Enhanced antitumor activity of sarCNU in comparison to BCNU in an extraneuronal monoamine transporter positive human glioma xenograft model.

摘要: A novel analogue of nitrosoureas, 2-chloroethyl-3-sarcosinamide-1-nitrosourea (SarCNU), has demonstrated increased anticancer effects in vitro and vivo. Our previous work suggested that SarCNU enters cells via the extraneuronal monoamine transporter (EMT), contributes to its enhanced cytotoxicity. In present study, comparative activities 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) were evaluated an EMT positive human glioma xenograft model. Athymic nude mice implanted subcutaneously or intracranially with SHG-44, a cell line been confirmed by using reverse-transcription polymerase chain reaction (RT-PCR) assay, treated at optimal dose 167 mg/kg, BCNU 20 mg/kg 30 q4d x 3 intraperitoneally (i.p.). 17 animals subcutaneous tumor grafts SarCNU, 9 became free 8 regression. While group, there only 2 out 10 group 7 which some There 4 drug related deaths (30 mg/kg) while no group. mice, median survival time was more than 130 days, it 22 days similar control (18 days). This is first demonstration comparison BCNU, activity