Ray, Sutapa ; Hazra, Banasri ; Mittra, Bidyottam ; Das, Aditi ; Majumder, Hemanta K. (1998) Diospyrin, a bisnaphthoquinone: a novel inhibitor of type I DNA topoisomerase of Leishmania donovani Molecular Pharmacology, 54 (6). pp. 994-999. ISSN 0026-895X
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Official URL: http://molpharm.aspetjournals.org/content/54/6/994...
Abstract
Diospyrin is a plant product that has significant inhibitory effect on the growth of Leishmania donovani promastigotes. This compound inhibits the catalytic activity of DNA topoisomerase I of the parasite. Like camptothecin, it induces topoisomerase I mediated DNA cleavage in vitro. Treatment of DNA with diospyrin before addition of topoisomerase I has no effect. Preincubation of topoisomerase I with diospyrin before the addition of DNA in the relaxation reaction increases this inhibition. Our results suggest that this bis-naphthoquinone compound exerts its inhibitory effect by binding with the enzyme and stabilizing the topoisomerase I-DNA "cleavable complex." Diospyrin is a specific inhibitor of the parasitic topoisomerase I. It does not inhibit type II topoisomerase ofL. donovani and requires much higher concentrations to inhibit type I topoisomerase of calf thymus. The potent inhibitory effect of diospyrin on type I DNA topoisomerase from L. donovani can be exploited for rational drug design in human leishmaniasis.
Item Type: | Article |
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Source: | Copyright of this article belongs to American Society for Pharmacology and Experimental Therapeutics. |
ID Code: | 70385 |
Deposited On: | 21 Nov 2011 09:19 |
Last Modified: | 21 Nov 2011 09:19 |
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