Lipophilic Mediated Assays for β-Hematin Inhibitors

Author(s): Melissa D. Carter, Vanessa V. Phelan, Rebecca D. Sandlin, Brian O. Bachmann, David W. Wright.

Journal Name: Combinatorial Chemistry & High Throughput Screening

Volume 13 , Issue 3 , 2010

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The growing drug resistance of Plasmodia spp. to current antimalarial agents in the quinine and artemisinin families further asserts the need for novel drug classes to combat malaria infection. One approach to the discovery of new antimalarials is the screening of natural product extracts for activity against the formation of hemozoin, a biomineral essential to parasite survival. By mimicking the in vivo lipid-water interface at which native hemozoin is found, hemozoin can be synthesized outside the parasite. In this work, a variety of lipophilic mediators was used to determine the optimal platform for in vitro hemozoin formation and then tested for efficacy in preliminary screens containing crude natural product extracts. The complete optimization and validation of a NP-40 detergent-mediated assay provide a screening template with an expedited 4-hour incubation time and identical IC50 values to those measured from the parasites native lipid component.

Keywords: Malaria, hemozoin, β-hematin, antimalarial, high-throughput screen

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Article Details

Year: 2010
Page: [285 - 292]
Pages: 8
DOI: 10.2174/138620710790980496
Price: $58

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