Furamidine, a methyltransferase inhibitor, is a potential anti-Babesia spp. chemotherapeutic.

ABSTRACT: Epigenetic inhibitors targeting histone methyltransferases (HMTs) have been proven to be promising for blood protozoan treatment. However, little is known about the effects of HMT inhibitors on Babesia parasites. Here, in vitro and in vivo drug tests were performed to evaluate the efficacy of several compounds targeting various HMTs for Babesia treatment. Their cytotoxicity to MDOK cells was also assessed. Among these compounds, furamidine demonstrated outstanding activity in vitro at the nanomolar level (IC₅₀s of 0.03 ± 0.55, 0.02 ± 0.50, and0.02 ± 0.76 μM at 48, 72, and 96 h, respectively). Furthermore, the IC₅₀ of furamidine on MDOK cells was ~ 100 μM after 24 h, ~ 45 μM after 48 h and ~ 40 μM after 72 h. The therapeutic index of furamidine was greater than 1,500.

SUBMITTER: Liang Q 

PROVIDER: S-EPMC12675685 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature