School of Science, Xihua University, Chengdu, China.
Asymmetric Synthesis and Chiral Technology Key Laboratory of Sichuan Province, Xihua University, Chengdu, China.
J Sep Sci. 2024 Jul;47(14):e2400342. doi: 10.1002/jssc.202400342.
In this study, a ligand fishing method for the screening of α-glucosidase inhibitors from Ginkgo biloba leaf was established for the first time using α-glucosidase immobilized on the magnetic metal-organic framework. The immobilized α-glucosidase exhibited enhanced resistance to temperature and pH, as well as good thermal stability and reusability. Two ligands, namely quercitrin and quercetin, were screened from Ginkgo biloba leaf and identified by ultra-high performance liquid chromatography-tandem mass spectrometry. The half-maximal inhibitory concentration values for quercitrin and quercetin were determined to be 105.69 ± 0.39 and 83.49 ± 0.79 µM, respectively. Molecular docking further confirmed the strong inhibitory effect of these two ligands. The proposed approach in this study demonstrates exceptional efficiency in the screening of α-glucosidase inhibitors from complex natural medicinal plants, thus exhibiting significant potential for the discovery of antidiabetic compounds.
本研究首次建立了一种利用固定化α-葡萄糖苷酶的磁性金属有机骨架筛选银杏叶α-葡萄糖苷酶抑制剂的配体钓取方法。固定化α-葡萄糖苷酶表现出对温度和 pH 的增强抗性，以及良好的热稳定性和可重复使用性。从银杏叶中筛选出两种配体槲皮素和槲皮苷，并通过超高效液相色谱-串联质谱法进行鉴定。确定槲皮素和槲皮苷的半最大抑制浓度值分别为 105.69±0.39 和 83.49±0.79 μM。分子对接进一步证实了这两种配体的强烈抑制作用。本研究中提出的方法在从复杂的天然药用植物中筛选α-葡萄糖苷酶抑制剂方面表现出了极高的效率，因此在发现抗糖尿病化合物方面具有显著的潜力。
