Primaquine (PQ) is the only commercially available drug that clears dormant liver stages of malaria and blocks transmission to mosquito vectors. Although an old drug, much remains to be known about the mechanism(s) of action. Herein we develop a fluorescent tagged PQ to discover cellular localization in the human malaria parasite, Plasmodium falciparum. Successful synthesis and characterization of a primaquine-coumarin fluorescent probe (PQCP) demonstrated potency equivalent to the parent drug and the probe was not cytotoxic to HepG2 carcinoma cells. Cellular localization was found primarily in the cytosol of the asexual erythrocytic and gametocyte stages of parasite development.

primaquine（PQ）是唯一可清除疟疾的休眠肝脏阶段并阻止向蚊媒传播的市售药物。尽管是旧药，但关于作用机理尚有许多未知。本文中，我们开发了荧光标记的PQ，以发现人类疟疾寄生虫恶性疟原虫中的细胞定位。伯氨喹-香豆素荧光探针（PQCP）的成功合成和表征证明其效力等同于母体药物，并且该探针对HepG2癌细胞没有细胞毒性。细胞定位主要发现在寄生虫发育的无性红细胞和配子细胞阶段的细胞质中。