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Aminothiol multidentate chelators as antimalarials

M Loyevsky1, C John, I Zaloujnyi

  • 1Department of Medicine, George Washington University Medical Center, Washington, DC 20037, USA. Loyevsky@gwis2.circ.gwu.edu

Biochemical Pharmacology
|August 15, 1997
PubMed
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Two novel aminothiol chelators, ethane-1,2-bis(N-1-amino-3-ethylbutyl-3-thiol) (BAT) and N

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Malaria remains a significant global health challenge, necessitating the development of new antimalarial drugs.
  • Existing treatments face challenges with drug resistance and toxicity.
  • Aminothiol compounds are explored for their potential therapeutic properties.

Purpose of the Study:

  • To evaluate the antimalarial efficacy of two novel multidentate chelators, ethane-1,2-bis(N-1-amino-3-ethylbutyl-3-thiol) (BAT) and N',N',N'-tris(2-methyl-2-mercaptopropyl)-1,4,7-triazacyclononane (TAT).
  • To investigate the mechanism of action, focusing on iron chelation.
  • To assess the safety profile in mammalian cells.

Main Methods:

  • Culturing of Plasmodium falciparum in erythrocytes.

Related Experiment Videos

  • Quantification of parasite growth inhibition using [3H]hypoxanthine incorporation.
  • Determination of 50% inhibitory concentrations (IC50).
  • Iron withholding assays using calcein probe.
  • Assessment of cytotoxicity in mammalian cells via [3H]thymidine incorporation.

    • Main Results:

    • Both BAT and TAT demonstrated significant inhibition of P. falciparum growth, with IC50 values of 7.6 ± 1.2 µM and 3.3 ± 0.3 µM, respectively.
    • Antimalarial activity was 5-10 times greater than desferrioxamine B.
    • Inhibitory effects were reversed by iron pre-complexation, indicating iron withholding as the primary mechanism.
    • Trophozoite and schizont stages were most susceptible.
    • Mammalian cell IC50 values were 10-20 times higher than those for parasite inhibition.

    Conclusions:

    • BAT and TAT exhibit potent antimalarial activity against Plasmodium falciparum.
    • Their mechanism involves iron chelation, crucial for parasite survival.
    • These compounds demonstrate a favorable therapeutic margin, suggesting potential for clinical development.