Inhibition of phospholipase A2 purified from human herniated disc.
The effect on human herniated intervertebral disc phospholipase A2 (HD-PLA2) of a number of retinoids, antirheumatic drugs and reported PLA2 inhibitors was evaluated using autoclaved [1-14C]-oleate-labeled Escherichia coli membranes as the substrate. Dexamethasone, non-steroidal antiinflammatory drugs, aristolochic acid and retinol were inactive, whereas a marked inhibition was found for manoalide, retinal, nordihydroguaiaretic acid and p-bromophenacyl bromide after preincubation with the enzyme (IC50 values 0.25, 4, 5 and 5 microM, respectively). The results are parallel to those obtained with the PLA2 purified from human synovial fluid.
Carabaza
A
A
R&D Department, Laboratorios Menarini S.A., Badalona, Spain.
Cabré
F
F
García
A M
AM
Gómez
M
M
Sánchez
J
J
Mauleón
D
D
Carganico
G
G
D000098:Acetophenones / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D006801:Humans; D007403:Intervertebral Disc / Q000201:enzymology*; D007405:Intervertebral Disc Displacement / Q000201:enzymology*; D007796:Laminectomy; D009637:Masoprocol / Q000494:pharmacology; D010741:Phospholipases A / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D054467:Phospholipases A2; D012172:Retinaldehyde / Q000494:pharmacology; D013582:Synovial Fluid / Q000201:enzymology; D013729:Terpenes / Q000494:pharmacology
D000098:Acetophenones; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D013729:Terpenes; D009637:Masoprocol; C045673:manoalide; D010741:Phospholipases A; D054467:Phospholipases A2; C006821:4-bromophenacyl bromide; D012172:Retinaldehyde