A Monastrol-derived Compound, LaSOM 63, Inhibits Ecto-5 ' Nucleotidase/CD73 Activity and Induces Apoptotic Cell Death of Glioma Cell Lines

作者：Figueiro Fabricio; Mendes Franciane Brackmann; Corbelini Patricia Frasson; Janarelli Fernanda; Farias Jandrey Elisa Helena; Russowsky Dennis; Eifler Lima Vera Lucia; Oliveira Battastini Ana Maria

来源：Anticancer Research, 2014, 34(4): 1837-1842.

• Glioma
• ecto-5 ' nucleotidase
• monastrol
• LaSOM 63

Background/Aim: Glioblastoma multiforme is the most malignant type of glioma. Ecto-5'-nucleotidase (ecto-5'NT), a glioma-overexpressed enzyme can induce a protective effect on tumor cells. Monastrol, a kinesin spindle protein-specific inhibitor, is reported to be an interesting prototype for cancer therapy. We describe the effect of LaSOM 63, a monastrol derivative, on ecto-5'NT activity and on glioma cell survival. Materials and Methods: Glioma cells were treated with LaSOM 63 and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), trypan blue assay (viability), flow cytometry (cell cycle/cell death) and malachite green method for ecto-5'NT activity were carried out. Results and Discussion: Treatment with LaSOM 63 reduces glioma cell viability and cell growth. In contrast to monastrol, LaSOM 63 did not cause glioma cell-cycle arrest, but inhibited ecto-5'NT enzyme activity. Furthermore, this compound induces apoptotic death of C6 and U138 glioma cells. Conclusion: LaSOM 63 may be useful for in vivo experiments on the treatment of GBM.

• 出版日期2014-4