Mode of action of pentavalent antimonials: specific inhibition of type I DNA topoisomerase of Leishmania donovani

Biochem Biophys Res Commun. 1988 Apr 29;152(2):605-11. doi: 10.1016/s0006-291x(88)80081-0.

Abstract

Sodium stibogluconate and Ureastibamine, two potent antileishmanial drugs specifically inhibit the relaxation of supercoiled plasmid pBR322 catalyzed by DNA topoisomerase I of Leishmania donovani. Dose dependent inhibition suggests that the drugs interact with the enzyme rather than the DNA. The inhibition reported here concerning a type I DNA topoisomerase demonstrates at least one possible mode of action of these antileishmanial drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimony / pharmacology*
  • Antimony Sodium Gluconate / pharmacology*
  • DNA Topoisomerases, Type I / genetics
  • Gluconates / pharmacology*
  • Leishmania donovani / drug effects
  • Leishmania donovani / enzymology*
  • Leishmania donovani / genetics
  • Organometallic Compounds / pharmacology*
  • Plasmids / drug effects
  • Topoisomerase I Inhibitors*
  • Urea / analogs & derivatives*
  • Urea / pharmacology

Substances

  • Gluconates
  • Organometallic Compounds
  • Topoisomerase I Inhibitors
  • Urea
  • Antimony
  • urea stibamine
  • DNA Topoisomerases, Type I
  • Antimony Sodium Gluconate