School of Pharmacy, Lanzhou University, Lanzhou, P. R. China.
Gansu Institute for Drug Control, Lanzhou, P. R. China.
J Sep Sci. 2022 Jul;45(14):2724-2733. doi: 10.1002/jssc.202200232. Epub 2022 May 11.
In this study, α-glucosidase was successfully immobilized on cellulose filter paper and further applied to screening inhibitors from traditional Chinese medicines combined with capillary electrophoresis analysis. For α-glucosidase immobilization, a cellulose filter paper was used as the carrier and grafted with amino groups by coating chitosan, then α-glucosidase was covalently bonded on the amino-modified carrier via epoxy ring-opening reaction using polyethylene glycol diglycidyl ether as the crosslinker. Several parameters influencing the enzyme immobilization were optimized and the optimal values were enzyme concentration of 4 U/mL, polyethylene glycol diglycidyl ether concentration of 1.25%, chitosan concentration of 7.5 mg/mL, immobilization pH 7.0, crosslinking time of 4 h and immobilization time of 2 h. The immobilized α-glucosidase exhibited good batch-to-batch reproducibility (RSD = 2.1%, n = 5), excellent storage stability (73.5% of its initial activity after being stored at 4°C for 15 days), and reusability (75% of its initial activity after 10 repeated cycles). The Michaelis constant of immobilized α-glucosidase and half-maximal inhibitory concentration of acarbose were calculated to be 1.12 mM and 0.38 μM, respectively. Finally, the immobilized α-glucosidase was used for screening inhibitors from 14 kinds of Traditional Chinese Medicine extracts, and Sanguisorbae Radix showed the strongest inhibitory effect on α-glucosidase.
在本研究中,成功地将α-葡萄糖苷酶固定在纤维素滤纸上,并进一步应用于结合毛细管电泳分析从中药中筛选抑制剂。为了固定α-葡萄糖苷酶,我们使用纤维素滤纸作为载体,通过涂覆壳聚糖接枝氨基,然后使用聚乙二醇二缩水甘油醚作为交联剂通过环氧化开环反应将α-葡萄糖苷酶共价键合在氨基修饰的载体上。优化了影响酶固定化的几个参数,最佳值为酶浓度 4 U/mL、聚乙二醇二缩水甘油醚浓度 1.25%、壳聚糖浓度 7.5 mg/mL、固定化 pH 值 7.0、交联时间 4 h 和固定化时间 2 h。固定化α-葡萄糖苷酶表现出良好的批间重现性(RSD = 2.1%,n = 5)、优异的储存稳定性(在 4°C 下储存 15 天后,其初始活性的 73.5%)和可重复使用性(重复 10 次后,其初始活性的 75%)。固定化α-葡萄糖苷酶的米氏常数和阿卡波糖的半最大抑制浓度分别计算为 1.12 mM 和 0.38 μM。最后,将固定化α-葡萄糖苷酶用于从 14 种中药提取物中筛选抑制剂,发现地榆显示出对α-葡萄糖苷酶最强的抑制作用。