2. Academic Validation
  3. Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine

Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine

  • Bioorg Med Chem Lett. 2017 Oct 15;27(20):4597-4600. doi: 10.1016/j.bmcl.2017.09.030.
Adonis McQueen 1,  Lynn D Blake 1,  Ala Azhari 2,  M Trent Kemp 1,  Tommy W McGaha Jr 2,  Niranjan Namelikonda 3,  Randy W Larsen 3,  Roman Manetsch 4,  Dennis E Kyle 5
Affiliations

Affiliations

  • 1 Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, FL, USA.
  • 2 Department of Global Health, College of Public Health, University of South Florida, Tampa, FL, USA.
  • 3 Department of Chemistry, College of Arts and Sciences, University of South Florida, Tampa, FL, USA.
  • 4 Department of Chemistry, College of Arts and Sciences, University of South Florida, Tampa, FL, USA; Department of Chemistry and Chemical Biology, and Department of Pharmaceutical Sciences, College of Science and Bouvé College of Health Sciences, Northeastern University, Boston, MA, USA.
  • 5 Department of Global Health, College of Public Health, University of South Florida, Tampa, FL, USA. Electronic address: dennis.kyle@uga.edu.
PMID: 28939120 DOI: 10.1016/j.bmcl.2017.09.030
Abstract

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.

Keywords

8-Aminoquinoline; Fluorescent probe; Malaria; Plasmodium falciparum; Primaquine.

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