Mabeza G F, Loyevsky M, Gordeuk V R, Weiss G
Department of Medicine, University of Zimbabwe Medical School, Harare.
Pharmacol Ther. 1999 Jan;81(1):53-75. doi: 10.1016/s0163-7258(98)00037-0.
Malaria is one of the major global health problems, and an urgent need for the development of new antimalarial agents faces the scientific community. A considerable number of iron(III) chelators, designed for purposes other than treating malaria, have antimalarial activity in vitro, apparently through the mechanism of withholding iron from vital metabolic pathways of the intra-erythrocytic parasite. Certain iron(II) chelators also have antimalarial activity, but the mechanism of action appears to be the formation of toxic complexes with iron rather than the withholding of iron. Several of the iron(III)-chelating compounds also have antimalarial activity in animal models of plasmodial infection. Iron chelation therapy with desferrioxamine, the only compound of this nature that is widely available for use in humans, has clinical activity in both uncomplicated and severe malaria in humans.
疟疾是全球主要的健康问题之一,科学界面临着开发新型抗疟药物的迫切需求。相当数量为其他目的设计的铁(III)螯合剂在体外具有抗疟活性,显然是通过从红细胞内寄生虫的重要代谢途径中扣留铁的机制实现的。某些铁(II)螯合剂也具有抗疟活性,但其作用机制似乎是与铁形成有毒复合物,而不是扣留铁。几种铁(III)螯合化合物在疟原虫感染的动物模型中也具有抗疟活性。去铁胺作为这种性质中唯一广泛可供人类使用的化合物,其铁螯合疗法在人类单纯性疟疾和重症疟疾中均具有临床活性。