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沉香叶茶中天然α-葡萄糖苷酶抑制剂的靶向生物亲和筛选、鉴定及抑制机制

Natural α-glucosidase inhibitors from Aquilaria sinensis leaf-tea: Targeted bio-affinity screening, identification, and inhibition mechanism.

机构信息

School of Food Science and Engineering, Hainan University, Haikou 570228, PR China.

School of Food Science and Engineering, Hainan University, Haikou 570228, PR China; Key Laboratory of Food Nutrition and Functional Food of Hainan Province, Hainan University, Haikou 570228, PR China.

出版信息

Food Chem. 2025 Jan 15;463(Pt 2):141329. doi: 10.1016/j.foodchem.2024.141329. Epub 2024 Sep 17.

DOI:10.1016/j.foodchem.2024.141329
PMID:39305674
Abstract

Aquilaria sinensis leaves have long been consumed as a popular replacement tea for lowering postprandial blood glucose levels, but their specific functional components remain unclear. In this study, Aquilaria sinensis leaf-tea 70 % ethanol extract (ALTE) exhibited excellent anti-α-glucosidase activity (IC = 6.93 ± 1.91 μg/mL) and promoted glucose consumption ability in 3 T3-L1 preadipocyte cells. Subsequently phenolic compositions of ALTE were identified for the first time. After that, five potential α-glucosidase inhibitors (α-GIs) including cynaroside-3,5-diglucose, malvidin 3-glucose, epicatechin, epigallocatechin gallate, and dihydromyricetin in ALTE were screened using a targeted bio-affinity ultrafiltration-HPLC/MS method. Moreover, these five α-GIs all showed good anti-α-glucosidase effects and glucose consumption-promoting ability. Furthermore, the binding properties and inhibition mechanisms of five α-GIs to α-glucosidase were further analyzed via enzyme inhibition kinetics, molecular docking, and molecular dynamics simulation. This study confirms that Aquilaria sinensis leaf-tea is effective in preventing post-hyperglycemia in vitro models, suggesting potential for future research in human trials.

摘要

白木香叶长期以来一直被用作降低餐后血糖水平的流行代茶,但它们的特定功能成分仍不清楚。在这项研究中,白木香叶茶 70%乙醇提取物(ALTE)表现出优异的抗α-葡萄糖苷酶活性(IC=6.93±1.91μg/mL),并能促进 3T3-L1 前体脂肪细胞的葡萄糖消耗能力。随后首次鉴定了 ALTE 的酚类成分。之后,采用靶向生物亲和超滤 HPLC/MS 方法筛选了 ALTE 中的 5 种潜在的α-葡萄糖苷酶抑制剂(α-GIs),包括梓醇-3,5-二葡萄糖、矢车菊素-3-葡萄糖、表儿茶素、没食子酸表儿茶素酯和二氢杨梅素。此外,这 5 种 α-GIs 均表现出良好的抗α-葡萄糖苷酶作用和促进葡萄糖消耗能力。此外,还通过酶抑制动力学、分子对接和分子动力学模拟进一步分析了 5 种 α-GIs 与α-葡萄糖苷酶的结合特性和抑制机制。这项研究证实,白木香叶茶在体外模型中有效预防高血糖后状态,提示在临床试验中进行进一步研究的潜力。

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