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

IF 3.1 2区 农林科学 Q2 CHEMISTRY, APPLIED Plant Foods for Human Nutrition Pub Date : 2024-03-01 Epub Date: 2023-11-25 DOI:10.1007/s11130-023-01123-0
Yao Jiang, Feifei Liu, Dan Zhang, Xiujuan Fu, Siwei Chen, Mei Wei, Zhi Li, Hui Lei, Hong Niu
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Abstract

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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新型葡萄糖苷酶抑制剂的鉴定利用光谱学和分子对接。
牛蒡子(Syzygium jambos, L.)的果实被认为是一种“食物”,具有显著的抗糖尿病活性。然而,目前还没有研究证实其对α-葡萄糖苷酶的抑制作用。摘要本研究共从黄芪中分离得到14个化合物。其中8种化合物对α-葡萄糖苷酶均有显著抑制作用,IC50值在0.011 ~ 0.665 mM之间,其中化合物1 ~ 3 (IC50分别为0.013、0.011和0.030 mM)的抑制活性明显高于阿卡波糖(IC50为2.329±0.109 mM)。酶动力学研究表明,化合物1为非竞争性抑制剂,化合物2 ~ 8为混合型抑制剂。此外,通过分子对接研究了化合物与α-葡萄糖苷酶的相互作用,进一步揭示了十六烷基酚的烯烃双键数和2-COOH对α-葡萄糖苷酶的抑制活性有显著影响。本研究表明,牛蒡果可作为一种预防糖尿病的功能性食品。
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来源期刊
Plant Foods for Human Nutrition
Plant Foods for Human Nutrition 工程技术-食品科技
CiteScore
6.80
自引率
7.50%
发文量
89
审稿时长
12-24 weeks
期刊介绍: Plant Foods for Human Nutrition (previously Qualitas Plantarum) is an international journal that publishes reports of original research and critical reviews concerned with the improvement and evaluation of the nutritional quality of plant foods for humans, as they are influenced by: - Biotechnology (all fields, including molecular biology and genetic engineering) - Food science and technology - Functional, nutraceutical or pharma foods - Other nutrients and non-nutrients inherent in plant foods
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