title: Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives.
abstract: 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.
authors.affiliation: Department of Pharmacological Sciences, University of Milan, Italy. mario.dellagli@unimi.it
authors.forename: Mario
authors.initials: M
authors.lastname: Dell'Agli
authors.forename: Germana V
authors.initials: GV
authors.lastname: Galli
authors.forename: Enrica
authors.initials: E
authors.lastname: Bosisio
authors.forename: Michele
authors.initials: M
authors.lastname: D'Ambrosio
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D003503:Cyclobutanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015536:Down-Regulation; D006801:Humans; D020128:Inhibitory Concentration 50; D020780:Matrix Metalloproteinase 9 / Q000378:metabolism*; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014158:Transcription, Genetic
chemical_list: D003503:Cyclobutanes; D016328:NF-kappa B; D012717:Sesquiterpenes; C002669:parthenolide; D020780:Matrix Metalloproteinase 9; D015107:4-Butyrolactone