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- Title
Telomerase Inhibitors from Cyanobacteria: Isolation and Synthesis of Sulfoquinovosyl Diacylglycerols from Microcystis aeruguinosa PCC 7806.
- Authors
Makhlouf Brahmi, Malika; Portmann, Cyril; D'Ambrosio, Danilo; Woods, Tom M.; Banfi, Damiano; Reichenbach, Patrick; Da Silva, Laeticia; Baudat, Emilie; Turcatti, Gerardo; Lingner, Joachim; Gademann, Karl
- Abstract
By using the Telospot assay, 27 different extracts of cyanobacteria were evaluated for telomerase inhibition. All extracts showed varying, but significant activity. We selected Microcystis aeruguinosa PCC 7806 to identify the active compound and a bioassay guided fractionation led us to isolate mixtures of sulfoquinovosyl diacylglycerols (SQDGs), which were identified by 2D NMR and MS/MS experiments. Pure SQDG derivatives were then synthesized. The IC50 values of pure synthetic sulfoquinovosyl dipalmitoylglycerol and the monopalmitoylated derivative against telomerase were determined to be 17 and 40 μ M, respectively. A structure-activity relationship study allowed the identification of compounds with modified lipophilic acyl groups that display improved activity.
- Publication
Chemistry - A European Journal, 2013, Vol 19, Issue 14, p4596
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201203296