Base de dados : MEDLINE
Pesquisa : D02.478.480 [Categoria DeCS]
Referências encontradas : 661 [refinar]
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[PMID]:29242020
[Au] Autor:Chen W; Shen S; Dong L; Zhang J; Yang Q
[Ad] Endereço:School of Life Science and Biotechnology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
[Ti] Título:Selective inhibition of ß-N-acetylhexosaminidases by thioglycosyl-naphthalimide hybrid molecules.
[So] Source:Bioorg Med Chem;26(2):394-400, 2018 01 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To develop selective inhibitors for ß-N-acetylhexosaminidases which are involved in a myriad of physiological processes, a series of novel thioglycosyl-naphthalimide hybrid inhibitors were designed, synthesized and evaluated for inhibition activity against glycosyl hydrolase family 20 and 84 (GH20 and GH84) ß-N-acetylhexosaminidases. These compounds which incorporate groups with varied sizes and lengths at the linker region between thioglycosyl moiety and naphthalimide moiety are designed to improve the selectivity and stacking interactions. The GH84 human O-GlcNAcase (hOGA) was sensitive to the subtle changes in the linker region and the optimal choice is a small size linker with six atoms length. And the GH20 insect ß-N-acetylhexosaminidase OfHex1 could tolerate compounds with a hydrophobic bulky linker. Especially, the compound 5c (hOGA, K = 3.46 µM; OfHex1, K > 200 µM) and the compound 6f (hOGA, K > 200 µM; OfHex1, K = 21.81 µM) displayed high selectivity. The molecular docking results indicated that the inhibition mechanism was different between the two families due to their different structural characteristics beyond the active sites. These results provide some promising clues to improve selectivity of potent molecules against ß-N-acetylhexosaminidases.
[Mh] Termos MeSH primário: Inibidores Enzimáticos/farmacologia
Naftalimidas/farmacologia
Tioglicosídeos/farmacologia
beta-N-Acetil-Hexosaminidases/antagonistas & inibidores
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Seres Humanos
Estrutura Molecular
Naftalimidas/química
Relação Estrutura-Atividade
Tioglicosídeos/química
beta-N-Acetil-Hexosaminidases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Naphthalimides); 0 (Thioglycosides); EC 3.2.1.52 (beta-N-Acetylhexosaminidases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171216
[St] Status:MEDLINE


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[PMID]:29390898
[Au] Autor:Shen S; Chen W; Dong L; Yang Q; Lu H; Zhang J
[Ad] Endereço:a Department of Applied Chemistry , College of Science, China Agricultural University , Beijing , China.
[Ti] Título:Design and synthesis of naphthalimide group-bearing thioglycosides as novel ß-N-acetylhexosaminidases inhibitors.
[So] Source:J Enzyme Inhib Med Chem;33(1):445-452, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:GH20 human ß-N-acetylhexosaminidases (hsHex) and GH84 human O-GlcNAcase (hOGA) are involved in numerous pathological processes and emerged as promising targets for drug discovery. Based on the catalytic mechanism and structure of the catalytic domains of these ß-N-acetylhexosaminidases, a series of novel naphthalimide moiety-bearing thioglycosides with different flexible linkers were designed, and their inhibitory potency against hsHexB and hOGA was evaluated. The strongest potency was found for compound 15j (K = 0.91 µM against hsHexB; K > 100 µM against hOGA) and compound 15b (K = 3.76 µM against hOGA; K = 30.42 µM against hsHexB), which also exhibited significant selectivity between these two enzymes. Besides, inhibitors 15j and 15b exhibited an inverse binding patterns in docking studies. The determined structure-activity relationship as well as the established binding models provide the direction for further structure optimizations and the development of specific ß-N-acetylhexosaminidase inhibitors.
[Mh] Termos MeSH primário: Desenho de Drogas
Inibidores Enzimáticos/farmacologia
Naftalimidas/farmacologia
Tioglicosídeos/farmacologia
beta-N-Acetil-Hexosaminidases/antagonistas & inibidores
[Mh] Termos MeSH secundário: Biocatálise
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Naftalimidas/síntese química
Naftalimidas/química
Relação Estrutura-Atividade
Tioglicosídeos/química
beta-N-Acetil-Hexosaminidases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Naphthalimides); 0 (Thioglycosides); EC 3.2.1.52 (beta-N-Acetylhexosaminidases)
[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:10.1080/14756366.2017.1419217


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[PMID]:28632960
[Au] Autor:Wang C; Song X; Xiao Y
[Ad] Endereço:State Key Laboratory of Fine Chemicals, Dalian University of Technology, Linggong Road 2, Dalian, 116024, China.
[Ti] Título:SNAP-Tag-Based Subcellular Protein Labeling and Fluorescent Imaging with Naphthalimides.
[So] Source:Chembiochem;18(17):1762-1769, 2017 Sep 05.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Genetically encoded technologies provide methods for the specific labeling and imaging of proteins, which is essential to understand the subcellular localization of these proteins and their function. Herein, we employed naphthalimide, an efficient two-photon fluorophore, to develop O -benzylguanine (BG) derivatives for specific labeling of subcellular proteins and fluorescent imaging through the SNAP-tag. Three naphthalimide-BG derivatives, TNI-BG, QNI-BG, and ONI-BG, were conveniently synthesized through modular "click chemistry" in high yields. All of them showed high labeling efficiency with SNAP-tag in solution (≈1-2×10  s m ) and in bacteria. Among them, ONI-BG showed high specificity to diffused, histone H2B and mitochondria COX8A targeted SNAP-tag in mammalian cells. The protein-labeled naphthalimides exhibited high two-photon absorption cross-sections, which indicated their potential application in protein-specific two-photon fluorescent imaging, such as two-photon fluorescent lifetime imaging and two-photon multicolor imaging. Therefore, ONI-BG is a versatile tool that can be used to track subcellular proteins through multiple fluorescent techniques.
[Mh] Termos MeSH primário: Metilases de Modificação do DNA/metabolismo
Enzimas Reparadoras do DNA/metabolismo
Corantes Fluorescentes/química
Naftalimidas/química
Proteínas Supressoras de Tumor/metabolismo
[Mh] Termos MeSH secundário: Animais
Células COS
Cercopithecus aethiops
Química Click
Metilases de Modificação do DNA/genética
Enzimas Reparadoras do DNA/genética
Complexo IV da Cadeia de Transporte de Elétrons/química
Complexo IV da Cadeia de Transporte de Elétrons/metabolismo
Histonas/química
Histonas/metabolismo
Seres Humanos
Microscopia de Fluorescência por Excitação Multifotônica
Proteínas Recombinantes de Fusão/biossíntese
Proteínas Recombinantes de Fusão/química
Proteínas Supressoras de Tumor/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fluorescent Dyes); 0 (Histones); 0 (Naphthalimides); 0 (Recombinant Fusion Proteins); 0 (Tumor Suppressor Proteins); EC 1.9.3.1 (Electron Transport Complex IV); EC 2.1.1.- (DNA Modification Methylases); EC 2.1.1.63 (MGMT protein, human); EC 6.5.1.- (DNA Repair Enzymes)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170621
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700161


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[PMID]:28527428
[Au] Autor:Pulido-Reyes G; Martín E; Gu Coronado JL; Leganes F; Rosal R; Fernández-Piñas F
[Ad] Endereço:Departamento de Biología, Facultad de Ciencias, Universidad Autónoma de Madrid, E-28049, Spain; Departamento de Ingeniería Química, Universidad de Alcalá, E-28871 Alcalá de Henares, Madrid, Spain. Electronic address: gerardo.pulido@uam.es.
[Ti] Título:Physicochemical and biological interactions between cerium oxide nanoparticles and a 1,8-naphthalimide derivative.
[So] Source:J Photochem Photobiol B;172:61-69, 2017 Jul.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Cerium (Ce) oxide nanoparticles (CNPs) have attracted attention due to their high bioactivity and unique redox-chemistry. The oxygen vacancies at the surface of the nanoparticle explain the autocatalytic properties of CNPs in which the Ce atoms occupy the center of the oxygen vacancies surrounded by Ce atoms. Until now, CNPs have been associated with organic molecules at the synthesis stage to extend their applications or improve their stability. However, there is a lack of information regarding the post-synthesis interaction of CNPs and organic molecules that could enhance or induce new properties. Due to their unique optical properties and their many uses in different areas such as supramolecular chemistry or biomedicine, we have chosen a derivative from the family of naphthalimides (the 4-amino-1,8-naphthalimide-N-substituted; ANN) to study the interaction with different CNPs (CNP1-4) and their joint bioactivity compared to that of the same compounds alone. ANN-CNP complexes were formed as revealed by spectroscopic studies, but, the interaction was markedly different depending on the physicochemical properties of CNPs and their surface content of Ce sites. The ANN adsorption on all CNPs involved the amino group in the naphthalene moiety as shown by NMR spectroscopy, while the pyrrolidine ring was mainly involved in the specific interaction between ANN and CNP1. The biological effect of each CNP and ANN individually and forming complexes was assessed using a bioluminescent model bacterium. The results showed that ANN and CNP with the higher content of surface Ce (CNP1) when combined acted additively towards the used model organism. In the opposite, ANN-CNP2, ANN-CNP3 and ANN-CNP4 complexes were antagonistic when the nanoparticles dominated the mixture. The results of this study contribute to expand the knowledge of the interaction between nanoparticles and organic molecules which may be useful for understanding the behavior of nanoparticles in complex matrices.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Cério/química
Nanopartículas Metálicas/química
Naftalimidas/química
Quinolonas/química
[Mh] Termos MeSH secundário: 1-Naftilamina/química
Complexos de Coordenação/química
Complexos de Coordenação/metabolismo
Difusão Dinâmica da Luz
Espectroscopia de Ressonância Magnética
Photorhabdus/metabolismo
Espectrometria de Fluorescência
Espectroscopia de Infravermelho com Transformada de Fourier
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coordination Complexes); 0 (Naphthalimides); 0 (Quinolones); 1742-95-6 (4-amino-1,8-naphthalimide); 30K4522N6T (Cerium); 619G5K328Y (ceric oxide); 9753I242R5 (1-Naphthylamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170521
[St] Status:MEDLINE


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[PMID]:28241441
[Au] Autor:Ge C; Chang L; Zhao Y; Chang C; Xu X; He H; Wang Y; Dai F; Xie S; Wang C
[Ad] Endereço:Pharmaceutical College, Henan University, Kaifeng 475001, China. gechao1234365@163.com.
[Ti] Título:Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma.
[So] Source:Molecules;22(2), 2017 Feb 22.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Two kinds of naphthalimide derivatives were synthesized and evaluated for in vitro their anti-hepatocellular carcinoma properties. Compound with a fused thiazole fragment to naphthalimide skeleton inhibited cell migration of SMMC-7721 and HepG2, and further in vivo trials with two animal models confirmed that compound moderately inhibited primary H22 tumor growth (52.6%) and potently interrupted lung metastasis (75.7%) without obvious systemic toxicity at the therapeutic dose. Mechanistic research revealed that compound inhibited cancerous liver cell growth mostly by inducing G2/M phase arrest. Western blotting experiments corroborated that could up-regulate the cell cycle related protein expression of cyclin B1, CDK1 and p21, and inhibit cell migration by elevating the E-cadherin and attenuating integrin α6 expression. Our study showed that compound is a valuable lead compound worthy of further investigation.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Carcinoma Hepatocelular/tratamento farmacológico
Neoplasias Hepáticas/tratamento farmacológico
Naftalimidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Apoptose
Caderinas/metabolismo
Carcinoma Hepatocelular/patologia
Ciclo Celular
Linhagem Celular Tumoral
Células Hep G2
Seres Humanos
Neoplasias Hepáticas/patologia
Neoplasias Pulmonares/tratamento farmacológico
Neoplasias Pulmonares/secundário
Camundongos
Estrutura Molecular
Naftalimidas/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cadherins); 0 (Naphthalimides)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170614
[Lr] Data última revisão:
170614
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170301
[St] Status:MEDLINE


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[PMID]:28233678
[Au] Autor:Quintana-Espinoza P; Martín-Acosta P; Amesty Á; Martín-Rodríguez P; Lorenzo-Castrillejo I; Fernández-Pérez L; Machín F; Estévez-Braun A
[Ad] Endereço:Instituto Universitario de Bio-Orgánica Antonio González (CIBICAN), Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez 2, 38206 La Laguna, Tenerife, Spain.
[Ti] Título:5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation.
[So] Source:Bioorg Med Chem;25(6):1976-1983, 2017 Mar 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A set of 5-ethynylarylnaphthalimides was synthesized by Sonogashira cross-coupling reactions and evaluated for antiproliferative and antitopoisomerase II in vitro activities. Furthermore docking studies of these molecules as DNA-intercalators were carried out and the in vivo DNA-damaging activity was also determined with the model organism Saccharomyces cerevisiae. From the obtained results three naphthalimides 6, 13 and 14 showed strong topoisomerase II inhibitory activity. These three molecules also presented good docking scores as DNA-intercalators using a self-complementary oligodeoxynucleotide d(ATGCAT) as a model, and compounds 13 and 14 were among the most cytotoxic in the in vivo DNA-damaging activity.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Naftalimidas/síntese química
Naftalimidas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Espectroscopia de Ressonância Magnética Nuclear de Carbono-13
Linhagem Celular Tumoral
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Simulação de Acoplamento Molecular
Naftalimidas/química
Espectroscopia de Prótons por Ressonância Magnética
Saccharomyces cerevisiae/efeitos dos fármacos
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Naphthalimides)
[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:170225
[St] Status:MEDLINE


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[PMID]:28177238
[Au] Autor:Dai F; Li Q; Wang Y; Ge C; Feng C; Xie S; He H; Xu X; Wang C
[Ad] Endereço:Key Laboratory of Natural Medicine and Immuno-Engineering, ‡College of Chemistry and Chemical Engineering, and §Pharmaceutical College, Henan University , Kaifeng 475004, Henan, China.
[Ti] Título:Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity.
[So] Source:J Med Chem;60(5):2071-2083, 2017 Mar 09.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Approximately 90% of cancer-associated deaths result from disseminated tumors, indicating the ineffectiveness of current therapies and the imperative need of antimetastatic drugs. A novel pharmacophore with flavonoid and naphthalimide moieties was constructed by using a fragment-based drug design and a series of eight flavone-naphthalimide-polyamine conjugates were synthesized. In vitro evaluation revealed that compound 6c with a homospermidine motif displayed better cell selectivity between cancerous and normal liver cells than amonafide did. The in vivo assays on two hepatocellular carcinoma (HCC) models verified that 6c potently suppressed pulmonary metastasis with improved organ indexes compared to amonafide. Various experiments showed that 6c as a potential fluorescent chemical probe could target the mitochondria. Preliminary investigation into the mechanism of action of 6c indicated that it might harness a polyamine transporter for cell entrance, localize in the mitochondria, selectively cause reactive oxygen species (ROS) overproduction in hepatoma cells instead of normal liver cells, and finally lead to HCC cell apoptosis and migration inhibition via multiple ROS-mediated signaling pathways.
[Mh] Termos MeSH primário: Flavonas/farmacologia
Mitocôndrias/efeitos dos fármacos
Naftalimidas/farmacologia
Metástase Neoplásica/prevenção & controle
Poliaminas/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular
Desenho de Drogas
Seres Humanos
Espécies Reativas de Oxigênio/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavones); 0 (Naphthalimides); 0 (Polyamines); 0 (Reactive Oxygen Species)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170807
[Lr] Data última revisão:
170807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170209
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b01846


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[PMID]:28106753
[Au] Autor:Korycka-Machala M; Nowosielski M; Kuron A; Rykowski S; Olejniczak A; Hoffmann M; Dziadek J
[Ad] Endereço:Institute of Medical Biology, Polish Academy of Sciences, Lodz 93-232, Poland. mkorycka@cbm.pan.pl.
[Ti] Título:Naphthalimides Selectively Inhibit the Activity of Bacterial, Replicative DNA Ligases and Display Bactericidal Effects against Tubercle Bacilli.
[So] Source:Molecules;22(1), 2017 Jan 17.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The DNA ligases, enzymes that seal breaks in the backbones of DNA, are essential for all organisms, however bacterial ligases essential for DNA replication use ß-nicotinamide adenine dinucleotide as their co-factor, whereas those that are essential in eukaryotes and viruses use adenosine-5'-triphosphate. This fact leads to the conclusion that NAD⁺-dependent DNA ligases in bacteria could be targeted by their co-factor specific inhibitors. The development of novel alternative medical strategies, including new drugs, are a top priority focus areas for tuberculosis research due to an increase in the number of multi-drug resistant as well as totally drug resistant tubercle bacilli strains. Here, through the use of a virtual high-throughput screen and manual inspection of the top 200 records, 23 compounds were selected for in vitro studies. The selected compounds were evaluated in respect to their NAD⁺ DNA ligase inhibitory effect by a newly developed assay based on Genetic Analyzer 3500 Sequencer. The most effective agents (e.g., pinafide, mitonafide) inhibited the activity of NAD⁺-dependent DNA ligase A at concentrations of 50 µM. At the same time, the ATP-dependent (phage) DNA LigT4 was unaffected by the agents at concentrations up to 2 mM. The selected compounds appeared to also be active against actively growing tubercle bacilli in concentrations as low as 15 µM.
[Mh] Termos MeSH primário: Antituberculosos/farmacologia
DNA Ligases/antagonistas & inibidores
Mycobacterium tuberculosis/efeitos dos fármacos
Naftalimidas/farmacologia
[Mh] Termos MeSH secundário: Proteínas de Bactérias/antagonistas & inibidores
Inibidores Enzimáticos/farmacologia
Ensaios de Triagem em Larga Escala
Isoquinolinas/farmacologia
Simulação de Acoplamento Molecular
NAD
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (Bacterial Proteins); 0 (Enzyme Inhibitors); 0 (Isoquinolines); 0 (Naphthalimides); 06Q0V17SI9 (mitonafide); 0U46U6E8UK (NAD); 1OZ94FI615 (pinafide); EC 6.5.1.- (DNA Ligases)
[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:170121
[St] Status:MEDLINE


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[PMID]:28039778
[Au] Autor:He D; Wang L; Wang L; Li X; Xu Y
[Ad] Endereço:School of Life Science and Technology, Dalian University of Technology, Dalian 116024, China; Ministry of Education Center for Food Safety of Animal Origin, Dalian 116620, China.
[Ti] Título:Spectroscopic studies on the interactions between novel bisnaphthalimide derivatives and calf thymus DNA.
[So] Source:J Photochem Photobiol B;166:333-340, 2017 Jan.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The types of interactions between six novel bisnaphthalimide derivatives (AITHN, BITHN, PITHN, PyITHN, DN6 and DNT6) and calf thymus DNA in a physiological buffer (Tris-HCl buffer solutions, pH=7.4) were investigated using UV-vis spectrophotometry, fluorescence spectroscopy, and a competition experiment, in order to explore the relationships between the linkers of bisnaphthalimide derivatives and their activity. The absorption spectra of the six bisnaphthalimide derivatives with DNA showed a slight red shift and hypochromic effect. DNA quenched the compounds (AITHN, PITHN, PyITHN and DN6) by a static quenching process. Using acridine orange (AO) dye as a fluorescence probe, fluorescence quenching of the emission peak was observed in the AO-DNA system with the addition of PITHN, but the maximum emission intensity was elevated for AITHN and DN6 while the other three compounds showed no obvious change. The calculated binding constants of AITHN, PITHN, PyITHN and DN6 with DNA were 2.09×10 Lmol , 1.14×10 Lmol , 0.95×10 Lmol and 2.39×10 Lmol respectively, and the number of binding sites were 0.618, 0.323, 0.297 and 0.769. Intercalative and electrostatic binding were the two major modes between the six bisnaphthalimide derivatives and calf thymus DNA. The strength of the intercalation was related to the type of linker. Moreover, DN6 and AITHN had the greatest intercalative ability. The electrostatic binding ability of the six compounds was independent of the type of linker present.
[Mh] Termos MeSH primário: DNA/química
Naftalimidas/química
[Mh] Termos MeSH secundário: Animais
Bovinos
Espectrometria de Fluorescência
Espectrofotometria Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Naphthalimides); 9007-49-2 (DNA)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170411
[Lr] Data última revisão:
170411
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170101
[St] Status:MEDLINE


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[PMID]:28024642
[Au] Autor:Hu Y; Zeng F
[Ad] Endereço:College of Materials Science and Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address: yinyangscut@163.com.
[Ti] Título:A theranostic prodrug based on FRET for real-time drug release monitoring in response to biothiols.
[So] Source:Mater Sci Eng C Mater Biol Appl;72:77-85, 2017 Mar 01.
[Is] ISSN:1873-0191
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The clinical applications of tradition prodrug are restricted to a certain extent due to its some defects such as side effects, low selectivity and single function. Herein, we designed a theranostic strategy based on the fluorescence resonance energy transfer (FRET) mechanism. The theranostic prodrug was constructed with an anticancer drug camptothecin (CPT), a cleavable linker based on disulfide bonds (SS) and a fluorophore naphthalimide derivative (NAP). For this drug delivery and reporting system (NAP-SS-CPT), FRET occurs between CPT (energy donor) and NAP (energy receptor); and upon cellular uptake by GSH-overexpressing cancer cells, disulfide bonds could be successfully cleaved by the high concentration of GSH, and FRET process was interrupted to achieve dual fluorescence response and specifically release of CPT. The drug delivery system features some favorable properties, like excellent pH-stability, high selectivity and cytotoxicity towards GSH-overexpressing cells and relatively lower cytotoxicity towards normal cells. Fluorescence analysis reveals that NAP-SS-CPT shows a ratiometric fluorescence signal under excitation at 400nm for quantitative detection of GSH. Intracellular fluorescence imaging studies indicate that the prodrug can be efficiently internalized in HeLa cells and used for real-time monitoring of drug release. Moreover, MTT and flow cytometry assay indicate that NAP-SS-CPT exhibits high pro-apoptotic effect for cancer cells. This strategy may provide a new approach for cancer diagnosis and therapy.
[Mh] Termos MeSH primário: Portadores de Fármacos/química
Pró-Fármacos/química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/análise
Antineoplásicos/química
Antineoplásicos/metabolismo
Antineoplásicos/toxicidade
Camptotecina/análise
Camptotecina/química
Camptotecina/metabolismo
Camptotecina/toxicidade
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Cromatografia Líquida de Alta Pressão
Dissulfetos/química
Liberação Controlada de Fármacos
Transferência Ressonante de Energia de Fluorescência
Glutationa/química
Células HeLa
Seres Humanos
Espectrometria de Massas
Camundongos
Microscopia de Fluorescência
Naftalimidas/química
Pró-Fármacos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Disulfides); 0 (Drug Carriers); 0 (Naphthalimides); 0 (Prodrugs); GAN16C9B8O (Glutathione); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161228
[St] Status:MEDLINE



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