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Inhibition Mechanism of α-Amylase/α-Glucosidase by Silibinin, Its Synergism with Acarbose, and the Effect of Milk Proteins
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-08-31 , DOI: 10.1021/acs.jafc.1c01765
Jichen Yang 1 , Huan Li 1 , Xiaoli Wang 1 , Chuanying Zhang 1 , Guo Feng 1 , Xin Peng 2, 3
Affiliation  

As a natural flavonolignan, silibinin is reported to possess multiple biological activities, while the inhibitory potential of silibinin on carbohydrate-hydrolyzing enzymes is still unclear. Therefore, in this study, the inhibitory effect and underlying mechanism of silibinin against α-amylase/α-glucosidase were investigated. The results indicated that silibinin showed a strong inhibitory efficiency against α-amylase/α-glucosidase in noncompetitive manners and exhibited synergistic inhibition against α-glucosidase with acarbose. However, interestingly, the inhibitory effect of silibinin was significantly hindered in various milk protein-rich environments, but this phenomenon disappeared after simulated gastrointestinal digestion of milk proteins in vitro. Furthermore, silibinin could combine with the inactive site of α-amylase/α-glucosidase and change the microenvironment and secondary structure of the enzymes, thereby influencing the catalytic efficiency of enzymes. This research suggested that silibinin could be used as a novel carbohydrate-hydrolyzing enzyme inhibitor, and milk beverages rich in silibinin had the potential for further application in antidiabetic dietary or medicine.

中文翻译:

水飞蓟宾对α-淀粉酶/α-葡萄糖苷酶的抑制机制、与阿卡波糖的协同作用及乳蛋白的作用

据报道,作为一种天然黄酮木脂素,水飞蓟宾具有多种生物活性,而水飞蓟宾对碳水化合物水解酶的抑制潜力尚不清楚。因此,在本研究中,研究了水飞蓟宾对α-淀粉酶/α-葡萄糖苷酶的抑制作用和潜在机制。结果表明,水飞蓟宾对α-淀粉酶/α-葡萄糖苷酶具有很强的非竞争性抑制作用,并与阿卡波糖对α-葡萄糖苷酶具有协同抑制作用。然而,有趣的是,水飞蓟宾的抑制作用在各种富含乳蛋白的环境中受到显着阻碍,但在体外模拟胃肠道消化乳蛋白后,这种现象消失了. 此外,水飞蓟宾可以与α-淀粉酶/α-葡萄糖苷酶的非活性位点结合,改变酶的微环境和二级结构,从而影响酶的催化效率。该研究表明,水飞蓟宾可以作为一种新型的碳水化合物水解酶抑制剂,富含水飞蓟宾的乳饮料具有进一步应用于抗糖尿病饮食或药物的潜力。
更新日期:2021-09-15
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