文献类型：期刊文献

英文题名：Fabrication of a Magnetic Porous Organic Polymer for ?-Glucosidase Immobilization and Its Application in Inhibitor Screening

作者：Wan, Guang-Zhen[1];Ma, Xiao-Hui[2];Jin, Ling[2];Chen, Juan[1]

第一作者：Wan, Guang-Zhen

通信作者：Chen, J[1];Jin, L[2]

机构：[1]Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China;[2]Gansu Univ Chinese Med, Coll Pharm, Lanzhou 730000, Peoples R China

第一机构：Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China

通信机构：[1]corresponding author), Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China;[2]corresponding author), Gansu Univ Chinese Med, Coll Pharm, Lanzhou 730000, Peoples R China.|[1073501e14fb35863569f]甘肃中医药大学药学院（西北中藏药协同创新中心办公室）;[10735]甘肃中医药大学;

年份：2023

卷号：39

期号：15

起止页码：5239

外文期刊名：LANGMUIR

收录：;EI(收录号：20231513882718);Scopus(收录号：2-s2.0-85152129959);WOS:【SCI-EXPANDED(收录号:WOS:000967758600001)】；

基金：This work was supported by the Special Foundation for National Science and Technology Basic Resources of China (No. 2018FY100701) , the Key Program of Natural Science Foundation of Gansu Province, China (No. 20JR10RA584) , the 2021 Project of the State Drug Administration-Key Laboratory of Quality Control of Chinese Medicinal Materials and Decoction Pieces, China (No. 2021GSMPAKL12) , andthe 2021 Project of Gansu Medical Products Administration (No. 2021GSMPA008) .

语种：英文

外文关键词：Capillary electrophoresis - Core shell nanoparticles - Crosslinking - Diagnosis - Drug delivery - Enzyme activity - Enzyme immobilization - High resolution transmission electron microscopy - Nanomagnetics - Reusability - Shells (structures)

摘要：The technology based on immobilized enzymes was employed to screen the constituents inhibiting disease-related enzyme activity from traditional Chinese medicine, which is expected to become an important approach of innovative drug development. Herein, the Fe3O4@POP composite with a core- shell structure was constructed for the first time with Fe3O4 magnetic nanoparticles as the core, 1,3,5-tris (4-aminophenyl) benzene (TAPB) and 2,5divinylterephthalaldehyde (DVA) as organic monomers, and used as the support for immobilizing alpha-glucosidase. Fe3O4@POP was characterized by transmission electron microscopy, energy-dispersive spectrometry, Fourier transform infrared, powder X-ray diffraction, X-ray photoelectron spectroscopy, and vibrating sample magnetometry. Fe3O4@POP exhibited a distinct core-shell structure and excellent magnetic response (45.2 emu g-1). alpha-Glucosidase was covalently immobilized on core-shell Fe3O4@POP magnetic nanoparticles using glutaraldehyde as the cross-linking agent. The immobilized alpha-glucosidase possessed improved pH stability and thermal stability as well as good storage stability and reusability. More importantly, the immobilized enzyme exhibited a lower Km value and enhanced affinity for the substrate than the free one. The immobilized alpha-glucosidase was subsequently used for inhibitor screening from 18 traditional Chinese medicines in combination with capillary electrophoresis analysis among which Rhodiola rosea exhibited the highest enzyme inhibitory activity. These positive results demonstrated that such magnetic POP-based core-shell nanoparticles were a promising carrier for enzyme immobilization and the screening strategy based on immobilized enzyme provided an effective way to rapidly explore the targeted active compounds from medicinal plants.