Recently, in-situ polymerization inside living cells has attracted much attention due to the efficient cellular internalization and elevated drug retention. However, the lack of tracking of the in-situ polymerization process and the unclear effects of polymerization on cellular functions restrict its biomedical applications. Herein, we designed a Y-shaped diacetylene-containing lipidated peptide amphiphile (Y-DLPA1) with positive charges, which underwent in-situ polymerization initiated by reactive oxygen species in the intracellular microenvironment. In comparison, zwitterionic Y-DLPA2 and negatively charged Y-DLPA3 were polymerized in aqueous solution, but cannot polymerize in the intracellular microenvironment. The polymerized Y-DLPA1 with red fluorescence provides a platform to label cells for long-term tracking studies. This polymerization reaction induced tumor cell apoptosis, increased cell viscosity and decreased cell motility, which potentially inhibited tumor metastasis and served as a novel antitumor agent. This work provides a novel strategy to track in-situ polymerization process and modulate cell biofunctions.

最近，活细胞内的原位聚合由于有效的细胞内化和提高的药物保留而引起了广泛关注。然而，缺乏对原位聚合过程的跟踪以及聚合对细胞功能的影响不明确限制了其在生物医学上的应用。在此，我们设计了一种带有正电荷的 Y 形含二乙炔的脂化肽两亲物 (Y-DLPA1)，它在原位进行由细胞内微环境中的活性氧引发的聚合。相比之下，两性离子Y-DLPA2和带负电荷的Y-DLPA3在水溶液中聚合，但不能在细胞内微环境中聚合。具有红色荧光的聚合 Y-DLPA1 为标记细胞以进行长期跟踪研究提供了一个平台。这种聚合反应诱导肿瘤细胞凋亡，增加细胞粘度和降低细胞运动性，从而潜在地抑制肿瘤转移并作为一种新型抗肿瘤剂。这项工作提供了一种跟踪原位聚合过程和调节细胞生物功能的新策略。