Chemical synthesis, inhibitory activity and molecular mechanism of 1-deoxynojirimycin-chrysin as a potent alpha-glucosidase inhibitor
文献类型： 外文期刊
作者： Zhang, Ran 1 ; Zhang, Yueyue 1 ; Huang, Gaiqun 1 ; Xin, Xiangdong 1 ; Tang, Liumei 1 ; Li, Hao 1 ; Lee, Kwang Sik 4 ; Jin 1 ;
作者机构： 1.Jiangsu Univ Sci & Technol, Sch Biotechnol, Zhenjiang 212100, Jiangsu, Peoples R China
2.Chinese Acad Agr Sci, Sericultural Res Inst, Zhenjiang 212100, Jiangsu, Peoples R China
3.Sichuan Acad Agr Sci, Sericultural Res Inst, Nanchong 637000, Sichuan, Peoples R China
4.Dong A Univ, Coll Nat Resources & Life Sci, Busan 49315, South Korea
期刊名称：RSC ADVANCES （ 影响因子：3.361； 五年影响因子：3.39 ）
ISSN：
年卷期： 2021 年 11 卷 61 期
页码：
收录情况： SCI
摘要： Hyperglycemia can be efficaciously regulated by inhibiting alpha-glucosidase activity and this is regarded as an effective strategy to treat type 2 diabetes. 1-Deoxynojimycin, an alpha-glucosidase inhibitor, can penetrate cells rapidly to potently inhibit alpha-glucosidase in a competitive manner. However, the application of 1-deoxynojimycin is limited by its poor lipophilicity and low bioavailability. Herein, three 1-deoxynojimycin derivatives 4-6 were designed and synthesized by linking 1-deoxynojimycin and chrysin to ameliorate the limitations of 1-deoxynojimycin. Among them, compound 6, a conjugate of 1-deoxynojimycin and chrysin linked by an undecane chain, could better bind to the alpha-glucosidase catalytic site, thereby exhibiting excellent alpha-glucosidase inhibitory activity (IC50 = 0.51 +/- 0.02 mu M). Kinetics analyses revealed that compound 6 inhibited the activity of alpha-glucosidase in a reversible and mixed competitive manner. Fluorescence quenching and UV-Vis spectra showed that compound 6 changed the conformation of the alpha-glucosidase via complex formation, which triggered a static fluorescence quenching of the enzyme protein.
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