Mode of action of pentavalent antimonials: specific inhibition of type I DNA topoisomerase of Leishmania donovani.
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.
Chakraborty
A K
AK
Molecular Parasitology Laboratory, Indian Institute of Chemical Biology, Calcutta.
Majumder
H K
HK
D000818:Animals; D000965:Antimony / Q000494:pharmacology*; D000967:Antimony Sodium Gluconate / Q000494:pharmacology*; D004264:DNA Topoisomerases, Type I / Q000235:genetics; D005942:Gluconates / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects / Q000201:enzymology* / Q000235:genetics; D009942:Organometallic Compounds / Q000494:pharmacology*; D010957:Plasmids / Q000187:drug effects; D059004:Topoisomerase I Inhibitors; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology
D005942:Gluconates; D009942:Organometallic Compounds; D059004:Topoisomerase I Inhibitors; D014508:Urea; D000965:Antimony; C053921:urea stibamine; D004264:DNA Topoisomerases, Type I; D000967:Antimony Sodium Gluconate