Systematic synthesis of sulfated oligofucosides and their effect on breast cancer MCF-7 cells.

Sulfated tetrafucosides with different sulfation patterns, and a non-sulfated tetrafucoside , were designed and systematically synthesized from the common key intermediate . In addition, their anti-proliferative activities and apoptosis-inducing activities against human breast cancer MCF-7 cells were evaluated. Our results demonstrated that the sulfated tetrafucosides reduced the number of MCF-7 cells in a dose-dependent manner, and of these, 3,4-O-sulfated type showed the highest anti-proliferative activity, comparable to the activity of fucoidan isolated from Fucus vesiculosus. Furthermore, it was revealed that both and exhibited apoptosis-inducing activities through activation of caspase-8 on MCF-7 cells.