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| DOI | 10.3390/molecules26154566 |
| Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel alpha-Glucosidase Inhibitor | |
| Dong, Qi; Hu, Na; Yue, Huilan; Wang, Honglun | |
| 通讯作者 | Wang, HL (通讯作者)，Northwest Inst Plateau Biol, CAS Key Lab Tibetan Med Res, Xining 810008, Peoples R China. ; Wang, HL (通讯作者)，Qinghai Prov Key Lab Tibetan Med Res, Xining 810008, Peoples R China. |
| 发表日期 | 2021 |
| EISSN | 1420-3049 |
| 卷号 | 26期号:15 |
| 英文摘要 | alpha-glucosidase is a major enzyme that is involved in starch digestion and type 2 diabetes mellitus. In this study, the inhibition of hypericin by alpha-glucosidase and its mechanism were firstly investigated using enzyme kinetics analysis, real-time interaction analysis between hypericin and alpha-glucosidase by surface plasmon resonance (SPR), and molecular docking simulation. The results showed that hypericin was a high potential reversible and competitive alpha-glucosidase inhibitor, with a maximum half inhibitory concentration (IC50) of 4.66 +/- 0.27 mg/L. The binding affinities of hypericin with alpha-glucosidase were assessed using an SPR detection system, which indicated that these were strong and fast, with balances dissociation constant (KD) values of 6.56 x 10(-5) M and exhibited a slow dissociation reaction. Analysis by molecular docking further revealed that hydrophobic forces are generated by interactions between hypericin and amino acid residues Arg-315 and Tyr-316. In addition, hydrogen bonding occurred between hypericin and alpha-glucosidase amino acid residues Lys-156, Ser-157, Gly-160, Ser-240, His-280, Asp-242, and Asp-307. The structure and micro-environment of alpha-glucosidase enzymes were altered, which led to a decrease in alpha-glucosidase activity. This research identified that hypericin, an anthracene ketone compound, could be a novel alpha-glucosidase inhibitor and further applied to the development of potential anti-diabetic drugs. |
| 关键词 | SURFACE-PLASMON RESONANCEPOSTPRANDIAL HYPERGLYCEMIADIABETES-MELLITUSKINETICSBINDINGFLAVONOIDSHYPERFORININCREASESEXTRACTACID |
| 英文关键词 | hypericin; alpha-glucosidase inhibitor; mechanism |
| 语种 | 英语 |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| WOS类目 | Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary |
| WOS记录号 | WOS:000682251500001 |
| 来源期刊 | MOLECULES
 |
| 来源机构 | 中国科学院西北生态环境资源研究院 |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://gcip.llas.ac.cn/handle/2XKMVOVA/254020 |
| 作者单位 | [Dong, Qi; Hu, Na; Yue, Huilan; Wang, Honglun] Northwest Inst Plateau Biol, CAS Key Lab Tibetan Med Res, Xining 810008, Peoples R China; [Dong, Qi; Hu, Na; Yue, Huilan; Wang, Honglun] Qinghai Prov Key Lab Tibetan Med Res, Xining 810008, Peoples R China; [Dong, Qi] Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dong, Qi,Hu, Na,Yue, Huilan,et al. Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel alpha-Glucosidase Inhibitor[J]. 中国科学院西北生态环境资源研究院,2021,26(15). |
| APA | Dong, Qi,Hu, Na,Yue, Huilan,&Wang, Honglun.(2021).Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel alpha-Glucosidase Inhibitor.MOLECULES,26(15). |
| MLA | Dong, Qi,et al."Inhibitory Activity and Mechanism Investigation of Hypericin as a Novel alpha-Glucosidase Inhibitor".MOLECULES 26.15(2021). |
| 条目包含的文件 | 条目无相关文件。 | |||||
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