Cytotoxic action of retinoidal butenolides on mouse neuroblastoma and rat glioma cells

Publisher Website
Google Scholar
Abstract
Proliferation and death were measured in cultures of mouse neuroblastoma N18TG‐2 and rat glioma C6BU‐1 cells when treated with up to 100 μM retinoidal butenolides (RB 1‐6). The number of viable cells in each case was measured with various concentrations of the compounds, of which RB‐3 (5‐hydroxy‐4‐[2‐(2,6,6‐trimethyl‐1‐cyclohexen‐1‐yl) ethenyl]‐2(5H)‐furanone) was the most potent in destroying the cells after 2 days' incubation. ED50 of RB‐3 was about 5 × 10−7 M for both types of cell. RB‐3 was 80 times more potent than retinoic acid. Ten analogues of RB‐3 had a similar inhibitory effect on DNA synthesis in N18TG‐2 cells. The degenerative changes caused by RB‐3 in C6BU‐1 cells were irreversible even when the cells were exposed to it for 2 h. Tumor weights of N18TG‐2 cells that had been inoculated subcutaneously onto the backs of A/J mice were 30‐40% lower than those of untreated controls after 14 days of single daily i.p. injections of RB‐3 doses of 100 mg/kg of body weight. The results indicate that RB‐3 is cytotoxic in murine tumor cells originating from the nervous system and has an inhibitory effect on neuroblastoma‐tumor growth in mice.