Search results for "β"
showing 10 items of 509 documents
Biodegradable hydrogels obtained by photocrosslinking of dextran and polyaspartamide derivatives
2003
The functionalization of dextran with glycidyl methacrylate (GMA) leads to the formation of a derivative that generates hydrogels for irradiation at 365nm. The effects of various polymer concentrations and irradiation times on the yield and the properties of the obtained hydrogels are reported. The networks have been characterized by FT-IR spectra, dimensional analysis and swelling measurements carried out at different pH values. In vitro studies suggest that all samples undergo a partial chemical hydrolysis, whereas the incubation with dextranases causes a total degradation whose rate depends on the degree of crosslinking. In addition, aqueous solutions of functionalized dextran have been …
Design, Synthesis and Biological Evaluation of 7-Chloro-9
2019
Glycogen synthase kinase-3β (GSK-3β) represents a relevant drug target for the treatment of neurodegenerative pathologies including Alzheimer’s disease. We herein report on the optimization of a novel class of GSK-3β inhibitors based on the tofacitinib-derived screen hit 3-((3R,4R)-3-((7-chloro-9H-pyrimido[4,5-b]indol-4-yl)(methyl)amino)-4-methylpiperidin-1-yl)-3-oxopropanenitrile (1). We synthesized a series of 19 novel 7-chloro-9H-pyrimido[4,5-b]indole-based derivatives and studied their structure–activity relationships with focus on the cyanoacetyl piperidine moiety. We unveiled the crucial role of the nitrile group and its importance for the activity of this compound series. A successfu…
Chemical composition and biological activity of Salvia verbenaca essential oil
2011
Salvia verbenaca L. (syn. S. minore) is a perennial herb known in the traditional medicine of Sicily as “spaccapetri” and is used to resolve cases of kidney stones, chewing the fresh leaves or in decoction. The chemical composition of the essential oil obtained from aerial parts of S. verbenaca collected in Piano Battaglia (Sicily) on July 2009, was analyzed by GC and GC-MS. The oil was strongly characterized by fatty acids (39.5%) and carbonylic compounds (21.2%), with hexadecanoic acid (23.1%), ( Z)-9-octadecenoic acid (11.1%) and benzaldehyde (7.3%) as the main constituents. The in vitro activity of the essential oil against some microorganisms in comparison with chloramphenicol by the …
The chemical composition of the aerial parts essential oil of four Phagnalon species collected in Sicily (Italy) and Greece
2022
The genus Phagnalon Cass., included in the Asteraceae family, has a wide distribution, expanding from Macaronesia in the West to the Himalayas in the East, from South France and Nord Italy to Ethiopia and Arabian Peninsula. Various species of Phagnalon have been used in the popular medicine of several countries as medicinal herbs and food. The extracts and the secondary metabolites, have a varied application spectrum at several biological levels, with antimicrobial, antioxidant, antidiabetic, antitumor, etc. properties having been reported. The essential oils of four taxa, Phagnalon rupestre, Phagnalon saxatile var. viride, and Phagnalon rupestre subsp. illyricum var. metlesicsii collected …
Macrophage MerTK promotes profibrogenic cross-talk with hepatic stellate cells via soluble mediators
2022
Background & aims: Activation of Kupffer cells and recruitment of monocytes are key events in fibrogenesis. These cells release soluble mediators which induce the activation of hepatic stellate cells (HSCs), the main fibrogenic cell type within the liver. Mer tyrosine kinase (MerTK) signaling regulates multiple processes in macrophages and has been implicated in the pathogenesis of non-alcoholic steatohepatitis-related fibrosis. In this study, we explored if MerTK activation in macrophages influences the profibrogenic phenotype of HSCs. Methods: Macrophages were derived from THP-1 cells or differentiated from peripheral blood monocytes towards MerTK+/CD206+/CD163+/CD209- macrophages. Th…
Intrinsic defects induced by β-irradiation in silica
2002
We report an electron paramagnetic resonance study of defects induced by β-irradiation in natural and synthetic samples of high purity commercial silica. Data are collected for the E′ centers and a resonance satellite signal split by 1.36 mT. By comparison with the effects of γ-irradiation it is shown that the mechanisms of defect generation are the same for the two irradiation sources and that in the high-dose limit they involve intrinsic defects of the glassy matrix. Moreover, the high concentration of defects generated by β-irradiation modifies the EPR spectrum due to spin–spin interaction.
Mutilation of RNA phage Qβ virus-like particles: from icosahedrons to rods
2000
Icosahedral virus-like particles (VLPs) of RNA phage Qbeta are stabilized by four disulfide bonds of cysteine residues 74 and 80 within the loop between beta-strands F and G (FG loop) of the monomeric subunits, which determine the five-fold and quasi-six-fold symmetry contacts of the VLPs. In order to reduce the stability of Qbeta VLPs, we mutationally converted the amino acid stretch 76-ANGSCD-81 within the FG loop into the 76-VGGVEL-81 sequence. It led to production in Escherichia coli cells of aberrant rod-like Qbeta VLPs, along with normal icosahedral capsids. The length of the rod-like particles exceeded 4-30 times the diameter of icosahedral Qbeta VLPs.
Neuronal activity and secreted amyloid β lead to altered amyloid β precursor protein and presenilin 1 interactions.
2013
Deposition of amyloid β (Aβ) containing plaques in the brain is one of the neuropathological hallmarks of Alzheimer's disease (AD). It has been suggested that modulation of neuronal activity may alter Aβ production in the brain. We postulate that these changes in Aβ production are due to changes in the rate-limiting step of Aβ generation, APP cleavage by γ-secretase. By combining biochemical approaches with fluorescence lifetime imaging microscopy, we found that neuronal inhibition decreases endogenous APP and PS1 interactions, which correlates with reduced Aβ production. By contrast, neuronal activation had a two-phase effect: it initially enhanced APP-PS1 interaction leading to increased …
Updated insights into the mechanism of action and clinical profile of the immunoadjuvant QS-21: A review
2019
Background Vaccine adjuvants are compounds that significantly enhance/prolong the immune response to a co-administered antigen. The limitations of the use of aluminium salts that are unable to elicite cell responses against intracellular pathogens such as those causing malaria, tuberculosis, or AIDS, have driven the development of new alternative adjuvants such as QS-21, a triterpene saponin purified from Quillaja saponaria. Purpose The aim of this review is to attempt to clarify the mechanism of action of QS-21 through either receptors or signaling pathways in vitro and in vivo with special emphasis on the co-administration with other immunostimulants in new adjuvant formulations, called a…
Action of low doses of Aspirin in Inflammation and Oxidative Stress induced by aβ
2019
Aspirin has been used as anti-inflammatory and anti-aggregate for decades but the precise mechanism(s) of action after the presence of the toxic peptide Aβ1-42 in cultured astrocytes remains poorly resolved. Here we use low-doses of aspirin (10-7 M) in astrocytes in primary culture in presence or absence of Aβ1-42 toxic peptide. We noted an increase of cell viability and proliferation with or without Aβ1-42 peptide presence in aspirin treated cells. In addition, a decrease in apoptosis, determined by Caspase 3 activity and the expression of Cyt c and Smac/Diablo, were detected. Also, aspirin diminished necrosis process (LDH levels), pro-inflammatory mediators (IL-β and TNF-α) and NF-ᴋB prot…