Guo Fengyu, An Jie, Wang Minlong, Zhang Weibo, Chen Chong, Mao Xueying, Liu Siyuan, Wang Pengjie, Ren Fazheng
College of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, China.
Department of Nutrition and Health, China Agricultural University, Beijing 100083, China.
Foods. 2023 Sep 13;12(18):3415. doi: 10.3390/foods12183415.
In this study, 12 flavonoid glycosides were selected based on virtual screening and the literature, and Quercimeritrin was selected as the best selective inhibitor of α-glucosidase through in vitro enzyme activity inhibition experiments. Its IC value for α-glucosidase was 79.88 µM, and its IC value for α-amylase >250 µM. As such, it could be used as a new selective inhibitor of α-glucosidase. The selective inhibition mechanism of Quercimeritrin on the two starch-digesting enzymes was further explored, and it was confirmed that Quercimeritrin had a strong binding affinity for α-glucosidase and occupied the binding pocket of α-glucosidase through non-covalent binding. Subsequently, animal experiments demonstrated that Quercimeritrin can effectively control postprandial blood glucose in vivo, with the same inhibitory effect as acarbose but without side effects. Our results, therefore, provide insights into how flavone aglycones can be used to effectively control the rate of digestion to improve postprandial blood glucose levels.
在本研究中，基于虚拟筛选和文献选择了12种黄酮苷，并通过体外酶活性抑制实验将金丝桃苷选为α-葡萄糖苷酶的最佳选择性抑制剂。其对α-葡萄糖苷酶的IC值为79.88 μM，对α-淀粉酶的IC值>250 μM。因此，它可作为一种新型的α-葡萄糖苷酶选择性抑制剂。进一步探究了金丝桃苷对两种淀粉消化酶的选择性抑制机制，证实金丝桃苷对α-葡萄糖苷酶具有很强的结合亲和力，并通过非共价结合占据了α-葡萄糖苷酶的结合口袋。随后的动物实验表明，金丝桃苷可有效控制体内餐后血糖，其抑制作用与阿卡波糖相同，但无副作用。因此，我们的研究结果为黄酮苷元如何有效控制消化速率以改善餐后血糖水平提供了见解。
