文献类型： 外文期刊

作者： Wang, Lei ¹ ; Chen, Yinglu ¹ ; Wu, Feng ¹ ; Wu, Shasha ¹ ; Hu, Xiaojun ² ; Shi, Yawei ¹ ;

作者机构： 1.Shanxi Univ, Minist Educ, Key Lab Chem Biol & Mol Engn, Inst Biotechnol, Taiyuan 030006, Shanxi, Peoples R China

2.Shanxi Acad Agr Sci, Inst Agr Prod Proc, Taiyuan 030006, Shanxi, Peoples R China

关键词： alpha-glucosidase inhibitor; bifunctional inhibitor; LUTI; protein expression

期刊名称：ACTA BIOCHIMICA ET BIOPHYSICA SINICA （ 影响因子：3.848； 五年影响因子：3.67 ）

ISSN： 1672-9145

年卷期： 2019 年 51 卷 10 期

页码：

收录情况： SCI

摘要： Acute glucose fluctuation during the postprandial period causes a risk for type 2 diabetes mellitus (T2DM). alpha-Glucosidase inhibitors have been approved as therapeutic agents for diabetes. In the present study, a protein with alpha-glucosidase inhibitory activity from Flax (Linum usitatissimum) seeds was isolated using a one-step purification with Q-Sepharose4B column, followed by Sephacryl S-200 size-exclusion chromatography. It was identified as a trypsin inhibitor, named L. usitatissimum trypsin inhibitor (LUTI). The half maximal inhibitory concentration (IC50) of LUTI was 113.92 mu M for alpha-glucosidase and 6.17 mu M for trypsin. Lineweaver-Burk kinetic experiment showed that the protein exhibited two distinct inhibitory modes, a competitive inhibitor type for a-glucosidase and a non-competitive type for trypsin. The interaction between LUTI and alpha-glucosidase was detected through gel filtration chromatography and dynamic light scattering. Increased glucose consumption and lactic acid production were also observed following LUTI treatment in Caco-2 and HepG2 cells. LUTI inhibits not only the activity of trypsin but also the activity of alpha-glucosidase. It is expected that LUTI will become an oral hypoglycemic polypeptide drug for T2DM.