RESUMEN
A new compound, ethyl 5-phenyl-2-(p-tolyl)-2H-1,2,3-triazole-4-carboxylate was successfully introduced and synthesized as a novel rhodamine B derivative named REPPC, and characterized by 1 H nuclear magnetic resonance (NMR), 13 C NMR, and high resolution mass spectrometry (HRMS). It showed an obvious fluorescence and UV-visible light absorption enhancement towards Hg2+ ion without interference from common metal ions in N,N-dimethylformamide-H2 O (pH 7.4). The spirolactam ring moiety of rhodamine in REPPC was converted to the open-ring form generating a 1:1 complex with the intervention of a mercury ion, verified by electrospray ionization-mass spectroscopy testing and density functional theory calculation. REPPC was used to visualize the level of mercury ions in living HeLa cells with encouraging results.
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Colorantes Fluorescentes/química , Mercurio/análisis , Imagen Óptica , Triazoles/química , Colorantes Fluorescentes/síntesis química , Células HeLa , Humanos , Concentración de Iones de Hidrógeno , Iones/análisis , Estructura Molecular , Espectrometría de Fluorescencia , Triazoles/síntesis químicaRESUMEN
A polysaccharide (MPS) isolated from Cristaria plicata (Leach) consisted of d-glucose. Its structural characteristics were investigated by High Performance Liquid Chromatography (HPLC), infrared analysis, gas chromatography-MS, total acid hydrolysis, methylation analysis, periodate oxidation and Smith degradation. The results indicated that the polysaccharide of C. plicata (Leach) has the weight-average molecular weight of about 2.97 × 106 Da. The structure of the polysaccharide was composed of glucose with α-(1 â 4)-linkages with short exterior chains. The fundamental information obtained from this work is beneficial to the interpretation in the relationship of the polysaccharide structure and its biological functions, and suggests that the polysaccharide from mussel may contribute to be used as a dietary supplement for health foods and therapeutics.
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Glucosa/análisis , Polisacáridos/química , Unionidae/química , Animales , Suplementos Dietéticos , Estructura Molecular , Peso Molecular , Polisacáridos/aislamiento & purificaciónRESUMEN
Proton pump inhibitors use increases hepatic encephalopathy risk in patients with liver disease.
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Encefalopatía Hepática/inducido químicamente , Hepatopatías/complicaciones , Hepatopatías/tratamiento farmacológico , Metaanálisis como Asunto , Inhibidores de la Bomba de Protones/efectos adversos , Humanos , RiesgoRESUMEN
PURPOSE: Liver metastasis is the final stage of cancer progression and is associated with poor prognosis. Although numerous indicators have been identified as having prognostic value for lung cancer and liver metastasis, liver metastases are still not diagnosed by imaging in many patients. To provide a more accurate method for clinical prediction of liver metastasis, we analyzed multiple factors to identify potential predictive factors for liver metastasis of lung cancer. METHODS: Patients first diagnosed with lung cancer between 2002 and 2016 (n = 1746) were divided into two groups, with and without liver metastasis. Serum concentrations of calcium, carcinoembryonic antigen (CEA), cancer antigen-125 (CA125), cancer antigen-153 (CA153), carbohydrate antigen-199 (CA199), cytokeratin fraction 21-1 (CYFRA21-1), total prostate-specific antigen (TPSA), and neuron-specific enolase (NSE) were analyzed in both patient groups. RESULTS: There was no significant difference in age or sex between the two groups. CA125 and NSE were significantly associated with liver metastasis. Compared with CA125, NSE was more specific, while it was less sensitive (P < 0.001). Further analysis of NSE concentrations was conducted in patients with non-small-cell lung cancer and indicated that NSE concentration differed significantly between those with and without liver metastasis (P = 0.023). We conducted analysis with NSE and CA125 combined, resulting in acceptable sensitivity (51.2%), specificity (72.6%), and area under the curve (0.64) values; sensitivity and area under the curve values were higher than those for individual factors, while specificity was higher than that for CA125. CONCLUSIONS: The combination of CA125 and NSE can assist prediction of liver metastasis of lung cancer, providing improved diagnostic accuracy.
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Biomarcadores de Tumor/sangre , Antígeno Ca-125/sangre , Neoplasias Hepáticas/diagnóstico , Neoplasias Hepáticas/secundario , Neoplasias Pulmonares/patología , Fosfopiruvato Hidratasa/sangre , Anciano , Antígenos de Neoplasias/sangre , Antígeno Carcinoembrionario/sangre , Femenino , Proteínas Ligadas a GPI/sangre , Humanos , Queratina-19/sangre , Masculino , Persona de Mediana Edad , PronósticoRESUMEN
AIM: To use the voxel-wise degree centrality (DC) method to explore the underlying functional network brain-activity in patients with ophthalmectomy. METHODS: A total of 32 ophthalmic surgery patients (10 women and 22 men), and 32 healthy subjects (10 women and 22 men) highly matched in gender, age, and the same operation method. Everyone experienced a resting-state functional magnetic resonance imaging scan. The spontaneous brain activity could be assessed by DC. Correlation analysis was used to explore the relationships between the average DC signal values and behavior performance in different regions. Receiver operating characteristic (ROC) curve analysis was utilized to differentiate between ophthalmectomy patients and healthy controls (HCs). RESULTS: Compared with HCs, ophthalmectomy patients had greatly reduced DC values in left lingual gyrus, bilateral lingual lobe, left cingulate gyrus, and increased DC values of left cerebellum posterior lobe, left middle frontal gyrus1, right supramarginal gyrus, left middle frontal gyrus2, right middle frontal gyrus. However, we did not find that there was a correlation between the average DC values from various brain regions and clinical manifestations. CONCLUSION: Dysfunction may be caused by ophthalmectomy in lots of cerebral areas, which may show the potential pathological mechanism of ophthalmectomy and it is beneficial to clinical diagnosis.
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One known bis-indole alkaloid-voacamine was isolated from Voacanga africana Stapf and Surface Plasmon Resonance imaging (SPRi) exprement showed that this alkaloid could be combine with Protein Tyrosine Phosphatase1B (PTP1B). Then the PTP1B activity inhibition experiment display that the compound showed an outstanding promoting activity to PTP1B.
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Ibogaína/análogos & derivados , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Resonancia por Plasmón de Superficie/métodos , Voacanga/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Humanos , Ibogaína/aislamiento & purificación , IndolesRESUMEN
AIM: To determine typical corneal changes of congenital aniridic keratopathy (CAK) using corneal topography and confocal systems, and to identify characteristics that might assist in early diagnosis. METHODS: Patients with CAK and healthy control subjects underwent detailed ophthalmic examinations including axial length, corneal thickness, tear film condition, corneal topography, and laser-scanning in vivo confocal microscopy (IVCM). RESULTS: In early stage aniridic keratopathy, Schirmer I test (SIT), break-up time (BUT), mean keratometry (mean K) and simulated keratometry (sim K) were reduced relative to controls (P<0.05), while simulation of corneal astigmatism (sim A) and corneal thickness were increased (P<0.05). In addition, significantly more eyes exhibited flat cornea compared with the control group. Inflammatory dendritic cells were present in the aniridic epithelium, with significantly increased density relative to controls (P<0.05). Palisade ridge-like features and abnormal cell morphology were observed in six out of sixteen CAK cases. In central cornea area, the aniridic corneas had the increased subbasal nerve density. CONCLUSION: These changes in corneal morphology in borderline situations can be useful to confirm the diagnosis of CAK.
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AIM: To compare the effectiveness of combined fenofibrate and spironolactone with fenofibrate alone for treatment of central serous chorioretinopathy (CSCR). METHODS: Totally 60 patients (60 eyes) with a history of acute CSCR were randomed into two groups: group A with combination of fenofibrate (200 mg) and spironolactone (100 mg), and group B with only fenofibrate (200 mg). They were taken half an hour before meals and once per day for 8wk. The changes of the visual acuity, subjective symptom, ocular surface disease index (OSDI), the tear film and optical coherence tomography were observed at 2, 4, 6, and 8wk before and after treatment. RESULTS: The best corrected visual acuity (BCVA, logMAR) was improved to 0.22 and 0.27 after treatment from baseline of 0.35 and 0.36 in groups A and B (P<0.05), respectively. After 8wk treatment, the central subfield thickness (CST), and subretinal fluid volumn (SFV) decreased significantly to 49.5% and 78.8% in group A and 37.0% and 57.2% in group B. There were significant differences of CST and SFV in both groups (all P<0.05). CONCLUSION: Fenofibrate combined with spironolactone may have more clinical efficacy in the treatment of CSCR than fenofibrate only.
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An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.
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Pirimidinas/farmacología , Receptores de Interleucina-8B/antagonistas & inhibidores , Administración Oral , Animales , Células CHO , Cricetinae , Humanos , Pruebas de Sensibilidad Microbiana , Pirimidinas/administración & dosificación , Pirimidinas/farmacocinética , Proteínas Recombinantes/antagonistas & inhibidoresRESUMEN
Many naturally occurring peptide acids, e.g., somatostatins, conotoxins, and defensins, contain a cysteine residue at the C-terminus. Furthermore, installation of C-terminal cysteine onto epitopic peptide sequences as a preliminary to conjugating such structures to carrier proteins is a valuable tactic for antibody preparation. Anchoring of N(alpha)-Fmoc, S-protected C-terminal cysteine as an ester onto the support for solid-phase peptide synthesis is known to sometimes occur in low yields, has attendant risks of racemization, and may also result in conversion to a C-terminal 3-(1-piperidinyl)alanine residue as the peptide chain grows by Fmoc chemistry. These problems are documented for several current strategies, but can be circumvented by the title anchoring strategy, which features the following: (a). conversion of the eventual C-terminal cysteine residue, with Fmoc for N(alpha)-amino protection and tert-butyl for C(alpha)-carboxyl protection, to a corresponding S-xanthenyl ((2)XAL(4)) preformed handle derivative; and (b). attachment of the resultant preformed handle to amino-containing supports. This approach uses key intermediates that are similar to previously reported Fmoc-XAL handles, and builds on earlier experience with Xan and related protection for cysteine. Implementation of this strategy is documented here with syntheses of three small model peptides, as well as the tetradecapeptide somatostatin. Anchoring occurs without racemization, and the absence of 3-(1-piperidinyl)alanine formation is inferred by retention of chains on the support throughout the cycles of Fmoc chemistry. Fully deprotected peptides, including free sulfhydryl peptides, are released from the support in excellent yield by using cocktails containing a high concentration (i.e., 80-90%) of TFA plus appropriate thiols or silanes as scavengers. High-yield release of partially protected peptides is achieved by treatment with cocktails containing a low concentration (i.e., 1-5%) of TFA. In peptides with two cysteine residues, the corresponding intramolecular disulfide-bridged peptide is obtained by either (a). oxidation, in solution, of the dithiol product released by acid; (b). simultaneous acidolytic cleavage and disulfide formation, achieved by addition of the mild oxidant DMSO to the cleavage cocktail; or (c). concomitant cleavage/cooxidation (involving a downstream S-Xan protected cysteine), using reagents such as iodine or thallium tris(trifluoroacetate) in acetic acid.