کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370446 981819 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Selectivity of 3′-O-methylponkoranol for inhibition of N- and C-terminal maltase glucoamylase and sucrase isomaltase, potential therapeutics for digestive disorders or their sequelae
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Selectivity of 3′-O-methylponkoranol for inhibition of N- and C-terminal maltase glucoamylase and sucrase isomaltase, potential therapeutics for digestive disorders or their sequelae
چکیده انگلیسی

Human maltase glucoamylase (MGAM) and sucrase isomaltase (SI) are two human intestinal glucosidases responsible for the final step of starch hydrolysis.MGAM and SI are anchored to the small intestinal brush border epithelial cells and contain two catalytic N-terminal and C-terminal subunits. In this study, we report the inhibition profile of 3′-O-methylponkoranol for the individual recombinant N and C terminal enzymes and compare the inhibitory activities of this compound with de-O-sulfonated ponkoranol. We show that 3′-O-methylponkoranol inhibits the different subunits to different extents, with extraordinary selectivity for C-terminal SI (Ki = 7 ± 2 nM). The enzymes themselves could serve as therapeutic targets for the treatment of digestive disorders or their sequelae.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6491–6494
نویسندگان
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