• Corpus ID: 606469

Anti-parasite activity of nucleoside analogues: the metabolism of carbocyclic inosine in promastigotes of Leishmania tropica and Leishmania donovani and its activity against amastigotes of Leishmania donovani in vitro.

@article{Wataya1986AntiparasiteAO,
  title={Anti-parasite activity of nucleoside analogues: the metabolism of carbocyclic inosine in promastigotes of Leishmania tropica and Leishmania donovani and its activity against amastigotes of Leishmania donovani in vitro.},
  author={Yusuke Wataya and Hiroyasu Satake and Osamu Hiraoka and Toshiki Aji and Kazuhisa Morishige and Julieta Yuri Kimura and Akira I. Ishii and Akira Minamishinkawa-K Matsuda and Tohru Ueda and Kiyofumi Fukukawa},
  journal={Nucleic acids symposium series},
  year={1986},
  volume={17},
  pages={
          149-51
        }
}

• Y. Wataya, H. Satake, +7 authors K. Fukukawa
• Published 1986
• Chemistry, Biology
• Nucleic acids symposium series

Carbocyclic inosine is a potent inhibitor for the growth of the promastigote form of Leishmania tropica and Leishmania donovani. In culture, the EC50 values of carbocyclic inosine are 8.3 X 10(-8) and 1.3 X 10(-7) M for the promastigotes of L. tropica and L. donovani, respectively. On the other hand, it is less toxic towards mouse mammary tumor FM3A cells: the EC50 value is 2.7 X 10(-4)M. Carbocyclic inosine is metabolized by Leishmania promastigotes to give carbocyclic adenosine-5'-triphosphate(aristeromycin-5'-triphosphate) and carbocyclic guanosine-5'-triphosphate. This metabolic conversion provides a mechanism for the parasite-selective toxicity of carbocyclic inosine. Carbocyclic inosine was found to be active against L. donovani amastigotes in an in vivo-like cultivation in vitro.