Photoactive agents based on natural products have attracted substantial attention in clinical applications because of their distinct biological activity, molecular structure multiformity, and low biotoxicity. Herein, we initially modify hypocrellin B (HB) with 1,2-diamino-2-methyl propane to form near-infrared (NIR) light (>700 nm)-responsive amino-substituted HB derivative (DPAHB). The DPAHB exhibit broad absorption (400–800 nm), NIR emission (maximum emission peak at 710 nm), and high singlet oxygen (¹O₂) quantum yield (∼0.33) under NIR light (721 nm) irradiation. After self-assembly by using DPAHB with PEG-PLGA, the as-prepared nanovesicles (DPAHB NVs) retain efficient ¹O₂ generation, more interestingly, show high photothermal conversion efficiency (∼0.24) under NIR light (721 nm) irradiation for synergistic photodynamic therapy (PDT) and photothermal therapy toward hypoxic tumor. The DPAHB NVs can not only be as a fluorescence/photoacoustic imaging agent but also exhibit an even stronger PDT efficiency than that of chlorin e6 (a widely used classic photosensitizer). In vitro and in vivo studies demonstrate that DPAHB NVs possess high photothermal stability, enhanced tumor accumulation, and suitable biodegradation rate, thus, show a highly promising clinical potential as a new photoactive agent for cancer therapy.

基于天然产物的光敏剂由于其独特的生物活性，分子结构的多态性和低的生物毒性而在临床应用中引起了广泛的关注。在本文中，我们最初用1,2-二氨基-2-甲基丙烷修饰hypercrelinin B（HB），以形成近红外（NIR）光（> 700 nm）响应的氨基取代HB衍生物（DPAHB）。DPAHB在NIR光（721 nm）照射下表现出宽吸收（400–800 nm），NIR发射（最大发射峰在710 nm）和高单线态氧（¹ O ₂）量子产率（〜0.33）。通过使用DPAHB和PEG-PLGA自组装后，制备的纳米囊泡（DPAHB NVs）保留了有效的¹ O ₂更有趣的是，在近红外光（721 nm）照射下，用于产生协同光动力疗法（PDT）和对缺氧肿瘤的光疗的高热转换效率（〜0.24）。DPAHB NVs不仅可以用作荧光/光声成像剂，而且比二氢卟酚e6（一种广泛使用的经典光敏剂）具有更高的PDT效率。体外和体内研究表明，DPAHB NVs具有高的光热稳定性，增强的肿瘤蓄积性和合适的生物降解速率，因此，作为一种新型的用于癌症治疗的光敏剂，具有很高的临床潜力。