Structure-activity of three phospholipid analogues towards inhibition of phospholipase A2 in macrophages.
At concentrations 1-20 microns in culture medium of rat peritoneal macrophages which were stimulated with ionophore A23187, the phospholipid analogues 1-decyl-2-octyl-glycerophosphocholine and 1-dodecyl-2-octanamido-2-deoxy glycerophosphocholine were found more potent inhibitors than 1-octyl-2-deoxy glycerophosphocholine to lower the phospholipase A2 activities. The inhibitory effect was measured by [3H] eicosatetraenoic acid ([3H]20:4) release in macrophages and extracellular fluids and synthesis of [3H] eicosanoids after incubation of macrophages with traces of the molecular species of lecithin 1-octadecanoyl-2-[3H] eicosatetraenoyl glycerophosphocholine. The three phospholipid analogues developed higher inhibitory effects than mepacrine, dexamethasone or bromophenacyl bromide, at corresponding concentrations in medium.
Letourneux
Y
Y
Laboratoire de synthèse et études des substances naturelles à activité biologique, pole sciences, La Rochelle, France.
Bourass
J
J
Boucrot
P
P
Elkihel
L
L
Petit
J Y
JY
D000098:Acetophenones / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D002478:Cells, Cultured; D003470:Culture Media; D003907:Dexamethasone / Q000494:pharmacology; D015777:Eicosanoids / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000201:enzymology*; D008297:Male; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D010743:Phospholipids / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D011796:Quinacrine / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D014316:Tritium
D000098:Acetophenones; D000893:Anti-Inflammatory Agents; D003470:Culture Media; D015777:Eicosanoids; D004791:Enzyme Inhibitors; D010743:Phospholipids; D014316:Tritium; D003907:Dexamethasone; D010741:Phospholipases A; D054467:Phospholipases A2; D011796:Quinacrine; C006821:4-bromophenacyl bromide