Atividade anti-tumoral do composto LaSOM 65, derivado do monastrol, em linhagens de gliomas

AUTOR(ES)
FONTE

IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia

DATA DE PUBLICAÇÃO

2011

RESUMO

Gliomas are the most common primary cancer in the central nervous system. Despite recent progress in the treatment of glioblastoma, the median survival of the patients still remains at 15 months. Kinesin Spindle Protein (KSP) has been reported as an interesting target for cancer therapy. Followed by the first specific KSP inhibitor, Monastrol, several other structural analogues have also been studied. Here we describe the effect of LaSOM 65, a monastrol derivated compound, against glioma. LaSOM 65 was able to decrease cell growth and cell viability of gliomas cells, but, in contrast with monastrol, the molecule did not cause blockage in the cell cycle on G2/M phase. Analysis by flow cytometry showed that LaSOM 65 leads cells to necrosis and ¿late apoptosis¿ after 24h and 48h of treatment. We also investigate the effect of LaSOM 65 on ecto-5 NT activity, an enzyme whose expression level is associated with neovascularization, invasiveness and metastasis of tumors. The treatment did not alter the enzyme activity compared to control cells. Experiments in vivo shown that LaSOM 65 was not able to decrease the tumor size in rat gliomas model. More studies are necessary to understand the mechanisms by which LaSOM 65 is exerting its cytotoxic effects.

ASSUNTO(S)

glioma monastrol sistema purinérgico ensaios de seleção de medicamentos antitumorais

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