title: Four new carvotanacetone derivatives from Sphaeranthus ukambensis, inhibitors of the ubiquitin-proteasome pathway.
abstract: Six carvotanacetone derivatives (1- 6), amongst which four new compounds (1- 4), were isolated from the aerial parts of Sphaeranthus ukambensis Vatke & O. Hoffm. The structures of the molecules were elucidated by complementary spectroscopic methods, and their biological properties were investigated using human DLD-1 colon cancer cells engineered to stably express a 4 ubiquitin-luciferase (4 Ub-Luc) reporter protein. Five of the isolated carvotanacetone derivatives (2- 6) were found to inhibit the proliferation of the colon cancer cells and interfere with the ubiquitin-proteasome pathway, with potencies in a micromolar range.
authors.affiliation: Unité Mixte de Service 2597, Centre National de la Recherche Scientifique (CNRS)-Pierre Fabre, Institut des Sciences et Technologies du Médicament de Toulouse, Toulouse, France. isabelle.pouny@pierre-fabre.com
authors.forename: Isabelle
authors.initials: I
authors.lastname: Pouny
authors.forename: Stéphane
authors.initials: S
authors.lastname: Vispé
authors.forename: Laurence
authors.initials: L
authors.lastname: Marcourt
authors.forename: Christophe
authors.initials: C
authors.lastname: Long
authors.forename: Isabelle
authors.initials: I
authors.lastname: Vandenberghe
authors.forename: Yannick
authors.initials: Y
authors.lastname: Aussagues
authors.forename: Roselyne
authors.initials: R
authors.lastname: Raux
authors.forename: Patrick B
authors.initials: PB
authors.lastname: Chalo Mutiso
authors.forename: Georges
authors.initials: G
authors.lastname: Massiot
authors.forename: François
authors.initials: F
authors.lastname: Sautel
mesh_terms: D019659:Asteraceae / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007630:Kenya; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry*; D011480:Protease Inhibitors / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism*; D013729:Terpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D025801:Ubiquitin / Q000378:metabolism*
chemical_list: D010936:Plant Extracts; D011480:Protease Inhibitors; D013729:Terpenes; D025801:Ubiquitin; D046988:Proteasome Endopeptidase Complex