Cell Biology and Toxicology

, Volume 22, Issue 3, pp 183–187 | Cite as

The antitrypanosomal drug melarsoprol competitively inhibits thiamin uptake in mouse neuroblastoma cells

  • P. Szyniarowski
  • L. Bettendorff
  • M. E. Schweingruber


Melarsoprol is the main drug used for the treatment of late-stage sleeping sickness, although it causes severe side-effects such as encephalopathy and polyneuropathy leading to death in some patients. Recent data suggest that melarsoprol and its active metabolite melarsenoxide interfere with thiamin transport and metabolism in E. coli and yeast, but there are no data concerning their possible effects on thiamin metabolism in mammalian cells. We tested both drugs on thiamin transport in cultured mouse neuroblastoma cells using 14C-labeled thiamin. Melarsoprol, competitively inhibits high-affinity thiamin transport in mouse neuroblastoma cells with a Ki of 44 μmol/L. However, the active compound melarsenoxide has no inhibitory effect. This suggests that the side effects of melarsoprol treatment are unlikely to be due to inhibition of thiamin transport by melarsenoxide, its main metabolite in the brain.


encephalopathies melarsoprol melarsenoxide sleeping sickness thiamin transport trypanosomiasis 


Mel B


Mel Ox



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Copyright information

© Springer Science + Business Media, Inc. 2006

Authors and Affiliations

  • P. Szyniarowski
    • 1
    • 2
  • L. Bettendorff
    • 1
    • 4
  • M. E. Schweingruber
    • 3
  1. 1.Center for Cellular and Molecular NeurobiologyUniversity of LiègeLiègeBelgium
  2. 2.Department of Analytical Biochemistry, Faculty of BiotechnologyJagiellonian UniversityCracowPoland
  3. 3.Institute of Cell BiologyUniversity of BernBernSwitzerland
  4. 4.Center for Cellular and Molecular NeurobiologyUniversity of LiègeLiège 1 (Sart-Tilman)Belgium

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