Luo Dong, Zhang Xin, Li Xiaoying, Zhen Yi-Yu, Zeng Xingyi, Xiong Zhuang, Zhang Yinghui, Li Hongguang
School of Biotechnology and Health Science, Wuyi University, Jiangmen, China.
Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine, South China Institute of Large Animal Models for Biomedicine, Wuyi University, Jiangmen, China.
Front Chem. 2022 Jun 28;10:927624. doi: 10.3389/fchem.2022.927624. eCollection 2022.
α-Glucosidase is a potent drug target for treating type II diabetes mellitus. A great number of α-glucosidase inhibitors have been developed based on the molecular skeletons of bioactive natural products. However, efficient fluorescent probes for α-glucosidase detection are still limited, not to mention the probes with additional inhibitory functions. In this work, aiming for the enzyme's highly specific detection, we designed and synthesized two environmentally sensitive fluorescent probes, namely, LD01 and LD02, respectively, based on conjugates of coumarin and cinnamic acid derivatives. We found a significant responsive emission enhancement upon LD02's binding to α-glucosidase. These newly designed probes can act as a simple but efficient tool to evaluate the binding affinity of α-glucosidase to their inhibitors.
α-葡萄糖苷酶是治疗II型糖尿病的有效药物靶点。基于生物活性天然产物的分子骨架，已经开发出了大量的α-葡萄糖苷酶抑制剂。然而，用于检测α-葡萄糖苷酶的高效荧光探针仍然有限，更不用说具有额外抑制功能的探针了。在这项工作中，为了实现对该酶的高特异性检测，我们分别基于香豆素和肉桂酸衍生物的共轭物设计并合成了两种对环境敏感的荧光探针，即LD01和LD02。我们发现，LD02与α-葡萄糖苷酶结合后，发射响应显著增强。这些新设计的探针可以作为一种简单而有效的工具，用于评估α-葡萄糖苷酶与其抑制剂的结合亲和力。
