Publication: Cleavage of DNA induced by 9-anilinoacridine inhibitors of topoisomerase II in the malaria parasite Plasmodium falciparum
Issued Date
2000-03-16
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ISSN
0006291X
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2-s2.0-0034673530
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Mahidol University
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SCOPUS
Bibliographic Citation
Biochemical and Biophysical Research Communications. Vol.269, No.2 (2000), 406-409
Suggested Citation
Saranya Auparakkitanon, Prapon Wilairat Cleavage of DNA induced by 9-anilinoacridine inhibitors of topoisomerase II in the malaria parasite Plasmodium falciparum. Biochemical and Biophysical Research Communications. Vol.269, No.2 (2000), 406-409. doi:10.1006/bbrc.2000.2305 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/25877
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Title
Cleavage of DNA induced by 9-anilinoacridine inhibitors of topoisomerase II in the malaria parasite Plasmodium falciparum
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Abstract
Due to resistance by Plasmodium falciparum, the most virulent strain of the four species of human malaria parasites, to most currently used antimalarial drugs, development of new effective antimalarials is urgently needed. Derivatives of 9-anilinoacridine, an antitumor drug, have been shown to inhibit P. falciparum growth in culture and to inhibit parasite DNA topoisomerase II activity in vitro. Using KCl-SDS precipitation assay to detect the presence of protein-DNA complexes within parasite cells, an indicator of DNA topoisomerase II inactivation, derivatives containing 3,6-diNH2substitutions with 1'-electron donating (NMe2, CH2NMe2, NHSO2Me, OH, OMe), and 1'-electron withdrawing (SO2NH2) groups produced protein-DNA complexes. However, the antimalarial pyronaridine, 9-anilinoazaacridine, did not generate protein-DNA complexes, although it was capable of inhibiting P. falciparum DNA topoisomerase II activity in vitro. These results should prove useful in future designs of novel antimalarial compounds directed against parasite DNA topoisomerase II. (C) 2000 Academic Press.