Nifurtimox (Synonyms: BAY-2502, BAY-A-2502)

Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of a reduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH is determined after 4 h treatment with 50 µg/mL Nifurtimox. Compared to the untreated control, the LDH activity is significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065). Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. To characterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to several experiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 µg/mL to an average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). The reduction is significant compared to the untreated control (P<0.01) and the vehicle control with DMSO (P<0.05) for all cell lines[1].

References:
[1]. Cabanillas Stanchi KM, et al. Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma. Cancer Biol Ther. 2015;16(9):1353-63.