کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1359894 981419 2010 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I
چکیده انگلیسی

Glyoxalase I (GLO I) is the rate-limiting enzyme for detoxification of methylglyoxal (MG), a side-product of glycolysis, which is able to induce apoptosis. Since GLO I is known to be highly expressed in the most tumor cells and little in normal cells, inhibitors of this enzyme has been expected to be new anticancer drugs. Here, we examined the inhibitory abilities to the human GLO I of anthocyanidins, such as delphinidin, cyanidin and pelargonidin. Among them, delphinidin was found to have the most potent inhibitory effect on human GLO I. Also, only delphinidin-induced apoptosis in HL-60 cells in a dose- and time-dependent manner. Furthermore, we determined a pharmacophore for delphinidin binding to the human GLO I by computational simulation analyses of the binding modes of delphinidin, cyanidin and pelargonidin to the enzyme hot spot. These results suggest that delphinidin could be a useful lead compound for the development of novel GLO I inhibitory anticancer drugs.

The structure of delphinidin and its predicted binding mode on the human GLO I.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 19, 1 October 2010, Pages 7029–7033
نویسندگان
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