刺梨中的生物活性类黄酮通过抑制α-葡萄糖苷酶和α-淀粉酶来改善餐后高血糖。

Bioactive flavonoids from Rubus corchorifolius inhibit α-glucosidase and α-amylase to improve postprandial hyperglycemia.

机构信息

College of Food Science, Shenyang Agricultural University, National R&D Professional Center For Berry Processing, National Engineering and Technology of Research Center For Small Berry, Key Laborotary of Healthy Food Nutrition and Innovative Manufacturing, Liaoning Province, Shenyang, Liaoning 110866, China.

出版信息

Food Chem. 2021 Mar 30;341(Pt 1):128149. doi: 10.1016/j.foodchem.2020.128149. Epub 2020 Sep 22.

DOI:10.1016/j.foodchem.2020.128149

PMID:33039745

Abstract

This research established an optimized method for the extraction and enrichment of flavonoids from R. corchorifolius fruit. Under the optimized extraction conditions, 12 flavonoids (1-12) were isolated, of which six (2-4, 9-10, 12) were obtained from R. corchorifolius for the first time. Compound 4 showed significant α-glucosidase (4.96 μM) and α-amylase (8.04 μM) inhibitory effects. Molecular modeling revealed that compound 4 exhibits strong binding with the active sites of α-glucosidase and α-amylase. Lineweaver-Burk plot analysis and surface plasmon resonance revealed the possible dynamic binding mechanism of the flavonoids with α-glucosidase and α-amylase. The enriched flavonoids and compound 4 showed significant hypoglycemic effects in mice administered a high dose of glucose. In this study, a variety of flavonoids with hypoglycemic activity were found for the first time, revealing the rich chemical composition of R. corchorifolius fruit and highlighting the potential value of R. corchorifolius fruit flavonoids as dietary supplements.

摘要

本研究建立了从黄蜀葵花中提取和富集类黄酮的优化方法。在优化的提取条件下，分离得到了 12 种类黄酮（1-12），其中 6 种（2-4、9-10、12）为黄蜀葵花中的首次发现。化合物 4 对 α-葡萄糖苷酶（4.96 μM）和 α-淀粉酶（8.04 μM）具有显著的抑制作用。分子对接表明，化合物 4 与 α-葡萄糖苷酶和 α-淀粉酶的活性部位具有较强的结合能力。Lineweaver-Burk 作图分析和表面等离子体共振实验揭示了类黄酮与 α-葡萄糖苷酶和 α-淀粉酶的可能动态结合机制。高剂量葡萄糖给药的小鼠中，富集的类黄酮和化合物 4 表现出显著的降血糖作用。本研究首次发现了具有降血糖活性的多种类黄酮，揭示了黄蜀葵花果实丰富的化学成分，并强调了黄蜀葵花果实类黄酮作为膳食补充剂的潜在价值。