Search results for "Amide"

An Efficient Synthesis of γ-Aminoacids and Attempts to Drive Its Enantioselectivity

2008

Addition of carboxylic acid dianions to bromoacetonitrile lead, in good yields,to the corresponding gamma-cyanoacids, which on hydrogenation yielded gamma-amino acids. This two step methodology improves upon previously described results. Poor e.e's resultedfrom our attempts to drive the enantioselectivity of this transformation by chiral amide induction.

High Levels of Exogenous C2-Ceramide Promote Morphological and Biochemical Evidences of Necrotic Features in Thyroid Follicular Cells

2002

CD95 and ceramide are known to be involved in the apoptotic mechanism. The triggering of CD95 induces a cascade of metabolic events that progressively and dramatically modifies the cell shape by intense membrane blebbing, leading to apoptotic bodies production. Although the CD95 pathway has been abundantly described in normal thyrocytes, the effects of cell permeable synthetic ceramide at morphological and biochemical levels are not fully known. In the present study, we show that thyroid follicular cells (TFC) exposed to 20 μM of C2-ceramide for 4 h are characterized by morphological features of necrosis, such as electron-lucent cytoplasm, mitochondrial swelling, and loss of plasma membrane…

Synthesis, Characterization, Thermal and Antimicrobial studies of N-substituted Sulfanilamide derivatives

2014

Abstract Four sulfanilamide derivatives N -[4-(phenylsulfamoyl)phenyl]acetamide (1), 4-amino- N -phenylbenzenesulfonamide (2), N -[4-(phenylsulfamoyl)phenyl]benzamide (3) and N -{4-[(3-chlorophenyl)sulfamoyl]phenylbenzamide (4) were synthesized and characterized by Infra-Red (IR), Nuclear Magnetic Resonance (NMR) and UV–visible (UV–Vis) spectra. Also Liquid Chromatographic (LCMS) and High Resolution Mass Spectrometric (HRMS) methods were used. Crystal structures of 1–4 were determined by single crystal X-ray diffraction (XRD) and their conformational and hydrogen bond (HB) network properties were examined with survey of the literature data. Compounds 1 and 2 crystallize in the same orthorho…

Plasma membrane and lysosomal localization of CB1 cannabinoid receptor are dependent on lipid rafts and regulated by anandamide in human breast cance…

2005

AbstractIn this report we show, by confocal analysis of indirect immunofluorescence, that the type-1 cannabinoid receptor (CB1R), which belongs to the family of G-protein-coupled receptors, is expressed on the plasma membrane in human breast cancer MDA-MB-231 cells. However, a substantial proportion of the receptor is present in lysosomes. We found that CB1R is associated with cholesterol- and sphyngolipid-enriched membrane domains (rafts). Cholesterol depletion by methyl-β-cyclodextrin (MCD) treatment strongly reduces the flotation of the protein on the raft-fractions (DRM) of sucrose density gradients suggesting that CB1 raft-association is cholesterol dependent. Interestingly binding of …

Evidence for a modulatory role of cannabinoids on the excitatory NANC neurotransmission in mouse colon

2007

Abstract It is well accepted that endogenous cannabinoids and CB1 receptors are involved in the regulation of smooth muscle contractility and intestinal motility, through a mechanism mainly related to reduction of acetylcholine release from cholinergic nerve endings. Because, few data exist on a possible modulatory action of the cannabinoid agents on the non-adrenergic non-cholinergic (NANC) excitatory and inhibitory neurotransmission, the aim of the present study was to investigate the effects of cannabinoid drugs on the NANC responses elicited by electrical field stimulation (EFS) in the circular muscle of mouse proximal colon. Colonic contractions were monitored as changes in endoluminal…

Carbonyl reductase 1 is a predominant doxorubicin reductase in the human liver.

2008

A first step in the enzymatic disposition of the antineoplastic drug doxorubicin (DOX) is the reduction to doxorubicinol (DOX-OL). Because DOX-OL is less antineoplastic but more cardiotoxic than the parent compound, the individual rate of this reaction may affect the antitumor effect and the risk of DOX-induced heart failure. Using purified enzymes and human tissues we determined enzymes generating DOX-OL and interindividual differences in their activities. Human tissues express at least two DOX-reducing enzymes. High-clearance organs (kidney, liver, and the gastrointestinal tract) express an enzyme with an apparent Km of approximately 140 microM. Of six enzymes found to reduce DOX, Km valu…

Link between Intestinal CD36 Ligand Binding and Satiety Induced by a High Protein Diet in Mice

2012

International audience; CD36 is a ubiquitous membrane glycoprotein that binds long-chain fatty acids. The presence of a functional CD36 is required for the induction of satiety by a lipid load and its role as a lipid receptor driving cellular signal has recently been demonstrated. Our project aimed to further explore the role of intestinal CD36 in the regulation of food intake. Duodenal infusions of vehicle or sulfo-N-succinimidyl-oleate (SSO) was performed prior to acute infusions of saline or Intralipid (IL) in mice. Infusion of minute quantities of IL induced a decrease in food intake (FI) compared to saline. Infusion of SSO had the same effect but no additive inhibitory effect was obser…

SYNTHETIC AND BIOLOGICAL EVALUATION OF SOME NEW 2-CINNAMAMIDOBENZAMIDES AS POTENTIAL ANTAGONIST OF THE HDM2-P53 PROTEIN-PROTEIN INTERACTIONS

2008

The dynamic properties of neuronal chromatin are modulated by triiodothyronine.

1992

The effect of triiodothyronine (T3) on the rate of synthesis of nuclear proteins was studied during terminal differentiation of rat cortical neurons cultured in a serum-free medium. To this aim total and acid soluble nuclear proteins were analyzed by different electrophoretic techniques. Our results show that: 1) during maturation in vitro, neuronal nuclei undergo a dramatic change in the rate at which different classes of histones and high mobility group (HMG) proteins are synthesized; the synthetic activity, measured as incorporation of radioactive precursors into nuclear proteins, slows indeed down with age: especially evident is the decrease in core histones synthesis; at day 15, on the…

Kopējo cukuru un pentožu noteikšana bērza koksnes hidrotermiskās apstrādes šķidrumos

2017

Kopējo cukuru un pentožu noteikšana bērza koksnes hidrotermiskās apstrādes šķidrumos. Briede L., zinātniskie vadītāji: Dr. chem. Vīksna A. un Dr. sc. ing Aivars Žūriņš, konsultante MSc. Meile K. Maģistra darbs, 55 lappuses, 29 attēli, 10 tabulas, 4 pielikumi, 45 literatūras avoti. Latviešu valodā. Maģistra darbā pētīts, pie kādiem bērza koksnes hidrotermiskās apstrādes apstākļiem, temperatūras un laika, izmainās saturs – sausnei, kopējiem cukuriem un kopējām pentozēm hidrotermiskās apstrādes šķidrumos. Kopējie cukuri noteikti, izmantojot jodometrisko titrēšanu, bet kopējās pentozes – UPLC apvienojumā ar ELSD detektoru. Eksperimentāli noteikti nepieciešamie hromatogrāfijas metodes apstākļi –…