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1.
J Prosthodont ; 28(1): e376-e382, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29855119

RESUMO

PURPOSE: To evaluate the effect of light-cured resin cement application based on etching and silanization on the translucent property of ceramic veneers in different thicknesses, testing the hypothesis that the surface treatment and subsequent resin cement application could influence the translucency of ceramic veneers. The relationship between translucency of ceramic veneers and light transmission irradiated by LED polymerization units was also determined. MATERIALS AND METHODS: 40 specimens (10 mm diameter) were fabricated from IPS e.max Press HT A2 ceramic ingots, and polished to 0.3 ± 0.01 mm, 0.5 ± 0.01 mm, 0.7 ± 0.01 mm, 1.0 ± 0.01 mm, and 1.5 ± 0.01 mm thick (n = 8/group). One surface of each disc was etched with HF acid, silanized with Monobond-S, and applied with a light-cured resin cement (Variolink N Transparent Base). Before and after the above procedure, the total luminous transmittance (τ) of all specimens was assessed by a spectrophotometer in a wavelength range of 380-780 nm. A handheld radiometer was used to measure the light intensity irradiated by three LED polymerization units. Light transmission (LT) through ceramic specimens after resin cement application was calculated. Data were statistically analyzed using two-way ANOVA (p = 0.05) and Tukey's test. The correlation between translucency (τ) of ceramic veneers after resin cement application and light transmission (LT) of curing units was statistically evaluated using Spearman correlation test (p = 0.05). RESULTS: With the increase of ceramic thickness, the transmittance decreased significantly (p < 0.05). For the 0.3-mm, 0.5-mm, and 0.7-mm-thick groups, the transmittance of ceramic specimens was statistically significantly lower after resin cement application (p < 0.05). The r value of Bluephase C8 was 0.988, 0.977 for Bluphase, and 0.883 for Bluephase 20i, indicating that the light transmission (LT%) was positively correlated to the translucency of ceramic veneers, regardless of the type of curing units. CONCLUSION: After the light-cured resin cement application based on etching and silanization, the ceramic veneers (less than 0.7-mm thick) were less translucent, and the translucency decreased when the thickness increased. Because of the lower translucency of ceramic veneers, the light intensity of LED units transmitted to resin layer would decrease when curing.


Assuntos
Cerâmica , Lâmpadas de Polimerização Dentária , Materiais Dentários , Facetas Dentárias , Cimentos de Resina/uso terapêutico , Luz , Cura Luminosa de Adesivos Dentários , Microscopia Eletrônica de Varredura , Polimerização/efeitos da radiação
2.
FASEB J ; 27(11): 4561-71, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23925653

RESUMO

This study was designed to evaluate and characterize the molecular basis of antitumor activity of naturally occurring resveratrol (RES; 3,5,4'-trihydroxy-trans-stilbene) derivatives. The compounds were isolated from plants in previous studies and characterized spectroscopically. The antitumor activities of 31 RES derivatives, including dimers, trimers, and tetramers of RES, were evaluated using cell-based assays and validated on a murine model. Several trimeric and a tetrameric stilbenoids induced tumor cell apoptosis or growth arrest of several tumor cell lines with IC50 values (2.8-19.7 µM), significantly lower than that of RES (IC50>70 µM). Using pauciflorol B (PauB) as an example, we showed that the compound induced apoptosis p53 dependently, inducing p53 accumulation and p53-modulated gene expression in cells with wild-type p53, but not in those with nonfunctional p53. Reexpression of p53 in p53-null cells rescued cell death response. In parallel, the MAPK/p38 was activated and critical for PauB-induced killing. Interestingly, activation of p38 in p53 deficient cells was sufficient to drive cells into senescence via the p16-pRb pathway. Finally, PauB dose-dependently inhibited tumor growth on nude mice. Naturally occurring trimeric and tetrameric stilbenoids are potent antitumor agents. Those compounds exert antitumor effect through p53-dependent induction of apoptosis or senescence.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Estilbenos/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Genes p16 , Células HeLa , Humanos , Células MCF-7 , Camundongos , Camundongos Nus , Neoplasias/tratamento farmacológico , Polímeros/química , Resveratrol , Estilbenos/química , Estilbenos/uso terapêutico , Proteína Supressora de Tumor p53/genética , Proteína Supressora de Tumor p53/metabolismo , Ensaios Antitumorais Modelo de Xenoenxerto , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
4.
Chem Biol Interact ; 259(Pt B): 78-84, 2016 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-27297626

RESUMO

Natural product inhibitors of AChE are of interest both because they offer promise as inexpensive drugs for symptomatic relief in Alzheimer's disease and because they may provide insights into the structural features of the AChE catalytic site. Hopeahainol A is an uncharged polyphenol AChE inhibitor from the stem bark of Hopea hainanensis with a constrained, partially dearomatized bicyclic core. Molecular modeling indicates that hopeahainol A binds at the entrance of the long but narrow AChE active site gorge because it is too bulky to be accommodated within the gorge without severe distortion of the gorge as depicted in AChE crystal structures. We conducted inhibitor competition experiments in which AChE inhibition was measured with hopeahainol A together with either edrophonium (which binds at the base of the gorge) or thioflavin T (which binds to the peripheral or P-site near the gorge mouth). The results agreed with the molecular modeling and indicated that hopeahainol A at lower concentrations (<200 µM) bound only to the P-site, as hopeahainol A and thioflavin T were unable to form a ternary complex with AChE while hopeahainol A and edrophonium did form a ternary complex with essentially no competition between them. Inhibition increased to a striking extent at higher concentrations of hopeahainol A, with plots analogous to classic Dixon plots showing a dependence on hopeahainol A concentrations to the third- or fourth order. The inhibition at higher hopeahainol A concentrations was completely reversed on dilution and blocked by bound edrophonium. We hypothesize that bound hopeahainol A induces conformational changes in the AChE active site that allow binding of additional hopeahainol A molecules, a phenomenon that would be unprecedented for a reversible inhibitor that apparently forms no covalent bonds with AChE.


Assuntos
Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/metabolismo , Compostos Heterocíclicos de 4 ou mais Anéis/metabolismo , Acetilcolinesterase/química , Benzotiazóis , Sítios de Ligação , Domínio Catalítico , Inibidores da Colinesterase/química , Dipterocarpaceae/química , Dipterocarpaceae/metabolismo , Edrofônio/química , Edrofônio/metabolismo , Compostos Heterocíclicos de 4 ou mais Anéis/química , Cinética , Simulação de Acoplamento Molecular , Casca de Planta/química , Casca de Planta/metabolismo , Especificidade por Substrato , Termodinâmica , Tiazóis/química , Tiazóis/metabolismo
5.
Artigo em Inglês | MEDLINE | ID: mdl-25817261

RESUMO

In this work, the separation and purification of fumigaclavine C (FC), an ergot alkaloid with strong anti-inflammatory activity from fermented mycelia of Aspergillus fumigatus was systematically evaluated. Among the eight tested resins, the non-polar resin D101 displayed the best adsorption and desorption based on of static adsorption and desorption tests. Adsorption isotherms were constructed on D101 resin and fitted well to the Freundlich model. Dynamic adsorption and desorption tests on a column packed with D101 resin have been investigated for optimization of chromatographic parameters. Under optimized conditions, the contents of FC increased from 7.32% (w/w) in the crude extract to 67.54% in the final product with a recovery yield of 90.35% (w/w) via one run. Furthermore, a lab scale-up separation was carried out, in which the FC content and recovery yield were 65.83% and 90.13%, respectively. These results demonstrated that this adsorption-desorption strategy by using D101 resin was simple and efficient, thus showing potential for large scale purification and preparation of FC in the future.


Assuntos
Aspergillus fumigatus/metabolismo , Cromoterapia/métodos , Alcaloides de Claviceps/isolamento & purificação , Alcaloides Indólicos/isolamento & purificação , Micélio/química , Resinas Sintéticas/química , Adsorção , Aspergillus fumigatus/química , Cromoterapia/instrumentação , Alcaloides de Claviceps/metabolismo , Fermentação , Alcaloides Indólicos/metabolismo , Micélio/metabolismo , Porosidade
6.
Artigo em Inglês | MEDLINE | ID: mdl-23554831

RESUMO

Enterovirus 71 (EV71) and coxsackievirus A16 (CVA16) are the causative agents of hand, foot, and mouth disease (HFMD). During recent epidemics of HFMD in China, medicinal herbals and preparations containing herbal extracts have demonstrated therapeutic efficacy with relative safety profiles. There have been no microbiological studies to validate their usefulness for HFMD. We selected 12 commonly used herbs for HFMD from government recommended guidelines as well as published reports and tested for their antiviral activity and anti-inflammatory activity. A water extract of Houttuynia cordata Thunb. (HCT) inhibited EV71 infection significantly and was marginally active against CVA16 infection. The IC50 (concentration to have 50% inhibitory effect) values of HCT against a Fuyang strain and a BrCr strain of EV71 were determined at 8.9 µ g/mL and 20.6 µ g/mL, respectively. Mentha haplocalyx Briq. (MHB) water extract was active against CVA16, with an IC50 value of 70.3 µ g/mL. The extract did not exhibit activity against EV71 infection. Although the majority of the extracts showed no activity against viral infection, several extracts demonstrated activity in blocking proinflammatory response by viral infection. This study therefore validates the effectiveness of Chinese herbs for HFMD since some formulations containing the correct combination of the herbs can block viral replication as well as proinflammatory response of HFMD.

7.
Nat Prod Commun ; 6(3): 353-5, 2011 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-21485273

RESUMO

Two new compounds, named 2-formylpyrrole-4-acrylamide (1) and dihydrostreptazolin (2) were isolated from the fermentation broth of BY-4, an actinomycetes residing in the gut of Odontotermes formosanus. The structures of 1 and 2 were elucidated by extensive spectral analysis (1H, 13C, 2D NMR, and HR-ESIMS). The isolated compounds were assayed for cytotoxic and antimicrobial activities.


Assuntos
Acrilamidas/química , Isópteros/microbiologia , Oxazóis/química , Piperidinas/química , Pirróis/química , Streptomyces/química , Acrilamidas/farmacologia , Animais , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Fermentação , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Oxazóis/farmacologia , Piperidinas/farmacologia , Pirróis/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta
8.
Cytokine Growth Factor Rev ; 20(1): 7-17, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-19046922

RESUMO

Osteoclasts are responsible for bone resorption and play a pivotal role in the pathogenesis of osteolytic disorders. NF-kappaB is a set of nuclear factors that bind to consensus DNA sequences called kappaB sites, and is essential for osteoclast formation and survival. NF-kappaB signalling pathways are strictly regulated to maintain bone homeostasis by cytokines such as RANKL, TNF-alpha and IL-1, which differentially regulate classical and/or alternative NF-kappaB pathways in osteoclastic cells. These pathways are also modulated by NF-kappaB mediators, including TRAF6, aPKC, p62/SQSTM1 and deubiquitinating enzyme CYLD that are involved in the ubiquitin-proteasome system during RANK-mediated osteoclastogenesis. Abnormal activation of NF-kappaB signalling in osteoclasts has been associated with excessive osteoclastic activity, and frequently observed in osteolytic conditions, including periprosthetic osteolysis, arthritis, Paget's disease of bone, and periodontitis. NF-kappaB modulators such as parthenolide and NEMO-binding domain peptide demonstrate therapeutic effects on inflammation-induced bone destruction in mouse models. Unravelling the structure and function of NF-kappaB pathways in osteoclasts and other cell types will be important in developing new strategies for treatments of bone diseases.


Assuntos
NF-kappa B/fisiologia , Animais , Artrite Reumatoide/metabolismo , DNA/metabolismo , Modelos Animais de Doenças , Humanos , Inflamação , Camundongos , Modelos Biológicos , Modelos Químicos , NF-kappa B/metabolismo , Osteoartrite/metabolismo , Osteoclastos/metabolismo , Periodontite/metabolismo , Ligação Proteica , Transdução de Sinais
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