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1.
J Clin Gastroenterol ; 2024 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-38457410

RESUMEN

BACKGROUND: Gastric structure recognition systems have become increasingly necessary for the accurate diagnosis of gastric lesions in capsule endoscopy. Deep learning, especially using transformer models, has shown great potential in the recognition of gastrointestinal (GI) images according to self-attention. This study aims to establish an identification model of capsule endoscopy gastric structures to improve the clinical applicability of deep learning to endoscopic image recognition. METHODS: A total of 3343 wireless capsule endoscopy videos collected at Nanfang Hospital between 2011 and 2021 were used for unsupervised pretraining, while 2433 were for training and 118 were for validation. Fifteen upper GI structures were selected for quantifying the examination quality. We also conducted a comparison of the classification performance between the artificial intelligence model and endoscopists by the accuracy, sensitivity, specificity, and positive and negative predictive values. RESULTS: The transformer-based AI model reached a relatively high level of diagnostic accuracy in gastric structure recognition. Regarding the performance of identifying 15 upper GI structures, the AI model achieved a macroaverage accuracy of 99.6% (95% CI: 99.5-99.7), a macroaverage sensitivity of 96.4% (95% CI: 95.3-97.5), and a macroaverage specificity of 99.8% (95% CI: 99.7-99.9) and achieved a high level of interobserver agreement with endoscopists. CONCLUSIONS: The transformer-based AI model can accurately evaluate the gastric structure information of capsule endoscopy with the same performance as that of endoscopists, which will provide tremendous help for doctors in making a diagnosis from a large number of images and improve the efficiency of examination.

2.
Math Biosci Eng ; 21(1): 984-1016, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38303451

RESUMEN

Bio-inspired optimization algorithms are competitive solutions for engineering design problems. Chicken swarm optimization (CSO) combines the advantages of differential evolution and particle swarm optimization, drawing inspiration from the foraging behavior of chickens. However, the CSO algorithm may perform poorly in the face of complex optimization problems because it has a high risk of falling into a local optimum. To address these challenges, a new CSO called chicken swarm optimization combining Pad$ \acute{e} $ approximate, random learning and population reduction techniques (PRPCSO) was proposed in this work. First, a Pad$ \acute{e} $ approximate strategy was combined to help agents converge to the approximate real solution area quickly. Pad$ \acute{e} $ approximate was grounded in a rational function aligning with the power series expansion of the approximated function within a defined number of terms. The fitting function used in this strategy employs the above rational function and the extreme points are calculated mathematically, which can significantly improve the accuracy of the solution. Second, the random learning mechanism encouraged agents to learn from other good agents, resulting in better local exploitation capability compared to traditional CSO. This mechanism has a special idea that when it comes to selecting random individuals, it selects from the same type of high-performing agents, rather than selecting them completely at random. Third, a new intelligent population size shrinking strategy was designed to dynamically adjust the population size to prevent premature convergence. It considers fitness function calls and variations in recent optimal solutions creatively. To validate the algorithm's efficacy, PRPCSO was rigorously tested across 23 standard test functions and six kinds of practical engineering problems. We then compared PRPCSO with several mainstream algorithms, and the results unequivocally established PRPCSO's superior performance in most instances, highlighting its substantial practical utility in real engineering applications.

3.
iScience ; 26(10): 108018, 2023 Oct 20.
Artículo en Inglés | MEDLINE | ID: mdl-37841581

RESUMEN

Patients with HNF1A variants may develop liver steatosis, while the underlying mechanism is still unclear. Here, we established a mouse model carrying the dominant-negative HNF1α P291fsinsC mutation (hHNF1Amut/-) and found that the mutant mice developed liver steatosis spontaneously under the normal chow diet. Transcriptome analysis showed significant upregulation of Cfd and other genes related to innate immune response in the liver of hHNF1Amut/- mice. The changes in lipid metabolism and complement pathways were also confirmed by proteomics. We demonstrated that HNF1α inhibited CFD expression in hepatocytes, and the P291fsinsC mutant could reverse this inhibitory effect. Furthermore, the suppression of CFD with specific inhibitor or siRNAs reduced triglyceride levels in hepatocytes, suggesting that CFD regulated hepatocyte lipid deposition. Our results demonstrate that the HNF1α P291fsinsC mutant promotes hepatic steatosis and inflammation by upregulating CFD expression, and targeting CFD may delay the progression of nonalcoholic fatty liver disease.

4.
Front Pharmacol ; 14: 1234885, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37538172

RESUMEN

Objective: In this study, we utilized bibliometric methods to assess the worldwide scientific output and identify hotspots related to the research on the volume-regulated anion channel (VRAC) from 2014 to 2022. Methods: From Web of Science, we obtained studies related to VRAC published from 2014 to 2022. To analyzed the data, we utilized VOSviewer, a tool for visualizing network, to create networks based on the collaboration between countries, institutions, and authors. Additionally, we performed an analysis of journal co-citation, document citation, and co-occurrence of keywords. Furthermore, we employed CiteSpace (6.1. R6 Advanced) to analyzed keywords and co-cited references with the strongest burst. Results: The final analysis included a total of 278 related articles and reviews, covering the period from 2014 to 2022. The United States emerged as the leading country contributing to this field, while the University of Copenhagen stood out as the most prominent institution. The author with most publications and most citations was Thomas J. Jentsch. Among the cited references, the article by Voss et al. published in Science (2014) gained significant attention for its identification of LRRC8 heteromers as a crucial component of the volume-regulated anion channel VRAC. Pflügers Archiv European Journal of Physiology and Journal of Physiology-London were the leading journals in terms of the quantity of associated articles and citations. Through the analysis of keyword co-occurrence, it was discovered that VRAC is involved in various physiological processes including cell growth, migration, apoptosis, swelling, and myogenesis, as well as anion and organic osmolyte transport including chloride, taurine, glutamate and ATP. VRAC is also associated with related ion channels such as TMEM16A, TMEM16F, pannexin, and CFTR, and associated with various diseases including epilepsy, leukodystrophy, atherosclerosis, hypertension, cerebral edema, stroke, and different types of cancer including gastric cancer, glioblastoma and hepatocellular carcinoma. Furthermore, VRAC is involved in anti-tumor drug resistance by regulating the uptake of platinum-based drugs and temozolomide. Additionally, VRAC has been studied in the context of pharmacology involving DCPIB and flavonoids. Conclusion: The aim of this bibliometric analysis is to provide an overall perspective for research on VRAC. VRAC has become a topic of increasing interest, and our analysis shows that it continues to be a prominent area. This study offers insights into the investigation of VRAC channel and may guide researchers in identifying new directions for future research.

5.
Cell Metab ; 35(4): 585-600.e5, 2023 04 04.
Artículo en Inglés | MEDLINE | ID: mdl-36931274

RESUMEN

Breakthrough SARS-CoV-2 infections of vaccinated individuals are being reported globally, resulting in an increased risk of hospitalization and death among such patients. Therefore, it is crucial to identify the modifiable risk factors that may affect the protective efficacy of vaccine use against the development of severe COVID-19 and thus to initiate early medical interventions. Here, in population-based studies using the UK Biobank database and the 2021 National Health Interview Survey (NHIS), we analyzed 20,362 participants aged 50 years or older and 2,588 aged 18 years or older from both databases who tested positive for SARS-COV-2, of whom 33.1% and 67.7% received one or more doses of vaccine, respectively. In the UK Biobank, participants are followed from the vaccination date until October 18, 2021. We found that obesity and metabolic abnormalities (namely, hyperglycemia, hyperlipidemia, and hypertension) were modifiable factors for severe COVID-19 in vaccinated patients (all p < 0.05). When metabolic abnormalities were present, regardless of obesity, the risk of severe COVID-19 was higher than that of metabolically normal individuals (all p < 0.05). Moreover, pharmacological interventions targeting such abnormalities (namely, antihypertensive [adjusted hazard ratio (aHR) 0.64, 95% CI 0.48-0.86; p = 0.003], glucose-lowering [aHR 0.55, 95% CI 0.36-0.83; p = 0.004], and lipid-lowering treatments [aHR 0.50, 95% CI 0.37-0.68; p < 0.001]) were significantly associated with a reduced risk for this outcome. These results show that more proactive health management of patients with obesity and metabolic abnormalities is critical to reduce the incidence of severe COVID-19 after vaccination.


Asunto(s)
COVID-19 , Humanos , SARS-CoV-2 , Vacunación , Obesidad , Factores de Riesgo
6.
Environ Res ; 217: 114914, 2023 01 15.
Artículo en Inglés | MEDLINE | ID: mdl-36427635

RESUMEN

Microbial reduction of hexavalent chromium (Cr (VI)) shows better efficiency and cost-effectiveness. However, immobilization of Cr (III) remains a challenge as there is a limited supply of electron donors. A greener and cleaner option for donating external electrons was using bioelectrochemical systems to perform the microbial reduction of Cr(VI). In this system, we constructed a polydopamine (PDA) decorated Shewanella oneidensis MR-1 (S. oneidensis MR-1) bioelectrode with bidirectional electron transport, abbreviated as PDA@S. oneidensis MR-1. The conjugated PDA distributed on the intracellular and extracellular of individual S. oneidensis MR-1 has been shown to accelerate electron transfer by outer membrane C-type cytochromes and flavin-bound MtrC/OmcA pathway by various electrochemical analyses. As expected, the PDA@S. oneidensis MR-1 biofilm achieved 88.1% Cr (VI) removal efficiency (RE) and 58.1% Cr (III) immobilization efficiency (IE) within 24 h under the autotrophic conditions at the optimal voltage (-150 mV) compared with the control potential (0 mV). The PDA@S. oneidensis MR-1 biofilm showed increased RE activity was attributed to the shortening of the distance between individual bacteria by PDA. This research provides a viable strategy for in situ bioremediation of Cr(VI) polluted aquatic environment.


Asunto(s)
Electrones , Shewanella , Transporte de Electrón , Oxidación-Reducción , Shewanella/metabolismo
7.
Environ Res ; 216(Pt 2): 114567, 2023 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-36244441

RESUMEN

The recovery of heavy metals from electroplating sludge is important for alleviating heavy metal pollution and recycling metal resources. However, the selective recovery of metal resources is limited by the complexity of electroplating sludge. Herein, CuFe bimetallic Fenton-like catalysts were successfully prepared from electroplating sludge by a facile room-temperature ultrasonic-assisted co-precipitation method. The prepared CuFe-S mainly consisted of nanorods with diameters of 20-30 nm and lengths of 100-200 nm and a small number of irregular particles. Subsequently, we performed tetracycline (TC) degradation experiments, and the results showed that the product CuFe-S had very good performance over a wide pH range (2-11). At an initial pH = 2, CuFe-S could degrade 91.9% of 50 mg L-1 TC aqueous solution within 30 min, which is better than that of a single metal catalyst. Free radical scavenging experiments and electron paramagnetic resonance (EPR) tests revealed that ·OH was the main active species for the degradation of TC by CuFe-S. In conclusion, a CuFe bimetallic Fenton-like catalyst was developed for the catalytic degradation of antibiotics, which provides a novel technical route for the resource utilization of electroplating sludge and shows an important practical application prospect.


Asunto(s)
Metales Pesados , Aguas del Alcantarillado , Galvanoplastia , Cobre , Catálisis , Antibacterianos , Peróxido de Hidrógeno
8.
Biosens Bioelectron ; 220: 114895, 2023 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-36375257

RESUMEN

Anode performance has been regarded as a crucial factor determining long-term stability and electricity generation of microbial fuel cells (MFCs), which restricts by the difficult extracellular electron transfer (EET) on the microbe/anode interface. Herein, inspired by biological enzyme systems, this study synthesized the biomimetic nanozymes with Fe-N-S-C active sites as the anode materials of MFCs, which was similar to the hemes of c-type cytochromes (c-Cyts) for boosting EET process. As excepted, an obviously faster start-up and a much higher power density were achieved by the MFCs equipped with Fe-N-S-C nanozymes (startup time, 3.5 d; power density, 2366 ± 34 mW m-2) than that based on traditional carbon cloth (startup time, 5.6 d; power density, 1009 ± 26 mW m-2). Such unique features of Fe-N-S-C nanozymes anode not only greatly favored the bacterial adhesion and the electroactive bacteria enrichment on the anode surface, but also efficiently facilitated the EET process between the electroactive bacteria and anode surface. This study provided a feasible strategy for designing the novel MFC anode materials from the perspective of bionic enzyme.


Asunto(s)
Fuentes de Energía Bioeléctrica , Técnicas Biosensibles , Fuentes de Energía Bioeléctrica/microbiología , Biomimética , Electrodos , Electricidad
9.
Polymers (Basel) ; 14(19)2022 Sep 21.
Artículo en Inglés | MEDLINE | ID: mdl-36235896

RESUMEN

The basalt fibers (BF) and the basalt fibers etched by H2SO4 (BFH) were modified by polydopamine (PDA) or synergistically modified by PDA and silicon carbon black (SiCB). The effects of modified BF, BFH and SiCB on the basic mechanical properties and magnetorheological (MR) effects of natural rubber/butadiene rubber-based magnetorheological elastomer precursors (MREs) were investigated. The results show that the tensile strength, tear strength and stress at 300% strain of MREs/PDA-BFH-SiCB prepared with BFH synergistically modified by PDA and SiCB reach the maximum values, which are 9.58 MPa, 24.07 kN/m and 4.13 MPa, respectively. Additionally, its MR effect is more than three times higher than that of MREs before composite modification.

10.
Front Psychol ; 13: 904298, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35874332

RESUMEN

The education level and social participation of contemporary Chinese women have reached their historical peak; work is fast becoming the dominant theme of their lives. However, influenced by traditional attitudes, women are still expected to undertake the main family care tasks, thus, facing dual constraints of family and work, which seriously affect their life happiness. Based on the theory of subjective well-being and feminist geography, this study used the questionnaire survey and in-depth interview results of professional females in Dalian High-tech Industrial Zone as basic data to explore the life satisfaction and emotional cognition in intra- and extra-household life of professional females (Professional females: In this study, they are the women who have received formal education and currently have full-time and steady job (including regular employees in the national systems and those who have signed labor contracts with labor units).). The following results were obtained: (1) Most professional females reported higher life satisfaction in intra- rather than extra-household life, and it varied with individual attributes, reflecting the internal differences among them. (2) The positive emotions of professional females came from the company of family and friends in intra-household life, and satisfaction with the working environment and treatment in extra-household life. (3) The negative emotions came from the pressure of "marriage," "birth," and other traditional concepts in intra-household life. In extra-household life, it came from the health problems caused by working stress, interpersonal problems and gender inequality in the workplace, and the anxiety of age and future career development. Therefore, this study committed to revealing the living status and subjective feelings of contemporary professional females in China, hoping to improve women's life quality and enhance their life happiness from a theoretical and realistic perspective.

11.
Chemosphere ; 304: 135303, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-35691392

RESUMEN

Biochar derived from municipal sludge can be applied to adsorption. But it usually requires activation and pickling due to the generation of impurities such as metal oxide particles, which is uneconomical. Here, a facile strategy, acidification-one-step calcination, was developed and sludge-based Fe-C materials with good Cr(VI) removal effect were obtained by regulating the amount of hydrochloric acid. The results show that the adsorption capacity of Fe/C-5 (the best sample) for Cr(VI) was 150.84 mg g-1. According to the Langmuir isotherm and pseudo-second-order kinetic model, the removal of Cr(VI) by Fe/C-5 is spontaneous and endothermic chemisorption process. In addition, Fe/C-5 has good ability to remove Cr(VI) under the interference of coexisting ions, and has good cycle stability. The removal of Cr(VI) by Fe/C-5 is considered to be synergistic process of adsorption and reduction. The Fe atoms were highly dispersed in Fe/C-5 and tightly bonded with C atoms, which not only strengthened the Cr(VI) adsorption by electrostatic attraction, but also activated the C atoms in the biochar material, so that the C atoms can reduce Cr(VI) to Cr(III) under acidic conditions. This may be due to the fact that acid pretreatment converted the iron in municipal sludge in the form of Fe-O/OH to free Fe3+ and entered the C lattice during the calcination process. In this work, Fe-C materials with excellent Cr(VI) adsorption capacity were prepared by one-step calcination method, which has important reference significance for the resource utilization of municipal sludge.


Asunto(s)
Aguas del Alcantarillado , Contaminantes Químicos del Agua , Adsorción , Carbón Orgánico , Cromo/análisis , Cinética , Contaminantes Químicos del Agua/análisis
12.
J Transl Med ; 20(1): 38, 2022 01 24.
Artículo en Inglés | MEDLINE | ID: mdl-35073917

RESUMEN

BACKGROUND: The prevalence of diffuse-type gastric cancer (GC), especially signet ring cell carcinoma (SRCC), has shown an upward trend in the past decades. This study aimed to develop computed tomography (CT) based radiomics nomograms to distinguish diffuse-type and SRCC GC preoperatively. METHODS: A total of 693 GC patients from two centers were retrospectively analyzed and divided into training, internal validation and external validation cohorts. Radiomics features were extracted from CT images, and the Lauren radiomics model was established with a support vector machine (SVM) classifier to identify diffuse-type GC. The Lauren radiomics nomogram integrating radiomics features score (Rad-score) and clinicopathological characteristics were developed and evaluated regarding prediction ability. Further, the SRCC radiomics nomogram designed to identify SRCC from diffuse-type GC was developed and evaluated following the same procedures. RESULTS: Multivariate analysis revealed that Rad-scores was significantly associated with diffuse-type GC and SRCC (p < 0.001). The Lauren radiomics nomogram showed promising prediction performance with an area under the curve (AUC) of 0.895 (95%CI, 0.957-0.932), 0.841 (95%CI, 0.781-0.901) and 0.893 (95%CI, 0.831-0.955) in each cohort. The SRCC radiomics nomogram also showed good discrimination, with AUC of 0.905 (95%CI,0.866-0.944), 0.845 (95%CI, 0.775-0.915) and 0.918 (95%CI, 0.842-0.994) in each cohort. The radiomics nomograms showed great model fitness and clinical usefulness by calibration curve and decision curve analysis. CONCLUSION: Our CT-based radiomics nomograms had the ability to identify the diffuse-type and SRCC GC, providing a non-invasive, efficient and preoperative diagnosis method. They may help guide preoperative clinical decision-making and benefit GC patients in the future.


Asunto(s)
Carcinoma de Células en Anillo de Sello , Neoplasias Gástricas , Carcinoma de Células en Anillo de Sello/diagnóstico por imagen , Humanos , Nomogramas , Estudios Retrospectivos , Neoplasias Gástricas/diagnóstico por imagen , Neoplasias Gástricas/cirugía , Tomografía Computarizada por Rayos X/métodos
13.
J Hazard Mater ; 404(Pt B): 124113, 2021 02 15.
Artículo en Inglés | MEDLINE | ID: mdl-33068998

RESUMEN

This work demonstrated that electroplating sludges (EPS) of specific composition may be used for the synthesis of layered double hydroxide (LDH) materials for energy applications after appropriate treatment. The unique composition and structure of EPS render it with good electrochemical energy storage performance. The EPS containing Ni, Fe, and Al was dissolved by acid and added with urea precipitator. The LDH material was prepared by a facile hydrothermal method. The increase of urea in a certain range is conducive to the formation of intact LDH. However excessive urea levels promoted the transformation from LDH to Ni(HCO3)2. Various active Ni bridged by N in ‒O‒CN promoted electron transfer, ‒O‒CN content in LDHs was proportional to the urea amount. The prepared LDHs exhibited a specific capacitance of 1652.20 F g-1 at 0.5 A g-1, and the value remained at 766.69 F g-1 after 1000 cycles. The prepared LDH has excellent supercapacitor performance, which is closely related to its structure. Therefore, the proposed recycling strategy of EPS resources can be used to prepare LDH supercapacitors, paving the way for new applications of EPS in the field of energy storage.

14.
Chem Commun (Camb) ; 55(77): 11543-11546, 2019 Sep 24.
Artículo en Inglés | MEDLINE | ID: mdl-31490483

RESUMEN

In this work, a simulated enzyme inhibition-based strategy was transplanted from natural peroxidase-based sensing methods for colorimetric nanoperoxidase-based biothiol detection. This work might provide some new perspectives for the construction and biomimetic regulation of mimicked biological signalling systems based on nanoperoxidases.


Asunto(s)
Colorantes Fluorescentes/química , Glutatión/análisis , Mercurio/química , Nanopartículas del Metal/química , Peroxidasas/química , Puntos Cuánticos/química , Compuestos de Sulfhidrilo/análisis , Materiales Biomiméticos/química , Técnicas Biosensibles/métodos , Carbono/química , Catálisis , Colorimetría/métodos , Oro/química , Peróxido de Hidrógeno/química , Concentración de Iones de Hidrógeno , Límite de Detección , Oxidación-Reducción , Peroxidasas/antagonistas & inhibidores , Propiedades de Superficie
15.
Int J Mol Sci ; 20(11)2019 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-31151189

RESUMEN

Cells possess the capability to adjust their volume for various physiological processes, presumably including cell proliferation and migration. The volume-regulated anion channel (VRAC), formed by LRRC8 heteromers, is critically involved in regulatory volume decrease of vertebrate cells. The VRAC has also been proposed to play a role in cell cycle progression and cellular motility. Indeed, recent reports corroborated this notion, with potentially important implications for the VRAC in cancer progression. In the present study, we examined the role of VRAC during cell proliferation and migration in several cell types, including C2C12 myoblasts, human colon cancer HCT116 cells, and U251 and U87 glioblastoma cells. Surprisingly, neither pharmacological inhibition of VRAC with 4-[(2-Butyl-6,7-dichloro-2-cyclopentyl-2,3-dihydro-1-oxo-1H-inden-5-yl)oxy]butanoic acid (DCPIB), carbenoxolone or 5-nitro-2-(3-phenylpropyl-amino)benzoic acid (NPPB), nor siRNA-mediated knockdown or gene knockout of the essential VRAC subunit LRRC8A affected cell growth and motility in any of the investigated cell lines. Additionally, we found no effect of the VRAC inhibition using siRNA treatment or DCPIB on PI3K/Akt signaling in glioblastoma cells. In summary, our work suggests that VRAC is dispensable for cell proliferation or migration.


Asunto(s)
Movimiento Celular , Proliferación Celular , Canales Iónicos/genética , Proteínas de la Membrana/genética , Animales , Línea Celular Tumoral , Movimiento Celular/genética , Proliferación Celular/genética , Ciclopentanos/farmacología , Técnicas de Silenciamiento del Gen , Humanos , Indanos/farmacología , Canales Iónicos/antagonistas & inhibidores , Canales Iónicos/química , Canales Iónicos/metabolismo , Proteínas de la Membrana/antagonistas & inhibidores , Proteínas de la Membrana/química , Proteínas de la Membrana/metabolismo , Ratones , Mioblastos , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal/efectos de los fármacos
16.
Biol Chem ; 400(11): 1481-1496, 2019 10 25.
Artículo en Inglés | MEDLINE | ID: mdl-31091194

RESUMEN

The volume-regulated anion channel (VRAC) is a key player in the volume regulation of vertebrate cells. This ubiquitously expressed channel opens upon osmotic cell swelling and potentially other cues and releases chloride and organic osmolytes, which contributes to regulatory volume decrease (RVD). A plethora of studies have proposed a wide range of physiological roles for VRAC beyond volume regulation including cell proliferation, differentiation and migration, apoptosis, intercellular communication by direct release of signaling molecules and by supporting the exocytosis of insulin. VRAC was additionally implicated in pathological states such as cancer therapy resistance and excitotoxicity under ischemic conditions. Following extensive investigations, 5 years ago leucine-rich repeat-containing family 8 (LRRC8) heteromers containing LRRC8A were identified as the pore-forming components of VRAC. Since then, molecular biological approaches have allowed further insight into the biophysical properties and structure of VRAC. Heterologous expression, siRNA-mediated downregulation and genome editing in cells, as well as the use of animal models have enabled the assessment of the proposed physiological roles, together with the identification of new functions including spermatogenesis and the uptake of antibiotics and platinum-based cancer drugs. This review discusses the recent molecular biological insights into the physiology of VRAC in relation to its previously proposed roles.


Asunto(s)
Proteínas de la Membrana/metabolismo , Humanos , Canales Iónicos/metabolismo
17.
Chem Pharm Bull (Tokyo) ; 64(11): 1570-1575, 2016 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-27568484

RESUMEN

A series of novel quinazoline derivatives have been designed and synthesized, and their inhibitory activities have also been tested against A549 (carcinomic human alveolar basal epithelial cell), MCF-7 (breast cancer) and HeLa (cervical cancer cell). Of these compounds, compound 4t showed the most potent inhibitory activity (IC50=0.22 µg/mL for HeLa, IC50=0.15 µg/mL for A549 and IC50=0.24 µg/mL for MCF-7). Docking simulation had been performed to position compound 4t into the vascular endothelial growth factor receptor (VEGFR) active site to determine the probable binding model. These results suggested that compound 4t with potent inhibitory activity in tumor growth inhibition may be a potential anticancer agent.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Modelos Moleculares , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/farmacología , Quinazolinas/farmacología , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Inhibidores de Proteínas Quinasas/química , Quinazolinas/síntesis química , Quinazolinas/química , Relación Estructura-Actividad , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo
18.
Analyst ; 140(21): 7165-9, 2015 Nov 07.
Artículo en Inglés | MEDLINE | ID: mdl-26401525

RESUMEN

We have developed a novel colorimetric and ratiometric fluorescence probe for the selective and sensitive monitoring of hydrogen sulfide based on a dicyanoisophorone platform. An excellent linear relationship of fluorescence intensity ratio (I637/I558) (R(2) = 0.9867) versus hydrogen sulfide concentration in the range of 1-12 µM was obtained. This probe exhibited a remarkable fluorescence response to hydrogen sulfide over other physiological thiols or biological species, which fluoresces in the red region with a large Stokes shift (172 nm). This probe was successfully utilized to monitor H2S under in vitro physiological conditions and for imaging H2S in living cells and living zebrafish in vivo.


Asunto(s)
Colorantes Fluorescentes/química , Sulfuro de Hidrógeno/química , Microscopía Fluorescente , Nitrilos/química , Animales , Ciclohexanonas/química , Células HeLa , Humanos , Microscopía Confocal , Modelos Químicos , Pez Cebra
19.
Talanta ; 132: 727-32, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25476371

RESUMEN

A novel highly selective and sensitive fluorescent probe (NJ1) had been designed and synthesized for Cu(2+) detection by fluorescence quenching mechanism, and then the enhancement of fluorescence intensity with the addition of hydrogen sulfide in complex NJ1Cu aqueous solution at physiological conditions were described. This "on-off-on" type fluorescence recognition system was a reversible process, which could be utilized to monitor copper ion and hydrogen sulfide based on a complex NJ1Cu formation-Cu(2+) displacement approach. Importantly, this real-time recognition process of Cu(2+) and hydrogen sulfide exhibited excellent anti-interference ability. In addition, this new fluorescent probe also has potential utility for Cu(2+) and hydrogen sulfide detection in living cells, providing a potential tool for investigating copper ion and hydrogen sulfide in living systems or environment.


Asunto(s)
Cobre/análisis , Colorantes Fluorescentes/química , Hidrazonas/química , Sulfuro de Hidrógeno/análisis , Imagen Molecular/métodos , Naftoles/química , Colorantes Fluorescentes/síntesis química , Células HeLa , Humanos , Hidrazonas/síntesis química , Naftoles/síntesis química , Sensibilidad y Especificidad , Espectrometría de Fluorescencia
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