Identification of Novel -Glucosidase Inhibitors from Syzygium jambos (L.) Using Spectroscopy and Molecular Docking

被引:0
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作者
Yao Jiang
Feifei Liu
Dan Zhang
Xiujuan Fu
Siwei Chen
Mei Wei
Zhi Li
Hui Lei
Hong Niu
机构
[1] Southwest Medical University,School of Pharmacy
[2] Jiangsu Normal University,School of Life Sciences
[3] The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University,undefined
来源
关键词
Type 2 diabetes; (L.) Alston fruit; Alkylphenol derivatives; -glucosidase inhibition; Molecular docking;
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学科分类号
摘要
Fruits of Syzygium jambos (L.) are recognized as a “food”, exhibiting significant antidiabetic activities. However, the α-glucosidase inhibition of the components from Syzygium jambos (L.) have not yet been investigated. In this study, a total of 14 compounds were isolated from Syzygium jambos (L.) Alston, eight of which showed significant inhibitory effects on α-glucosidase, with IC50 values in the range of 0.011–0.665 mM. Notably, compounds 1–3 (IC50: 0.013, 0.011 and 0.030 mM, respectively) exhibited much stronger activity than acarbose (IC50: 2.329 ± 0.109 mM). The enzyme kinetics study indicated that compound 1 was an uncompetitive inhibitor, and compounds 2–8 were mixed-type inhibitors. Moreover, the interactions between compounds and α-glucosidase were investigated by molecular docking, which further revealed that the number of olefin double bonds and 2-COOH of heptadeca-phenols had a notable effect on the α-glucosidase inhibitory activity. This study demonstrated that Syzygium jambos (L.) fruit might serve as a functional food for the prevention of diabetes mellitus.
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页码:73 / 82
页数:9
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