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1.
Macromol Rapid Commun ; 42(14): e2100186, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33987942

RESUMO

This study reports for the first time the excellent nonvolatile and volatile digital memory characteristics of polymers bearing 2-pyrrolidone and succinimide moieties. A series of new polymers is synthesized from poly(ethylene-alt-maleic anhydride) and four alcohol derivatives with and without 2-pyrrolidone and succinimide moieties. All polymers, including polyvinylpyrrolidone, are found to be thermally stable up to 195 °C or higher, and characterized regarding their molecular orbital energy levels, bandgap, and resistive digital memory behaviors. Excitingly, the polymers bearing either 2-pyrrolidone or succinimide moiety demonstrate p-type digital memory behaviors with high ON/OFF current ratios and long reliabilities. Nonvolatile digital memory performance is achieved over the film thickness range of 10-80 nm, whereas volatile digital memory is demonstrated over a much narrower range of film thickness. All digital memory performances can be originated from the 2-pyrrolidone and succinimide moieties possessing high affinity and stabilization power to charges via charge traps and transformations based on a hopping conduction process. Hence, these new polymers are suitable for the production of high-performance p-type nonvolatile and volatile digital memory devices. Moreover, 2-pyrrolidone and succinimide can be used as new and economical electroactive building blocks for the development of advanced digital memory materials.


Assuntos
Polímeros , Pirrolidinonas , Succinimidas
2.
Bioorg Med Chem Lett ; 28(2): 107-112, 2018 01 15.
Artigo em Inglês | MEDLINE | ID: mdl-29208521

RESUMO

Dysfunction or progressive degeneration of retinal pigment epithelium (RPE) contributes in the initial pathogenesis of age-related macular degeneration (AMD) causing irreversible vision loss, which makes RPE the prime target of the disease. The present study aimed to identify compounds to protect 4-hydroxynonenal (4-HNE)-induced RPE cell death by inhibiting NADPH oxidase 4 (NOX4) activity, not just as free radical scavengers, using ARPE-19, a human adult retinal pigment epithelial cell line, as a RPE representative. Novel thirty-two 6-ureido/thioureido-2,4,5-trimethylpyridin-3-ol derivatives 17 were synthesized and tested. We found that there was a strong correlation between level of protective effect of compounds 17 against 4-HNE-induced APRE-19 cell death and that of inhibitory activity against 4-HNE-induced superoxide production, and that most of the compounds 17 showed minimal DPPH radical scavenging activity. Compound 17-28 showed the best protective activity against 4-HNE-induced superoxide production (79.5% inhibition) and cell death (85.1% recovery) at 10 µM concentration, which was better than that of VAS2870, a NOX2/4 inhibitor. In addition, compound 17-28 blocked 4-HNE-induced apoptosis of ARPE-19 cells in a concentration-dependent manner. The results indicate that compound 17-28 may be a lead compound to develop AMD therapeutics.


Assuntos
Aldeídos/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Piridinas/farmacologia , Adulto , Aldeídos/farmacologia , Morte Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Estrutura Molecular , NADPH Oxidase 4/antagonistas & inibidores , NADPH Oxidase 4/metabolismo , Piridinas/síntese química , Piridinas/química , Relação Estrutura-Atividade , Superóxidos/antagonistas & inibidores , Superóxidos/metabolismo
3.
Pharmaceutics ; 11(1)2018 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-30577564

RESUMO

This study aimed to design phosphatidylcholine (PC)-based solid dispersion (SD) systems for enhancing the apparent aqueous solubility and dissolution of celecoxib (CLC), a selective cyclooxygenase-2 inhibitor with a highly hydrophobic property. Although PC-based dispersion formulations considerably increased solubilities of CLC, the lipidic texture of PC was not appropriate as a solid dosage form for oral administration of CLC. To mask the lipidic texture of PC-based matrices, Neusilin® US2, an adsorbent material with a porous structure and large surface area widely used in the pharmaceutical industry, was employed and thereby fully powderized PC-based dispersion formulations could be fabricated. However, PC matrices containing CLC strongly adsorbed to the pores of Neusilin® US2 was not able to be rapidly released. To address this problem, different hydrophilic materials were examined to promote the release of the CLC-dispersed PC matrices from Neusilin® US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin® US2 particles, showing significantly enhanced apparent aqueous solubility and dissolution behavior of CLC. Through differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy (FT-IR) analysis, a considerably reduced crystallinity of CLC dispersed in the PC-based dispersion formulations was demonstrated. The PC-based SD formulations developed in this study would be useful for improving the oral bioavailability of poorly soluble drugs such as CLC.

4.
Korean J Radiol ; 13(6): 812-5, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23118582

RESUMO

We report a case of malignant melanoma of Eustachian tube with extension to the middle ear cavity and nasopharynx in a 51-year-old woman who presented with right ear fullness. Computed tomography showed a soft tissue mass in the middle ear cavity and caused the widening and eroding of the bony eustachian tube. Magnetic resonance imaging showed well enhancing mass in eustachian tube extending nasopharynx to middle ear cavity. A biopsy of the middle ear cavity mass revealed a malignant amelanotic melanoma.


Assuntos
Neoplasias da Orelha/diagnóstico , Tuba Auditiva , Melanoma/diagnóstico , Orelha Média/patologia , Feminino , Humanos , Imageamento por Ressonância Magnética , Pessoa de Meia-Idade , Nasofaringe/patologia , Invasividade Neoplásica , Tomografia Computadorizada por Raios X
5.
J Agric Food Chem ; 57(8): 3164-72, 2009 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-19317483

RESUMO

The influence of conjugated linoleic acid (CLA) on the growth of some foodborne and pathogenic bacteria was examined. A potassium salt of CLA (CLA-K) was tested against three Gram-positive strains ( Bacillus cereus , Staphylococcus aureus , and Streptococcus mutans ) and five Gram-negative strains ( Pseudomonas aeruginosa , Salmonella typhimurium , Vibrio parahemolyticus , Klebsiella pneumoniae , and Proteus mirabilis ). CLA-K-mediated growth inhibition was evident for all tested strains, particularly the Gram-positive strains. The IC(50) value of CLA-K was 0.3 mM for B. cereus, 1.2 mM for S. aureus, and 0.3 mM for S. mutans, whereas the value was 1.2 mM for K. pneumoniae, 1.2 mM for P. aeruginosa, 1.8 mM for S. typhimurium, 1.8 mM for V. parahemolyticus, and 2.4 mM for P. mirabilis. The CLA-K delayed the growth of all the tested strains at lower CLA-K concentrations, but completely inhibited the growth at higher concentrations. All cells grown in the medium containing CLA-K contained CLA in their membranes and exhibited irregular cell surface and cell disruption, which were greater in Gram-positive than Gram-negative strains. Higher lactic dehydrogenase activity (LDH), protein content, and malondialdehyde (MDA) content were evident in Gram-positive strains than in Gram-negative strains. These results suggest that the broad spectrum of growth inhibition by CLA mediated through the lipid peroxidation of CLA in the membranes and in the medium.


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Microbiologia de Alimentos , Ácidos Linoleicos Conjugados/farmacologia , Bactérias/ultraestrutura , Membrana Celular/química , Ácidos Graxos/análise , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Ácidos Linoleicos Conjugados/análise , Peroxidação de Lipídeos , Microscopia Eletrônica de Varredura
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