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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 40M, respectively. A structureactivity relationship study allowed the identification of compounds with modified lipophilic acyl groups that display improved activity.
Geoffrey Bodenhausen, Fabien Ferrage
David Lyndon Emsley, Aaron James Rossini, Brennan James Walder
David Lyndon Emsley, Dominik Józef Kubicki, Moreno Lelli, Jasmine Viger-Gravel, Claudia Esther Avalos, David Benjamin Roger Antoine Gajan