Center for Design and Applications of Molecular Catalysts, Department of Chemistry and Chemical Engineering, Inha University , Incheon 402-751, South Korea.
ACS Appl Mater Interfaces. 2018 Jan 24;10(3):2282-2290. doi: 10.1021/acsami.7b15411. Epub 2018 Jan 9.
The detection of fluorescent probes for biomolecules and control of the function of a complex through a recognition process have not been investigated intensively. A fluorescent peptidyl probe (1) based on the self-assembly stimulated by heparin was synthesized. The fluorescent probe with an aggregation-induced emission fluorophore formed a self-assembling complex with heparin, resulting in a sensitive and selective turn-on response to heparin compared to its biological competitors. The detection limits for heparin were measured to be 138.0 pM (R = 0.976) in aqueous solution and 2.6 nM (R = 0.996) in aqueous solution containing human serum. Nanosized aggregates formed through the self-assembly of the complex showed potent resistance against the heparin-digestive enzyme. The dual role of the probe for the detection of heparin and the inhibition of heparinase-mediated digestion through the recognition process was used for the real-time monitoring of the enzyme activity of heparinase for the digestion of heparin. Furthermore, the dual role of the probe was applied for the detection of the oversulfated chondroitin sulfate contaminant in heparin.
基于肝素诱导的自组装，我们合成了一种荧光肽探针（1）。该荧光探针带有聚集诱导发射荧光团，可与肝素形成自组装复合物，与肝素的生物竞争物相比，对肝素表现出灵敏且选择性的开启响应。在水溶液中，肝素的检测限低至 138.0 pM（R = 0.976），在含有人血清的水溶液中，检测限低至 2.6 nM（R = 0.996）。通过该复合物的自组装形成的纳米级聚集体对肝素消化酶具有很强的抵抗力。探针通过识别过程检测肝素和抑制肝素酶介导的消化的双重作用，可用于实时监测肝素酶对肝素的酶解活性。此外，该探针的双重作用还可用于检测肝素中的过度硫酸化硫酸软骨素污染物。
