INHIBITION OF PHOSPHOLIPASE-A2 PURIFIED FROM HUMAN HERNIATED DISK

被引:12
作者
CARABAZA, A [1 ]
CABRE, F [1 ]
GARCIA, AM [1 ]
GOMEZ, M [1 ]
SANCHEZ, J [1 ]
MAULEON, D [1 ]
CARGANICO, G [1 ]
机构
[1] LABS MENARINI SA, DEPT R&D, ALFONSO XII 587, E-08912 BADALONA, SPAIN
关键词
D O I
10.1016/0006-2952(93)90158-S
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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-C-14]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 muM, respectively). The results are parallel to those obtained with the PLA2 purified from human synovial fluid.
引用
收藏
页码:783 / 786
页数:4
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