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Telomerase Inhibitors from Cyanobacteria: Isolation and Synthesis of Sulfoquinovosyl Diacylglycerols from Microcystis aeruguinosa PCC 7806

2013; Wiley; Volume: 19; Issue: 14 Linguagem: Inglês

10.1002/chem.201203296

1521-3765

Malika Makhlouf Brahmi, Cyril Portmann, Danilo D’Ambrosio, Tom M. Woods, Damiano Banfi, Patrick Reichenbach, Laeticia Da Silva, Emilie Baudat, Gerardo Turcatti, Joachim Lingner, Karl Gademann,

Photodynamic Therapy Research Studies

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 IC 50 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.