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生物亲和超滤结合高效液相色谱-电喷雾串联质谱法从石榴皮中筛选潜在的α-葡萄糖苷酶抑制剂

Bioaffinity ultrafiltration coupled with HPLC-ESI-MS/MS for screening potential α-glucosidase inhibitors from pomegranate peel.

作者信息

Shi Rujie, Zhou Nong, Zhang Han, Gong Min, Han Lin

机构信息

College of Biology and Food Engineering, Chongqing Three Gorges University, Chongqing, China.

College of Food Science and Engineering, Northwest A&F University, Yangling, China.

出版信息

Front Nutr. 2022 Oct 18;9:1014862. doi: 10.3389/fnut.2022.1014862. eCollection 2022.

Abstract

Pomegranate peel (PoP) contains plenty of bioactive compounds and exhibits strong activity to prevent postprandial hyperglycaemia and improve diabetes mellitus. Presently, bioaffinity ultrafiltration coupled with high performance liquid chromatography-electrospray ionization mass spectrometry (HPLC-ESI-MS/MS) is employed to screen and identify the efficient α-glucosidase inhibitors in PoP and the detailed inhibitory mechanisms are further investigated. The results show that many substances, including ellagic acid, kaempferol, gallic acid, and resveratrol in PoP reveal strong activity to inhibit α-glucosidase and ellagic acid (EA) is screened as the most effective compound. Further research indicates that EA plays a competitive and reversible inhibition role against α-glucosidase with the value of i was 6.24 × 10 mol/L. EA also directly interacts with the amino acids of α-glucosidase mainly van der Waals forces and hydrogen bonds, thereby, influencing the secondary structure and stability of α-glucosidase. Finally, the α-glucosidase inhibitory activity of EA is further confirmed to significantly reduce postprandial blood glucose .

摘要

石榴皮含有大量生物活性化合物,对预防餐后高血糖和改善糖尿病具有很强的活性。目前,采用生物亲和超滤结合高效液相色谱 - 电喷雾电离质谱(HPLC - ESI - MS/MS)来筛选和鉴定石榴皮中有效的α - 葡萄糖苷酶抑制剂,并进一步研究其详细的抑制机制。结果表明,石榴皮中的许多物质,包括鞣花酸、山奈酚、没食子酸和白藜芦醇,都具有很强的抑制α - 葡萄糖苷酶的活性,其中鞣花酸(EA)被筛选为最有效的化合物。进一步研究表明,EA对α - 葡萄糖苷酶起竞争性和可逆性抑制作用,抑制常数Ki为6.24×10⁻⁵mol/L。EA还主要通过范德华力和氢键与α - 葡萄糖苷酶的氨基酸直接相互作用,从而影响α - 葡萄糖苷酶的二级结构和稳定性。最后,EA的α - 葡萄糖苷酶抑制活性进一步得到证实,可显著降低餐后血糖。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3824/9623087/5d191a2ac861/fnut-09-1014862-g001.jpg

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