Lipophilic mediated assays for beta-hematin inhibitors
Language: 
English
Abstract: 

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 parasite's native lipid component.

Author(s): 
Carter, Melissa D.
Phelan, Vanessa V.
Sandlin, Rebecca D.
Bachmann, Brian O.
Wright, David W.
Item Type: 
Journal Article
Publication Title: 
Combinatorial Chemistry & High Throughput Screening
Journal Abbreviation: 
Comb. Chem. High Throughput Screen.
Publication Date: 
3/10/2015
Publication Year: 
2010
Pages: 
285-292
Volume: 
13
Issue: 
3
ISSN: 
1875-5402
Library Catalog: 
PubMed
Extra: 
PMID: 20230372 PMCID: PMC2901836

Turabian/Chicago Citation

Melissa D. Carter, Vanessa V. Phelan, Rebecca D. Sandlin, Brian O. Bachmann and David W. Wright. 3/10/2015. "Lipophilic mediated assays for beta-hematin inhibitors." Combinatorial Chemistry & High Throughput Screening 13: 3: 285-292.

Wikipedia Citation

<ref> {{Cite journal | doi = | issn = 1875-5402 | volume = 13 | pages = 285-292 | last = Carter | first = Melissa D. | coauthors = Phelan, Vanessa V., Sandlin, Rebecca D., Bachmann, Brian O., Wright, David W. | title = Lipophilic mediated assays for beta-hematin inhibitors | journal = Combinatorial Chemistry & High Throughput Screening | date = 3/10/2015 | pmid = | pmc = }} </ref>