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  • 1
    Digitale Medien
    Digitale Medien
    Increased dose-response relationship of liver plasma membrane adenylate cyclase to glucagon stimulation in diabetic rats. A possible role of the guanyl nucleotide-binding regulatory protein (1982)
    Springer
    Diabetologia 22 (1982), S. 464-467 
    Details
    ISSN: 1432-0428
    Schlagwort(e): Streptozotocin diabetes ; glucagon stimulation ; adenylate cyclase dose response relationship ; stimulatory effect of guanosine triphosphate ; guanyl nucleotide-depending regulatory protein
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary In view of controversial findings regarding the mechanism for the increased intracellular hepatic cyclic 3′:5′ adenosine monophosphate levels in diabetic rats, we studied the dose-response relationship of the adenylate cyclase to glucagon stimulation in severely diabetic and in diabetic, insulin-treated rats. An enhanced response to glucagon and an additional augmenting effect of guanosine triphosphate on hormonal stimulation of the adenylate cyclase activity were found in diabetes which were reversible with insulin treatment. The results suggest a role of the regulatory guanyl nucleotide-binding protein in diabetes leading to an increased dose response relationship of the hepatic adenylate cyclase system to glucagon.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00282591
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  • 2
    Digitale Medien
    Digitale Medien
    Studies on the in vitro binding of D-penicillamine to cholestyramine (1982)
    Springer
    Cellular and molecular life sciences 38 (1982), S. 482-484 
    Details
    ISSN: 1420-9071
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary Adsorption of D-penicillamine to cholestyramine depends on the amount of the resin, the pH and the presence of other compounds such as bile salts. In the usual drug to resin ratio (150 mg D-penicillamine and 4–8 g cholestyramine per single dose) the percentage of D-penicillamine adsorbed to cholestyramine was about 10% of the applied dose; Bile salts (10 mmoles/1) inhibited this small adsorption by 87%.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01952651
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  • 3
    Digitale Medien
    Digitale Medien
    Human colonic (Na++K+)-ATPase and specific ouabain binding are not influenced by lipoxygenase products or superoxide radicals (1988)
    Springer
    Journal of molecular medicine 66 (1988), S. 599-600 
    Details
    ISSN: 1432-1440
    Schlagwort(e): Colonic (Na++K+)-ATPase ; Specific ouabain binding ; Lipoxygenase pathway products ; Superoxide radicals
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The effects of lipoxygenase products (5-, 12-, 15-HETE, LTB4) and superoxide radicals on human colonic (Na++K+)-ATPase and specific ouabain binding were measured. No significant inhibition in concentrations up to 3 × 10−5 M was observed. The results are discussed with regard to a possible role of lipoxygenase products and radicals in the pathogenesis of water and electrolyte disturbances in various diarrheal states including inflammatory bowel disease.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01720836
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  • 4
    Digitale Medien
    Digitale Medien
    Soybean lipoxygenase inhibition: Studies with the sulphasalazine metabolites N-acetylaminosalicylic acid, 5-aminosalicylic acid and sulphapyridine (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 449-451 
    Details
    ISSN: 1432-1041
    Schlagwort(e): lipoxygenase inhibition ; antiinflammatory drugs ; N-acetyl-aminosalicylic acid ; 5-aminosalicylic acid ; sulphapyridine ; soybean ; therapeutic actions ; ulcerative colitis
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Soybean lipoxygenase inhibition has been proposed as an in vitro biochemical model for the antiinflammatory action of certain drugs used in the treatment of ulcerative colitis. In an extension of a recent study which showed that therapeutically active compounds, such as sulphasalazine and its colonic metabolite 5-aminosalicylic acid were soybean lipoxygenase inhibitors, it has now been shown that N-acetylaminosalicylic acid, the principal metabolite of 5-aminosalicylic acid, also inhibits soybean lipoxygenase in a dose dependent and noncompetitive manner (Ki 3.0×10−8M, IC50 250 µM). Sulphapyridine, the other major metabolite of sulphasalazine, which has been demonstrated to be inactive in the treatment of ulcerative colitis, did not inhibit the lipoxygenase activity. The findings further support the hypothesis that only the therapeutically active compounds are soybean lipoxygenase inhibitors.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00542139
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  • 5
    Digitale Medien
    Digitale Medien
    Lack of effect of haemodialysis on mebendazole kinetics: Studies in a patient with echinococcosis and renal failure (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 243-245 
    Details
    ISSN: 1432-1041
    Schlagwort(e): mebendazole ; haemodialysis ; echinococcosis ; pharmacokinetics ; protein binding
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The effect of haemodialysis on mebendazole kinetics has been studied in a patient receiving both mebendazole therapy and haemodialysis. The procedure of haemodialysis did not influence the plasma concentration — time profiles or the mean daily plasma levels. The arterio-venous difference in the dialyser was negligible and no mebendazole could be detected in the dialysate. Protein binding of mebendazole was 90% before dialysis and 88% during dialysis and not significantly different from the binding in patients without renal disease (91.4±1.9%, n=22).
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00544053
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  • 6
    Digitale Medien
    Digitale Medien
    Comparative pharmacokinetics of sulphasalazine and sulphapyridine after rectal and oral administration to patients with ulcerative colitis (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 275-277 
    Details
    ISSN: 1432-1041
    Schlagwort(e): sulphapyridine ; sulphasalazine ; pharmacokinetics ; rectal administration ; oral administration ; plasma levels ; ulcerative colitis
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Rectal administration of sulphasalazine to patients with ulcerative colitis has recently been shown to have similar therapeutic activity but fewer side effects than oral treatment. The present study is a comparison of the pharmacokinetics of sulphasalazine (SASP) and its metabolite sulphapyridine (SP) after rectal and oral administration of SASP to 6 patients with ulcerative colitis. The areas under the concentration-time curves (AUC) and the maximum concentrations (Cmax) of SASP and SP were significantly lower after rectal than oral administration of SASP (p〈0.05). These findings support the view that the lower frequency of side effects after rectal administration of SASP may result from the lower plasma levels of SASP and SP.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00630300
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  • 7
    Digitale Medien
    Digitale Medien
    Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease (2003)
    Oxford, UK : Blackwell Publishing Ltd
    Alimentary pharmacology & therapeutics 18 (2003), S. 0 
    Details
    ISSN: 1365-2036
    Quelle: Blackwell Publishing Journal Backfiles 1879-2005
    Thema: Medizin
    Notizen: A series of epidemiological, experimental and preliminary clinical trials strongly suggest that mesalazine or 5-aminosalicyclic acid (5-ASA) may have antineoplastic and potentially prophylactic chemopreventive properties. It is assumed that mesalazine may have similar genetic and molecular targets as nonsteroidal anti-inflammatory drugs (NSAIDs), which is further supported by its close similarity with aspirin, differing only in its structure by the presence of an amino group at position 5 of the benzene ring. The putative chemopreventive actions include the inhibition of inflammatory cascades and/or reactions involved in cell growth and proliferation, such as cyclo-oxygenase (COX-1 and COX-2), which regulate cell proliferation through the formation of prostaglandins; lipoxygenase; nuclear factor κB (NFκB), responsible for the subsequent expression of pro-inflammatory molecules; MAP kinases and Bcl-2, as well as the activation of apoptotic processes, such as the stimulation of intestinal sphingomyelinase. The peroxisome-proliferator-activated receptor δ (PPARδ), which also regulates gene transcription, is thought to play a role in both inflammatory and non-inflammatory driven carcinogenesis. This may be another significant target. It is hypothesized that 5-ASAs may prevent the enhancing effect of prostaglandins on PPARδ binding to DNA by its COX inhibitory properties, decreasing proliferation of colorectal mucosal cells in non-inflammatory bowel disease patients with sporadic polyps of the large bowel.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1046/j.1365-2036.18.s2.1.x
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  • 8
    Digitale Medien
    Digitale Medien
    Clinical relevance of oxygen radicals in inflammatory bowel disease — Facts and fashion (1991)
    Springer
    Journal of molecular medicine 69 (1991), S. 1001-1003 
    Details
    ISSN: 1432-1440
    Schlagwort(e): Inflammatory bowel disease ; Oxygen radicals-superoxide ; Hydroxyl ; Myeloperoxidase ; Chemoluminescence ; Animal models ; Aminosalicylates
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary Oxygen radicals particularly superoxide and hydroxyl radicals are very reactive species believed to be involved in cell and tissue damage in a variety of diseases including inflammatory bowel disease (IBD). Today there are four major arguments for such a role in IBD: Infiltration of the inflamed intestinal mucosa with myeloperoxidase containing activated neutrophils able to produce superoxide, hydroxyl and hypochlorite, increased chemoluminescence response of peripheral and mucosal phagocytic cells to various stimuli, decreased inflammation following specific scavenger treatment in animal models of colitis and defined radical scavenger and inhibitory properties of drugs, especially aminosalicylates used in the therapy of IBD. In the absence of a specific therapy, radical scavenging and/or inhibition may be an adjunctive modality in IBD.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01645146
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  • 9
    Digitale Medien
    Digitale Medien
    Effect of olsalazine and mesalazine on human ileal and colonic (Na+ + K+)-ATPase (1993)
    Springer
    Journal of molecular medicine 71 (1993), S. 286-289 
    Details
    ISSN: 1432-1440
    Schlagwort(e): (Na+ + K+)-ATPase ; Inflammatory bowel disease ; Diarrhea ; 5-Aminosalicyclic acid ; Olsalazine ; Mesalazine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary Olsalazine (azodisalicylate) and mesalazine (5-aminosalicylic acid) have recently been developed as new treatment modalities for inflammatory bowel disease to avoid sulfasalazine-related side effects. However, there are reports regarding new and hitherto unexpected side effects in some patients receiving olsalazine or mesalazine, such as watery diarrhea. Since sodium pump activities play an important role in the pathogenesis of water and electrolyte disturbances, we investigated the influence of olsalazine and mesalazine on human ileal and colonic (Na+ + K+)-ATPase and its specific [3H]-ouabain binding. We found a concentration-dependent inhibition of ileal and colonic (Na+ + K+)-ATPase by olsalazine with an IC50 of 4.1 mM and 4.8 mM, respectively. Mesalazine inhibited this enzyme in the ileum with an IC50 of 4.5 mM and in the sigmoid colon with an IC50 3.5 mM. In addition, [3H]-ouabain binding was inhibited by mesalazine with an IC50 of 3.6 mM. The maximal inhibition, however, did not exceed 80% under any conditions (up to 10 mM drug concentration). Olsalazine and mesalazine induce inhibition of the ileal and colonic sodium pump activities that may (in addition to other possible mechanisms) mediate impaired water and electrolyte absorption. This is possibly of clinical relevance in patients with severely damaged mucosa. In patients with milder forms of mucosal inflammation, this inhibition most likely is of minor importance because of the great capacitiy of the (Na+ + K+)-ATPase and the incomplete inhibition leaving at least 20% of the enzyme activity intact.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00184728
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  • 10
    Digitale Medien
    Digitale Medien
    Can cyclosporin prevent proctocolectomy in severe steroid-refractory ulcerative colitis? Lessons from a case report (1993)
    Springer
    Digestive diseases and sciences 38 (1993), S. 380-382 
    Details
    ISSN: 1573-2568
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF01307563
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