiroaki-Sato VA; Joca SR
[Ad] Endereço:aDepartment of Pharmacology, School of Medicine of Ribeirão Preto bDepartment of Physics and Chemistry, School of Pharmaceutical Sciences of Ribeirão Preto cCenter for Interdisciplinary Research on Applied Neurosciences (NAPNA), University of São Paulo, Ribeirão Preto, São Paulo, Brazil.
[Ti] Título:Participation of hippocampal nitric oxide synthase and soluble guanylate cyclase in the modulation of behavioral responses elicited by the rat forced swimming test.
[So] Source:Behav Pharmacol;28(1):19-29, 2017 02.
[Is] ISSN:1473-5849
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Systemic or hippocampal administration of nitric oxide (NO) synthase inhibitors induces antidepressant-like effects in animals, implicating increased hippocampal levels of NO in the neurobiology of depression. However, the role played by different NO synthase in this process has not been clearly defined. As stress is able to induce neuroinflammatory mechanisms and trigger the expression of inducible nitric oxide synthase (iNOS) in the brain, as well as upregulate neuronal nitric oxide synthase (nNOS) activity, the aim of the present study was to investigate the possible differential contribution of hippocampal iNOS and nNOS in the modulation of the consequences of stress elicited by the forced swimming test. Male Wistar rats received intrahippocampal injections, immediately after the pretest or 1 h before the forced swimming test, of selective inhibitors of nNOS (N-propyl-L-arginine), iNOS (1400W), or sGC (ODQ), the main pharmacological target for NO. Stress exposure increased nNOS and phospho-nNOS levels at all time points, whereas iNOS expression was increased only 24 h after the pretest. All drugs induced an antidepressant-like effect. However, whereas the nNOS inhibitor was equally effective when injected at different times, the iNOS inhibitor was more effective 24 h after the pretest. These results suggest that hippocampal nNOS and iNOS contribute to increase in NO levels in response to stress, although with a differential time course after stress exposure.
[Mh] Termos MeSH primário: Óxido Nítrico Sintase Tipo II/metabolismo
Óxido Nítrico Sintase Tipo I/metabolismo
Guanilil Ciclase Solúvel/metabolismo
Estresse Psicológico/metabolismo
[Mh] Termos MeSH secundário: Amidinas/farmacologia
Animais
Arginina/análogos & derivados
Arginina/farmacologia
Benzilaminas/farmacologia
Modelos Animais de Doenças
Hipocampo/metabolismo
Masculino
Óxido Nítrico/metabolismo
Oxidiazóis/farmacologia
Ratos
Ratos Wistar
Natação
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1H-(1,2,4)oxadiazolo(4,3-a)-quiloxalin-1-one); 0 (Amidines); 0 (Benzylamines); 0 (N(omega)-propylarginine); 0 (N-(3-(aminomethyl)benzyl)acetamidine); 0 (Oxadiazoles); 31C4KY9ESH (Nitric Oxide); 94ZLA3W45F (Arginine); EC 1.14.13.39 (Nitric Oxide Synthase Type I); EC 1.14.13.39 (Nitric Oxide Synthase Type II); EC 4.6.1.2 (Soluble Guanylyl Cyclase)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180228
[Lr] Data última revisão:
180228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE
[do] DOI:10.1097/FBP.0000000000000263


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[PMID]:29061821
[Au] Autor:Mazur L; Opydo-Chanek M; Sladowska K; Janota B; Klaput U; Lukawska M; Oszczapowicz I
[Ad] Endereço:Department of Experimental Hematology, Institute of Zoology and Biomedical Research, Jagiellonian University, Krakow, Poland lidia.mazur@uj.edu.pl.
[Ti] Título: Antileukemic Activity of Formamidine Epidoxorubicin Analogs.
[So] Source:Anticancer Res;37(11):6363-6372, 2017 11.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: Epidoxorubicin is an anthracycline agent. The present study was undertaken to compare the antileukemic potential of epidoxorubicin and its two formamidine analogs containing either a morpholine moiety (EPIFmor) or a hexamethyleneimine moiety (EPIFhex) in the amidine group. MATERIALS AND METHODS: The experiments were performed in vitro on MOLT-4 cells using spectrophotometry, Coulter electrical impedance, flow cytometry, and light microscopy methods. RESULTS: The leukemia cell responses to the action of the anthracyclines were manifested in their different viability, count and volume, degree of apoptosis and necrosis, activity of caspases -8, -9, and -3/7, mitochondrial membrane potential, and in the cell-cycle distribution. In general, epidoxorubicin appeared to be the most active, and EPIFmor was more active than EPIFhex against MOLT-4 cells. CONCLUSION: The structural modifications of epidoxorubicin in the amidine group were responsible for the varied action of its formamidine analogs on human acute lymphoblastic leukemia cells.
[Mh] Termos MeSH primário: Amidinas/farmacologia
Antraciclinas/farmacologia
Antineoplásicos/farmacologia
Caspases/metabolismo
Leucemia-Linfoma Linfoblástico de Células Precursoras/metabolismo
[Mh] Termos MeSH secundário: Amidinas/química
Antraciclinas/química
Antineoplásicos/química
Apoptose
Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Epirubicina/análogos & derivados
Seres Humanos
Técnicas In Vitro
Potenciais da Membrana/efeitos dos fármacos
Leucemia-Linfoma Linfoblástico de Células Precursoras/tratamento farmacológico
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Anthracyclines); 0 (Antineoplastic Agents); 3Z8479ZZ5X (Epirubicin); EC 3.4.22.- (Caspases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171026
[Lr] Data última revisão:
171026
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171025
[St] Status:MEDLINE


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[PMID]:28868786
[Au] Autor:Shukla S; Shukla S; Haur LJ; Dintakurti SSH; Han G; Priyadarshi A; Baikie T; Mhaisalkar SG; Mathews N
[Ad] Endereço:Energy Research Institute @ NTU (ERIAN), Nanyang Technological University, Singapore, Research Techno Plaza, 50 Nanyang Drive, 637553, Singapore.
[Ti] Título:Effect of Formamidinium/Cesium Substitution and PbI on the Long-Term Stability of Triple-Cation Perovskites.
[So] Source:ChemSusChem;10(19):3804-3809, 2017 Oct 09.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Altering cation and anion ratios in perovskites has proven an excellent means of tuning the perovskite properties and enhancing the performance. Recently, methylammonium/formamidinium/cesium triple-cation mixed-halide perovskites have demonstrated efficiencies up to 22 %. Similar to the widely explored methylammonium lead halide, excess PbI is added to these perovskite films to enhance their performances. The excess PbI is known to be beneficial for the performance. However, its impact on stability is less well known. Triple-cation perovskites deploy excess PbI up to 8 %. Thus, it is imperative to analyze the role of excess PbI in the degradation kinetics. In this study, the amount of PbI in the triple-cation perovskite films is varied and the degradation kinetics monitored by X-ray diffraction and optical absorption spectroscopy. The inclusion of excess PbI is shown to adversely affect the stability of the material. Faster degradation kinetics are observed for samples with higher PbI contents. However, samples with excess PbI also showed superior properties such as enhanced grain sizes and better optical absorption. Thus, careful management of the PbI quantity is required to obtain better stability and alternative pathways should be explored to achieve better device performance rather than adding excess PbI .
[Mh] Termos MeSH primário: Amidinas/química
Compostos de Cálcio/química
Césio/química
Fontes de Energia Elétrica
Iodetos/química
Chumbo/química
Óxidos/química
Energia Solar
Titânio/química
[Mh] Termos MeSH secundário: Flúor/química
Compostos de Estanho/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Calcium Compounds); 0 (Iodides); 0 (Oxides); 0 (Tin Compounds); 12194-71-7 (perovskite); 1KSV9V4Y4I (Cesium); 284SYP0193 (Fluorine); 2P299V784P (Lead); 463-52-5 (formamidine); D1JT611TNE (Titanium); KM7N50LOS6 (stannic oxide)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170905
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201701203


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[PMID]:28844803
[Au] Autor:Pickens JB; Wang F; Striegler S
[Ad] Endereço:University of Arkansas, Department of Chemistry and Biochemistry, 345N Campus Drive, Fayetteville, AR 72701, USA.
[Ti] Título:Picomolar inhibition of ß-galactosidase (bovine liver) attributed to loop closure.
[So] Source:Bioorg Med Chem;25(20):5194-5202, 2017 Oct 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In an effort to examine similarities in the active sites of glycosidases within the GH35 family, we performed a structure-activity-relationship study using our recently described library of galactonoamidines. The kinetic evaluation based on UV/Vis spectroscopy disclosed inhibition of ß-galactosidase (bovine liver) in the picomolar concentration range indicating significantly higher inhibitor affinity than previously determined for ß-galactosidase (A. oryzae). Possible alterations in the secondary protein structure or folding were excluded after further examination of the inhibitor binding using CD spectroscopy. Molecular dynamics studies suggested loop closing interactions as a rationale for the disparity of the active sites in the ß-galactosidases under investigation.
[Mh] Termos MeSH primário: Amidinas/farmacologia
Inibidores Enzimáticos/farmacologia
Fígado/efeitos dos fármacos
beta-Galactosidase/antagonistas & inibidores
[Mh] Termos MeSH secundário: Amidinas/química
Animais
Bovinos
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/química
Fígado/enzimologia
Simulação de Dinâmica Molecular
Estrutura Molecular
Relação Estrutura-Atividade
beta-Galactosidase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Enzyme Inhibitors); EC 3.2.1.23 (beta-Galactosidase)
[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:170829
[St] Status:MEDLINE


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[PMID]:28789935
[Au] Autor:Zhou R; Liu ZQ
[Ad] Endereço:Department of Organic Chemistry, College of Chemistry, Jilin University, Changchun 130021, China.
[Ti] Título:Tetramer as efficient structural mode for organizing antioxidative carboxylic acids: The case in inhibiting DNA oxidation.
[So] Source:Arch Biochem Biophys;631:1-10, 2017 Oct 01.
[Is] ISSN:1096-0384
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:To overcome the problem on the relationship of antioxidative effect with the branch number in a tetramer, we herein designed a series of antioxidants with pentaerythritol, glycerol, and ethylene glycol as the cores, and gallic, ferulic, caffeic, and p-hydroxybenzoic acids as the antioxidative moieties. In the case of DNA oxidation mediated by 2,2'-azobis(2-amidinopropane hydrochloride, AAPH), it was found that the stoichiometric factor (n) of a carboxylic acid increased rapidly when the acid was esterified with ethylene glycol, glycerol, and pentaerythritol to form a dimer, trimer, and tetramer, respectively. Interestingly, the coefficient in the equation of n∼{branch} ({branch} referred to the number of branches) was higher than one, indicating that the antioxidative effect was enhanced more promptly than the increase of the number of branches. Meanwhile, tetramer exhibited high intercalation effect with DNA strand. Therefore, additionally antioxidative effect was ascribed to the tethering effect resulting from tetrameric structure and strong intercalation with DNA strand generated by tetramer.
[Mh] Termos MeSH primário: Antioxidantes/química
Antioxidantes/farmacologia
Ácidos Carboxílicos/química
Ácidos Carboxílicos/farmacologia
DNA/química
Oxirredução/efeitos dos fármacos
[Mh] Termos MeSH secundário: Amidinas/química
Antioxidantes/síntese química
Ácidos Cafeicos/síntese química
Ácidos Cafeicos/química
Ácidos Cafeicos/farmacologia
Ácidos Carboxílicos/síntese química
Ácidos Cumáricos/síntese química
Ácidos Cumáricos/química
Ácidos Cumáricos/farmacologia
Dimerização
Esterificação
Ácido Gálico/síntese química
Ácido Gálico/química
Ácido Gálico/farmacologia
Hidroxibenzoatos/síntese química
Hidroxibenzoatos/química
Hidroxibenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Antioxidants); 0 (Caffeic Acids); 0 (Carboxylic Acids); 0 (Coumaric Acids); 0 (Hydroxybenzoates); 632XD903SP (Gallic Acid); 7381JDR72F (2,2'-azobis(2-amidinopropane)); 9007-49-2 (DNA); AVM951ZWST (ferulic acid); U2S3A33KVM (caffeic acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170810
[St] Status:MEDLINE


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[PMID]:28789891
[Au] Autor:Yang CJ; Song ZL; Goto M; Liu YQ; Hsieh KY; Morris-Natschke SL; Zhao YL; Zhang JX; Lee KH
[Ad] Endereço:School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.
[Ti] Título:Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
[So] Source:Bioorg Med Chem Lett;27(17):3959-3962, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In our continuing search for camptothecin (CPT)-derived antitumor drugs, novel 7-substituted CPT derivatives incorporating piperazinyl-sulfonylamidine moieties were designed, synthesized and evaluated for cytotoxicity against five tumor cell lines (A-549, MDA-MB-231, MCF-7, KB, and KB-VIN). All of the derivatives showed promising in vitro cytotoxic activity against the tested tumor cell lines, and were more potent than irinotecan. Remarkably, most of the compounds exhibited comparable cytotoxicity against the multidrug-resistant (MDR) KB-VIN and parental KB tumor cell lines, while irinotecan lost activity completely against KB-VIN. Especially, compounds 13r and 13p (IC 0.38 and 0.85µM, respectively) displayed the greatest cytotoxicity against the MDR KB-VIN cell line and merit further development into preclinical and clinical drug candidates for treating cancer, including MDR phenotype.
[Mh] Termos MeSH primário: Amidinas/farmacologia
Antineoplásicos/farmacologia
Camptotecina/farmacologia
Desenho de Drogas
Piperazinas/farmacologia
[Mh] Termos MeSH secundário: Amidinas/química
Antineoplásicos/síntese química
Antineoplásicos/química
Camptotecina/síntese química
Camptotecina/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Piperazinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amidines); 0 (Antineoplastic Agents); 0 (Piperazines); 1RTM4PAL0V (piperazine); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170810
[St] Status:MEDLINE


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[PMID]:28666079
[Au] Autor:Sun S; Isikgor FH; Deng Z; Wei F; Kieslich G; Bristowe PD; Ouyang J; Cheetham AK
[Ad] Endereço:Department of Materials Science and Metallurgy, University of Cambridge, CB3 0FS, Cambridge, U. K.
[Ti] Título:Factors Influencing the Mechanical Properties of Formamidinium Lead Halides and Related Hybrid Perovskites.
[So] Source:ChemSusChem;10(19):3740-3745, 2017 Oct 09.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The mechanical properties of formamidinium lead halide perovskites (FAPbX , X=Br or I) grown by inverse-temperature crystallization have been studied by nanoindentation. The measured Young's moduli (9.7-12.3 GPa) and hardnesses (0.36-0.45 GPa) indicate good mechanical flexibility and ductility. The effects of hydrogen bonding were evaluated by performing ab initio molecular dynamics on both formamidinium and methylammonium perovskites and calculating radial distribution functions. The structural and chemical factors influencing these properties are discussed by comparison with corresponding values in the literature for other hybrid perovskites, including double perovskites. Our results reveal that bonding in the inorganic framework and hydrogen bonding play important roles in determining elastic stiffness. The influence of the organic cation becomes more important for structures at the limit of their perovskite stability, indicated by high tolerance factors.
[Mh] Termos MeSH primário: Amidinas/química
Compostos de Cálcio/química
Halogênios/química
Chumbo/química
Fenômenos Mecânicos
Óxidos/química
Titânio/química
[Mh] Termos MeSH secundário: Cristalização
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Calcium Compounds); 0 (Halogens); 0 (Oxides); 12194-71-7 (perovskite); 2P299V784P (Lead); 463-52-5 (formamidine); D1JT611TNE (Titanium)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170701
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700991


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[PMID]:28647482
[Au] Autor:Simmler C; Lankin DC; Nikolic D; van Breemen RB; Pauli GF
[Ad] Endereço:UIC/NIH Center for Botanical Dietary Supplements Research, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, College of Pharmacy, 833 S. Wood Street, Chicago, IL 60612, USA. Electronic address: simmler@uic.edu.
[Ti] Título:Isolation and structural characterization of dihydrobenzofuran congeners of licochalcone A.
[So] Source:Fitoterapia;121:6-15, 2017 Sep.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In an effort to explore the residual complexity of naturally occurring chalcones from the roots of Glycyrrhiza inflata (Fabaceae), two new licochalcone A (LicA) derivatives were isolated as trace metabolites from enriched fractions. Both constituents contain a dihydrofuran moiety linked to carbons C-4 and C-5 of the retrochalcone core. Compound 1 (LicAF1) represents a new chemical entity, whereas compound 2 (LicAF2) has previously been reported as a Lewis acid catalyzed rearrangement of LicA. Evaluation of chirality revealed that both dihydrofuran derivatives existed as a mixture of R and S enantiomers. Interestingly, when solutions were exposed to sunlight, both dihydrofuran retrochalcones, initially isolated as trans isomers, were found to rapidly isomerize yielding trans and cis isomers. Analysis of the 1D H NMR spectra of the photolysis products revealed the presence of two sets of proton resonances ascribed to each of the geometric isomers. An up-field shift of all proton resonances arising from the cis isomer was observed, suggesting that anisotropic shielding effects were introduced through an overall perturbation of the 3-dimensional structure upon photoisomerization. Similar up-field shifts were observed in the C spectrum of the cis isomer, except for the CO, C-α, and C-6 carbons, which experienced downfield shifts. Analogous NMR results were observed for LicA. Hence, the results presented herein encompass the isolation and full characterization of LicAF analogs 1 and 2, and observations of their trans-to-cis photoisomerization through the systematic analysis of their NMR spectra.
[Mh] Termos MeSH primário: Amidinas/química
Benzofuranos/química
Chalconas/química
Glycyrrhiza/química
[Mh] Termos MeSH secundário: Amidinas/isolamento & purificação
Benzofuranos/isolamento & purificação
Chalconas/isolamento & purificação
Estrutura Molecular
Extratos Vegetais/química
Raízes de Plantas/química
Espectroscopia de Prótons por Ressonância Magnética
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Benzofurans); 0 (Chalcones); 0 (Plant Extracts); 0 (benzofuran-2-carboxamidine); JTV5467968 (licochalcone A)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170626
[St] Status:MEDLINE


  10 / 4247 MEDLINE  
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[PMID]:28609459
[Au] Autor:Borin TF; Shankar A; Angara K; Rashid MH; Jain M; Iskander A; Ara R; Lebedyeva I; Korkaya H; Achyut BR; Arbab AS
[Ad] Endereço:Georgia Cancer Center, Augusta University, Augusta, GA, United States of America.
[Ti] Título:HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model.
[So] Source:PLoS One;12(6):e0178830, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Distant metastasis is the primary cause of death in the majority of the cancer types. Recently, much importance has been given to tumor microenvironment (TME) in the development of invasive malignant tumors, as well as the metastasis potential. The ability of tumor cells to modulate TME and to escape immune-mediated attack by releasing immunosuppressive cytokines has become a hallmark of breast cancer. Our study shows the effect of IV formulation of HET0016 (HPßCD-HET0016) a selective inhibitor of 20-HETE synthesis, administered intravenously in immune-competent in vivo mouse model of murine breast cancer. 4T1 luciferase positive cells were implanted to the mammary fat pad in Balb/c mice. Treatment started on day 15, and was administered for 5 days a week for 3 weeks. The development of metastasis was detected via optical imaging. Blood, spleen, lungs, bone marrow and tumor were collected for flow cytometry, to investigate changes in myeloid-derived suppressive cells (MDSCs) populations and endothelial phenotype. Tumor and lungs were collected for protein analysis. Our results show that HPßCD-HET0016: (1) decreased tumor volume and lung metastasis compared to the vehicle group; (2) reduced migration and invasion of tumor cells and levels of metalloproteinases in the lungs of animals treated with HPßCD-HET0016 via PI3K/AKT pathway; and (3) decreased expression of pro-inflammatory cytokines, growth factors and granulocytic MDSCs population in the lung microenvironment in treated animals. Thus, HPßCD-HET0016 showed potential in treating lung metastasis in a preclinical mouse model and needs further investigations on TME.
[Mh] Termos MeSH primário: Amidinas/farmacologia
Modelos Animais de Doenças
Imunocompetência
Neoplasias Pulmonares/prevenção & controle
Neoplasias Mamárias Experimentais/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Intravenosa
Amidinas/administração & dosagem
Animais
Western Blotting
Caderinas/metabolismo
Linhagem Celular Tumoral
Movimento Celular/efeitos dos fármacos
Citocinas/metabolismo
Feminino
Seres Humanos
Imuno-Histoquímica
Mediadores da Inflamação/metabolismo
Neoplasias Pulmonares/metabolismo
Neoplasias Pulmonares/secundário
Neoplasias Mamárias Experimentais/metabolismo
Neoplasias Mamárias Experimentais/patologia
Camundongos Endogâmicos BALB C
Proteínas Quinases Ativadas por Mitógeno/metabolismo
Carga Tumoral/efeitos dos fármacos
Microambiente Tumoral/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amidines); 0 (Cadherins); 0 (Cytokines); 0 (Inflammation Mediators); 0 (N-hydroxy-N'-(4-butyl-2-methylphenyl)formamidine); EC 2.7.11.24 (Mitogen-Activated Protein Kinases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0178830



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