Journal
FEBS LETTERS
Volume 578, Issue 3, Pages 269-274Publisher
WILEY
DOI: 10.1016/j.febslet.2004.10.100
Keywords
anti-inflammatory compound; marine natural product; mass spectrometry; phospholipase A(2) inhibition
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25-Acetyl-petrosaspongiolide M (PMAc) (1), a mild non-covalent PLA(2) inhibitor, unexpectedly recovers, after incubation with bvPLA(2), the ability to covalently modify the enzyme target. This study demonstrates the catalytic effect of bvPLA(2) in converting 1 in its deacetylated congener petrosaspongiolide M (PM) (2), a strong covalent PLA(2) inhibitor whose molecular mechanism of inhibition has already been clarified. Moreover, our findings outline the potential role of PMAc as anti-inflammatory pro-drug, by virtue of its ability of delivering the active PM agent at the site of inflammation, functioning as a suicide inhibitor. (C) 2004 Published by Elsevier B.V. on behalf of the Federation of European Biochemical Societies.
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