The efficacy of anti-inflammatory agents with respect to extracellular phospholipase A2 activity.
The effects of steroidal and non-steroidal anti-inflammatory agents on extracellular phospholipase A2 (PLA2) activity were investigated. Enzyme release was inhibited by 5 x 10(-8) M dexamethasone but not by indomethacin, whereas the soluble extracellular enzyme was inactivated by mepacrine but not by dexamethasone or indomethacin. PLA2, released into the interstitium by activated macrophages is both pro-inflammatory and vasoactive. The anti-inflammatory efficacy of steroidal and non-steroidal drugs may partially reside in their ability to inhibit the release of PLA2, or inactivate preformed extracellular PLA2 in chronically inflamed sites.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D003513:Cycloheximide / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D007213:Indomethacin / Q000494:pharmacology; D010740:Phospholipases / Q000378:metabolism*; D010741:Phospholipases A / Q000037:antagonists & inhibitors / Q000378:metabolism*; D054467:Phospholipases A2; D011796:Quinacrine / Q000494:pharmacology; D011817:Rabbits
D000893:Anti-Inflammatory Agents; D003907:Dexamethasone; D003513:Cycloheximide; D010740:Phospholipases; D010741:Phospholipases A; D054467:Phospholipases A2; D011796:Quinacrine; D007213:Indomethacin