Abstract
We studied the antileishmanial activity of 3′-deoxy-3′-fluoroinosine (3′-FI) againstLeishmania tropica andL. donovani. In in vitro cultivation, the EC50 values (the concentration of drug necessary to inhibit the growth rate of cells to 50% of the control value) obtained for 3′-FI against the promastigotes ofL. tropica andL. donovani were 2.3×10−7 and 1.0×10−6 M, respectively. It was less toxic toward mouse mammary-tumor FM3A cells, a model host; the EC50 value was 1.9×10−4 M. Leishmania promastigote metabolized 3′-FI to 3′-deoxy-3′-fluoroadenosine 5′-triphosphate (3′-FATP) but FM3A cells did not. 3′-FI was effective againstL. donovani amastigotes in J774.1 cells in an in vitro cultivation system under conditions similar to those used in the in vivo assay. 3′-FI (50 mg/kg, given i.v.)showed a cytotoxic effect against the amastigotes ofL. donovani in mice.
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Shin, I.S., Tanifuji, H., Arata, Y. et al. 3′-Deoxy-3′-fluoroinosine as a potent antileishmanial agent. Parasitol Res 81, 622–626 (1995). https://doi.org/10.1007/BF00932030
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DOI: https://doi.org/10.1007/BF00932030