Effects of camptothecin, a topoisomerase I inhibitor, on Plasmodium falciparum

被引:58
作者
Bodley, AL
Cumming, JN
Shapiro, TA
机构
[1] Johns Hopkins Univ, Sch Med, Dept Med, Baltimore, MD 21205 USA
[2] Johns Hopkins Univ, Dept Pharmacol & Mol Sci, Baltimore, MD 21205 USA
[3] Johns Hopkins Univ, Dept Chem, Baltimore, MD 21205 USA
关键词
Plasmodium falciparum; malaria; topoisomerase; camptothecin;
D O I
10.1016/S0006-2952(97)00556-X
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. (C) 1998 Elsevier Science Inc.
引用
收藏
页码:709 / 711
页数:3
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