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1.
BMC Pediatr ; 23(1): 323, 2023 06 24.
Artigo em Inglês | MEDLINE | ID: mdl-37355569

RESUMO

BACKGROUND/AIMS: To investigate the clinical situation, treatment methods, and clinical predictors of surgical intervention in children with magnetic foreign bodies in the digestive tract. MATERIALS AND METHODS: From January 2019 to June 2022, we retrospectively analyzed the clinical data of 72 children who ingested magnetic foreign bodies inadvertently in our hospital, including their general information, admissions, clinical manifestations, and treatment methods, as well as pertinent literature and statistical data. Following software processing, univariate and multivariate logistic regression analyses were conducted to determine the independent risk factors of this study. RESULTS: In this study, 16 patients (22.2%) were discharged smoothly following conservative treatment and 19 patients (26.4%) were cured by gastroscopy. The remaining 37 patients (51.4%) were underwent surgery, in which 26 cases developed gastrointestinal perforation. There were statistical differences between surgery group and non- surgery group in the days of eating by mistake, clinical manifestations (nausea and vomiting, intermittent abdominal pain, abdominal muscle tension) and movement trajectory by every 24-h radiograph (P < 0.01). Logistic regression analysis showed that intermittent abdominal pain and abdominal muscle tension were independent risk factors for surgical treatment. CONCLUSION: Magnetic foreign bodies seriously endanger children's health. This study offers a single-center basis for the choice of surgical opportunity for intestinal obstruction or perforation caused by magnetic foreign bodies. Clinicians need immediate surgical intervention if the child shows symptoms of abdominal pain or abdominal tension.


Assuntos
Corpos Estranhos , Trato Gastrointestinal , Criança , Humanos , Estudos Retrospectivos , Dor Abdominal/etiologia , Corpos Estranhos/diagnóstico por imagem , Corpos Estranhos/cirurgia , Fenômenos Magnéticos
2.
Light Sci Appl ; 11(1): 235, 2022 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-35882840

RESUMO

The light-matter interaction between plasmonic nanocavity and exciton at the sub-diffraction limit is a central research field in nanophotonics. Here, we demonstrated the vertical distribution of the light-matter interactions at ~1 nm spatial resolution by coupling A excitons of MoS2 and gap-mode plasmonic nanocavities. Moreover, we observed the significant photoluminescence (PL) enhancement factor reaching up to 2800 times, which is attributed to the Purcell effect and large local density of states in gap-mode plasmonic nanocavities. Meanwhile, the theoretical calculations are well reproduced and support the experimental results.

3.
Bioorg Med Chem Lett ; 21(1): 121-4, 2011 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-21144750

RESUMO

A series of N-phenylnicotinamides (1-40) were designed and evaluated in vitro for their COX inhibitory activities. Most of the synthesized compounds were proved to be potent and selective inhibitors of COX-1. Compound 28 showed the most potent COX-1 inhibitory activity (COX-1 IC(50) = 0.68 ± 0.07 µM) and good selectivity (COX-2 IC(50)>100µM). This compound may be useful as a lead compound for superior COX-1 inhibitors. On the basis of the biological results, structure-activity relationships for the COX-1-inhibitory activities of the synthesized N-phenylnicotinamides were discussed concisely.


Assuntos
Anilidas/química , Ciclo-Oxigenase 1/química , Inibidores de Ciclo-Oxigenase/química , Niacinamida/análogos & derivados , Anilidas/síntese química , Anilidas/farmacologia , Sítios de Ligação , Domínio Catalítico , Simulação por Computador , Ciclo-Oxigenase 1/metabolismo , Inibidores de Ciclo-Oxigenase/síntese química , Inibidores de Ciclo-Oxigenase/farmacologia , Desenho de Fármacos , Niacinamida/síntese química , Niacinamida/química , Niacinamida/farmacologia , Relação Estrutura-Atividade
4.
J Enzyme Inhib Med Chem ; 26(1): 37-45, 2011 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-20583855

RESUMO

A series of salicylanilide derivatives (compounds 1-32) were synthesised by reacting substituted salicylic acids and anilines. The chemical structures of these compounds were determined by (1)H-NMR, electrospray ionisation mass spectrometry (ESI-MS) and elemental analysis. The compounds were assayed for their antiproliferative activities against the Hep-G2 cell line by the 3-(4,5-dimethylthylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Among the compounds tested, 22 and 28 showed the most favouable antiproliferative activities with 50% inhibitory concentration (IC(50)) values of 1.7 and 1.3 µM, respectively, which were comparable to the positive control of 5-fluorouracil (IC(50)=1.8 µM). A solid-phase ELISA assay was also performed to evaluate the ability of compounds 1-32 to inhibit the autophosphorylation of the epidermal growth factor receptor tyrosine kinase (EGFR TK). Docking simulations of 22 and 28 were carried out to illustrate the binding mode of the molecule into the EGFR active site, and the result suggested that both compounds 22 and 28 could bind the EGFR kinase well.


Assuntos
Antineoplásicos/farmacologia , Receptores ErbB/antagonistas & inibidores , Salicilanilidas/farmacologia , Compostos de Anilina/química , Antineoplásicos/síntese química , Antineoplásicos/metabolismo , Fluoruracila/farmacologia , Células Hep G2 , Humanos , Concentração Inibidora 50 , Simulação de Dinâmica Molecular , Ressonância Magnética Nuclear Biomolecular , Fosforilação , Ligação Proteica , Salicilanilidas/síntese química , Salicilanilidas/metabolismo , Salicilatos/química , Relação Estrutura-Atividade , Sais de Tetrazólio/análise , Tiazóis/análise
5.
Transl Pediatr ; 10(12): 3237-3247, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35070838

RESUMO

BACKGROUND: Circulating RNAs (Circ-RNAs) are tightly related to the processes of neuroblastoma. The circ-ACAP2 has been reported as dysregulated in various cancers; however, its biological roles and mechanisms in neuroblastoma remain largely unclear. METHODS: We collected 40 neuroblastoma tissues and adjacent noncancerous tissues. Quantitative reverse transcription polymerase chain reaction (qRT-RCR) or western blot were used to examine ACAP2, miR-143-3p, and HK2 abundances. Cell migration, invasion, glycolysis, and apoptosis were assessed via wound healing, transwell, glucose uptake and lactate, 3-(4,5-diamethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, and flow cytometry. The association between circRNA, microRNA (miRNA), and messenger RNA (mRNA) was examined by dual-luciferase reporter analysis and RNA immunoprecipitation. RESULTS: The abundances of ACAP2 and HK2 were remarkedly increased in neuroblastoma tissues and cell lines. Silencing ACAP2 significantly constrained neuroblastoma cell migration, invasion, and glycolysis, and promoted apoptosis. Bioinformatics prediction, luciferase assay, and RNA pull-down assay consistently demonstrated that ACAP2 sponged miR-143-3p to downregulate its expression in neuroblastoma cells. Furthermore, we identified that hexokinase 2, a glycolysis key enzyme, was a direct target of miR-143-3p in neuroblastoma cells. Rescue of miR-143-3p in ACAP2-overexpressing cells effectively mitigated the influence of ACAP2 on neuroblastoma cell processes. CONCLUSIONS: Our study revealed biological roles and molecular mechanisms for circ-ACAP2 in the oncogenic characteristics of neuroblastoma, facilitating the development of circRNA-based treatment approaches for anti-brain tumor therapy.

6.
World J Clin Cases ; 9(25): 7542-7550, 2021 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-34616824

RESUMO

BACKGROUND: Congenital biliary atresia is a type of obstruction of the bile ducts inside and outside the liver, which can lead to cholestatic liver cirrhosis and eventually liver failure. The preduodenal portal vein (PD-PV) is a rare developmental malformation of the PV. The PV courses in front of the duodenum. However, very few cases of neonatal biliary atresia combined with PD-PV have been reported in the scientific literature. CASE SUMMARY: A 1-mo-and-4-d-old child was admitted to the hospital in January because of yellowish skin. After surgical consultation, surgical intervention was recommended. The child underwent Hilar-jejunal anastomosis, duodenal rhomboid anastomosis, and abdominal drainage under general anesthesia. During the operation, the PV was located at the anterior edge of the duodenum. CONCLUSION: Diagnoses: (1) Congenital biliary atresia; (2) PD-PV; and (3) Congenital cardiovascular malformations. Outcomes: Recommendation for liver transplantation. Lessons: The choice of treatment options for neonatal biliary atresia combined with PD-PV.

7.
Bioorg Med Chem Lett ; 20(22): 6653-6, 2010 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-20943391

RESUMO

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in the process of cancer angiogenesis. A series of quinoline amide derivatives were prepared and found to be good inhibitors of VEGFR-2. The inhibitory activities were investigated against VEGFR-2 kinase and human umbilical vein endothelial cells (HUVEC) in vitro. Compound 6 (5-chloro-2-hydroxy-N-(quinolin-8-yl)benzamide) exhibited the most potent inhibitory activity (IC(50)=3.8 and 5.5 nM for VEGFR-2 kinase and HUVEC, respectively). Docking simulation supported the initial pharmacophoric hypothesis and suggested a common mode of interaction at the ATP-binding site of VEGFR-2, which demonstrates that compound 6 is a potential agent for cancer therapy deserving further researching.


Assuntos
Amidas/química , Quinolinas/síntese química , Quinolinas/farmacologia , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/antagonistas & inibidores , Células Cultivadas , Desenho de Fármacos , Humanos , Concentração Inibidora 50 , Modelos Moleculares , Quinolinas/química
8.
Bioorg Med Chem ; 18(4): 1659-64, 2010 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-20117937

RESUMO

A series of N-(2-morpholinoethyl)nicotinamide (1-13) and N-(3-morpholinopropyl)nicotinamide derivatives (14-26) have been designed, synthesized and evaluated in vitro for their monoamine oxidase (MAO) A and B inhibitory activity and selectivity. Most of these synthesized compounds proved to be potent, and selective inhibitors of MAO-A rather than of MAO-B. 5-Chloro-6-hydroxy-N-(2-morpholinoethyl)nicotinamide (13) displayed the highest MAO-A inhibitory potency (IC(50)=0.045 microM) and a good selectivity. 2-Bromo-N-(2-morpholinoethyl)nicotinamide (3) was the most potent MAO-B inhibitor with the IC(50) value of 0.32 microM, but it was not selective. Molecular dockings of compound 13 were performed in order to give structural insights regarding the MAO-A selectivity.


Assuntos
Inibidores da Monoaminoxidase/química , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/efeitos dos fármacos , Niacinamida/química , Niacinamida/farmacologia , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/enzimologia , Espectroscopia de Ressonância Magnética , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/enzimologia , Modelos Moleculares , Ratos , Espectrometria de Massas por Ionização por Electrospray , Relação Estrutura-Atividade
9.
Exp Ther Med ; 15(1): 85-92, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29387183

RESUMO

Cancer stem cells (CSCs) are considered to serve a key role in tumor progression, recurrence and metastasis. Tumorsphere culture is the most important method for enriching CSCs and is widely used in basic research and drug screening. However, the traditional suspension cell culture system has several disadvantages, including low efficiency, high cost and difficult procedure, making it difficult to produce tumorspheres on a large scale. In the present study, two biomaterials, methylcellulose (MC) and gellan gum (GG), were used to construct a novel culture system based on the traditional system. Subsequently, the characteristics of the novel three-dimensional (3D) culture system were evaluated, the design scheme was optimized, and the morphological and biological features of the tumorspheres cultured in this 3D system were compared with the traditional system. The results revealed that the tumorspheres cultured in the novel 3D system presented a higher seeding density and improved morphology, while maintaining stem-like properties. This evidence suggests that a simple, efficient and low-cost culture system that produces tumorspheres on a large scale was successfully constructed, which can be widely used in various aspects of stem cell research.

10.
Eur J Med Chem ; 45(9): 4358-64, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-20557983

RESUMO

Twenty new Schiff bases were synthesized by reacting 5-fluoro-salicylaldehyde and primary amine as potent inhibitors of FabH. These compounds were assayed for antibacterial activity against Escherichia coli, Pseudomonas fluorescence, Bacillus subtilis and Staphylococcus aureus. Compounds with potent antibacterial activities were tested for their E. coli FabH inhibitory activity. (E)-4-fluoro-2-((4-hydroxyphenethylimino)methyl)phenol (10) showed the most potent antibacterial activity with MIC of 1.56-6.25 microg/mL against the tested bacterial strains and exhibited the most potent E. coli FabH inhibitory activity with IC(50) of 2.7 microM. Docking simulation was performed to position compound 10 into the E. coli FabH active site to determine the probable binding conformation.


Assuntos
3-Oxoacil-(Proteína de Transporte de Acila) Sintase/antagonistas & inibidores , Antibacterianos/síntese química , Antibacterianos/farmacologia , Desenho de Fármacos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , 3-Oxoacil-(Proteína de Transporte de Acila) Sintase/química , Aldeídos/síntese química , Aldeídos/química , Aldeídos/farmacologia , Antibacterianos/química , Domínio Catalítico , Cristalografia por Raios X , Inibidores Enzimáticos/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/enzimologia , Modelos Moleculares
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