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随着恶性疟原虫对氯喹抗性的产生及扩散,药物作用机理的研究对寻找、设计新药极有意义。目前有两种解释氯喹作用机理的理论。Fitch指出:氯喹等是通过阻碍铁卟啉原Ⅸ(FP)形成疟色素而发挥抗疟作用的。疟色素中含有大量FP,红内期裂殖体杀灭剂的选择性抗疟作用常常与疟色素的形成有关。对氯喹有抗性的鼠疟原虫往往不产生疟色素,或当接触氯喹时便停止产生。迄今为止仅发现氯喹有间接抑制血红蛋白降解的作用。实验证明,FP和FP-氯喹复合物对纯化的恶性疟原虫酸性蛋白酶有抑制作用,推
With the emergence and spread of chloroquine resistance in Plasmodium falciparum, the study on the mechanism of drug action is of great significance in finding and designing new drugs. There are currently two theories that explain the mechanism of action of chloroquine. Fitch pointed out: Chloroquine exerts its anti-malarial effect by hindering the formation of malaria pigment by protoporphyrin Ⅸ (FP). The malaria pigment contains a large amount of FP, and the selective anti-malarial effect of the red-late schizonticide is often associated with the formation of malaria pigment. Plasmodium plasmodia, which is resistant to chloroquine, often does not produce malarial pigment or stops producing when exposed to chloroquine. To date, only chloroquine has been found to indirectly inhibit hemoglobin degradation. Experiments show that FP and FP-chloroquine complexes have an inhibitory effect on purified P. falciparum acid protease and push