Search results for " α"
showing 10 items of 85 documents
New crystal structures of fluorinated α-aminophosphonic acid analogues of phenylglycine
2020
The four novel phosphonic acid analogues of phenylglycine with various substituents in phenyl ring (mostly fluorine atoms) have been synthesized by using procedure of amidoalkylation of phosphorus trichloride with aromatic aldehydes and acetamide. The NMR, ESI-MS spectroscopy, and single-crystal X-Ray diffraction methods were used to characterize unusual structures: the amino-(4-trifluoromethylbenzyl)-(1), amino-(3,4-difluorobenzyl)-(2), amino-(2,4,6-trifluorobenzyl)-(3), and amino-(2-fluoro-4-hydroxybenzyl)-(4) phosphonic acids. Since the α-aminophosphonates have a potential for biological activity and could be used as building blocks in medicinal chemistry, it is important to know their d…
Antioxidant activity and enzymes inhibitory properties of several extracts from two Moroccan Asteraceae species
2018
Abstract The present work reports investigation on phenolic compounds, antioxidant activity and enzyme inhibitory activities (acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase and α-glucosidase) of different extracts from two Moroccan Asteraceae species; Bubonium imbricatum Cav. and Cladanthus arabicus (L.) Cass. B. imbricatum extracts contained the highest amounts of phenolics and flavonoids, and also exhibited higher antioxidant activity. In this species, the highest total phenolic (1611.13 ± 14.23 μmolGAE/gextract) and flavonoid (376.11 ± 8.22 μmolQE/gextract) contents were observed in aqueous-methanol extract obtained by maceration. Further, UHPLC–MS analysis of C. arab…
[1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors
2016
Abstract A series of [1,2]Oxazolo [5,4- e ]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the 1 HNMR spectra, the typical signal in the 8.34–8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosi…
Safety and efficacy of intra-articular anti-tumor necrosis factor α agents compared to corticosteroids in a treat-to-target strategy in patients with…
2015
The aim of this study was to assess safety and efficacy of ultrasonography (US)-guided intra-articular injections using tumor necrosis factor (TNF) blockers compared to corticosteroids in rheumatoid arthritis (RA) or psoriatic arthritis (PsA) patients, experiencing refractory monoarthritis despite the current systemic therapy. Eighty-two patients were randomized to receive three intra-articular injections monthly of either corticosteroid or TNF blockers. Primary endpoints were the safety and an improvement greater than 20% for visual analogic scales of involved joint pain in patients injected with anti-TNFα. Further clinical, US, and magnetic resonance imaging (MRI) evaluations were consid…
PPMS onset upon adalimumab treatment extends the spectrum of anti-TNF-α therapy-associated demyelinating disorders
2020
Since their introduction in 1999, anti-tumour necrosis factor-α (anti-TNF-α) therapies have been suspected repeatedly to be associated with the occurrence of central nervous system (CNS) demyelinating disorders, including multiple sclerosis (MS). However, recent publications were restricted to descriptions of monophasic demyelinating events or cases of relapsing–remitting MS (RRMS). We here provide the first case report of primary progressive MS (PPMS) onset upon anti-TNF-α therapy as well as a literature review of previously published cases of anti-TNF-α therapy-associated MS onset. The 51-year old male patient was treated with adalimumab due to psoriasis arthritis. About 18 months after …
The Small Heat Shock Protein α-Crystallin B Shows Neuroprotective Properties in a Glaucoma Animal Model
2017
Glaucoma is a neurodegenerative disease that leads to irreversible retinal ganglion cell (RGC) loss and is one of the main causes of blindness worldwide. The pathogenesis of glaucoma remains unclear, and novel approaches for neuroprotective treatments are urgently needed. Previous studies have revealed significant down-regulation of α-crystallin B as an initial reaction to elevated intraocular pressure (IOP), followed by a clear but delayed up-regulation, suggesting that this small heat-shock protein plays a pathophysiological role in the disease. This study analyzed the neuroprotective effect of α-crystallin B in an experimental animal model of glaucoma. Significant IOP elevation induced b…
Activity of the α-glucoside transporter Agt1 in Saccharomyces cerevisiae cells during dehydration-rehydration events
2018
Microbial cells can enter a state of anhydrobiosis under desiccating conditions. One of the main determinants of viability during dehydration-rehydration cycles is structural integrity of the plasma membrane. Whereas much is known about phase transitions of the lipid bilayer, there is a paucity of information on changes in activity of plasma membrane proteins during dehydration-rehydration events. We selected the α-glucoside transporter Agt1 to gain insights into stress mechanisms/responses and ecophysiology during anhydrobiosis. As intracellular water content of S. cerevisiae strain 14 (a strain with moderate tolerance to dehydration-rehydration) was reduced to 1.5 g water/g dry weight, th…
Anti-Tumor Necrosis Factor α Therapeutics Differentially Affect Leishmania Infection of Human Macrophages
2018
Tumor necrosis factor α (TNFα) drives the pathophysiology of human autoimmune diseases and consequently, neutralizing antibodies (Abs) or Ab-derived molecules directed against TNFα are essential therapeutics. As treatment with several TNFα blockers has been reported to entail a higher risk of infectious diseases such as leishmaniasis, we established an in vitro model based on Leishmania-infected human macrophages, co-cultured with autologous T-cells, for the analysis and comparison of anti-TNFα therapeutics. We demonstrate that neutralization of soluble TNFα (sTNFα) by the anti-TNFα Abs Humira®, Remicade®, and its biosimilar Remsima® negatively affects infection as treatment with these agen…
Trajectories of stress biomarkers and anxious-depressive symptoms from pregnancy to postpartum period in women with a trauma history
2019
Background: Cross-sectional studies have found that a trauma history can be associated with anxious-depressive symptomatology and physiological stress dysregulation in pregnant women. Methods: This prospective study examines the trajectories of both anxiety and depressive symptoms and salivary cortisol and alpha-amylase biomarkers from women with (n = 42) and without (n = 59) a trauma history at (i) 38th week of gestation (T1), (ii) 48 hours after birth (T2), and (iii) three months after birth (T3). Results: The quantile regression model showed that trauma history was associated with higher cortisol levels at T1 and this difference was sustained along T2 and T3. Conversely, there were no si…
Offline commissioning of a new gas cell for the MARA Low-Energy Branch
2023
Results of offline commissioning tests for a new dedicated gas cell for the Mass Analysing Recoil Apparatus (MARA) Low-Energy Branch are reported. Evacuation time, ion survival and transport efficiency in helium buffer gas were characterized with a radioactive 223Ra 𝛼-recoil source. Suppression of the ion signal, originating from non-neutralized species in the gas cell, was explored with 219Rn ions, the daughter recoil of 223Ra, as a function of voltage applied to one of the ion-collector electrodes. Two-step laser resonance ionization of stable tin isotopes produced inside the gas cell from a heated bronze filament was demonstrated, and broadening of the atomic resonances in argon buffer …