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将胆酸钠修饰的 MOF 杂化脂肪酶与疏水性候选物的增溶相结合,用于从荷叶中钓取脂肪酶抑制剂配体。

Integrating sodium cholate-modified MOF hybrid lipase and solubilization of hydrophobic candidates into a step for liganding fishing lipase inhibitors from Nelumbinis Folium.

机构信息

College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, PR China.

College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, PR China.

出版信息

J Pharm Biomed Anal. 2024 Dec 15;251:116430. doi: 10.1016/j.jpba.2024.116430. Epub 2024 Aug 27.

Abstract

Enzyme immobilization by metal organic frameworks (MOFs) is an efficient way for screening active constituents in natural products. However, the enzyme's biocatalysis activity is usually decreased due to unfavorable conformational changes during the immobilization process. In this study, sodium cholate was firstly used as the modifier for zeolitic imidazolate framework-8 (ZIF-8) immobilized lipase to increase both the stability and activity. More importantly, with the help of solubilization of sodium cholate, a total of 3 flavonoids and 6 alkaloids candidate compounds were fished out. Their structures were identified and the enzyme inhibitory activities were verified. In addition, the binding information between the candidate compound and the enzyme was displayed by molecular docking. This study provides valuable information for the improvement of immobilized enzyme activity and functional active ingredients in complicated medicinal plant extracts.

摘要

金属有机骨架(MOFs)固定化酶是筛选天然产物中活性成分的有效方法。然而,由于固定化过程中酶的构象发生不利变化,酶的生物催化活性通常会降低。在这项研究中,首先使用胆酸钠作为沸石咪唑酯骨架-8(ZIF-8)固定化脂肪酶的修饰剂,以提高其稳定性和活性。更重要的是,借助胆酸钠的增溶作用,共筛选出 3 种黄酮类和 6 种生物碱候选化合物。鉴定了它们的结构,并验证了它们对酶的抑制活性。此外,通过分子对接展示了候选化合物与酶的结合信息。这项研究为提高复杂药用植物提取物中固定化酶的活性和功能活性成分提供了有价值的信息。

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