State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang, P. R. China.
Institute for Advanced Study, Nanchang University, Nanchang, P. R. China.
J Food Biochem. 2022 Oct;46(10):e14328. doi: 10.1111/jfbc.14328. Epub 2022 Jul 27.
Peptides derived from egg protein hydrolysate have potential hypoglycemic benefits by inhibiting α-glucosidase. Herein, fluorescence spectroscopy and molecular docking were performed to investigate the α-glucosidase inhibitory mechanism of the oligopeptides ARDASVLK and HNKPEVEVR from soft-shelled turtle eggs. Gastrointestinal digestion characteristics of the two oligopeptides were further determined by LC-QTOF-MS/MS. The static fluorescence quenching of α-glucosidase by ARDASVLK and HNKPEVEVR indicated the formation of a stable α-glucosidase-peptide complex, mainly driven by hydrogen bonds and hydrophobic interactions. ARDASVLK and HNKPEVEVR could easily insert into the active pocket of α-glucosidase (docking scores of -157.1 and -158.4, respectively), thereby inhibiting enzyme activity by preventing substrate binding and inducing enzymatic conformation change. After gastrointestinal digestion, 14.3% and 30.4% of ARDASVLK and HNKPEVEVR were maintained intact, respectively, and their digestive products (mainly DASVLK and HNKPEVEV) still showed high inhibitory effects on α-glucosidase (about 35% inhibition). This study sheds light on the mechanism of oligopeptides derived from soft-shelled turtle eggs as a novel α-glucosidase inhibitor for diabetes. PRACTICAL APPLICATIONS: Oligopeptides from egg protein hydrolysate have potential hypoglycemic properties by inhibiting α-glucosidase. This study has provided insights into the inhibitory mechanism of oligopeptides from soft-shelled turtle egg on α-glucosidase. Interestingly, despite the fact that the oligopeptides are largely degraded during gastrointestinal digestion, their digestive metabolites displayed strong α-glucosidase inhibitory activities. Because α-glucosidase is highly expressed in small intestine brush border, our findings support the possibility of these oligopeptides as an attractive health-benefit compound to control glucose without being absorbed by intestinal epithelial cells, unlike other enzyme inhibitors such as ACE inhibitors, which have poor oral bioavailability. This study may facilitate the applications of oligopeptides from soft-shelled turtle egg as α-glucosidase inhibitors and food functional ingredients for the therapy of diabetes.
从卵蛋白水解物中衍生的肽通过抑制α-葡萄糖苷酶具有潜在的降血糖益处。在此,通过荧光光谱和分子对接研究了软壳龟卵来源的寡肽 ARDASVLK 和 HNKPEVEVR 对α-葡萄糖苷酶的抑制机制。通过 LC-QTOF-MS/MS 进一步确定了这两种寡肽的胃肠消化特性。ARDASVLK 和 HNKPEVEVR 对α-葡萄糖苷酶的静态荧光猝灭表明形成了稳定的α-葡萄糖苷酶-肽复合物,主要由氢键和疏水相互作用驱动。ARDASVLK 和 HNKPEVEVR 可以很容易地插入α-葡萄糖苷酶的活性口袋(对接评分分别为-157.1 和-158.4),从而通过阻止底物结合和诱导酶构象变化来抑制酶活性。经胃肠消化后,ARDASVLK 和 HNKPEVEVR 分别有 14.3%和 30.4%保持完整,其消化产物(主要为 DASVLK 和 HNKPEVEV)仍对α-葡萄糖苷酶表现出高抑制作用(约 35%抑制)。这项研究揭示了软壳龟卵来源的寡肽作为新型α-葡萄糖苷酶抑制剂用于糖尿病的机制。实际应用:卵蛋白水解物衍生的寡肽通过抑制α-葡萄糖苷酶具有降血糖作用。本研究深入探讨了软壳龟卵来源的寡肽对α-葡萄糖苷酶的抑制机制。有趣的是,尽管寡肽在胃肠消化过程中大部分被降解,但它们的消化代谢产物仍表现出很强的α-葡萄糖苷酶抑制活性。由于α-葡萄糖苷酶在小肠刷状缘高度表达,我们的研究结果支持这些寡肽作为一种有吸引力的健康益处化合物来控制葡萄糖的可能性,而不像其他酶抑制剂(如 ACE 抑制剂)那样,由于肠道上皮细胞的吸收不良,其口服生物利用度较差。本研究可能有助于将软壳龟卵来源的寡肽作为α-葡萄糖苷酶抑制剂和食品功能成分应用于糖尿病的治疗。