Abstract

Artesunate (AS), as an effective new tumour treatment drug, induces cancer cell death based on high intracellular reactive oxygen species (ROS) produced by interacting with ferrous ions. However, the relatively low intracellular ferrous iron ion concentrations and the low efficiency of ROS generation limit its clinical application. Herein, we developed a metal-organic framework-Fe²⁺ (MOF), and AS was loaded in the MOF and then coated with hyaluronic acid (HA) on the surface of the MOF (HA@MOF-AS) for targeted and enhanced cancer treatment. HA@MOF-AS has high loading efficiency, good monodispersity, biocompatibility, strong cell uptake capacity and high intracellular ROS production, and it can target tumour tissues. In addition, in vivo anticancer studies have shown that HA@MOF-AS not only has high accumulation in tumours but also significantly inhibits tumour growth without significant damage to major organs. Therefore, HA@MOF-AS has excellent potential and may open a new approach for targeted cancer treatment.

摘要

青蒿琥酯 (AS) 作为一种有效的新型肿瘤治疗药物，基于与亚铁离子相互作用产生的高细胞内活性氧 (ROS) 诱导癌细胞死亡。然而，细胞内亚铁离子浓度相对较低和活性氧生成效率低限制了其临床应用。在此，我们开发了一种金属有机骨架-Fe ²⁺ (MOF)，将 AS 负载在 MOF 中，然后在 MOF (HA@MOF-AS) 表面涂覆透明质酸 (HA) 以进行靶向和增强癌症治疗。HA@MOF-AS负载效率高、单分散性好、生物相容性好、细胞摄取能力强、细胞内ROS产生量高，可靶向肿瘤组织。此外，体内抗癌研究表明，HA@MOF-AS不仅在肿瘤中具有高蓄积性，而且在不显着损伤主要器官的情况下显着抑制肿瘤生长。因此，HA@MOF-AS 具有极好的潜力，可能为靶向癌症治疗开辟一条新途径。