Inhibition of rat glioma cell migration and proliferation by a calix[8]arene scaffold exposing multiple GlcNAc and ureido functionalities

b1,4-Galactosyltransferases (b1,4-GalTase) exposed on the
cell surface are involved in cell migration. Specifically, b1,4-
GalTase V is highly expressed in glioma and promotes invasion,
growth, and survival of glioma cells. A glycocalix[8]arene
exposing N-acetylglucosamine (GlcNAc) residues (compound
1) inhibited rat C6 glioma cell migration as assessed in a
scratch wound model. This effect was related to inhibition of
focal adhesion kinase phosphorylation, measured by western
blot analysis, and specifically observed in the area bordering
the scratch wound. Compound 1 inhibited also C6 cell proliferation,
an effect unrelated to its ability to interact with Gal-
Tase as it was mimicked by different calix[8]arene derivatives,
all characterized by multivalency and ureido groups. Compound
1 did not induce apoptotic death, but caused a different
distribution of C6 cells within the cell cycle. The results here
reported identify compound 1 as a molecule able to exert
inhibitory effects on C6 cell migration and proliferation, independently,
because of distinct components in its structure.