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The lipase inhibitory effect of mulberry leaf phenolic glycosides: The structure-activity relationship and mechanism of action

文献类型： 外文期刊

作者： Zou, Yuxiao 1 ; Mei, Chunying 1 ; Liu, Fan 1 ; Xing, Dongxu 1 ; Pang, Daorui 1 ; Li, Qian 1 ;

作者机构： 1.Guangdong Acad Agr Sci, Sericultural & Agrifood Res Inst, Minist Agr & Rural Affairs, Key Lab Funct Foods,Guangdong Key Lab Agr Prod Pr, Guangzhou 510610, Peoples R China

2.South China Agr Univ, Coll Food Sci, Guangzhou 510642, Peoples R China

关键词： Mulberry leaf; Phenolic glycoside; Molecular docking

期刊名称：FOOD CHEMISTRY （ 影响因子：8.5； 五年影响因子：8.2 ）

ISSN： 0308-8146

年卷期： 2024 年 458 卷

页码：

收录情况： SCI

摘要： The present study found for the first time that phenolic glycosides were an important material basis for mulberry leaves to inhibit lipase. The corresponding IC 50 for hyperoside, rutin, astragalin and quercetin were 68, 252, 385 and 815 mu g/mL respectively. The inhibitory effect was ranked as monoglycosides > phenolic hydroxyl groups > disaccharides on the benzone ring. Hyperoside bound to lipase in competitive inhibition type with one binding site, while the others bound to lipase in a mixed inhibition type by two similar sites. All four compounds altered the microenvironment and secondary conformation of lipase through static quenching. The docking score, stability, and binding energy were consistent with the compound inhibitory activity. The main binding between compounds and lipase amino acid residues were spontaneously though hydrophobic interactions and hydrogen bonding. The strong hydrogen bonds formed with SER-152 inside the lipase pocket, might be important for the strong inhibitory activity of hyperoside.

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