Planta Med 2009; 75 - SL37
DOI: 10.1055/s-0029-1234292

Rapid screening and targeted isolation of antimalarial hits using β-Hematin assay

K Ndjoko Ioset 1, S Vargas 1, AE Hay 1, JR Ioset 2, K Hostettmann 1
  • 1Laboratory of Pharmacognosy and Phytochemistry, School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, CH-1211 Geneva 4, Switzerland
  • 2Drug for Neglected Disease (DNDi), Chemin Louis-Dunant 15, 1202 Geneva, Switzerland

Malaria is one of the most devastating infectious diseases killing approximately one million people annually, mostly young children [1]. Natural resources – especially plants with the examples of quinine and artemisinin – have already been demonstrated to be a very successful source of effective and safe antimalarial drugs. The assay on β-hematin is based on the selective detection of the non polymerized hematin after complexation with pyridine [2]. The test was implemented in our laboratory and optimized for the screening of crude plant extracts and pure natural products on 96 well-plates [3]. A total of 70 natural products belonging to various chemical classes and 320 extracts have been tested qualitatively. Inhibitors of the β-hematin synthesis were submitted to the in vitro test on P. falciparum. Qualitative response obtained correlated more that 80% of cases. 50% of the identified hits presented IC50<10mg/ml. A strategy based on the colorimetric test and chemical screening was settled in order to rapidly identify antimalarial hits [3].

References: [1] Ioset, J.-R. (2009) Curr. Org. Chem. 12:643–666.

[2] Egan, T.J. et al. (2005)J. Inorg. Biochem. 99:1532–1539.

[3] Vargas, S. (2009). PhD Thesis (Submitted).