Search results for "A2"
showing 10 items of 1101 documents
Synthesis and pharmacological evaluation of 2'-hydroxychalcones and flavones as inhibitors of inflammatory mediators generation.
1995
2'-Hydroxy-3,4-dimethoxy-3',4'-dimethylchalcone (3a), 2'-hydroxy-3',4',3,4-tetramethoxychalcone (3b), and their corresponding flavones, 3',4'-dimethoxy-7,8-dimethylflavone (4a) and 3',4',7,8-tetramethoxyflavone (4b), were prepared from 3,4-dimethoxycinnamic acid and the respective phenol. The four compounds inhibited enzymic lipid peroxidation and showed weak peroxyl scavenging activity. They also reduced LTB 4 release from human neutrophils stimulated by A23187. The chalcone 3b was the only compound able to inhibit in a concentration-dependent way, synovial human recombinant phospholipase A 2 activity, human platelet TXB 2 generation, and human neutrophil degranulation. This chalcone exert…
Mixed monolayers of natural and polymeric phospholipids: structural characterization by physical and enzymatic methods
1990
This study has focused on physical characterization and enzymatic hydrolysis of mixed monolayers of a natural phospholipid substrate and a polymerizable phospholipid analogue. Such a mixed system presents the possibility to stabilize model biomembranes, vary the molecular environment within the layer through polymerization and simultaneously examine these influences on monolayer structure. Phospholipase A2 was used here as a sensitive probe of the molecular environment within these mixed, polymerizable monolayers to complement information obtained from isotherm and isobar data. The results clearly show a strong influence of molecular environment on phospholipase A2 activity, even if differe…
Role of the central gold atom in ligand-protected biicosahedral Au 24 and Au25 clusters
2013
The crystal structures of the ligand-protected clusters [Au24(PPh3)10(SC2H4Ph)5Cl2]+ and [Au25(PPh3)10(SC2H4Ph)5Cl2]2+ have been elucidated recently, and they comprise the same biicosahedral structural motif for the Au core. The only difference is the central Au atom joining two icosahedra which is absent in the Au24 cluster. On the basis of density functional simulations, we have evaluated the structural, electronic, optical, and vibrational properties of the clusters in question with a full presentation for the thiolate and phosphine side groups. Our spherical harmonics analysis of the electronic structure shows that the chemical stability of both clusters can be understood based on an 8 …
Calcium signatures and signaling in cytosol and organelles of tobacco cells induced by plant defense elicitors
2011
Calcium signatures induced by two elicitors of plant defense reactions, namely cryptogein and oligogalacturonides, were monitored at the subcellular level, using apoaequorin-transformed Nicotiana tabacum var Xanthi cells, in which the apoaequorin calcium sensor was targeted either to cytosol, mitochondria or chloroplasts. Our study showed that both elicitors induced specific Ca2+ signatures in each compartment, with the most striking difference relying on duration. Common properties also emerged from the analysis of Ca2+ signatures: both elicitors induced a biphasic cytosolic [Ca2+] elevation together with a single mitochondrial [Ca2+] elevation concomitant with the first cytosolic [Ca2+] p…
Determination of major human cytochrome P450s activities in 96-well plates using liquid chromatography tandem mass spectrometry.
2007
At the early stage of drug discovery, thousands of new chemical entities (NCEs) may be screened before a single candidate can be identified for development. Evaluation of the effect of NCEs on human CYP450 enzyme activities is a key issue in pharmaceutical development as it may explain inter-subject variability, drug-drug interactions, non-linear pharmacokinetics and toxic effects. A liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method has been developed for the fast and routine analysis of major human CYP450s enzyme activities (CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4) in primary hepatocyte cell cultures. The high sensitivity and selectivity of mass …
Metabolism of Phenanthrene, Benz[a]anthracene, Benzo[a]pyrene, Chrysene and Benzo[c]phenanthrene by Eight cDNA-expressed Human and Rat Cytochromes P4…
1996
Abstract Phenanthrene, benz[a]anthracene, chrysene, benzo[c]phenanthrene, and benzo[a]pyrene have been studied for their regiospecific oxidation by five human (1A1, 1A2, 2A6, 2E1, 3A4) and three rat (1A1, 1A2, 2B1) CYP isoforms. All substrates are preferentially metabolized by CYP1A1 and CYP1A2 in human and rat. Other isoforms play a minor role if at all. Significant differences between human and rat CYP isoforms can be recognized with regard to the regiospecific oxidation of PAH. For instance, K-region oxidation is more pronounced in rat than in human CYP1A1 and CYP1A2. Hence, extrapolation from metabolism studies in rodents to human may be limited.
Some new fixed point results in non-Archimedean fuzzy metric spaces
2013
In this paper, we introduce the notions of fuzzy $(\alpha,\beta,\varphi)$-contractive mapping, fuzzy $\alpha$-$\phi$-$\psi$-contractive mapping and fuzzy $\alpha$-$\beta$-contractive mapping and establish some results of fixed point for this class of mappings in the setting of non-Archimedean fuzzy metric spaces. The results presented in this paper generalize and extend some recent results in fuzzy metric spaces. Also, some examples are given to support the usability of our results.
Radical innovation by theoretical abstraction - a challenge for the user-centred designer
2016
AbstractIt is generally accepted that scientific disciplines such as psychology, sociology, and anthropology contribute beneficially to design by providing understanding of users’ needs, experiences, and desires. Arguably, however, these disciplines have more to contribute, because they include theories and models that can be applied as design frames and principles. More specifically, goal-setting, visualization, thematization, and conceptual reconfiguration are general mechanisms through which theories translate into design contributions. Actualizing radical design solutions via these mechanisms is discussed: theories provide appropriate means of abstraction, which allows ‘distance’ from u…
Existence, uniqueness and comparison results for BSDEs with Lévy jumps in an extended monotonic generator setting
2018
We show existence of a unique solution and a comparison theorem for a one-dimensional backward stochastic differential equation with jumps that emerge from a L\'evy process. The considered generators obey a time-dependent extended monotonicity condition in the y-variable and have linear time-dependent growth. Within this setting, the results generalize those of Royer (2006), Yin and Mao (2008) and, in the $L^2$-case with linear growth, those of Kruse and Popier (2016). Moreover, we introduce an approximation technique: Given a BSDE driven by Brownian motion and Poisson random measure, we consider BSDEs where the Poisson random measure admits only jumps of size larger than $1/n$. We show con…
SAGECELL: Software-Defined Space-Air-Ground Integrated Moving Cells
2018
Ultra-dense networks (UDNs) provide an effective solution to accommodate the explosively growing data traffic of multimedia services and real-time applications. However, the densification of large numbers of static small cells faces many fundamental challenges, including deployment cost, energy consumption and control, and so on. This motivates us to develop software-defined space-air-ground integrated moving cells (SAGECELL), a programmable, scalable, and flexible framework to integrate space, air, and ground resources for matching dynamic traffic demands with network capacity supplies. First, we provide a comprehensive review of state-of-the-art literature. Then the conceptual architectur…