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Inhibition of alveolar macrophage 5-lipoxygenase metabolism by auranofin.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Peters-Golden, Marc Shelly, Candace A. |
| Copyright Year | 1989 |
| Abstract | We have examined the effect of the oral gold compound auranofin (AF) on calcium ionophore A23187-induced arachidonic acid metabolism in the rat alveolar macrophage. Both reverse-phase high performance liquid chromatographic and radioimmunoassay analyses revealed that AF dose-dependently inhibited leukotriene B4 and 5-hydroxyeicosatetraenoic acid synthesis in a parallel fashion with an IC50 approximately 4.3 micrograms/ml. At the same time, AF augmented A23187-induced arachidonate release and cyclooxygenase metabolism. A possible mechanism for the inhibition of 5-lipoxygenase was suggested by the capacity of AF to dose-dependently deplete ATP (IC50 approximately 5.9 micrograms/ml), a cofactor for 5-lipoxygenase. These data indicate that, at therapeutic concentrations, AF acts in vitro as a selective inhibitor of macrophage 5-lipoxygenase metabolism. This likely represents an important mechanism of action of AF in chronic inflammatory disorders. |
| Starting Page | 137 |
| Ending Page | 139 |
| Page Count | 3 |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | https://deepblue.lib.umich.edu/bitstream/handle/2027.42/27937/0000363.pdf;jsessionid=1E551E7BE0479C108DE8CCFFBC18F570?sequence=1 |
| PubMed reference number | 2499339v1 |
| Volume Number | 38 |
| Issue Number | 10 |
| Journal | Biochemical pharmacology |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | Adenosine Triphosphate Arachidonate 15-Lipoxygenase Arachidonate 5-Lipoxygenase Arachidonic Acid Auranofin Calcium Gold Compounds Inhibitory Concentration 50 Ionophores Leukotriene B4 Leukotrienes Macrophages, Alveolar |
| Content Type | Text |
| Resource Type | Article |