The Naphthoquinone Diospyrin is an Inhibitor of DNA Gyrase with a Novel Mechanism of Action *S
نویسندگان
چکیده
Present address: Novartis Institute of Biomedical Research, Basel 4056, Switzerland. Present address: Inspiralis Ltd., Norwich Bioincubator, Norwich Research Park Colney Lane, Norwich, NR4 7UH, UK To whom correspondence may be addressed: Department of Biological Chemistry, John Innes Centre, Norwich Research Park, Norwich, NR4 7UH, UK. Tel +44-1603-450771; Fax +44-1603-450018, Email [email protected]
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The Naphthoquinone Diospyrin Is an Inhibitor of DNA Gyrase with a Novel Mechanism of Action*
Tuberculosis and other bacterial diseases represent a significant threat to human health. The DNA topoisomerases are excellent targets for chemotherapy, and DNA gyrase in particular is a well-validated target for antibacterial agents. Naphthoquinones (e.g. diospyrin and 7-methyljuglone) have been shown to have therapeutic potential, particularly against Mycobacterium tuberculosis. We have found...
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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 ...
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