Four new carvotanacetone derivatives from Sphaeranthus ukambensis, inhibitors of the ubiquitin-proteasome pathway |
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Authors: | Pouny Isabelle Vispé Stéphane Marcourt Laurence Long Christophe Vandenberghe Isabelle Aussagues Yannick Raux Roselyne Chalo Mutiso Patrick B Massiot Georges Sautel François |
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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 |
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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. |
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