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首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Relationship between Antimalarial Drug Activity Accumulation and Inhibition of Heme Polymerization in Plasmodium falciparum In Vitro
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Relationship between Antimalarial Drug Activity Accumulation and Inhibition of Heme Polymerization in Plasmodium falciparum In Vitro

机译：体外恶性疟原虫抗疟药活性积累和抑制血红素聚合的关系

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摘要

We have investigated the contribution of drug accumulation and inhibition of heme polymerization to the in vitro activities of a series of antimalarial drugs. Only those compounds exhibiting structural relatedness to the quinolines inhibited heme polymerization. We could find no direct correlation between in vitro activity against chloroquine-susceptible or chloroquine-resistant isolates and either inhibition of heme polymerization or cellular drug accumulation for the drugs studied. However, in vitro activity against a chloroquine-susceptible isolate but not a chloroquine-resistant isolate showed a significant correlation with inhibition of heme polymerization when the activity was normalized for the extent of drug accumulation. The importance of these observations to the rational design of new quinoline-type drugs and the level of agreement of these conclusions with current views on quinoline drug action and resistance are discussed.
机译：我们研究了药物积累和血红素聚合抑制对一系列抗疟药体外活性的贡献。只有那些与喹啉具有结构相关性的化合物才抑制血红素聚合。我们发现对氯喹敏感或耐氯喹分离株的体外活性与抑制血红素聚合或研究药物的细胞药物蓄积之间没有直接关系。但是，当针对药物积累的程度将活性标准化时，针对氯喹敏感性分离物的体外活性而不是针对氯喹抗性的分离物的体外活性显示与血红素聚合的抑制作用显着相关。讨论了这些观察对合理设计新喹啉类药物的重要性以及这些结论与当前有关喹啉类药物作用和耐药性观点的一致程度。

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