کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2514028 1118444 2009 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Epigallocatechin-3-gallate is an inhibitor of Na+,K+-ATPase by favoring the E1 conformation
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی داروشناسی
پیش نمایش صفحه اول مقاله
Epigallocatechin-3-gallate is an inhibitor of Na+,K+-ATPase by favoring the E1 conformation
چکیده انگلیسی

Four catechins, epigallocatechin-3-gallate, epigallocatechin, epicatechin-3-gallate, and epicatechin, inhibited activity of the Na+,K+-ATPase. The two galloyl-type catechins were more potent inhibitors, with IC50 values of about 1 μM, than were the other two catechins. Inhibition by epigallocatechin-3-gallate was noncompetitive with respect to ATP. Epigallocatechin-3-gallate reduced the affinity of vanadate, shifted the equilibrium of E1P and E2P toward E1P, and reduced the rate of the E1P to E2P transition. Epigallocatechin-3-gallate potently inhibited membrane-embedded P-type ATPases (gastric H+,K+-ATPase and sarcoplasmic reticulum Ca2+-ATPase) as well as the Na+,K+-ATPase, whereas soluble ATPases (bacterial F1-ATPase and myosin ATPase) were weakly inhibited. Solubilization of the Na+,K+-ATPase with a nonionic detergent reduced sensitivity to epigallocatechin-3-gallate with an elevation of IC50 to 10 μM. These results suggest that epigallocatechin-3-gallate exerts its inhibitory effect through interaction with plasma membrane phospholipid.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 78, Issue 8, 15 October 2009, Pages 1069–1074
نویسندگان
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