Search results for "CYP"
showing 10 items of 480 documents
Induction of apoptosis by arachidonic acid in human retinoblastoma Y79 cells: involvement of oxidative stress
2000
Arachidonic acid administration caused apoptosis in Y79 cells, as shown by typical morphological changes, phosphatidylserine externalization, chromatin condensation, processing and activation of caspase-3 and cleavage of the endogenous caspase substrate poly-(ADP-ribose)-polymerase. Arachidonic acid also caused lamin B cleavage, suggesting caspase-6 activation. Arachidonic acid treatment was accompanied by increased formation of the lipid peroxidation end products malondialdehyde and 4-hydroxy-2-nonenal, lowering in reduced glutathione content and in mitochondrial membrane potential. Inhibiting glutathione synthesis sensitized Y79 cells to apoptosis-inducing stimuli, whilst replenishing red…
Oxysterols: Influence on plasma membrane rafts microdomains and development of ocular diseases
2015
Oxidation of cholesterol into oxysterols is a major way of elimination of cholesterol from the liver and extrahepatic tissues, including the brain and the retina. Oxysterols are involved in various cellular processes. Numerous links have been established between oxysterols and several disorders such as neurodegenerative pathologies, retinopathies and atherosclerosis. Different components of the lipid layer such as sphingolipids, sterols and proteins participate to membrane fluidity and forme lipid rafts microdomains. Few data are available on the links between lipids rafts and oxysterols. The purpose of this review is to suggest the potential role of lipid rafts microdomains in the developm…
Role of cAMP in mediating AHR signaling.
2009
Regulation of the nuclear import of many transcription factors represents a step in gene regulation which is crucial for a number of cellular processes. The aryl hydrocarbon receptor (AHR), a basic helix-loop-helix protein of the PAS (PER-ARNT-SIM) family of transcriptional regulators is a cytosol-associated and ligand-activated receptor. The environmental toxin dioxin binds with high affinity to AHR rendering it nuclear and leading to the activation of AHR sensitive genes. However, the fact, that the AHR mediates a large variety of physiological events without the involvement of any known exogenous ligand, including liver and vascular system development, maturation of the immune system, re…
CPMAS 13C NMR Characterization of Leaves and Litters from the Reafforestated Area of Mustigarufi in Sicily (Italy)
2010
Reafforestation is generally based on the planting of exotic fast growing tree species suitable for adapting to even harsh environments. Once the introduced plants ameliorate soil conditions, they can be progressively replaced by au- tochthonous plant species. Reafforestation is applied worldwide. However, only few studies on the effect of reafforesta- tion on lands from Mediterranean regions are available. This paper reports the characterization by cross polarization 13C NMR spectroscopy of fresh leaves and superficial litters from a reafforestated area in central Sicily (Italy). NMR assign- ment is attempted. A differentiation among the molecular systems within leaves and litters is also …
Lysine-specific demethylase 1 (LSD1/KDM1A/AOF2/BHC110) is expressed and is an epigenetic drug target in chondrosarcoma, Ewing's sarcoma, osteosarcoma…
2011
Summary Lysine-specific demethylase 1 (GeneID 23028), a flavin-dependent monoamine oxidoreductase and a histone demethylase, serves as an epigenetic coregulator of transcription. Lysine-specific demethylase 1 is up-regulated in neuroblastoma and in bladder, breast, colorectal, gastric, lung, and neuroendocrine cancers, and its overexpression drives the cell cycle of otherwise nontransformed human cells, suggesting oncogenic properties. Lysine-specific demethylase 1 was recently reported to be also overexpressed in several different mesenchymal tumors. We investigated lysine-specific demethylase 1 expression in over 500 sarcomas by gene expression profiling and tissue microarray-coupled immu…
Antimicrobial and antioxidant properties of the essential oil of Salvia lanigera from Cyprus
2010
The essential oil of aerial parts of Salvia lanigera Poir. (Lamiaceae) growing wild in Cyprus was obtained by hydrodistillation and was analysed by GC and GC-MS. A total of 67 compounds, representing 93.6% of the oil, were identified, and the major components were showed to be thymol (12.1%), hexadecanoic acid (6.0%), carvacrol and α-thujone (5.7%). The essential oil was assayed for its antioxidant and antimicrobial activities. Antimicrobial activity of the oil, evaluated using the broth dilution method, resulted higher against Gram-positive bacteria than the other referenced strains tested. Antioxidant activity of the oil was evaluated by using DPPH and FRAP methods together with three ant…
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.
On Antarctoscyphus (Cnidaria, Hydrozoa), a new genus of antarctic hydroids and the description of two new species
1997
A new genus of the hydroid family Sertulariidae is established. Several species formerly assigned to the genus Symplectoscyphus Marktanner-Turneretscher, 1890 are included. A review of those species is given, including their main features along with some remarks. Two species new to science are added; the material of those species was collected in the Scotia Sea by the Spanish Antarctic Expedition “Antartida 8611”. Present autecological data are discussed.
Polymorphism of cytochrome P450 (CYP) genes and response to chemiotherapy in patients with colorectal cancer (CRC)
2014
Background: Genes coding for the cytochrome P450 (CYP) enzyme system implied in antineoplastic drug metabolism pathways are highly polymorphic. This may influence both carcinogen metabolism and drug pharmacodynamics modifying their therapeutic efficacy and side effects. Methods: We investigated the influence of genetic polymorphisms of CYP enzymes: rs1799853 (CYP2C9), rs35742686 (CYP2D), rs5030655 (CYP2D6/3), rs2740574 (CYP3A4/1) rs776746 (CYP3A5) on the response of chemotherapy and clinical outcomes, in a group of 56 patients affected by sporadic CRC, treated with the standard protocols. A total of 44 patients were in complete remission after treatment, 12 had persistence of the disease. P…