Literature DB >> 8023742

Ebselen is a specific inhibitor of LTB4-mediated migration of human neutrophils.

R A Patrick1, P A Peters, A C Issekutz.   

Abstract

Ebselen is a seleno-organic anti-inflammatory compound with glutathione peroxidase-like activity that has the unique characteristic of mediating the isomerization of 5-HETE and LTB4 to their biologically inactive trans isomers, both directly in fluid phase and indirectly through metabolic pathways in stimulated peripheral blood leukocytes. LTB4 is an inflammatory mediator with potent chemotactic activity for neutrophilic leukocytes. We studied the effects of ebselen on the chemotactic and chemokinetic responses with human-blood-derived neutrophils. With the use of 120-microns-thick 5-microns-pore durapore filters and low BSA concentrations (0.05%) in the chemotaxis buffers, ebselen was evaluated for its effect on both chemotactic and chemokinetic responses to LTB4, C5a, and fMLP. Ebselen at 3-20 microM concentrations inhibited both chemotactic and chemokinetic responses to optimal concentrations of LTB4 without altering chemotactic responses to C5a or fMLP. Likewise, ebselen at 20 microM specifically inhibited LTB4-stimulated transendothelial migration of neutrophils, while not altering responses to C5a nor fMLP.

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Year:  1993        PMID: 8023742     DOI: 10.1007/bf01984060

Source DB:  PubMed          Journal:  Agents Actions        ISSN: 0065-4299


  29 in total

Review 1.  5-Lipoxygenase: a rational target for therapy of inflammatory bowel disease?

Authors:  J L Wallace
Journal:  Trends Pharmacol Sci       Date:  1990-02       Impact factor: 14.819

2.  Acute antiinflammatory and gastric effects of the seleno-organic compound ebselen.

Authors:  S Leyck; M J Parnham
Journal:  Agents Actions       Date:  1990-06

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Authors:  J Grabbe; B M Czarnetzki; M Mardin
Journal:  Lancet       Date:  1982-12-25       Impact factor: 79.321

4.  Control of vascular permeability by polymorphonuclear leukocytes in inflammation.

Authors:  C V Wedmore; T J Williams
Journal:  Nature       Date:  1981-02-19       Impact factor: 49.962

5.  Ebselen reduces the formation of LTB4 in human and porcine leukocytes by isomerisation to its 5S, 12R-6-trans-isomer.

Authors:  P Kuhl; H O Borbe; H Fischer; A Römer; H Safayhi
Journal:  Prostaglandins       Date:  1986-06

6.  Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.

Authors:  D M Gapinski; B E Mallett; L L Froelich; W T Jackson
Journal:  J Med Chem       Date:  1990-10       Impact factor: 7.446

7.  A novel biologically active seleno-organic compound--II. Activity of PZ 51 in relation to glutathione peroxidase.

Authors:  A Wendel; M Fausel; H Safayhi; G Tiegs; R Otter
Journal:  Biochem Pharmacol       Date:  1984-10-15       Impact factor: 5.858

8.  Effect of Ebselen on polymorphonuclear leukocyte adhesion to and migration through cytokine-activated vascular endothelium.

Authors:  A C Issekutz; N Lopes
Journal:  Int J Immunopharmacol       Date:  1992-11

9.  Inhibition of superoxide anion production in guinea pig polymorphonuclear leukocytes by a seleno-organic compound, ebselen.

Authors:  S Ichikawa; K Omura; T Katayama; N Okamura; T Ohtsuka; S Ishibashi; H Masayasu
Journal:  J Pharmacobiodyn       Date:  1987-10

10.  Heterogeneity of human polymorphonuclear leukocyte receptors for leukotriene B4. Identification of a subset of high affinity receptors that transduce the chemotactic response.

Authors:  D W Goldman; E J Goetzl
Journal:  J Exp Med       Date:  1984-04-01       Impact factor: 14.307

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  2 in total

1.  Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening.

Authors:  Daniel J Urban; Wei Zheng; Ozlem Goker-Alpan; Ajit Jadhav; Mary E Lamarca; James Inglese; Ellen Sidransky; Christopher P Austin
Journal:  Comb Chem High Throughput Screen       Date:  2008-12       Impact factor: 1.339

2.  Ebselen improves ischemia-reperfusion injury after rat lung transplantation.

Authors:  Jürg Hamacher; Uz Stammberger; Elvira Weber; Rudolf Lucas; Albrecht Wendel
Journal:  Lung       Date:  2009-02-07       Impact factor: 2.584

  2 in total

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