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

Chakraborty, Asit K. ; Majumder, Hemanta K. (1988) Mode of action of pentavalent antimonials: specific inhibition of type I DNA topoisomerase of Leishmania donovani Biochemical and Biophysical Research Communications, 152 (2). pp. 605-611. ISSN 0006-291X

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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S00062...

Related URL: http://dx.doi.org/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.

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