Publication:
Cleavage of DNA induced by 9-anilinoacridine inhibitors of topoisomerase II in the malaria parasite Plasmodium falciparum

dc.contributor.authorSaranya Auparakkitanonen_US
dc.contributor.authorPrapon Wilairaten_US
dc.contributor.otherMahidol Universityen_US
dc.date.accessioned2018-09-07T09:08:37Z
dc.date.available2018-09-07T09:08:37Z
dc.date.issued2000-03-16en_US
dc.description.abstractDue 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.en_US
dc.identifier.citationBiochemical and Biophysical Research Communications. Vol.269, No.2 (2000), 406-409en_US
dc.identifier.doi10.1006/bbrc.2000.2305en_US
dc.identifier.issn0006291Xen_US
dc.identifier.other2-s2.0-0034673530en_US
dc.identifier.urihttps://repository.li.mahidol.ac.th/handle/20.500.14594/25877
dc.rightsMahidol Universityen_US
dc.rights.holderSCOPUSen_US
dc.source.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=0034673530&origin=inwarden_US
dc.subjectBiochemistry, Genetics and Molecular Biologyen_US
dc.titleCleavage of DNA induced by 9-anilinoacridine inhibitors of topoisomerase II in the malaria parasite Plasmodium falciparumen_US
dc.typeArticleen_US
dspace.entity.typePublication
mu.datasource.scopushttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=0034673530&origin=inwarden_US

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