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疟原虫感染红细胞对氯喹摄取的研究。高亲和力摄取与低亲和力摄取以及葡萄糖及其类似物的影响。

A study of the uptake of chloroquine in malaria-infected erythrocytes. High and low affinity uptake and the influence of glucose and its analogues.

作者信息

Diribe C O, Warhurst D C

出版信息

Biochem Pharmacol. 1985 Sep 1;34(17):3019-27. doi: 10.1016/0006-2952(85)90143-1.

Abstract

A study of concentration- and substrate-dependence of chloroquine uptake has been carried out on mouse erythrocytes infected with the chloroquine-sensitive NK65 and the chloroquine-resistant RC strains of Plasmodium berghei. The presence of drug binding sites of high and low affinity in such strains of P. berghei was confirmed. High affinity uptake sites in cells parasitized with chloroquine-sensitive and chloroquine-resistant parasites have similar characteristics, but in the sensitive strain the major component of chloroquine-uptake is at high affinity and dependent on the availability of ATP whilst in the resistant strain the major component of uptake is at low affinity and independent of energy. An absolute increase in the quantity of the low affinity site in erythrocytes parasitized with chloroquine-resistant P. berghei was noted, which may be related to an increase in quantity of parasite membrane.

摘要

对感染了氯喹敏感的NK65株和氯喹抗性的RC株伯氏疟原虫的小鼠红细胞进行了氯喹摄取的浓度和底物依赖性研究。证实了在这些伯氏疟原虫株中存在高亲和力和低亲和力的药物结合位点。感染氯喹敏感和氯喹抗性寄生虫的细胞中的高亲和力摄取位点具有相似的特征,但在敏感株中,氯喹摄取的主要成分是高亲和力的,并且依赖于ATP的可用性,而在抗性株中,摄取的主要成分是低亲和力的,并且不依赖于能量。注意到感染氯喹抗性伯氏疟原虫的红细胞中低亲和力位点的数量绝对增加,这可能与寄生虫膜数量的增加有关。

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