Diospyrin, A Bisnaphthoquinone: A Novel Inhibitor of Type I DNA Topoisomerase of Leishmania donovani
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
Diospyrin, A Bisnaphthoquinone: A Novel Inhibitor of Type I
DNA Topoisomerase of Leishmania donovani
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| Creator |
Ray, Sutapa
Hazra, Banasri Mittra, Bidyottam Das, Aditi Majumder, Hemanta K |
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| Subject |
Infectious Diseases and Immunology
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| Description |
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 of L. donovani and requires much higher concentrations to inhibit type I topoisomerase of calf thymus. The potent inhibitory effect of diospyrin on type I DNAtopoisomerase from L. donovani can be exploited for rational
drug design in human leishmaniasis.
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| Date |
1998
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://www.eprints.iicb.res.in/829/1/MOLECULAR_PHARMACOLOGY%2C_54(_6)%2C_994%2D999_[3].pdf
Ray, Sutapa and Hazra, Banasri and Mittra, Bidyottam and Das, Aditi and 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. |
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| Relation |
http://dx.doi.org/
http://www.eprints.iicb.res.in/829/ |
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