Fabrication of a Magnetic Porous Organic Polymer for α-Glucosidase Immobilization and Its Application in Inhibitor Screening

Abstract

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 Fe 3 O 4 @POP composite with a core− shell structure was constructed for the first time with Fe 3 O 4 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 α-glucosidase. Fe 3 O 4 @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. Fe 3 O 4 @POP exhibited a distinct core−shell structure and excellent magnetic response (45.2 emu g −1 ). α-Glucosidase was covalently immobilized on core−shell Fe 3 O 4 @POP magnetic nanoparticles using glutaraldehyde as the cross-linking agent. The immobilized α-glucosidase possessed improved pH stability and thermal stability as well as good storage stability and reusability. More importantly, the immobilized enzyme exhibited a lower K m value and enhanced affinity for the substrate than the free one. The immobilized α-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.

α-Glucosidase immobilization on the metal–organic framework composite membrane for enzyme inhibitor screening

“…Additionally, compared to other immobilized α-glucosidase materials, the ZIF-8@PDA@PVDF system demonstrates significantly superior reusability. For instance, after being reused 10 times, enzyme activity of only 72.4% and 68.4% was retained for magnetic porous organic polymer 30 and cellulose filter paper 31 immobilized α-glucosidase, respectively.…”

Reactive Polymer Composite Microparticles Based on Glycidyl Methacrylate and Magnetite Nanoparticles

“…Polymer coatings can be used to prevent MNPs from aggregation and agglomeration, increase compatibility between MNPs and the aqueous environment, prevent their surface from oxidizing, reduce toxicity, prevent direct contact of the magnetic substance with the environment, increase colloidal and chemical stability, and facilitate storage or transportation. At the same time, the modification of the iron oxide surface with polymers can expand the scope of the use of materials that have embedded magnetic nanoparticles with completely new applications, such as water purification [25][26][27], cell separation and detection [28,29], proteins, nucleic acids, enzymes [30][31][32], and catalyst immobilization [33][34][35], as well as in various fields of biotechnology and biomedicine, for example, as systems for targeted drug delivery, DNA isolation, and magnetic hyperthermia targeted drug delivery, and magnetic resonance imaging (MRI) [18,[35][36][37][38].…”