کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10533240 961859 2005 14 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A colorimetric high-throughput β-hematin inhibition screening assay for use in the search for antimalarial compounds
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
A colorimetric high-throughput β-hematin inhibition screening assay for use in the search for antimalarial compounds
چکیده انگلیسی
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 (β-hematin) formation. Aqueous pyridine (5% v/v, pH 7.5) forms a low-spin complex with hematin but not with β-hematin. Its absorbance obeys Beer's law, making it useful for quantitating hematin concentration in hematin/β-hematin mixtures, allowing compounds to be investigated for inhibition of β-hematin formation. The assay is rapid (60 min incubation) and requires no centrifugation. The β-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 β-hematin inhibitors. In this mode, the assay successfully detected all 18 β-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 β-hematin inhibition values determined using the assay.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Analytical Biochemistry - Volume 338, Issue 2, 15 March 2005, Pages 306-319
نویسندگان
, ,