A Novel Platform Featuring Nanomagnetic Ligand Fishing Based on Fixed-Orientation Immobilized Magnetic Beads for Screening Potential Cyclooxygenase-2 Inhibitors from <i>Panax notoginseng</i> Leaves
A novel screening platform based on an Fe<sub>3</sub>O<sub>4</sub>@C@PDA-Ni<sup>2+</sup>@COX-2 ligand fishing combination with high-performance liquid chromatography–mass spectrometry was first designed, synthesized, and employed to screen and identify COX-2 inhib...
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| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-12-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/29/23/5801 |
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| Summary: | A novel screening platform based on an Fe<sub>3</sub>O<sub>4</sub>@C@PDA-Ni<sup>2+</sup>@COX-2 ligand fishing combination with high-performance liquid chromatography–mass spectrometry was first designed, synthesized, and employed to screen and identify COX-2 inhibitors from <i>Panax notoginseng</i> leaves. The obtained magnetic nanoparticles exhibit outstanding preconcentration ability that allows for controlling the enzyme orientation to avoid enzyme active site blocking, conformational changes, or denaturing during immobilization. The as-prepared Fe<sub>3</sub>O<sub>4</sub>@C@PDA-Ni<sup>2+</sup>@COX-2 composite was carefully characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier-transform infrared spectrometry (FT-IR), Xray powder diffraction (XRD), thermal gravimetric analyzer (TGA), vibrating sample magnetometer (VSM), and Zeta potential analysis. The analytical parameters influencing the magnetic solid-phase fishing efficiency were optimized by univariate and multivariate methods (Box–Behnken design) by testing a positive control and celecoxib with active and inactive COX-2. Under the optimized ligand fishing conditions, twelve potential COX-2 inhibitors were screened and characterized in <i>Panax notoginseng</i> leaves. The results indicate that the proposed method provides a simple, feasible, selective, and effective platform for the efficient screening and identification of active compounds from Chinese herbal medicine. It has guiding significance for the synthesis and development of novel anti-inflammatory drugs, and provides a reference for the efficient discovery of anti-inflammatory drugs or lead compounds from the complex system of Chinese herbal medicine. |
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| ISSN: | 1420-3049 |