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 inh...

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Veröffentlicht in:	Biochemical and biophysical research communications 1988-04, Vol.152 (2), p.605-611
Hauptverfasser:	Chakraborty, Asit K., Majumder, Hemanta K.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Animals Antimony - pharmacology Antimony Sodium Gluconate - pharmacology Biological and medical sciences DNA Topoisomerases, Type I - genetics Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Gluconates - pharmacology Leishmania donovani Leishmania donovani - drug effects Leishmania donovani - enzymology Leishmania donovani - genetics Organometallic Compounds - pharmacology Plasmids - drug effects Topoisomerase I Inhibitors Urea - analogs & derivatives Urea - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0006-291X 1090-2104
DOI:	10.1016/S0006-291X(88)80081-0