Analytical and Bioanalytical Chemistry ( IF 3.8 ) Pub Date : 2021-02-11 , DOI: 10.1007/s00216-021-03214-w Cong Li 1, 2 , Yuqiu Zi 1, 2 , Dawei Xu 1, 2 , Dafeng Jiang 3 , Fei Qu 1, 2 , Xian-En Zhao 1, 2
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Herein, the self-assembly of 1-dodecanethiol-capped Cu nanoclusters (DT-Cu NCs) is obtained by annealing of dibenzyl ether solution of nanoclusters. These aggregates are composed of small clusters and emit a high level of aggregation-induced emission (AIE) in water. Based on the quenching effect of 4-nitrophenol (4-NP) on DT-Cu NCs, a fluorescence strategy is developed to monitor α-glucosidase (α-Glu) activity and screen its inhibitors from Chinese herbal medicines. 4-Nitrophenyl-α-D-glucopyranoside (NGP) is selected as the substrate, which is further hydrolyzed to yield 4-NP through the catalysis of α-Glu. The quenching efficiency is positively correlated to the concentration of α-Glu. Furthermore, the inhibitory effects of the extracts from four Chinese herbal medicines (i.e., the rind of Punica granatum L., Momordica grosvenorii Swingle., Crataegus pinnatifida Bge., and Lycium barbarum L.) on the α-Glu activity have been studied. The IC50 values of extracts from the rind of Punica granatum L. and Momordica grosvenorii Swingle are 0.23 and 0.37 g/L, respectively, so they show obvious inhibitory effects on α-Glu. The extracts of Crataegus pinnatifida Bge. and Lycium barbarum L. exhibit relatively weak inhibitory effects. Hence, the proposed strategy can be applicable for screening α-Glu inhibitors from Chinese herbal medicines. Last but not the least, by immobilizing DT-Cu NCs into agarose hydrogels in polyethylene tubes, a visual device is fabricated to screen α-Glu inhibitors with high throughput and sensitivity.
Graphical abstract
中文翻译：
基于聚集诱导发射的Cu纳米簇的荧光策略监测α-葡萄糖苷酶活性并从中药中筛选其抑制剂
在此，通过将纳米簇的二苄基醚溶液退火而获得1-十二烷硫醇封端的Cu纳米簇（DT-Cu NCs）的自组装。这些聚集体由小簇组成，并在水中释放出高水平的聚集诱导排放物（AIE）。基于4-硝基苯酚（4-NP）对DT-Cu NCs的猝灭作用，开发了一种荧光策略来监测α-葡萄糖苷酶（α-Glu）活性并从中草药中筛选其抑制剂。选择4-硝基苯基-α-D-吡喃葡萄糖苷（NGP）作为底物，通过α-Glu的催化进一步水解生成4-NP。淬灭效率与α-Glu的浓度呈正相关。此外，四种中草药提取物（即石榴的外皮）的抑制作用研究了L.，grosvenorii Swingle。，Cretaegus pinnatifida Bge。和Lycium barbarum L.）对α-Glu活性的影响。石榴皮和罗汉果果皮提取物的IC 50值分别为0.23和0.37 g / L，因此它们对α-Glu具有明显的抑制作用。Crataegus pinnatifida Bge的提取物。和枸杞L.表现出相对较弱的抑制作用。因此，所提出的策略可适用于从中草药中筛选α-Glu抑制剂。最后但并非最不重要的一点是，通过将DT-Cu NCs固定在聚乙烯管中的琼脂糖水凝胶中，制造了一种可视设备，可高通量和高灵敏度地筛选α-Glu抑制剂。
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