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Inhibitory effects of epigallocatechin gallate and its glucoside on the human intestinal maltase inhibition
Authors:Thi Thanh Hanh Nguyen  Sun-Hwa Jung  Sun Lee  Hwa-Ja Ryu  Hee-Kyoung Kang  Young-Hwan Moon  Young-Min Kim  Atsuo Kimura  Doman Kim
Affiliation:1. School of Biological Sciences and Technology and Research Institute for Catalysis, Chonnam National University, Gwangju, 500-757, Korea
2. Interdisciplinary Program of Graduate School for Bioenergy and Biomaterials, Chonnam National University, Gwangju, 500-757, Korea
3. Audubon Sugar Institute, LSU Ag Center, Baton Rouge, LA, 70803, USA
4. Eco-Friendly Biomaterial Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Jeongeup, 580-185, Korea
5. Research Faculty of Agriculture, Hokkaido University, Sapporo, 060-8589, Japan
Abstract:Human intestinal maltase (HMA) is an ??-glucosidase responsible for the hydrolysis of ??-1,4-linkages from the non-reducing end of malto-oligosaccharides. HMA has become an important target in the treatment of type-2 diabetes. In this study, epigallocatechin gallate (EGCG) and EGCG glucoside (EGCG-G1) were identified as inhibitors of HMA by an in vitro assay with IC50 of 20 ± 1.0 and 31.5 ± 1.0 ??M, respectively. A Lineweaver-Burk plot confirmed that EGCG and EGCG-G1 were competitive inhibitors of maltose substrate against HMA and inhibition kinetic constants (K i ) calculated from a Dixon plot were 5.93 ± 0.26 and 7.88 ± 0.57 ??M, respectively. Both EGCG and EGCG-G1 bound to the active site of HMA with numerous hydrophobic and hydrogen bond interactions.
Keywords:
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