表没食子儿茶素没食子酸酯及其糖苷对人肠道麦芽糖酶的抑制作用。
Inhibitory effects of epigallocatechin gallate and its glucoside on the human intestinal maltase inhibition.
作者信息
Nguyen Thi Thanh Hanh, Jung Sun-Hwa, Lee Sun, Ryu Hwa-Ja, Kang Hee-Kyoung, Moon Young-Hwan, Kim Young-Min, Kimura Atsuo, Kim Doman
机构信息
1School of Biological Sciences and Technology and Research Institute for Catalysis, Chonnam National University, Gwangju, 500-757 Korea.
2Interdisciplinary Program of Graduate School for Bioenergy and Biomaterials, Chonnam National University, Gwangju, 500-757 Korea.
出版信息
Biotechnol Bioprocess Eng. 2012;17(5):966-971. doi: 10.1007/s12257-012-0242-8. Epub 2012 Oct 24.
Abstract
Human intestinal maltase (HMA) is an α-glucosidase responsible for the hydrolysis of α-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 assay with IC of 20 ± 1.0 and 31.5 ± 1.0 μM, respectively. A Lineweaver-Burk plot confirmed that EGCG and EGCG-G1 were competitive inhibitors of maltose substrate against HMA and inhibition kinetic constants ( ) calculated from a Dixon plot were 5.93 ± 0.26 and 7.88 ± 0.57 μM, respectively. Both EGCG and EGCG-G1 bound to the active site of HMA with numerous hydrophobic and hydrogen bond interactions.
摘要
人肠道麦芽糖酶（HMA）是一种α-葡萄糖苷酶，负责从麦芽寡糖的非还原端水解α-1,4-糖苷键。HMA已成为2型糖尿病治疗中的一个重要靶点。在本研究中，表没食子儿茶素没食子酸酯（EGCG）和表没食子儿茶素葡萄糖苷（EGCG-G1）通过一种测定法被鉴定为HMA的抑制剂，其IC分别为20±1.0和31.5±1.0μM。双倒数作图证实EGCG和EGCG-G1是麦芽糖底物针对HMA的竞争性抑制剂，根据Dixon作图计算的抑制动力学常数（）分别为5.93±0.26和7.88±0.57μM。EGCG和EGCG-G1均通过大量疏水和氢键相互作用与HMA的活性位点结合。
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