Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives.

Autor: Dell'Agli M; Department of Pharmacological Sciences, University of Milan, Italy. mario.dellagli@unimi.it, Galli GV, Bosisio E, D'Ambrosio M
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 01; Vol. 19 (7), pp. 1858-60. Date of Electronic Publication: 2009 Feb 25.
DOI: 10.1016/j.bmcl.2009.02.080
Abstrakt: Semisynthetic derivatives of parthenolide (1) were tested on NF-kB 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-kB 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-kB inhibition.
Databáze: MEDLINE