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

IF 8.5 1区农林科学 Q1 CHEMISTRY, APPLIED

Food Chemistry Pub Date : 2025-01-15 Epub Date: 2024-09-17 DOI:10.1016/j.foodchem.2024.141329

Yingxin Liu, Fangliang Li, Tao Fei, Xue Lin, Lu Wang, Zhonghua Liu

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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 (IC₅₀ = 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.

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水飞蓟叶茶中的天然α-葡萄糖苷酶抑制剂：靶向生物亲和性筛选、鉴定和抑制机制

长期以来，人们一直将水飞蓟叶作为降低餐后血糖水平的常用代用茶饮用，但其具体的功能成分仍不清楚。在这项研究中，水飞蓟叶茶 70% 乙醇提取物（ALTE）表现出卓越的抗α-葡萄糖苷酶活性（IC50 = 6.93 ± 1.91 μg/mL），并能促进 3 个 T3-L1 前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。随后，利用生物亲和超滤-高效液相色谱/质谱（Bio-affinity ultrafiltration-HPLC/MS）方法，筛选出了 ALTE 中五种潜在的 α-葡萄糖苷酶抑制剂（α-GIs），包括仙鹤草苷-3,5-二葡萄糖、麦冬苷-3-葡萄糖、表儿茶素、表没食子儿茶素没食子酸酯和二氢杨梅素。结果表明，这五种α-GIs均具有良好的抗α-葡萄糖苷酶作用和促进葡萄糖消耗的能力。此外，通过酶抑制动力学、分子对接和分子动力学模拟，进一步分析了五种α-GIs与α-葡萄糖苷酶的结合特性和抑制机制。这项研究证实了水飞蓟叶茶在体外模型中能有效预防后高血糖症，为今后的人体试验研究提供了可能。

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来源期刊

Food Chemistry 工程技术-食品科技

CiteScore

16.30

自引率

10.20%

发文量

3130

审稿时长

122 days

期刊介绍： Food Chemistry publishes original research papers dealing with the advancement of the chemistry and biochemistry of foods or the analytical methods/ approach used. All papers should focus on the novelty of the research carried out.