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  • 1
    Electronic Resource
    Electronic Resource
    Suppression of arthritis by an active center analogue of Cu2Zn2-superoxide dismutase (1994)
    Springer
    Rheumatology international 14 (1994), S. 119-126 
    Details
    ISSN: 1437-160X
    Keywords: Active center analogues of superoxide dismutase ; Collagen type II-induced arthritis ; Potassium peroxochromate arthritis ; Autoimmunity ; Chemiluminescence ; Inhibition of tumor necrosis factor alpha ; Reactive oxygen species
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The anti-arthritic and anti-inflammatory efficacy of CuPu(Py)2 {[N, N′-bis(2-pyridylmethylene)-1,4-butanediamine] (N, N′, N″, N‴)}-Cu(II), a serum-stable active center analogue of Cu2Zn2-superoxide dismutase (SOD; EC 1.15.1.1), was tested in male DBA/1xB10A (4R) mice suffering from potassium-peroxochromate-induced (PIA) or collagen type II-induced arthritis (CIA). Parameters including the arthritis index, the plasma SOD activity, and the inhibition of phagocytic responses in unseparated blood were used for the assessment of disease activity. A dose-dependent suppression of arthritis was noted in both models. The ED50 was 2.5±0.4 μmol/kg/day of CuPu(Py)2 for PIA and 4.0±1.1 μmol/kg/day for CIA. The arthritis index correlated with both the levels of reactive oxygen species (ROS) generated by phorbol ester-activated neutrophils and monocytes in unseparated blood (r=0.892) and the SOD-like activity in plasma (r=0.857). CuPu(Py)2 inhibited also the lipoplysaccharide-induced release of tumor necrosis factor alpha from human monocytes and neutrophils in a dose-dependent manner. Unlike SOD, which exerts successful anti-rheumatic activity mainly upon intra-articular injection, the SOD-mimic CuPu(Py)2 can be applied systemically. Non-proteinaceous low molecular weight antioxidases may well be suited to control oxidative stress-derived damage in rheumatic diseases by modulation of ROS-dependent signal transduction pathways.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00300814
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  • 2
    Electronic Resource
    Electronic Resource
    Dünnschicht- und gaschromatographische Untersuchungen zum Nachweis und zur Stabilität des Morazons (1976)
    Springer
    Archives of toxicology 35 (1976), S. 213-220 
    Details
    ISSN: 1432-0738
    Keywords: Morazone ; Phenmetrazine ; 4-Hydroxymethylantipyrine ; Bisantipyrylmethane ; Rosimon-Neu® ; Thin layer-chromatography ; Mass-spectrometry ; IR-spectroscopy ; 1H-Nuclear magnetic resonance ; Morazon ; Phenmetrazin ; 4-Hydroxymethylantipyrin ; Bisantipyrylmethan ; Rosimon-Neu® ; Dünnschichtchromatographie ; Massenspektrometrie ; IR-Spektroskopie ; 1H-NMR-Spektrometrie
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Beim Erhitzen von Morazon, welches in der Arzneimittelspezialität Rosimon-Neu® enthalten ist, im salz und weinsauren Milieu wurde eine Zersetzung der Ausgangsverbindung beobachtet. Die Spaltprodukte wurden dünnschichtchromatographisch isoliert und aufgrund der spektroskopischen Daten als Phenmetrazin, Bisantipyrylmethan und 4-Hydroxymethylantipyrin identifiziert. Nach Einnahme von Morazon in therapeutischer Dosierung kann durch zweidimensionale DC diese Substanz neben Phenmetrazin in alkalischen Harnextrakten nachgewiesen werden. Für das Vorliegen von geringen Spuren 4-Hydroxymethylantipyrin ergaben sich Anhaltspunkte. Saure Hydrolyse der Harnproben vor der extraktiven Aufbereitung, die zu den Spaltprodukten Phenmetrazin und Bisantipyrylmethan führt, erhöht die Nachweisempfindlichkeit einer Einnahme von Morazon.
    Notes: Abstract Three decomposition products of Morazone (ingredient of the pharmaceutical preparation Rosimon-Neu®) were observed following heat treatment in acid medium (hydrochloric or tartaric acid). These products were isolated by TLC and identified as bis-antipyryl-methane, phenmetrazine and 4-hydroxymethyl-antipyrine by mass spectrometry and IR-spectroscopy and 1H-nuclear magnetic resonance. Morazone and the metabolite phenmetrazine may be extracted from alkaline urine using chloroform, however acid hydrolysis (pH 1) of the urine before alkaline extraction will improve the sensitivity of detection of morazone by producing the metabolite phenmetrazine in addition to bis-antipyrylmethane. The metabolite 4-hydroxymethyl-antipyrine is barely detectable by TLC from alkaline extraction of urine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00293569
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    Paper (German National Licenses)
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