Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 7, Pages 1858-1860Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.080
Keywords
Metalloproteinase-9; Gene expression; Parthenolide; Sesquiterpenes; Parthenolide derivatives; NF-kappa B driven transcription
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Funding
- Centro Studi e Ricerche sulla Caratterizzazione e Sicurezza d'Uso di Sostanze Naturali-Giovanni Galli
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Semisynthetic derivatives of parthenolide (1) were tested on NF-kappa B driven transcription and metalloproteinase-9 (MMP-9) expression and secretion. The four membered ring compounds 5 and 6, obtained by acidic treatment of 1, exhibited a higher activity with respect to 1 in all the biological assays. Then an increased ability of the 5 and 6 to inhibit NF-kappa B driven transcription may lead to a down-regulation of MMP-9 expression and secretion. This work provides new details about the structural requisites for NF-kappa B inhibition. (C) 2009 Elsevier Ltd. All rights reserved.
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