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1.
Dentomaxillofac Radiol ; : 20210286, 2021 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-34762486

RESUMO

OBJECTIVES: To evaluate the diagnostic efficacy of CBCT-MRI fused image for anterior disc displacement and bone changes of temporomandibular joint (TMJ), which are the main imaging manifestations of temporomandibular disorders (TMD). METHODS: Two hundred and thirty-one TMJs of 120 patients who were diagnosed with TMD were selected for the study. The anterior disc displacement, bone defect and bone hyperplasia evaluated by three experts were used as a reference standard. Three residents individually evaluated all the three sets of images, which were CBCT images, MRI images and CBCT-MRI fused images from individual CBCT and MRI images in a random order for the above-mentioned three imaging manifestations with a five-point scale. Each set of images was observed at least 1 week apart. A second evaluation was performed 4 weeks later. Intra- and interobserver agreements were assessed using the intraclass correlation coefficient (ICC). The areas under the ROC curves (AUCs) of the three image sets were compared with a Z test, and p < 0.05 was considered statistically significant. RESULTS: One hundred and forty-five cases were determined as anterior disc displacement, 84 cases as bone defect and 40 cases as bone hyperplasia. The intra- and interobserver agreements in the CBCT-MRI fused image set (0.76-0.91) were good to excellent, and the diagnostic accuracy for bone changes was significantly higher than that of MRI image set (p<0.05). CONCLUSIONS: CBCT-MRI fused images can display the disc and surrounding bone structures simultaneously and significantly improve the observers' reliability and diagnostic accuracy, especially for inexperienced residents.

2.
Environ Sci Pollut Res Int ; 28(45): 64858-64870, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34322817

RESUMO

This study focused on the removal of organic matter and nitrogen and explored the feasible operation strategies to achieve short-cut nitrification and denitrification in two constructed wetlands (CWs), which were designed to treat the actual landfill leachate from a small county in parallel. The two CWs were horizontal sub-surface flow constructed wetlands (HFCW) with partial-area aeration and vertical sub-surface flow constructed wetlands (VFCW) with full-area aeration. The experimental results showed that both CWs could achieve an excellent organic matter and nitrogen removal performance under the conditions of intermittent aeration with high frequency and medium intensity (2 h of aeration and 4 h of rest). The removal efficiencies of COD and total nitrogen by HFCW were 89.08% and 73.22%, and the corresponding values of VFCW were 84.51% and 71.44%, respectively. Meanwhile, the inhibition kinetics model indicated that HFCW with partial-area aeration could enhance the free ammonium (FA) tolerance of ammonium-oxidizing bacteria (AOB) and reduce the conversion percentage of ammonia nitrogen. In addition, the intermittent aeration mode with high frequency and medium intensity could keep the DO concentration below under 0.60 mg L-1 in HFCW, which helped to achieve stable short-cut nitrification and ensure the average nitrite accumulation rate (NAR) reach 50.96%. These results suggested that the intermittent aeration in partial-area could achieve successful short-cut nitrification in HFCW, thereby improving the removal efficiency of nitrogen in landfill leachate.


Assuntos
Poluentes Químicos da Água , Áreas Alagadas , Análise da Demanda Biológica de Oxigênio , Desnitrificação , Nitrificação , Nitrogênio
3.
Nanotheranostics ; 5(1): 73-89, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33391976

RESUMO

Microfluidic chip is not a chip in the traditional sense. It is technologies that control fluids at the micro level. As a burgeoning biochip, microfluidic chips integrate multiple disciplines, including physiology, pathology, cell biology, biophysics, engineering mechanics, mechanical design, materials science, and so on. The application of microfluidic chip has shown tremendous promise in the field of cancer therapy in the past three decades. Various types of cell and tissue cultures, including 2D cell culture, 3D cell culture and tissue organoid culture could be performed on microfluidic chips. Patient-derived cancer cells and tissues can be cultured on microfluidic chips in a visible, controllable, and high-throughput manner, which greatly advances the process of personalized medicine. Moreover, the functionality of microfluidic chip is greatly expanding due to the customizable nature. In this review, we introduce its application in developing cancer preclinical models, detecting cancer biomarkers, screening anti-cancer drugs, exploring tumor heterogeneity and producing nano-drugs. We highlight the functions and recent development of microfluidic chip to provide references for advancing cancer diagnosis and treatment.


Assuntos
Técnicas Analíticas Microfluídicas/instrumentação , Neoplasias/diagnóstico , Antineoplásicos/uso terapêutico , Humanos , Neoplasias/tratamento farmacológico
4.
Cancer Commun (Lond) ; 41(2): 109-120, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33119215

RESUMO

Altered metabolism is a hallmark of cancer, and the reprogramming of energy metabolism has historically been considered a general phenomenon of tumors. It is well recognized that long noncoding RNAs (lncRNAs) regulate energy metabolism in cancer. However, lncRNA-mediated posttranslational modifications and metabolic reprogramming are unclear at present. In this review, we summarized the current understanding of the interactions between the alterations in cancer-associated energy metabolism and the lncRNA-mediated posttranslational modifications of metabolic enzymes, transcription factors, and other proteins involved in metabolic pathways. In addition, we discuss the mechanisms through which these interactions contribute to tumor initiation and progression, and the key roles and clinical significance of functional lncRNAs. We believe that an in-depth understanding of lncRNA-mediated cancer metabolic reprogramming can help to identify cellular vulnerabilities that can be exploited for cancer diagnosis and therapy.


Assuntos
Metabolismo Energético , Neoplasias , RNA Longo não Codificante , Humanos , Neoplasias/metabolismo , Processamento de Proteína Pós-Traducional , RNA Longo não Codificante/metabolismo
5.
Front Pharmacol ; 11: 579068, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33041823

RESUMO

Integrins are the adhesion molecules and receptors of extracellular matrix (ECM). They mediate the interactions between cells-cells and cells-ECM. The crosstalk between cancer cells and their microenvironment triggers a variety of critical signaling cues and promotes the malignant phenotype of cancer. As a type of transmembrane protein, integrin-mediated cell adhesion is essential in regulating various biological functions of cancer cells. Recent evidence has shown that integrins present on tumor cells or tumor-associated stromal cells are involved in ECM remodeling, and as mechanotransducers sensing changes in the biophysical properties of the ECM, which contribute to cancer metastasis, stemness and drug resistance. In this review, we outline the mechanism of integrin-mediated effects on biological changes of cancers and highlight the current status of clinical treatments by targeting integrins.

6.
Front Pharmacol ; 11: 722, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32528284

RESUMO

Cancer has been a major global health problem due to its high morbidity and mortality. While many chemotherapy agents have been studied and applied in clinical trials or in clinic, their application is limited due to its toxic side effects and poor tolerability. Monoclonal antibodies specific to the PD-1 and PD-L1 immune checkpoints have been approved for the treatment of various tumors. However, the application of PD-1/PD-L1 inhibitors remains suboptimal and thus another strategy comes in to our sight involving the combination of checkpoint inhibitors with other agents, enhancing the therapeutic efficacy. Various novel promising approaches are now in clinical trials, just as icing on the cake. This review summarizes relevant investigations on combinatorial therapeutics based on PD-1/PD-L1 inhibition.

7.
Ying Yong Sheng Tai Xue Bao ; 31(8): 2793-2803, 2020 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34494803

RESUMO

To understand the relationships among dominant species of cephalopods in offshore nor-thern South China Sea, we examined the niche characteristics of these dominant species from both spatial and temporal dimensions using the index of relative importance (IRI), the niche breadth and overlap indices based on fishery resources data from the bottom-trawl survey for four seasons during 2014-2015. The results showed that five dominant species of cephalopods were recorded for four seasons, including Loligo edulis, L. chinensis, L. beka, Sepia esculenta, and L. duvaucelii. The first two species were shared by all seasons. Compared with historical data, the composition of dominant cephalopods species had changed. The cephalopods resource exhibited obvious temporal and spatial variations. Stock density was higher in the sea area extending from the southern Hainan Island to eastern Guangdong Province than that in Beibu Gulf. The seasonal variation was characte-rized by the largest in summer but the smallest in winter. The temporal and spatial niche analysis showed that there was inconsistent in the order between temporal and spatial niche breadths for domi-nant species. L. edulis (1.32) and L. chinensis (3.90) occupied the largest temporal and spatial niche breadths, respectively. The smallest of temporal and spatial niche breadths were shown for S. esculenta (0.98) and L. duvaucelii (2.04), respectively. Though the temporal niche overlap was numerically larger than the spatial niche overlap, both of them had higher values in interspecies among L. edulis, L. chinensis, L. beka, and the lower overlap for the species pairs between L. duvaucelii and other species. The result of correlation analysis suggested that niche breadth exhibited a significant negative correlation with variation in abundance on both temporal and spatial scales. The ecological niche could reflect the tempo-spatial changes of species resource, which enriched the traditional methods of fishery communities.


Assuntos
Cefalópodes , Animais , China , Ecossistema , Pesqueiros , Estações do Ano
8.
Nat Commun ; 10(1): 5505, 2019 12 03.
Artigo em Inglês | MEDLINE | ID: mdl-31796737

RESUMO

In materials chiral fermions such as Weyl fermions are characterized by nonzero chiral charges, which are singular points of Berry curvature in momentum space. Recently, new types of chiral fermions beyond Weyl fermions have been discovered in structurally chiral crystals CoSi, RhSi and PtAl. Here, we have synthesized RhSn single crystals, which have opposite structural chirality to the CoSi crystals we previously studied. Using angle-resolved photoemission spectroscopy, we show that the bulk electronic structures of RhSn are consistent with the band calculations and observe evident surface Fermi arcs and helical surface bands, confirming the existence of chiral fermions in RhSn. It is noteworthy that the helical surface bands of the RhSn and CoSi crystals have opposite handedness, meaning that the chiral fermions are reversed in the crystals of opposite structural chirality. Our discovery establishes a direct connection between chiral fermions in momentum space and chiral lattices in real space.

9.
Environ Pollut ; 255(Pt 2): 112989, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31546078

RESUMO

Large-area hypoxia of urban landscape water often causes the emissions of harmful gases in summer, which not only reduces its sensory effects, but also brings a potential threat to aquatic ecosystem and human health. This study explored the dose effects of calcium peroxide (CaO2) on inhibiting harmful gases emissions and restoring the scenic effect (including visual sense and olfactory sense) of anoxic/anaerobic landscape water system. The results indicated that the emissions of H2S, CO2 and CH4 from the anoxic/anaerobic water system were obviously inhibited in the reactors with CaO2 additions and the effect was positively correlated with the CaO2 dose. Meanwhile, the concentrations of total chemical oxygen demand (TCOD) and soluble sulfide (S2-), and turbidity in the overlying water (the water-layer above the sediment-water interface) were also decreased in the reactors dosed with CaO2. The reason was ascribed to the improvement of the anoxic/anaerobic condition in the water system and the increase of the species richness, bacteria count and aerobic microorganism abundance in sediment. Furthermore, 0.12 kg-CaO2 m-2-sediment was selected as the optimal dose, which was based on considering the inhibiting effect of the harmful gases emissions, comprehensive influence and costs. Compared with control check (CK, the reactor without adding CaO2), the optimal dose of CaO2 could reduce 75.10% CH4, 81.02% CO2 and 100% H2S in gases, and decrease 81.52% S2-, 42.85% TCOD and 84.01% turbidity in the overlying water. In conclusion, all the dosages of CaO2 could improve the anoxic condition of water system and 0.12 kg-CaO2 m-2-sediment was the optimal dose in inhibiting harmful gases emissions, which could keep an excellent water quality in this simulation experiment. Therefore, this study may provide a feasible method and the optimal dose for inhibiting the emissions of harmful gases and restoring the scenic effect in the similar anoxic/anaerobic landscape water.


Assuntos
Peróxidos/análise , Poluentes Químicos da Água/análise , Anaerobiose , Ecossistema , Gases , Hipóxia , Água , Qualidade da Água
10.
Front Pharmacol ; 10: 746, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31354475

RESUMO

As a quinonemethide triterpenoid extracted from species of the Celastraceae and Hippocrateaceae, pristimerin has been shown potent anti-cancer effects. Specifically, it was found that pristimerin can affect many tumor-related processes, such as apoptosis, autophagy, migration and invasion, vasculogenesis, and drug resistance. Various molecular targets or signaling pathways are also involved, such as cyclins, reactive oxygen species (ROS), microRNA, nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (MAPK), and PI3K/AKT/mammalian target of rapamycin (mTOR) pathways. In this review, we will focus on the research about pristimerin-induced anti-cancer activities to achieve a deeper understanding of the targets and mechanisms, which offer evidences suggesting that pristimerin can be a potent anti-cancer drug.

11.
J Enzyme Inhib Med Chem ; 33(1): 1554-1564, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30244610

RESUMO

To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five cancer cell lines, including MGC-803 and BEL-7402. (Z)-3-(p-Tolyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile (6h) showed a strong inhibitory effect on MGC-803 cells (IC50 < 0.01 µM) and exhibited stronger anti-proliferative activity than taxol (IC50 < 0.06 ± 0.01 µM). The IC50 value of 6h in L-02 cells was 10,000-fold higher than in MGC-803 cells. Compound 6h inhibited proliferation of BEL-7402 cells by arresting at the G2/M phase through up-regulation of cyclin B1 expression, down-regulation of cyclin A and D1 expression, and induction of apoptosis. In addition, 6h inhibited the migration of BEL-7402 cells and the formation of cell colonies.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Estilbenos/síntese química , Estilbenos/farmacologia , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Estereoisomerismo , Estilbenos/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas
12.
Ann Bot ; 122(4): 555-568, 2018 09 24.
Artigo em Inglês | MEDLINE | ID: mdl-30252045

RESUMO

Background and Aims: The cuticular waxes sealing plant surfaces against excessive water loss are complex mixtures of very-long-chain aliphatics, with compositions that vary widely between plant species. To help fill the gap in our knowledge about waxes of non-flowering plant taxa, and thus about the cuticle of ancestral land plants, this study provides comprehensive analyses of waxes on temperate fern species from five different families. Methods: The wax mixtures on fronds of Pteridium aquilinum, Cryptogramma crispa, Polypodium glycyrrhiza, Polystichum munitum and Gymnocarpium dryopteris were analysed using gas chromatography-mass spectrometry for identification, and gas chromatography-flame ionization detection for quantification. Key Results: The wax mixtures from all five fern species contained large amounts of C36-C54 alkyl esters, with species-specific homologue distributions. They were accompanied by minor amounts of fatty acids, primary alcohols, aldehydes and/or alkanes, whose chain length profiles also varied widely between species. In the frond wax of G. dryopteris, C27-C33 secondary alcohols and C27-C35 ketones with functional groups exclusively on even-numbered carbons (C-10 to C-16) were identified; these are characteristic structures similar to secondary alcohols and ketones in moss, gymnosperm and basal angiosperm waxes. The ferns had total wax amounts varying from 3.9 µg cm-2 on P. glycyrrhiza to 16.9 µg cm-2 on G. dryopteris, thus spanning a range comparable with that on leaves of flowering plants. Conclusions: The characteristic compound class compositions indicate that all five fern species contain the full complement of wax biosynthesis enzymes previously described for the angiosperm arabidopsis. Based on the isomer profiles, we predict that each fern species, in contrast to arabidopsis, has multiple ester synthase enzymes, each with unique substrate specificities.


Assuntos
Gleiquênias/química , Ceras/química , Álcoois/química , Arabidopsis/química , Ésteres/química , Ácidos Graxos/química , Cromatografia Gasosa-Espectrometria de Massas , Epiderme Vegetal/química , Folhas de Planta/química
13.
Front Neurosci ; 12: 555, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30210272

RESUMO

Brain-computer interface (BCI) is a direct communication pathway between brain and external devices, and BCI-based prosthetic devices are promising to provide new rehabilitation options for people with motor disabilities. Electrocorticography (ECoG) signals contain rich information correlated with motor activities, and have great potential in hand gesture decoding. However, most existing decoders use long time windows, thus ignore the temporal dynamics within the period. In this study, we propose to use recurrent neural networks (RNNs) to exploit the temporal information in ECoG signals for robust hand gesture decoding. With RNN's high nonlinearity modeling ability, our method can effectively capture the temporal information in ECoG time series for robust gesture recognition. In the experiments, we decode three hand gestures using ECoG signals of two participants, and achieve an accuracy of 90%. Specially, we investigate the possibility of recognizing the gestures in a time interval as short as possible after motion onsets. Our method rapidly recognizes gestures within 0.5 s after motion onsets with an accuracy of about 80%. Experimental results also indicate that the temporal dynamics is especially informative for effective and rapid decoding of hand gestures.

14.
Environ Sci Process Impacts ; 20(7): 1020-1029, 2018 Jul 18.
Artigo em Inglês | MEDLINE | ID: mdl-29897361

RESUMO

Seven commonly utilized antidepressants (amitriptyline, fluoxetine, sertraline, citalopram, paroxetine, venlafaxine, and bupropion) and three of their metabolites were detected in four wastewater treatment plants (WWTPs) and corresponding receiving waters including the mainstream and three of the tributaries of Huangpu River, Shanghai. The concentration levels of selected antidepressants in wastewater and receiving water were both at ng L-1 level, but those antidepressants that were found in wastewater were typically in a range of one and even two orders of magnitude higher than those that were present in the receiving water except for the concentration levels of paroxetine, norfluoxetine, and nortriptyline. Venlafaxine and its metabolite O-desmethylvenlafaxine were the primary compounds (reaching up to 132.04 and 173.68 ng L-1 as well as 3.03 and 4.53 ng L-1 in wastewater and receiving water, respectively). Based on the mass loadings of selected antidepressants in four WWTPs, the mass loading of sertraline in effluent for this study was at the highest level when compared to other countries. The important finding was that the sampling sites H11 and H13 were much more likely to be polluted by side-pollution sources (the accumulation areas of Grade A of Class-three hospitals and pharmaceutical factories) than point pollution sources (WWTP 1 and WWTP2) through analysis of Spearman correlation. The results have shown that the RQs for these antidepressants were less than 0.1 except for the RQ of venlafaxine in an effluent for mollusks, which was less than 1. This indicated that the concentration levels of antidepressants would not pose a high risk for aquatic organisms, but sustained attention should still be paid.


Assuntos
Antidepressivos/análise , Antidepressivos/metabolismo , Monitoramento Ambiental/métodos , Rios/química , Águas Residuárias/análise , Poluentes Químicos da Água/análise , Antidepressivos/química , China , Águas Residuárias/química , Poluentes Químicos da Água/química
15.
Chem Biol Drug Des ; 92(2): 1419-1428, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29516624

RESUMO

Eighteen novel 2,3-diphenyl acrylonitrile derivatives bearing halogens were designed, synthesized, and evaluated for biological activity. Preliminary in vitro results indicated that the majority of the compounds with a para-substituted halogen had considerable antiproliferative activity against five human cancer cell lines, including MGC-803, AGS, and BEL-7402, with IC50 values in the range of 0.46-100 µm. No significant toxic effects on the non-cancerous human liver cell line L-02 were observed. The selective inhibitory activities against cancer cells were significantly better than that of the control lead compound CA-4 and CA-4P. Particularly, potent activities were found for the derivatives of 3-(4-halogen phenyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile, such as 5c (4-fluoro), 5f (4-bromo), 5h (4-chloro), and 5k (4-trifluoro- methyl), for AGS with IC50 values of 0.75 ± 0.24, 0.68 ± 0.21, 0.41 ± 0.05, and 1.49 ± 0.92 µm, respectively. The antiproliferative effects of 5f were attributed to cell-cycle arrest in the G2 /M phase, induction of cellular apoptosis, suppression of cell migration, and inhibition of cell colony formation in AGS cells.


Assuntos
Acrilonitrila/química , Antineoplásicos/síntese química , Halogênios/química , Acrilonitrila/síntese química , Acrilonitrila/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Humanos , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Relação Estrutura-Atividade
16.
Ecotoxicol Environ Saf ; 152: 98-103, 2018 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-29407787

RESUMO

The environmental behaviors of emerging pollutants, benzophenone-type UV filters (BP-UV filters) and their derivatives were investigated in four wastewater treatment plants (WWTPs), and their receiving surface waters in Shanghai. The concentration level of selected BP-UV filters in the WWTPs was detected from ngL-1 to µgL-1. BP (621-951ngL-1) and BP-3 (841-1.32 × 103ngL-1) were the most abundant and highest detection frequency individuals among the target BP-UV filters in influents, whereas BP (198-400ngL-1), BP-4 (93.3-288ngL-1) and BP-3 (146-258ngL-1) were predominant in effluents. BP-UV filters cannot be completely removed and the total removal efficiency varied widely (-456% to 100%) during the treatment process. It can be inferred that the usage of BP and BP-3 are higher than other BP-UV filters in the study area. The lowest and highest levels were BP-2 (ND-7.66ngL-1) and BP-3 (68.5-5.01 × 103ng L-1) in the receiving surface water, respectively. Interestingly, the seasonal variation of BP-3 is larger than those of other BP-UV filters in surface water from Shanghai. There is no obvious pollution pattern of BP-UV filters in the surface water from the cosmetic factory area. The correlation analysis of BP-UV filters between WWTPs effluents and nearby downstream water samples suggested that BP-UV filters emitted from some WWTPs might be the main source of receiving surface water. Preliminary risk assessment indicated that the levels of BP-UV filters detected by the effluent posed medium to high risk to fish as well as other aquatic organisms.


Assuntos
Benzofenonas/análise , Monitoramento Ambiental/métodos , Protetores Solares/análise , Poluentes Químicos da Água/análise , Purificação da Água/métodos , Animais , Organismos Aquáticos/efeitos dos fármacos , China , Medição de Risco , Rios/química , Estações do Ano , Águas Residuárias/análise
17.
J Enzyme Inhib Med Chem ; 32(1): 1111-1119, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28791908

RESUMO

A new series of novel 7-hydroxy-4-phenylchromen-2-one (1a)-linked 1,2,4-triazoles were synthesised using a click chemistry approach. All derivatives were subjected to 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazolium bromide (MTT) cytotoxicity screening against a panel of six different human cancer cell lines (AGS, MGC-803, HCT-116, A-549, HepG2, and HeLa) to assess their cytotoxic potential. Among the tested molecules, some of the analogues showed better cytotoxic activity than that shown by the 7-hydroxy-4-phenylchromen-2-one (1a). Of the synthesised 1,2,4-triazoles,the 7-((4-(4-Chlorophenyl)-4H-1,2,4-triazol-3-yl)methoxy)-4-phenyl-2H-chromen-2-one (4d) showed the best activity, with an IC50 of 2.63 ± 0.17 µM against AGS cells. Further flow cytometry assays demonstrated that compound 4d exerts its antiproliferative effects by arresting cells in the G2/M phase of the cell cycle and by inducing apoptosis. Collectively, our results indicate that the 1,2,4-triazole derivatives have a significantly stronger antitumour activity than 1,2,3-triazole derivatives. Most of the compounds exhibited better antitumour activity than the positive control drug 5-fluorouracil.


Assuntos
Antineoplásicos/farmacologia , Cumarínicos/farmacologia , Citotoxinas/farmacologia , Triazóis/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cumarínicos/química , Citotoxinas/síntese química , Citotoxinas/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/química
18.
Molecules ; 22(9)2017 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-28841191

RESUMO

Natural products from the genus Euphorbia show attention-attracting activities, such as anticancer activity. In this article, classical isolation and structure identification were used in a study on Caper Euphorbia Seed. Subsequently, MTT and wound healing assays, flow cytometry, western blotting, Hoechst 33258 staining and fluorescence microscopy examination were applied to investigate the anticancer activity of the obtained compounds. In a result, lathyrol-3-phenyl- acetate-5,15-diacetate (deoxy Euphorbia factor L1, DEFL1) was isolated from Caper Euphorbia Seed. Moreover, the NMR signals were totally assigned. DEFL1 showed potent inhibition against lung cancer A549 cells, with an IC50 value of 17.51 ± 0.85 µM. Furthermore, DEFL1 suppressed wound healing of A549 cells in a concentration-dependent manner. Mechanically, DEFL1 induced apoptosis, with involvement of an increase of reactive oxygen species (ROS), decrease of mitochondrial membrane potential (ΔΨm), release of cytochrome c, activity raise of caspase-9 and 3. Characteristic features of apoptosis were observed by fluorescence microscopy. In summary, DEFL1 inhibited growth and induced apoptosis in lung cancer A549 cells via a mitochondrial pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Euphorbia/química , Células A549 , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocromos c/metabolismo , Células HCT116 , Humanos , Células KB , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/fisiologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Sementes/química
19.
Methods Mol Biol ; 1530: 63-97, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28150196

RESUMO

Proteolysis has many important roles in physiological regulation. It is involved in numerous cell signaling processes and the pathogenesis of many diseases, including cancers. Methods of visualizing and assaying proteolytic activity are therefore in demand. Förster resonance energy transfer (FRET) probes offer several advantages in this respect. FRET supports end-point or real-time measurements, does not require washing or separation steps, and can be implemented in various assay or imaging formats. In this chapter, we describe methodology for preparing self-assembled concentric FRET (cFRET) probes for multiplexed tracking and imaging of proteolytic activity. The cFRET probe comprises a green-emitting semiconductor quantum dot (QD) conjugated with multiple copies of two different peptide substrates for two target proteases. The peptide substrates are labeled with different fluorescent dyes, Alexa Fluor 555 and Alexa Fluor 647, and FRET occurs between the QD and both dyes, as well as between the two dyes. This design enables a single QD probe to track the activity of two proteases simultaneously. Fundamental cFRET theory is presented, and procedures for using the cFRET probe for quantitative measurement of the activity of two model proteases are given, including calibration, fluorescence plate reader or microscope imaging assays, and data analysis. Sufficient detail is provided for other researchers to adapt this method to their specific requirements and proteolytic systems of interest.


Assuntos
Transferência Ressonante de Energia de Fluorescência , Imagem Molecular , Sondas Moleculares , Pontos Quânticos , Transferência Ressonante de Energia de Fluorescência/métodos , Cinética , Medições Luminescentes/métodos , Microscopia/métodos , Peptídeo Hidrolases/metabolismo , Peptídeos/química , Peptídeos/metabolismo , Proteólise
20.
Ther Clin Risk Manag ; 12: 1545-1551, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27785042

RESUMO

BACKGROUND: Fever of unknown origin (FUO) has always been a challenging problem for physicians since it was first reported half a century ago. This study aimed to investigate the clinical features of FUO and to compare the clinical significance of the classical diagnostic criteria and the Chinese revised diagnostic criteria of FUO. METHODS: We retrospectively collected a series of 140 patients admitted to our hospital between September 2011 and June 2013 because of prolonged febrile illnesses (lasting at least 2 weeks, temperature ≥38.5°C) without diagnosis and categorized them into two groups according to the Chinese revised diagnostic criteria (group A) and classical diagnostic criteria (group B) for FUO. The A group included patients presenting with fever persisting between 2 and 3 weeks with the diagnosis remaining uncertain after three outpatient visits or at least 3 days of hospital investigation. The B group included patients presenting with fever persisting for more than 3 weeks with no established diagnosis after 1 week of hospital investigation. The general conditions, etiologies, definite diagnosis times, and diagnostic methods of the two groups were compared. RESULTS: There were no significant differences in the general conditions, etiologies, definite diagnosis times, and diagnostic methods between the Chinese revised diagnostic criteria and classical diagnostic criteria. CONCLUSION: Both the examined FUO diagnostic criteria are suitable for clinical practice in this region.

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