Rapid screening of alpha-glucosidase inhibitors in Hypericum perforatum L. using bio-affinity chromatography coupled with UPLC/MS

	Rapid screening of alpha-glucosidase inhibitors in Hypericum perforatum L. using bio-affinity chromatography coupled with UPLC/MS
	Dong, Q; Hu, N; Yue, HL; Wang, HL; Wei, Y
刊名	BIOMEDICAL CHROMATOGRAPHY
	2022
英文摘要	alpha-glucosidase inhibitors (AGIs) are widely used for the treatment of type 2 diabetes, but their side effects have made it to develop novel and alternative AGIs immediately. In this study, the extract of Hypericum perforatum L. (HPE) has been confirmed to have alpha-glucosidase inhibitory activity in vitro and in vivo. Seven active compounds, rutin, hyperoside, isoquercitrin, avicularin, quercitrin, quercetin, and biapigenin, were screened based on a bio-affinity chromatography column with alpha-glucosidase enzyme-conjugated solid phase and UPLC/MS, which exhibited excellent alpha-glycosidase inhibitory effects by the determined IC50 values. The mechanism of alpha-glycosidase inhibitory activity of biapigenin was studied for the first time. The results showed that biapigenin was a high-potential, reversible, and mixed enzyme inhibitor. Analysis by molecular docking further revealed that hydrophobic interactions were generated by interactions between biapigenin and amino acid residues LYS156, PHE303, PHE314, and LEU313. In addition, hydrogen bonding occurred between biapigenin and alpha-glucosidase amino acid residues ASP307, SER241, and LYS156. This research identified that biapigenin could be a novel AGI and further applied to the development of potential anti-diabetic drugs. Furthermore, our studies established a rapid in vitro screening method for AGIs from plants.
内容类型	期刊论文
源URL	[http://210.75.249.4/handle/363003/61072]
专题	西北高原生物研究所_中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Dong, Q,Hu, N,Yue, HL,et al. Rapid screening of alpha-glucosidase inhibitors in Hypericum perforatum L. using bio-affinity chromatography coupled with UPLC/MS[J]. BIOMEDICAL CHROMATOGRAPHY,2022.
APA	Dong, Q,Hu, N,Yue, HL,Wang, HL,&Wei, Y.(2022).Rapid screening of alpha-glucosidase inhibitors in Hypericum perforatum L. using bio-affinity chromatography coupled with UPLC/MS.BIOMEDICAL CHROMATOGRAPHY.
MLA	Dong, Q,et al."Rapid screening of alpha-glucosidase inhibitors in Hypericum perforatum L. using bio-affinity chromatography coupled with UPLC/MS".BIOMEDICAL CHROMATOGRAPHY (2022).