Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 47
Filtrar
Más filtros













Base de datos
Intervalo de año de publicación
1.
Cancer Imaging ; 23(1): 55, 2023 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-37264400

RESUMEN

BACKGROUND: Lateral lymph node metastasis (LLNM) is frequent in papillary thyroid carcinoma (PTC) and is associated with a poor prognosis. This study aimed to developed a clinical-ultrasound (Clin-US) nomogram to predict LLNM in patients with PTC. METHODS: In total, 2612 PTC patients from two hospitals (H1: 1732 patients in the training cohort and 578 patients in the internal testing cohort; H2: 302 patients in the external testing cohort) were retrospectively enrolled. The associations between LLNM and preoperative clinical and sonographic characteristics were evaluated by the univariable and multivariable logistic regression analysis. The Clin-US nomogram was built basing on multivariate logistic regression analysis. The predicting performance of Clin-US nomogram was evaluated by calibration, discrimination and clinical usefulness. RESULTS: The age, gender, maximum diameter of tumor (tumor size), tumor position, internal echo, microcalcification, vascularization, mulifocality, and ratio of abutment/perimeter (A/P) > 0.25 were independently associated with LLNM metastatic status. In the multivariate analysis, gender, tumor size, mulifocality, position, microcacification, and A/P > 0.25 were independent correlative factors. Comparing the Clin-US nomogram and US features, Clin-US nomogram had the highest AUC both in the training cohort and testing cohorts. The Clin­US model revealed good discrimination between PTC with LLNM and without LLNM in the training cohort (AUC = 0.813), internal testing cohort (AUC = 0.815) and external testing cohort (AUC = 0.870). CONCLUSION: Our findings suggest that the ClinUS nomogram we newly developed can effectively predict LLNM in PTC patients and could help clinicians choose appropriate surgical procedures.


Asunto(s)
Nomogramas , Neoplasias de la Tiroides , Humanos , Cáncer Papilar Tiroideo/patología , Cáncer Papilar Tiroideo/secundario , Cáncer Papilar Tiroideo/cirugía , Neoplasias de la Tiroides/diagnóstico por imagen , Neoplasias de la Tiroides/cirugía , Metástasis Linfática/patología , Estudios Retrospectivos , Ganglios Linfáticos/diagnóstico por imagen , Ganglios Linfáticos/patología
2.
ACS Appl Mater Interfaces ; 15(6): 8022-8032, 2023 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-36723504

RESUMEN

With the high theoretical capacity and the ability of large current discharge, NiS2 has been expected as a new cathode material for thermal batteries. However, its lower decomposition temperature (∼500 °C) restricts its application on thermal batteries because of the high operating temperature of thermal batteries (500-600 °C). In this case, Cr, Fe, Co, and Cu multielement-doped NiS2 (NiS2-d) has been successfully prepared by low-temperature solid-phase sintering. Owing to the effect of high entropy, the multielement doping improved the thermodynamic system stability of NiS2, and the decomposition temperature (2NiS2 → 2NiS + S2) increased from 482 to 610 °C. Interestingly, doping also reduces the particle size of NiS2, resulting in defects on the surface of NiS2 particles and improving the conductivity of NiS2.The actual discharge capacity of NiS2 enhanced significantly from 516 to 643 mA h g-1 at 500 °C, with a current density of 100 mA cm-2 and a cut-off voltage of 1.5 V. This is due to a more complete release of the first discharge reaction (NiS2 + 2Li+ + 2e- → NiS + Li2S) as the decomposition temperature rises. The enhancement of conductivity, meanwhile, lessens polarization during the discharge process, raises the voltage of the NiS2 discharge platform, and improves the stability of the NiS2 later discharge platform. Additionally, the smaller particle size enables improved contact between the cathode and the electrolyte interface, allowing electrolyte ions to quickly come into touch with the NiS2 surface. These results show that the discharge performance of NiS2 at high temperatures could be effectively improved by multielement doping. It provides a new method for improving the stability of a metal sulfide and its application at high-temperature discharge.

3.
Pathog Dis ; 80(1)2022 11 12.
Artículo en Inglés | MEDLINE | ID: mdl-36316012

RESUMEN

Malaria, a mosquito-borne infectious disease, is caused by the unicellular apicomplexan protozoa of the genus Plasmodium. For malaria parasite transmission, the essential sexual stage includes production of gametocytes through gametocytogenesis in vertebrate hosts and formation of gametes from gametocytes through gametogenesis in mosquito vectors. Whereas each female gametocyte forms a single immotile macrogamete, a male gametocyte produces eight flagella-like microgametes in a process called exflagellation. We identified a conserved protein named as Py05543 (Pyp25α), required for male gametocyte exflagellation in Plasmodium yoelii, which is the ortholog of PFL1770c (PF3D7_1236600). Interestingly, PF3D7_1236600 was previously phenotypically screened to be gametocyte-essential genes during gametocytogenesis of Plasmodium falciparum, using piggyBac transposon-mediated insertional mutagenesis. In this study, using CRISPR/Cas9-mediated genome editing, the Pyp25α¯ (KO) parasite line was successfully established. We found that the KO parasites proliferated asexually in mouse blood normally. In addition, compared with that of the parental parasites, the KO parasites displayed similar levels of gametocytes formation. Unexpectedly, the KO parasites showed considerable deficiency in exflagellation of male gametes, by observing exflagellation centre formation. Taken together, our data suggested that Pyp25α gene, the ortholog of PF3D7_1236600, was nonessential for the growth of asexual parasites, required for male gametocyte exflagellation in P. yoelii.


Asunto(s)
Malaria , Plasmodium falciparum , Ratones , Animales , Masculino , Femenino , Gametogénesis/genética , Flagelos , Mutagénesis Insercional
4.
Front Pediatr ; 9: 713588, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34616698

RESUMEN

There have been good amounts of population pharmacokinetics (PPK) models of vancomycin for Chinese pediatric patients, but none of them had a special focus on modeling infant population with different levels of renal function. Since renal function variability is prominent among infant population and the clearance (CL) of vancomycin is heavily related to renal excretion, it is important to establish precise PPK models based on individual renal function levels. We employed a PPK approach to develop three models of vancomycin in parallel for Chinese pediatric patients with normal renal function [estimated glomerular filtration rate (eGFR) between 30 and 86 ml/min/1.73 m2, Model 1], with augmented renal function (eGFR ≥ 86 ml/min/1.73 m2, Model 2), or with all levels of renal function (Model 3). Three one-compartment models with first-order elimination kinetics were established. The predictive ability of Model 1 and Model 2 among each certain population is comparable with that of Model 3 with no statistical difference. Our study revealed that among the infant population with augmented renal function, only body weight was included as a covariate, which indicated that for an infant whose eGFR ≥ 86 ml/min/1.73 m2, taking blood sample is not compulsory for predicting vancomycin blood concentration, which avoids unnecessary injury to vulnerable infants.

5.
Int Immunopharmacol ; 98: 107827, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34284341

RESUMEN

The population pharmacokinetics (PPK) of tacrolimus (TAC) in children with refractory nephrotic syndrome (RNS) have not been well-characterized. This study aimed to investigate the significant factors affecting the TAC PPK characteristics of children with RNS and to optimize the dosing regimen. A total of 494 concentrations from 108 children were obtained from routine therapeutic drug monitoring between 2016 and 2018. Information regarding the demographic features, laboratory test results, genetic polymorphisms of CYP3A5 (rs776746) and co-therapy medications were collected. PPK analysis was performed using the nonlinear mixed-effects modelling (NONMEM) software and two modelling strategies (the linear one-compartment model and nonlinear Michaelis-Menten model) were evaluated and compared. CYP3A5 genotype, weight, daily dose of TAC and daily dose of diltiazem were retained in the final linear model. The absorption rate constant (Ka) was set at 4.48 h-1 in the linear model, and the apparent clearance (CL/F) and volume of distribution (V/F) in the final linear model were 14.2 L/h and 172 L, respectively. CYP3A5 genotype, weight and daily dose of diltiazem were the significant factors retained in the final nonlinear model. The maximal dose rate (Vmax) and the average steady-state concentration at half-Vmax (Km) in the final nonlinear model were 2.15 mg/day and 0.845 ng/ml, respectively. The nonlinear model described the pharmacokinetic data of TAC better than the linear model in children with RNS. A dosing regimen was proposed based on weight, CYP3A5 genotype and daily dose of diltiazem according to the final nonlinear PK model, which may facilitate individualized drug therapy with TAC.


Asunto(s)
Inmunosupresores/administración & dosificación , Modelos Biológicos , Síndrome Nefrótico/tratamiento farmacológico , Tacrolimus/administración & dosificación , Adolescente , Niño , Preescolar , Citocromo P-450 CYP3A/genética , Citocromo P-450 CYP3A/metabolismo , Diltiazem/administración & dosificación , Diltiazem/farmacocinética , Cálculo de Dosificación de Drogas , Monitoreo de Drogas/métodos , Resistencia a Medicamentos , Femenino , Humanos , Inmunosupresores/farmacocinética , Masculino , Síndrome Nefrótico/sangre , Síndrome Nefrótico/genética , Síndrome Nefrótico/inmunología , Dinámicas no Lineales , Variantes Farmacogenómicas , Polimorfismo de Nucleótido Simple , Medicina de Precisión/métodos , Estudios Retrospectivos , Tacrolimus/farmacocinética
6.
Neurotoxicology ; 81: 161-171, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-33053366

RESUMEN

Vincristine (VCR), an alkaloid extracted from vinca, is often used in combination with other chemotherapeutic drugs to treat a variety of cancers, such as acute lymphoblastic leukaemia (ALL), malignant lymphoma, and neuroblastoma. However, VCR possesses dose-dependent neurotoxicity, which is the main factor restricting its application. Vincristine-induced peripheral neuropathy (VIPN) not only limits the dose of VCR and leads to the discontinuation of treatment but also triggers serious damage to the physical and mental health of patients. In addition, VIPN brings huge healthcare costs to patients and society. Individuals with VIPN often exhibit mechanical allodynia, sensory/tactile disorders, and numbness in the hands and feet. Unfortunately, VIPN is easily ignored due to its variable symptoms, which gives rise to insufficient research on the aetiology and pathogenesis of this disease, thereby resulting in a lack of appropriate preventive and therapeutic management. We performed a comprehensive review of the latest findings on VIPN in terms of symptoms, risk factors, potential mechanisms, and prevention and treatment measures. The purpose was to help clinicians better understand and accurately diagnose VIPN, select appropriate intervention measures and reduce the damage to cancer patients.


Asunto(s)
Antineoplásicos Fitogénicos/efectos adversos , Síndromes de Neurotoxicidad/etiología , Nervios Periféricos/efectos de los fármacos , Enfermedades del Sistema Nervioso Periférico/inducido químicamente , Vincristina/efectos adversos , Animales , Humanos , Síndromes de Neurotoxicidad/metabolismo , Síndromes de Neurotoxicidad/patología , Síndromes de Neurotoxicidad/fisiopatología , Nervios Periféricos/metabolismo , Nervios Periféricos/patología , Nervios Periféricos/fisiopatología , Enfermedades del Sistema Nervioso Periférico/metabolismo , Enfermedades del Sistema Nervioso Periférico/patología , Enfermedades del Sistema Nervioso Periférico/fisiopatología , Medición de Riesgo , Factores de Riesgo
7.
Water Res ; 184: 116157, 2020 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-32679343

RESUMEN

There is growing pressure for wastewater treatment plants to mitigate the discharge of antibiotic resistant bacteria (ARB) and extracellular resistance genes (eARGs), which requires technological innovation. Here, hierarchical Bi2O2CO3 microspheres were wrapped with nitrogen-doped, reduced graphene oxide (NRGO) for enhanced inactivation of multidrug-resistant E. coli NDM-1 and degradation of the plasmid-encoded ARG (blaNDM-1) in secondary effluent. The NRGO shell enhanced reactive oxygen species (ROS) generation (•OH and H2O2) by about three-fold, which was ascribed to broadened light absorption region (red-shifted up to 459 nm) and decreased electron-transfer time (from 55.3 to 19.8 ns). Wrapping enhanced E. coli adsorption near photocatalytic sites to minimize ROS scavenging by background constituents, which contributed to the NRGO-wrapped microspheres significantly outperforming commercial TiO2 photocatalyst. ROS scavenger tests indicated that wrapping also changed the primary inactivation pathway, with photogenerated electron holes and surface-attached hydroxyl radicals becoming the predominant oxidizing species with wrapped microspheres, versus free ROS (e.g., •OH, H2O2 and •O2-) for bare microspheres. Formation of resistance plasmid-composited microsphere complexes, primary due to the π-π stacking and hydrogen bonding between the shell and nucleotides, also minimized ROS scavenging and kept free plasmid concentrations below 102 copies/mL. As proof-of-concept, this work offers promising insight into the utilization of NRGO-wrapped microspheres for mitigating antibiotic resistance propagation in the environment.


Asunto(s)
Antibacterianos , Escherichia coli , Adsorción , Antagonistas de Receptores de Angiotensina , Inhibidores de la Enzima Convertidora de Angiotensina , Antibacterianos/farmacología , Bacterias , Escherichia coli/genética , Grafito , Peróxido de Hidrógeno
8.
ACS Appl Mater Interfaces ; 12(31): 34755-34762, 2020 Aug 05.
Artículo en Inglés | MEDLINE | ID: mdl-32648734

RESUMEN

Two-dimensional (2D) nanomaterials possessing a unique sheet structure, compared to correlative bulk materials, exhibit excellent properties, especially in the energy storage and energy conversion field. In this case, NiCl2 nanosheets with thicknesses of 2-8 nm are first prepared by a simple chemical vapor deposition method. For the Li-B/LiF-LiCl-LiBr/NiCl2 thermal battery, the specific energy of NiCl2 nanosheets increases from 510 W h kg-1 (NiCl2 rods) to 616 W h kg-1 at an operation temperature of 500 °C and a current density of 0.2 A cm-2. The 2D morphology and large numbers of defects not only improve the redox reaction rates and the lithium storage capacity, but also enhance the adsorption capacity with the flake-like binder MgO, which prolong the discharge time by suppressing the discharge product diffusion to the electrolyte. These results indicate that NiCl2 nanosheets have a great possibility to become a desirable candidate of cathode materials for assisting in the development of high energy output and provide a new way to restrain the immersion between the electrode and electrolyte.

9.
J Hazard Mater ; 384: 121275, 2020 02 15.
Artículo en Inglés | MEDLINE | ID: mdl-31586914

RESUMEN

Photocatalytic degradation is considered as a promising strategy to address the environmental threat caused by antibiotics abuse. Visible light driven g-C3N4 decorated ZrO2-x nanotubes heterostructure photocatalysts for antibiotic degradation were successfully synthesized by anodic oxidation and following a thermal vapor deposition method. Compared with pure g-C3N4 or ZrO2-x nanotubes, the composite photocatalysts exhibited more extended visible light response and higher separation rate of photo-generated electron-holes pairs. The optimized heteroctructure with 7.1 wt.% g-C3N4 exhibited 90.6% degradation of tetracycline hydrochloride (TC-H) under 1 h visible light irradiation. The mainly active species of TC-H degradation were photo-generated h+ and O2-. The pathway of charge migration in the g-C3N4/ZrO2-x NTs system was also studied and a possible photocatalytic mechanism was proposed for TC-H degradation. Constructing the g-C3N4/ZrO2-x nanotubes heterostructure is anticipated to be an effective strategy for photocatalytic degradation of antibiotics.


Asunto(s)
Antibacterianos/química , Nanotubos/química , Tetraciclina/química , Eliminación de Residuos Líquidos/métodos , Contaminantes Químicos del Agua/química , Catálisis/efectos de la radiación , Grafito/química , Grafito/efectos de la radiación , Luz , Nanotubos/efectos de la radiación , Compuestos de Nitrógeno/química , Compuestos de Nitrógeno/efectos de la radiación , Oxidación-Reducción , Circonio/química , Circonio/efectos de la radiación
10.
Am J Physiol Renal Physiol ; 317(6): F1430-F1438, 2019 12 01.
Artículo en Inglés | MEDLINE | ID: mdl-31545926

RESUMEN

Renal fibrosis is a key pathological phenomenon of chronic kidney disease (CKD) contributing to the progressive loss of renal function. UK383,367 is a procollagen C proteinase inhibitor that has been selected as a candidate for dermal antiscarring agents, whereas its role in renal fibrosis is unclear. In the present study, UK383,367 was applied to a CKD mouse model of unilateral ureteral obstruction (UUO) and cell lines of renal tubular epithelial cells (mouse proximal tubular cells) and renal fibroblast cells (NRK-49F cells) challenged by transforming growth factor-ß1. In vivo, bone morphogenetic protein 1, the target of UK383,367, was significantly enhanced in UUO mouse kidneys and renal biopsies from patients with CKD. Strikingly, UK383,367 administration ameliorated tubulointerstitial fibrosis as shown by Masson's trichrome staining in line with the blocked expression of collagen type I/III, fibronectin, and α-smooth muscle actin in the kidneys from UUO mice. Similarly, the enhanced inflammatory factors in obstructed kidneys were also blunted. In vitro, UK383,367 pretreatment inhibited the induction of collagen type I/III, fibronectin, and α-smooth muscle actin in both mouse proximal tubular cells and NRK-49F cells treated with transforming growth factor-ß1. Taken together, these findings indicate that the bone morphogenetic protein 1 inhibitor UK383,367 could serve as a potential drug in antagonizing CKD renal fibrosis by acting on the maturation and deposition of collagen and the subsequent profibrotic response and inflammation.


Asunto(s)
Proteína Morfogenética Ósea 1/antagonistas & inhibidores , Oxadiazoles/uso terapéutico , Fármacos Renales/uso terapéutico , Insuficiencia Renal Crónica/tratamiento farmacológico , Animales , Línea Celular , Niño , Preescolar , Colágeno Tipo I/antagonistas & inhibidores , Colágeno Tipo I/biosíntesis , Colágeno Tipo III/antagonistas & inhibidores , Colágeno Tipo III/biosíntesis , Femenino , Fibronectinas/antagonistas & inhibidores , Fibronectinas/biosíntesis , Fibrosis/tratamiento farmacológico , Humanos , Inflamación/patología , Inflamación/prevención & control , Riñón/patología , Pruebas de Función Renal , Masculino , Ratones , Ratones Endogámicos C57BL , Insuficiencia Renal Crónica/complicaciones , Insuficiencia Renal Crónica/patología , Obstrucción Ureteral/complicaciones
11.
Bioorg Med Chem Lett ; 29(14): 1859-1863, 2019 07 15.
Artículo en Inglés | MEDLINE | ID: mdl-31103446

RESUMEN

In this work, a series of novel benzimidazole derivatives were designed and synthesized as Pin1 inhibitors. Protease-coupled assay was used to investigate the Pin1 inhibitory potency of all synthesized compounds. Thirteen of them showed preferable Pin1 inhibitory effects with IC50 values lower than 5 µM, and 12a, 15b, 15d and 16c exhibited the most promising Pin1 inhibitory activity at low micromolar level (0.33-1.00 µM) than the positive control compound Juglone. Flow cytometry results showed that treating PC-3 cells with 16c caused slight cycle arrest in a concentration-dependent manner. The structure-activity relationships of R1, R2, R3 and linker of the benzimidazole derivatives were analyzed in detail, which would help further exploration of new Pin1 inhibitors.


Asunto(s)
Antineoplásicos/farmacología , Bencimidazoles/farmacología , Inhibidores Enzimáticos/farmacología , Peptidilprolil Isomerasa de Interacción con NIMA/antagonistas & inhibidores , Antineoplásicos/síntesis química , Antineoplásicos/metabolismo , Bencimidazoles/síntesis química , Bencimidazoles/metabolismo , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Diseño de Fármacos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/metabolismo , Humanos , Simulación del Acoplamiento Molecular , Estructura Molecular , Peptidilprolil Isomerasa de Interacción con NIMA/metabolismo , Unión Proteica , Relación Estructura-Actividad
12.
Biomed Pharmacother ; 112: 108704, 2019 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-30818140

RESUMEN

Acetaminophen (APAP) overdose causes acute liver injury and leads to fatal liver damage. However, the therapies are quite limited. Shikonin is a natural product with antioxidant and anti-inflammatory activities. In the present study, the hepatoprotective effects and the underlying mechanisms of shikonin in APAP-induced hepatotoxicity in vivo and in vitro were investigated. APAP-induced acute liver injury and shikonin pretreatment models were established in vivo and in vitro, as evidenced by serum hepatic enzymes, histological changes, oxidative stress indicators and proinflammatory cytokines. The results revealed that shikonin pretreatment prevented the elevation of serum alanine transaminase (ALT), aspartate transaminase (AST) and lactate dehydrogenase (LDH) levels and markedly reduced APAP-induced histological alterations in liver tissues. Additionally, shikonin restored superoxide dismutase (SOD) expression and glutathione (GSH) content in line with the blockade of oxidative stress. The changes in gene expression involved in oxidative stress including methionine sulfoxide reductase (such as MsrA and MsrB1), heme oxygenase-1 (HO-1), SOD2 and cytochrome P450 2E1 (CYP2E1), were markedly reversed after shikonin therapy. Furthermore, shikonin markedly attenuated the APAP-induced production of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1ß (IL-1ß) and suppressed the expression of genes related to inflammation. In AML-12 cells, shikonin pretreatment decreased APAP-induced cytotoxicity as measured by CCK-8 assay and LDH release. The changes in gene expression involved in oxidative stress and the inflammatory response were consistent with those in mouse livers. This study indicated that shikonin attenuated APAP-induced acute liver injury via inhibiting oxidative stress and inflammatory responses in vivo and in vitro. These findings offer new insights into the potential therapy for APAP hepatotoxicity.


Asunto(s)
Acetaminofén/toxicidad , Antiinflamatorios no Esteroideos/uso terapéutico , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Naftoquinonas/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Analgésicos no Narcóticos/toxicidad , Animales , Antiinflamatorios no Esteroideos/farmacología , Inflamación/inducido químicamente , Inflamación/metabolismo , Inflamación/prevención & control , Masculino , Ratones , Ratones Endogámicos BALB C , Naftoquinonas/farmacología , Estrés Oxidativo/fisiología
13.
Drug Metab Rev ; 50(3): 369-397, 2018 08.
Artículo en Inglés | MEDLINE | ID: mdl-30221555

RESUMEN

There will be 642 million people worldwide by 2040 suffering from diabetes mellitus. Long-term multidrug therapy aims to achieve normal glycemia and minimize complications, and avoid severe hypoglycemic events. The appreciation of the drug-metabolizing enzymes and drug transporters as critical players in the treatment of diabetes has attracted much attention regarding their potential alterations in the pathogenesis of the disease. This review discusses pharmacokinetics-based alterations of cytochrome P450 enzymes, phase-II metabolizing enzymes, and membrane transporter proteins, as well as the potential mechanisms underlying these alterations. We also discuss the potential influences of altered enzymes and transporters on the disposition of commonly prescribed glucose-lowering medicines. Future studies should delve into the impact of altered drug-metabolizing enzymes and transporters on the progression toward abnormal glucose homeostasis.


Asunto(s)
Sistema Enzimático del Citocromo P-450/metabolismo , Diabetes Mellitus/metabolismo , Hipoglucemiantes/farmacocinética , Proteínas de Transporte de Membrana/metabolismo , Animales , Diabetes Mellitus/enzimología , Humanos
14.
Bioorg Med Chem ; 26(16): 4602-4614, 2018 09 01.
Artículo en Inglés | MEDLINE | ID: mdl-30115493

RESUMEN

A novel series of 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives featured with various C-2 substituents were designed and synthesized as Mnks inhibitors through fragment-based drug design. Among them, 5b, 5i, 5o and 8k showed the best Mnk2 inhibitory activity with IC50 values of 1.45, 1.16, 3.55 and 0.27 µM, respectively. And these compounds inhibited the activity of Mnk1 at the same time. Furthermore, compounds 5o and 8k exhibited anti-proliferative effects to human leukemia cancer THP-1 and MOLM-13 cell lines and colon cancer HCT-116 cell line. Moreover, Western blot assay suggested that 8k could decrease the levels of p-eIF4E in a dose-dependent manner in HCT-116 cells. Docking studies demonstrated strong interactions between 8k and Mnk2. Therefore, this unique benzofuran scaffold demonstrated great potential to be further explored as potent Mnks inhibitors with improved potency.


Asunto(s)
Amidas/química , Diseño de Fármacos , Péptidos y Proteínas de Señalización Intracelular/antagonistas & inhibidores , Inhibidores de Proteínas Quinasas/síntesis química , Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores , Amidas/síntesis química , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Benzofuranos/química , Sitios de Unión , Dominio Catalítico , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Humanos , Péptidos y Proteínas de Señalización Intracelular/metabolismo , Simulación de Dinámica Molecular , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Proteínas Serina-Treonina Quinasas/metabolismo , Relación Estructura-Actividad
15.
Zhongguo Zhen Jiu ; 38(7): 703-6, 2018 Jul 12.
Artículo en Chino | MEDLINE | ID: mdl-30014662

RESUMEN

OBJECTIVE: To observe the efficacy difference among medication, medication plus rehabilitation training and medication plus rehabilitation training plus acupuncture on injury of nervus peroneus communis. METHODS: A total of 81 patients were randomly divided into a control group, an observation 1 group and an observation 2 group; three patients dropped out and 78 patients were included into statistical analysis, 26 patients in each group. The patients in the control group were treated with oral administration of mecobalamin, 500 µg per time, 3 times a day for 60 days. Based on the treatment of control group, the patients in the observation 1 group were treated with rehabilitation training by computer-aided movable and measurable ankle-foot orthosis (CMM-AFO). Based on the treatment of observation 1 group, the patients in the observation 2 group were treated with acupuncture at Jiexi (ST 41), Fenglong (ST 40), Yanglingquan (GB 34) and Zusanli (ST 36), etc, 30 min per treatment, once a day for 60 days. After 60-day treatment, the clinical efficacy was evaluated; the muscle strengths of foot dorsal stretch and digital flexion were evaluated; the motor nerve conduction velocity (MCV) and sensory nerve conduction velocity (SCV) were recorded. RESULTS: After treatment, 20 patients were cured in the observation 2 group, which was significantly higher than 8 patients in the control group and 15 patients in the observation 1 group (both P<0.05). The muscle strengths, SCV and MCV in the observation 2 group were significantly higher than those in the control group and the observation 1 group (all P<0.05). CONCLUSION: Acupuncture combined with CMM-AFO have significant efficacy on injury of nervus peroneus communis, and improve muscle strengths, SCV and MCV, which are superior to medication alone and medication plus rehabilitation training.


Asunto(s)
Terapia por Acupuntura , Ortesis del Pié , Nervio Peroneo/lesiones , Tobillo , Pie , Humanos
16.
Materials (Basel) ; 11(5)2018 May 09.
Artículo en Inglés | MEDLINE | ID: mdl-29747440

RESUMEN

Silver-coated molybdenum is an optimum material selection to replace pure silver as solar cell interconnector. However, the low adhesive strength between Ag films and Mo substrate hinders the application of the interconnector, because it is difficult to form metallurgical bonding or compound in the film/substrate interface using conventional deposition. In order to improve the adhesion, some Ag particles were implanted into the surface of Mo substrate by ion beam-assisted deposition (IBAD) before the Ag films were deposited by magnetron sputtering deposition (MD). The objective of this work was to investigate the effect of different assisted ion beam energy on the film/substrate adhesive properties. In addition, the fundamental adhesion mechanism was illustrated. The results revealed that the adhesion between Ag films and Mo substrate could be greatly enhanced by IBAD. With the increase of the assisting ion beam energy, the adhesive strength first increased and then decreased, with the optimum adhesion being able to rise to 25.29 MPa when the energy of the assisting ion beam was 30 keV. It could be inferred that the combination of “intermixing layer” and “implanted layer” formed by the high-energy ion bombardment was the key to enhancing the adhesion between Ag films and Mo substrate effectively.

17.
Materials (Basel) ; 11(4)2018 Apr 13.
Artículo en Inglés | MEDLINE | ID: mdl-29652848

RESUMEN

Reduced graphene oxide (RGO) composite copper matrix powders were fabricated successfully by using a modified molecular-level mixing (MLM) method. Divalent copper ions (Cu2+) were adsorbed in oxygen functional groups of graphene oxide (GO) as a precursor, then were reduced simultaneously by one step chemical reduction. RGO showed a distribution converting from a random to a three-dimensional network in the copper matrix when its content increased to above 1.0 wt.% The tribological tests indicated that the friction coefficient of the composite with 1.0 wt.% RGO decreased markedly from 0.6 to 0.07 at an applied load of 10 N, and the wear rate was about one-third of pure copper. The excellent tribological properties were attributed to a three-dimensional and uniform distribution, which contributes to improving toughness and adhesion strength.

18.
Bioresour Technol ; 181: 54-61, 2015 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-25638404

RESUMEN

The cultivation of microalgae Chlorella pyrenoidosa (C. pyrenoidosa) using anaerobic digested starch wastewater (ADSW) and alcohol wastewater (AW) was evaluated in this study. Different proportions of mixed wastewater (AW/ADSW=0.176:1, 0.053:1, 0.026:1, v/v) and pure ADSW, AW were used for C. pyrenoidosa cultivation. The different proportions between ADSW and AW significantly influenced biomass growth, lipids production and pollutants removal. The best performance was achieved using mixed wastewater (AW/ADSW=0.053:1, v/v), leading to a maximal total biomass of 3.01±0.15 g/L (dry weight), lipids productivity of 127.71±6.31 mg/L/d and pollutants removal of COD=75.78±3.76%, TN=91.64±4.58% and TP=90.74±4.62%.


Asunto(s)
Alcoholes/química , Chlorella/crecimiento & desarrollo , Lípidos/biosíntesis , Nitrógeno/aislamiento & purificación , Fósforo/aislamiento & purificación , Almidón/química , Aguas Residuales/química , Anaerobiosis , Técnicas de Cultivo Celular por Lotes , Análisis de la Demanda Biológica de Oxígeno , Biomasa , Chlorella/metabolismo , Ésteres/análisis , Ácidos Grasos Volátiles/análisis , Microalgas/crecimiento & desarrollo , Microalgas/metabolismo , Compuestos Orgánicos/aislamiento & purificación
19.
Colloids Surf B Biointerfaces ; 125: 238-46, 2015 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-25559611

RESUMEN

The influence of extracellular organic matter (EOM) on membrane fouling is important for algae cultivation and harvest. Therefore, a deep understanding of EOM and a systematic extraction process are necessary. In this study, EOM from Chlorella pyrenoidosa was thoroughly studied by using different methods to stratify it into dEOM and bEOM. Among these methods, the centrifugation method was optimized for dEOM extraction, and the heating and NaOH methods were optimized for bEOM extraction. In addition, dEOM and bEOM were compared by using analytical methods to obtain their protein and polysaccharide contents, dissolved organic carbon (DOC) contents, specific UV absorbances (SUVA), zeta potentials, FTIR spectra, EEM fluorescence spectra, hydrophobicities and molecular weights. The dEOM and bEOM both primarily consisted of proteins and polysaccharides and carried negative charges with relatively low SUVAs. The protein/polysaccharide ratios in the bEOM were 6.35 (control), 12.54 (heating) and 7.54 (NaOH) mg mg(-1), which were greater than the ratio of the dEOM (2.93 mg mg(-1)). Furthermore, the hydrophobicity analysis indicated that the bEOM had higher hydrophobic fraction content than the dEOM. However, both types of EOM were more hydrophilic in terms of the DOC. Finally, size fraction analysis indicated that high-MW (>100 kDa) and low-MW fractions (<1 kDa) were the primary components in EOMs. Specifically, a greater high-MW fraction was observed in the bEOM, which primarily consisted of DOC and proteins. In contrast with the proteins, the polysaccharides of the dEOM and bEOM were primarily distributed in the hydrophilic and low-MW fractions. Using comparative analysis, centrifugation at 10,000×g for 10 min was chosen as the best method for extracting dEOM. In contrast, heating at 70°C for 20 min was the best method for extracting bEOM.


Asunto(s)
Proteínas Algáceas/aislamiento & purificación , Chlorella/química , Extracción Líquido-Líquido/métodos , Ácidos Nucleicos/aislamiento & purificación , Polisacáridos/aislamiento & purificación , Centrifugación , Calor , Interacciones Hidrofóbicas e Hidrofílicas , Peso Molecular , Electricidad Estática , Aguas Residuales/química , Purificación del Agua/métodos
20.
J Hazard Mater ; 286: 425-31, 2015 Apr 09.
Artículo en Inglés | MEDLINE | ID: mdl-25600582

RESUMEN

The catalytic reduction of nitrate is a promising technology for groundwater purification because it transforms nitrate into nitrogen and water. Recent studies have mainly focused on new catalysts with higher activities for the reduction of nitrate. Consequently, metal nanoparticles supported on mesoporous metal oxides have become a major research direction. However, the complex surface chemistry and porous structures of mesoporous metal oxides lead to a non-uniform distribution of metal nanoparticles, thereby resulting in a low catalytic efficiency. In this paper, a method for synthesizing the sustainable nitrate reduction catalyst Pd-In/Al2O3 with a dimensional structure is introduced. The TEM results indicated that Pd and In nanoparticles could efficiently disperse into the mesopores of the alumina. At room temperature in CO2-buffered water and under continuous H2 as the electron donor, the synthesized material (4.9 wt% Pd) was the most active at a Pd-In ratio of 4, with a first-order rate constant (k(obs) = 0.241 L min(-1) g(cata)(-1)) that was 1.3× higher than that of conventional Pd-In/Al2O3 (5 wt% Pd; 0.19 L min(-1) g(cata)(-1)). The Pd-In/mesoporous alumina is a promising catalyst for improving the catalytic reduction of nitrate.


Asunto(s)
Óxido de Aluminio/química , Indio/química , Nanopartículas del Metal/química , Nitratos/química , Paladio/química , Contaminantes Químicos del Agua/química , Catálisis , Nanopartículas del Metal/ultraestructura , Microscopía Electrónica de Transmisión , Oxidación-Reducción , Povidona/química
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA