Chen Dan, Chen Yifan, Liu Jianwen, Liu Xinyue, Liu Peiwen, Zhan Jiabing, Chen Zhiting, Gan Yong, Huang Mingdong, Chen Zhaoyang
Department of Cardiology, Heart Center of Fujian Province, Fujian Medical University Union Hospital, Fuzhou, Fujian 350001, China.
Department of Cardiology, Xiamen Cardiovascular Hospital, Xiamen University, Xiamen, Fujian 361004, China.
Sci Adv. 2025 May 2;11(18):eadu6676. doi: 10.1126/sciadv.adu6676.
Arterial thrombosis is commonly accompanied by poor recanalization and high recurrence, typically caused by a fibrinolysis-resistant microenvironment. We identify elevated levels of plasminogen activator inhibitor-1 (PAI-1) and, notably, its strong correlation with inflammation in arterial thrombosis. To address this, small molecular inhibitors of PAI-1 and inflammation are used as bioregulators to restore vascular homeostasis. We design a carrier-free supramolecular system based on the bioregulators-tuned self-assembly of a near-infrared thrombus probe, which preferentially forms protein corona in situ to enhance plasma stability. Under acidic conditions and increased shear stress, the supramolecular assemblies disintegrate, enabling site-specific cargo release. In vivo, the probe accumulates 22.8-fold more in the thrombotic than contralateral artery. Functionally, this nanomedicine improves outcomes in mice with carotid artery thrombosis and chronic cerebral ischemia. Mechanistically, it down-regulates NF-κB signaling, inhibits NETosis and glycolysis, and up-regulates cGMP-mediated signaling, thereby alleviating inflammation and promoting fibrinolysis. This study offers an innovative codelivery strategy using supramolecular assemblies to advance therapies for arterial thrombosis.
动脉血栓形成通常伴随着再通不良和高复发率,这通常是由抗纤维蛋白溶解的微环境引起的。我们发现纤溶酶原激活物抑制剂-1(PAI-1)水平升高,并且值得注意的是,它与动脉血栓形成中的炎症密切相关。为了解决这个问题,PAI-1和炎症的小分子抑制剂被用作生物调节剂来恢复血管稳态。我们基于生物调节剂调节的近红外血栓探针自组装设计了一种无载体超分子系统,该系统优先在原位形成蛋白冠以增强血浆稳定性。在酸性条件和增加的剪切应力下,超分子组装体解体,实现位点特异性货物释放。在体内,该探针在血栓形成的动脉中积累的量比在对侧动脉中多22.8倍。在功能上,这种纳米药物改善了患有颈动脉血栓形成和慢性脑缺血的小鼠的预后。从机制上讲,它下调NF-κB信号传导,抑制中性粒细胞胞外陷阱形成和糖酵解,并上调cGMP介导的信号传导,从而减轻炎症并促进纤维蛋白溶解。这项研究提供了一种创新的共递送策略,使用超分子组装体来推进动脉血栓形成的治疗。