Photodynamic therapy (PDT) has been demonstrated to be effective for cancer treatment. Design of photosensitizers (PS) featuring tumor targeting, long excitation wavelengths, and high singlet oxygen quantum yields (Φ(¹O₂)) is the crucial point of highly efficient PDT. However, it is especially difficult to integrate above features into one photosensitizer. Herein, we put forwards a PS J-aggregation method, simultaneously endowing PS with the ability of tumor targeting, the red-shift of spectra, and the increase of Φ(¹O₂). Cyanine PS 4-((E)-3-((E)-5-iodo-1,3,3-trimethylindolin -2-ylidene)prop-1-en-1-yl)-1-methylquinolin-1-ium iodide (IDMQ) is firstly designed and synthesized by us. IDMQ can form smart response-type J-aggregates under the control of negatively charge in microenvironments. In blood, IDMQ J-aggregates target tumor via “enhanced permeability and retention (EPR)” effect. Then the intracellular IDMQ J-aggregates assembled by RNA facilitate the red shift of absorption peak with deeper penetration, and compared to free state IDMQ, improve the Φ(¹O₂), resulting in the bathochromic shift of optimal PDT wavelength from 630 (free state IDMQ) to 700 nm (IDMQ J-aggregates). This intelligent J-aggregation method establishes a promising way for endowing photosensitizer with the ability of tumor-targeting and the synchronous improvement of PDT efficacy and further boosts the development of PDT.

光动力疗法（PDT）已被证明对癌症治疗有效。具有肿瘤靶向，长激发波长和高单线态氧量子产率（Φ（¹ O ₂））的光敏剂（PS）的设计是高效PDT的关键点。但是，将上述特征整合到一种光敏剂中特别困难。在这里，我们提出了一种PS J聚集方法，同时赋予PS具有靶向肿瘤的能力，光谱的红移和Φ（¹ O ₂）的增加。花青PS 4-（（E）-3-（（E）-5-iodo-1,3,3-trimethylindolin-2-yylne）prop-1-en-1-yl）-1-methylquinolin-1-ium碘化物（IDMQ）由我们首先设计和合成。IDMQ可以在微环境中带负电荷的控制下形成智能响应型J聚集体。在血液中，IDMQ J通过“增强的渗透性和保留（EPR）”效应聚集靶肿瘤。然后由RNA组装的细胞内IDMQ J聚集体促进了吸收峰的红移和更深的渗透，并且与自由状态IDMQ相比，改善了Φ（¹ O ₂），导致最佳PDT波长从630的红移。状态IDMQ）至700 nm（IDMQJ集合）。这种智能的J聚集方法为赋予光敏剂以肿瘤靶向的能力和PDT功效的同步提高建立了一种有前途的方法，并进一步促进了PDT的发展。