Source:http://linkedlifedata.com/resource/pubmed/id/15745752
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2005-3-4
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pubmed:abstractText |
Antimalarial drugs such as chloroquine are believed to act by inhibiting hemozoin formation in the food vacuole of the malaria parasite. We have developed a new assay for measuring and detecting inhibition of synthetic hemozoin (beta-hematin) formation. Aqueous pyridine (5% v/v, pH 7.5) forms a low-spin complex with hematin but not with beta-hematin. Its absorbance obeys Beer's law, making it useful for quantitating hematin concentration in hematin/beta-hematin mixtures, allowing compounds to be investigated for inhibition of beta-hematin formation. The assay is rapid (60 min incubation) and requires no centrifugation. The beta-hematin inhibition data show good agreement with alternative assay methods reported by four laboratories. The assay was adapted for high-throughput colorimetric screening, allowing visual identification of beta-hematin inhibitors. In this mode, the assay successfully detected all 18 beta-hematin inhibitors in a set of 47 compounds tested, with no false positive results. The quantitative in vitro antimalarial activities of a set of 13 aminoquinolines and quinoline methanols were found to correlate significantly with beta-hematin inhibition values determined using the assay.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antimalarials,
http://linkedlifedata.com/resource/pubmed/chemical/Chloroquine,
http://linkedlifedata.com/resource/pubmed/chemical/Hemeproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/hemozoin,
http://linkedlifedata.com/resource/pubmed/chemical/pyridine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0003-2697
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
338
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
306-19
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15745752-Animals,
pubmed-meshheading:15745752-Antimalarials,
pubmed-meshheading:15745752-Chloroquine,
pubmed-meshheading:15745752-Colorimetry,
pubmed-meshheading:15745752-Drug Evaluation, Preclinical,
pubmed-meshheading:15745752-Hemeproteins,
pubmed-meshheading:15745752-Inhibitory Concentration 50,
pubmed-meshheading:15745752-Pyridines
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pubmed:year |
2005
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pubmed:articleTitle |
A colorimetric high-throughput beta-hematin inhibition screening assay for use in the search for antimalarial compounds.
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pubmed:affiliation |
Department of Chemistry, University of Cape Town, Private Bag, Rondebosch 7701, South Africa.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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