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Alessia DAloia Federica Arrigoni Renata Tisi Alessandro Palmioli Michela Ceriani Valentina Artusa Cristina Airoldi Giuseppe Zampella Barbara Costa Laura Cipolla 《International journal of molecular sciences》2020,21(23)
Palmitoylethanolamide (PEA) belongs to the class of N-acylethanolamine and is an endogenous lipid potentially useful in a wide range of therapeutic areas; products containing PEA are licensed for use in humans as a nutraceutical, a food supplement, or food for medical purposes for its analgesic and anti-inflammatory properties demonstrating efficacy and tolerability. However, the exogenously administered PEA is rapidly inactivated; in this process, fatty acid amide hydrolase (FAAH) plays a key role both in hepatic metabolism and in intracellular degradation. So, the aim of the present study was the design and synthesis of PEA analogues that are more resistant to FAAH-mediated hydrolysis. A small library of PEA analogues was designed and tested by molecular docking and density functional theory calculations to find the more stable analogue. The computational investigation identified RePEA as the best candidate in terms of both synthetic accessibility and metabolic stability to FAAH-mediated hydrolysis. The selected compound was synthesized and assayed ex vivo to monitor FAAH-mediated hydrolysis and to confirm its anti-inflammatory properties. 1H-NMR spectroscopy performed on membrane samples containing FAAH in integral membrane protein demonstrated that RePEA is not processed by FAAH, in contrast with PEA. Moreover, RePEA retains PEA’s ability to inhibit LPS-induced cytokine release in both murine N9 microglial cells and human PMA-THP-1 cells. 相似文献
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Bruni Vittoria Tartaglione Michela Vitulano Domenico 《Multimedia Tools and Applications》2022,81(16):22653-22676
Multimedia Tools and Applications - This paper presents a method for Photo Response Non Uniformity (PRNU) pattern noise based camera identification. It takes advantage of the coherence between... 相似文献
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Agata Campisi Giuseppina Raciti Giovanni Sposito Rosaria Grasso Maria A. Chiacchio Michela Spatuzza Alessandro Attanzio Ugo Chiacchio Luisa Tesoriere Mario Allegra Rosalia Pellitteri 《International journal of molecular sciences》2021,22(7)
Herein, we assessed the effect of full native peptide of amyloid-beta (Aβ) (1-42) and its fragments (25-35 and 35-25) on tissue transglutaminase (TG2) and its isoforms (TG2-Long and TG2-Short) expression levels on olfactory ensheathing cells (OECs). Vimentin and glial fibrillary acid protein (GFAP) were also studied. The effect of the pre-treatment with indicaxanthin from Opuntia ficus-indica fruit on TG2 expression levels and its isoforms, cell viability, total reactive oxygen species (ROS), superoxide anion (O2−), and apoptotic pathway activation was assessed. The levels of Nestin and cyclin D1 were also evaluated. Our findings highlight that OECs exposure to Aβ(1-42) and its fragments induced an increase in TG2 expression levels and a different expression pattern of its isoforms. Indicaxanthin pre-treatment reduced TG2 overexpression, modulating the expression of TG2 isoforms. It reduced total ROS and O2− production, GFAP and Vimentin levels, inhibiting apoptotic pathway activation. It also induced an increase in the Nestin and cyclin D1 expression levels. Our data demonstrated that indicaxanthin pre-treatment stimulated OECs self-renewal through the reparative activity played by TG2. They also suggest that Aβ might modify TG2 conformation in OECs and that indicaxanthin pre-treatment might modulate TG2 conformation, stimulating neural regeneration in Alzheimer’s disease. 相似文献
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Forschung im Ingenieurwesen - Die Vorteile von elektrischen Hochdrehzahlantrieben mit Mehrganggetriebe gegenüber aktuellen elektrischen Antrieben, konnten durch jüngste... 相似文献
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Sasan?Amini Kristian?Beckers Markus?B?hm Fritz?Busch Nihan?Celikkaya Vittorio?Cozzolino Anne?Faber Michael?Haus Dominik?Huth Alfons?Kemper Andreas?Kipf Helmut?Krcmar Florian?MatthesEmail author J?rg?Ott Christian?Prehofer Alexander?Pretschner ?mer?Uluda? Wolfgang?W?rndl 《Informatik-Spektrum》2017,40(2):180-191