Mode of action of quinoline antimalarial drugs in red blood cells infected by <i>Plasmodium falciparum</i> revealed in vivo

Abstract

Significance The most widely used antimalarial drugs belong to the quinoline family. The question of their mode of action has been open for centuries. It has been recently narrowed down to whether these drugs interfere with the process of crystallization of heme in the malaria parasite. To date, all studies of the drug action on heme crystals have been done either on model systems or on dried parasites, which yielded limited data and ambiguity. This study was done in actual parasites in their near-native environment, revealing the mode of action of these drugs in vivo. The approach adopted in this study can be extended to other families of antimalarial drugs, such as artemisinins, provided appropriate derivatives can be synthesized.