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排序方式: 共有3006条查询结果,搜索用时 12 毫秒
1.
Claudia Giuseppina Fresta Giuseppe Caruso Annamaria Fidilio Chiara Bianca Maria Platania Nicol Musso Filippo Caraci Filippo Drago Claudio Bucolo 《International journal of molecular sciences》2020,21(23)
Activation of P2X7 signaling, due to high glucose levels, leads to blood retinal barrier (BRB) breakdown, which is a hallmark of diabetic retinopathy (DR). Furthermore, several studies report that high glucose (HG) conditions and the related activation of the P2X7 receptor (P2X7R) lead to the over-expression of pro-inflammatory markers. In order to identify novel P2X7R antagonists, we carried out virtual screening on a focused compound dataset, including indole derivatives and natural compounds such as caffeic acid phenethyl ester derivatives, flavonoids, and diterpenoids. Molecular Mechanics/Generalized Born Surface Area (MM/GBSA) rescoring and structural fingerprint clustering of docking poses from virtual screening highlighted that the diterpenoid dihydrotanshinone (DHTS) clustered with the well-known P2X7R antagonist JNJ47965567. A human-based in vitro BRB model made of retinal pericytes, astrocytes, and endothelial cells was used to assess the potential protective effect of DHTS against HG and 2′(3′)-O-(4-Benzoylbenzoyl)adenosine-5′-triphosphate (BzATP), a P2X7R agonist, insult. We found that HG/BzATP exposure generated BRB breakdown by enhancing barrier permeability (trans-endothelial electrical resistance (TEER)) and reducing the levels of ZO-1 and VE-cadherin junction proteins as well as of the Cx-43 mRNA expression levels. Furthermore, HG levels and P2X7R agonist treatment led to increased expression of pro-inflammatory mediators (TLR-4, IL-1β, IL-6, TNF-α, and IL-8) and other molecular markers (P2X7R, VEGF-A, and ICAM-1), along with enhanced production of reactive oxygen species. Treatment with DHTS preserved the BRB integrity from HG/BzATP damage. The protective effects of DHTS were also compared to the validated P2X7R antagonist, JNJ47965567. In conclusion, we provided new findings pointing out the therapeutic potential of DHTS, which is an inhibitor of P2X7R, in terms of preventing and/or counteracting the BRB dysfunctions elicited by HG conditions. 相似文献
2.
Evaluation of the effect of processing on cocoa polyphenols: antiradical activity,anthocyanins and procyanidins profiling from raw beans to chocolate 下载免费PDF全文
Matteo Bordiga Monica Locatelli Fabiano Travaglia Jean Daniel Coïsson Giuseppe Mazza Marco Arlorio 《International Journal of Food Science & Technology》2015,50(3):840-848
The content and composition of anthocyanins and procyanidins in fermented cocoa beans (from different geographic origins: Ecuador, Cameroon, Ivory Coast, Ghana and Nigeria), roasted nibs, cocoa mass and chocolate were determined, beside the determination of the total antiradical capacity. Concerning geographic origin, cocoa beans and processed products from Ecuador showed the highest levels of anthocyanins, followed by Nigeria and Cameroon. Generally, as cocoa beans were further processed, the levels of anthocyanins and flavan‐3‐ols decreased. The largest observed losses of phenolics occurred during roasting. A progressive decreasing trend in polyphenol concentration was observed in the other processed samples as well. Despite the original content of polyphenols in raw cocoa beans, technological processes imply a significant impact on cocoa quality, confirming the need of specific optimisation to obtain high value chocolate. 相似文献
3.
Lin Gao Stefano Selleri Giorgio Battistelli Luigi Chisci Giuseppe Pelosi 《国际射频与微波计算机辅助工程杂志》2020,30(9)
This paper presents a novel approach to the localization of moving targets in a complex environment based on the measurement of the perturbations induced by the target presence on an independently‐generated time‐varying electromagnetic field. Field perturbations are measured via a set of sensors deployed over the domain of interest and used to detect and track a possible target by resorting to a particle Bernoulli filter (PBF). To comply with real‐time operation, the PBF works along with an artificial neural network (ANN) model of the environment trained offline via finite elements (FEs). The performance of the proposed algorithm is assessed via simulation experiments. 相似文献
4.
A SAXS method for the quantitative assessment of the morphology of polymer layered silicate nanocomposites is proposed. Fitting the SAXS patterns, the number of clay layers, the periodicity of the layers in the tactoids, the thickness of the regions interposed between the clay platelets and their distributions can be measured. A good agreement with TEM data was obtained, avoiding the inconsistencies with microscopical observations often reported in the literature. 相似文献
5.
Evaluation of Slow Crack Growth Resistance in Ceramics for High-Temperature Applications 总被引:1,自引:0,他引:1
The slow (subcritical) crack growth (SCG) resistance of Si3 N4 and SiC ceramics has been evaluated by a stepwise loading test on bending bars precracked by Vickers indentation. Three highly refractory materials were selected for the evaluation: i.e., (1) high-purity Si3 N4 sintered by hot isostatic pressing (HIP) without additives and (2,3) α - and β - SiC pressureless sintered with B and C addition. Under the hypothesis of linear elastic behavior at high temperature, which was found satisfied in the present materials, the SCG resistance was expressed in terms of initial stress intensity factor critical for SCG failure within a predetermined lifetime. The present method was found useful in shortening the testing time and consistent with other traditional fatigue tests (e.g., static-fatigue test): It is recommended as a screening test for materials under research and development. Among the materials tested in the present study, the highest SCG resistance up to 1440°C was found in the high-purity Si3 N4 without additives. 相似文献
6.
Giuseppe G. G. Manzardo Sandra Kürsteiner-Laube und Daniel Perrin 《Zeitschrift für Lebensmitteluntersuchung und -Forschung A》1996,203(6):501-506
In diethyl ether extracts from celeriac (Apium graveolens L. var.rapaceum) all four stereoisomers of (3a–7a)-cis-3-butylhexahydrophthalide were found to be present. The analyses were carried out by means of GC, enantioselective GC and GC-MS. The assignment of the relative configuration of the diastereomers3 and4 was accomplished by NOE difference spectroscopy. 相似文献
7.
8.
A maximum for the coefficient of performance (COPf) is verified for a temperature difference between reservoirs and the hot isotherm of a closed irreversible cyclical refrigerator working at steady-state conditions. A maximum also exists when the COPf is considered as a function only of a parameter depending on the thermal characteristics of the heat exchangers. The influence of the parameter and entropy generation on the COPf maxima is described. 相似文献
9.
Designing Templates for Mining Association Rules 总被引:3,自引:0,他引:3
Current approaches to data mining usually address specific userrequests, while no general design criteria for the extraction of associationrules are available for the end-user. In this paper, we propose aclassification of association rule types, which provides a general frameworkfor the design of association rule mining applications. Based on theidentified association rule types, we introduce predefined templates as ameans to capture the user specification of mining applications. Furthermore,we propose a general language to design templates for the extraction ofarbitrary association rule types. 相似文献
10.
Enrico Saggese Giuseppe Chiassarini 《International Journal of Satellite Communications and Networking》1989,7(4):295-306
One key technology, for the implementation of future on-board processing payloads, is the multicarrier demodulator (MCD). The MCD is instrumental in allowing FDMA/TDM access schemes which optimize the use of on-board and ground resources in VSAT networks. This paper deals with the analogue and digital implementations of MCD, trying to assess the fields of application of each of the two technologies. 相似文献