抗疟药8-氨基喹啉伯氨喹荧光探针的合成、表征及细胞定位
Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine.
作者信息
McQueen Adonis, Blake Lynn D, Azhari Ala, Kemp M Trent, McGaha Tommy W, Namelikonda Niranjan, Larsen Randy W, Manetsch Roman, Kyle Dennis E
机构信息
Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, FL, USA.
Department of Global Health, College of Public Health, University of South Florida, Tampa, FL, USA.
出版信息
Bioorg Med Chem Lett. 2017 Oct 15;27(20):4597-4600. doi: 10.1016/j.bmcl.2017.09.030. Epub 2017 Sep 14.
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.
伯氨喹（PQ）是唯一可商购获得的能清除疟疾潜伏肝期并阻断向蚊媒传播的药物。尽管它是一种老药，但关于其作用机制仍有许多有待了解之处。在此，我们开发了一种荧光标记的PQ，以发现其在人类疟原虫恶性疟原虫中的细胞定位。成功合成并表征了一种伯氨喹-香豆素荧光探针（PQCP），证明其效力与母体药物相当，且该探针对肝癌细胞HepG2无细胞毒性。细胞定位主要发现于寄生虫发育的无性红细胞期和配子体期的胞质溶胶中。
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