KMID : 1094720120170050966
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Biotechnology and Bioprocess Engineering 2012 Volume.17 No. 5 p.966 ~ p.971
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Inhibitory effects of epigallocatechin gallate and its glucoside on the human intestinal maltase inhibition
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Nguyen Thi Thanh Hanh
Jung Sun-Hwa Lee Sun Ryu Hwa-Ja Kang Hee-Kyoung Moon Young-Hwan Kim Young-Min Kimura Atsuo Kim Do-Man
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Abstract
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Human intestinal maltase (HMA) is an ¥á-glucosidase responsible for the hydrolysis of ¥á-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 ¡¾ 1.0 and 31.5 ¡¾ 1.0 ¥ìM, 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 ¡¾ 0.26 and 7.88 ¡¾ 0.57 ¥ìM, respectively. Both EGCG and EGCG-G1 bound to the active site of HMA with numerous hydrophobic and hydrogen bond interactions.
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KEYWORD
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alpha-glucosidase, human intestinal maltase, EGCG, EGCG glucoside, molecular docking
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