Apoptosis-inducing activity and growth suppression by vesnarinone on human glioma transplanted in nude mice.

The growth and morphological change of human glioma transplanted subcutaneously and intracerebrally to nude mice with orally administered vesnarinone, 3,4-dihydro-6-4-(3,4-dimethoxy-benzoyl)-1-piperazinyl]-2(1H)-quinolinon e, were examined. The tumor volume of human glioma xenograft, GL-9, subcutaneously transplanted to nude mice, was significantly decreased by orally administered vesnarinone at a dose of 500 mg kg-1. Vesnarinone also significantly prolonged the survival of nude mice transplanted intracerebrally with GL-9. Apoptosis was observed in paraffin sections of both subcutaneous and intracerebral GL-9 by the method of direct immunoperoxidase detection of digoxigenin-dUTP-labeled nick ends introduced by terminal deoxynucleotidyl transferase. These findings suggest that vesnarinone suppresses the growth and induces apoptosis of glioma cells in vivo.