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- W2068164412 abstract "Tenidap (TD) was initially defined as a dual inhibitor of cyclooxygenase and lipoxygenase. This study was designed to assess its inhibitory activity against proinflammatory phospholipase A 2 . This study shows that TD inhibits the synthesis of pro-inflammatory secretory non-pancreatic phospholipase A 2 (sPLA 2 ). Concentrations as low as 0.25 μg/ml (0.725 μM) reduced the release of sPLA 2 by 40% from foetal rat calvarial osteoblasts stimulated with IL-1β and TNFα, whereas a concentration of 2.5 μg/ml (7.25 μM) reduced the release by over 80%. TD also markedly reduced the release of sPLA 2 from unstimulated cells. There was no direct inhibition of sPLA 2 enzymatic activity by TD in vitro . Northern blot analysis showed that TD did not affect the sPLA 2 mRNA levels; however, immunoblotting showed a dose-dependent reduction in sPLA 2 enzyme. These results, together with a marked reduction in sPLA 2 enzymatic activity, suggest that TD inhibits sPLA 2 synthesis at the post-transcriptional level. Therefore TD seems to inhibit the arachidonic acid cascade proximally to cyclooxygenase and lipoxygenase and its anti-inflammatory activity may be related at least in part to the inhibition of sPLA 2 synthesis." @default.
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- W2068164412 date "1995-01-01" @default.
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- W2068164412 title "Tenidap sodium inhibits secretory non-pancreatic phospholipase A2synthesis by foetal rat calvarial osteoblasts" @default.
- W2068164412 doi "https://doi.org/10.1155/s0962935195000123" @default.
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