Search results for "DASE"

Therapeutic effect of enhancing endothelial nitric oxide synthase (eNOS) expression and preventing eNOS uncoupling

2011

Nitric oxide (NO) produced by the endothelium is an important protective molecule in the vasculature. It is generated by the enzyme endothelial NO synthase (eNOS). Similar to all NOS isoforms, functional eNOS transfers electrons from nicotinamide adenine dinucleotide phosphate (NADPH), via the flavins flavin adenine dinucleotide and flavin mononucleotide in the carboxy-terminal reductase domain, to the heme in the amino-terminal oxygenase domain. Here, the substrate L-arginine is oxidized to L-citrulline and NO. Cardiovascular risk factors such as diabetes mellitus, hypertension, hypercholesterolaemia or cigarette smoking reduce bioactive NO. These risk factors lead to an enhanced productio…

Stereoselective synthesis of 1-aminoalkanephosphonic acids with two chiral centers and their activity towards leucine aminopeptidase

2003

The stereoselective synthesis of 1-amino-2-alkylalkanephosphonic acids, namely, compounds bearing two chiral centers, was achieved by the condensation of hypophosphorous acid salts of (R)(+) or (S)(-)-N-alpha-methylbenzylamine with the appropriate aldehydes in isopropanol. Simultaneous deprotection and oxidation by the action of bromine water provided equimolar mixtures of the RS:RR and SR:SS diastereomers of desired acids. They appeared to act as moderate inhibitors of kidney leucine aminopeptidase with potency dependent on the absolute configuration of both centers of chirality.

Über die Hemmung der Arginase durch Stickstofflost

1952

Liver arginase is completely inhibited by nitrogen mustard [tris-(β-chloroethyl)amine, HCl] at a final concentration of 4.6×10−4 M. This holds true for isolated liver cell nuclei also. The experimental conditions are described exactly.

A new method for the cytochemical demonstration ofp-diphenol: O2 oxidoreductase (laccase)

1971

Nachweis des Enzymsp-Diphenol: O2 oxidoreductase (Laccase) in den Zellen der PilzeAspergillus fumigatus, Aureobasidium pullulans undNeurospora sitophila durch einen Azofarbstoff, der mittels Kupplung des enzymatisch gebildetenp-Chinons mitBesthorn's Hydrazon(3-Methyl-benzthiazolon(2)-hydrazon-hydrochlorid) entsteht. Als Substrat wird Hydrochinon verwendet. Der Farbstoff wird in runden, rotbraunen Granula abgelagert. Kontrollreaktionen bestatigen die Spezifitat der Reaktion.

A phosphonamidate containing aromatic N-terminal amino group as inhibitor of leucine aminopeptidase-design, synthesis and stability.

2006

Fully deprotected phosphonamidate dipeptides, predicted as effective inhibitors of cytosolic leucine aminopeptidase, showed unexpected instability in water solution at pH below 12. Their hydrolysis rate was strictly correlated with basicity of the N-terminal amino group. To improve this feature a phosphonamidate analogue containing less basic, aromatic 2-aminophenylphosphonate residue in P1 position of the inhibitor was designed. The target compound was synthesised starting from diethyl 2-nitrophosphonate in several step procedure. The decrease in basicity of the terminal amino moiety of the modified analogue in fact resulted in satisfactory improvement of hydrolytic stability of the P–N bo…

Antidepressant drugs and memory: Insights from animal studies

2007

This is a selective review of the literature concerning the effects of antidepressant drugs on animal memory, which was performed with the aid of the PubMed database. Monoamine oxidase inhibitors tend to either have no effect on memory or result in its improvement. Studies with cyclic antidepressants have reported no effect or, more often, memory impairments. Pre-training administration of selective serotonin reuptake inhibitors (SSRIs) has been shown to have either no effect on memory or undermine it (with some isolated exceptions, in which improvements have been recorded), while post-training administration of SSRIs has been demonstrated to improve memory or have no effect. A small group …

A Phase III Extension Study of Aldurazyme®(Laronidase) in Mucopolysaccharidosis I

2007

Metabolism of phenol in the terrestrial snail Cepaea nemoralis L

1992

1. The metabolism of phenol in the terrestrial snail Cepaea nemoralis was studied after injection into the haemocoel of the dorsolateral foot region. 2. Excreted metabolites, and metabolites extracted from the body, were analysed by h.p.l.c. In addition to phenyl beta-D-glucoside, arbutine (quinol beta-D-glucoside), a new conjugate of phenol, was detected.

In vivo activity of pseudoguaianolide sesquiterpene lactones in acute and chronic inflammation.

2000

The pseudoguaianolide sesquiterpene lactones 4-alpha-O-acetyl-pseudoguaian-6beta-olide (1), hymenin (2), ambrosanolide (3), tetraneurin A (4), parthenin (5), hysterin (6) and confertdiolide (7) were evaluated for their ability to affect the inflammation responses induced by different agents. All the compounds showed activity against the 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced mouse ear edema. The ethyl phenylpropiolate (EPP)-induced mouse ear edema was inhibited by compounds 3, 5 and 7. However, when sesquiterpene-lactones were assayed on the arachidonic acid (AA)-induced mouse ear edema, none of them were active. The only sesquiterpene lactone orally active against the paw mouse…

The effect of sea water on cytochrome oxidase and oxidative phosphorylation.

1961

Piccole quantita di acqua di mare causano una forte inibizione della fosforilazione ossidativa, mentre l'effetto sulla attivita citocromossidasica e piuttosto modesto. L'ione responsabile di questo effetto e il Calcio.