Neurostatin, a natural
glycosphingolipid inhibitor of astroblast and
astrocytoma division, present in mammalian brain, is the modified
ganglioside O-acetylated GD1b. It is
cytostatic for rat astroblasts, C6
glioma cells and various human
astrocytoma lines grades III and IV, with median inhibitory dose values ranging 1 - 5 μM.
Neurostatin was shown not to affect primary or transformed fibroblast division at concentrations of ≥ 10 μM. A synthetic
neurostatin analogue,
NF-115, consisting of an octyl N-acetylglucosaminide derivative with a
pentaerythritol chain at position 6, loaded on a slow-delivery
polymer disc, caused the destruction of cultured human
astroblastoma, obtained after surgical biopsy, and destroyed human neuroectodermic tumours implanted in rats and human
astrocytoma implanted in immunodeficient mice. Future antitumourals should combine the high activity of
neurostatin with the ease of synthesis of
NF-115.