光动力疗法 (PDT) 是一种成熟的治疗方式，通常采用单波长照射进行，但对于不同的肿瘤位置和大小来说，这可能并不总是最佳的。为了解决这个问题，正在探索吸收波长范围为 550 至 760 nm 的光敏剂。在此，合成了一系列5,15-二芳基四苯并卟啉（Ar2TBP）。所有化合物在550-700 nm（特别是~668 nm）处均表现出明显的吸收、强烈的荧光、高效的单线态氧产生和良好的光动力抗肿瘤作用。值得注意的是，化合物I3（5,15-双[（4-羧甲氧基）苯基]四苯并卟啉）在红光照射下对Eca-109细胞系表现出优异的细胞毒性，IC50值为0.45 μM，光疗指数为25.8。流式细胞术显示I3可以诱导明显的细胞凋亡。体内研究表明，化合物I3选择性地在肿瘤部位积累，在单次给药和光照射下表现出突出的PDT效果和抗肿瘤活性，并且比临床光敏剂维替泊芬更有效。这些发现强调了 I3 作为一种强大的治疗诊断剂的巨大前景，提供实时荧光成像功能，并作为肿瘤个性化和精确光动力治疗的有效光敏剂。版权所有 © 2024 Elsevier Inc. 保留所有权利。

Photodynamic therapy (PDT) is a well-established treatment modality, typically conducted with single-wavelength irradiation, which may not always be optimal for varying tumor locations and sizes. To address this, photosensitizers with absorption wavelengths ranging from 550 to 760 nm are being explored. Herein, a series of 5,15-diaryltetrabenzoporphyrins (Ar2TBPs) were synthesized. All compounds displayed obvious absorption at 550-700 nm (especially at ∼668 nm), intense fluorescence, efficient generation of singlet oxygen and good photodynamic antitumor effects. Notably, compound I3 (5,15-bis[(4-carboxymethoxy)phenyl]tetrabenzoporphyrin) showed excellent cytotoxicity against Eca-109 cell line upon red light irradiation, with an IC50 value of 0.45 μM, and phototherapeutic index of 25.8. Flow cytometry revealed that I3 could induce distinct cell apoptosis. In vivo studies revealed that compound I3 selectively accumulated at tumor site and exhibited outstanding PDT effect with antitumor activity under single-time administration and light irradiation, and revealed more efficiency than the clinical photosensitizer Verteporfin. These findings underscore the considerable promise of I3 as a robust theranostic agent, offering capabilities in real-time fluorescence imaging and serving as a potent photosensitizer for personalized and precise photodynamic therapy of tumors.Copyright © 2024 Elsevier Inc. All rights reserved.