Effects of Camptothecin, a Topoisomerase I Inhibitor, on Plasmodium falciparum

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• 作者：Bodley ; Annette L. ; Cumming ; Jared N. ; Shapiro ; Theresa A.
• 关键词：Plasmodium falciparum ; malaria ; topoisomerase ; camptothecin
• 刊名：Biochemical Pharmacology
• 出版年：1998
• 出版时间：March 1, 1998
• 年：1998
• 卷：55
• 期：5
• 页码：709-711
• 全文大小：301 K

文摘

Currently, the treatment of falciparum malaria is seriously compromised by spreading drug resistance. We studied the effects of camptothecin, a potent and specific topoisomerase I inhibitor, on erythrocytic malaria parasites in vitro. In Plasmodium falciparum, camptothecin trapped protein-DNA complexes, inhibited nucleic acid biosynthesis, and was cytotoxic. These results provide proof for the concept that topoisomerase I is a vulnerable target for new antimalarial drug development.