School of Chemistry and Chemical Engineering, Nanchang University, Nanchang, China.
School of Chemical Engineering and Advanced Materials, The University of Adelaide, Adelaide, South Australia, Australia.
Luminescence. 2024 Jan;39(1):e4668. doi: 10.1002/bio.4668.
Curcumin (Cur) is an acidic polyphenol with some effects on α-glucosidase (α-Glu), but Cur has disadvantages such as being a weak target, lacking passing the blood-brain barrier and having low bioavailability. To enhance the curative effect of Cur, the hybrid composed of ZnO nanoparticles decorated on rGO was used to load Cur (ZnO@rGO-Cur). The use of the multispectral method and enzyme inhibition kinetics analysis certify the inhibitory effect and interaction mechanism of ZnO@rGO-Cur with α-Glu. The static quenching of α-Glu with both Cur and ZnO@rGO-Cur is primarily driven by hydrogen bond and van der Waals interactions. The conformation-changing ability by binding to the neighbouring phenolic hydroxyl group of Cur increased their ability to alter the secondary structure of α-Glu, resulting in the inhibition of enzyme activity. The inhibition constant (K > K ) showed that the inhibition effect of ZnO@rGO-Cur on α-Glu was larger than that of Cur. The CCK-8 experiments proved that ZnO@rGO nanocomposites have good biocompatibility. These results suggest that the therapeutic potential of ZnO@rGO-Cur composite is an emerging nanocarrier platform for drug delivery systems for the potential treatment of diabetes mellitus.
姜黄素（Cur）是一种酸性多酚，对α-葡萄糖苷酶（α-Glu）有一定的作用，但 Cur 存在作用靶点弱、缺乏血脑屏障穿透能力和生物利用度低等缺点。为了增强 Cur 的疗效，使用负载 Cur 的 ZnO 纳米粒子修饰的 rGO 复合材料（ZnO@rGO-Cur）。多谱法和酶抑制动力学分析证明了 ZnO@rGO-Cur 对 α-Glu 的抑制作用和相互作用机制。α-Glu 与 Cur 和 ZnO@rGO-Cur 的静态猝灭主要是由氢键和范德华相互作用驱动的。通过与 Cur 的邻位酚羟基结合改变构象的能力增强了它们改变α-Glu 二级结构的能力，从而抑制了酶活性。抑制常数（K > K ）表明，ZnO@rGO-Cur 对 α-Glu 的抑制作用大于 Cur。CCK-8 实验证明 ZnO@rGO 纳米复合材料具有良好的生物相容性。这些结果表明，ZnO@rGO-Cur 复合材料具有治疗潜力，是用于治疗糖尿病的药物输送系统的新兴纳米载体平台。
