<br>光敏剂协同效应：具有增强荧光和单线态氧量子产率的 D–A–D 结构有机分子，用于光动力治疗†,Chemical Science

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光敏剂协同效应：具有增强荧光和单线态氧量子产率的 D–A–D 结构有机分子，用于光动力治疗†
Chemical Science ( IF 7.6 ) Pub Date : 2018-01-18 00:00:00 , DOI: 10.1039/c7sc04694d
Jianhua Zou ₁ , Zhihui Yin ₁ , Peng Wang ₁ , Dapeng Chen ₁ , Jinjun Shao ₁ , Qi Zhang ₂ , Liguo Sun ₃ , Wei Huang ₄ , Xiaochen Dong ₁

Affiliation

开发具有高荧光强度和单线态氧（ ¹ O ₂ ）量子产率（QY）的光敏剂对于癌症诊断和光动力治疗（PDT）具有重要意义。二酮吡咯并吡咯（DPP）和二吡咯亚甲基硼（BODIPY）是两种具有巨大PDT潜力的结构单元。在此，设计并合成了一种新型供体-受体-供体（D-A-D）结构的有机光敏剂DPPBDPI，其以苯环作为π桥连接DPP和BODIPY。结果表明，DPP与BODIPY联合使用，通过两种光敏剂的协同作用，可以同时显着提高荧光QY（5.0%）和¹ O ₂ QY（高达80%）。通过纳米沉淀，DPPBDPI 可以形成直径小于 100 nm 的均匀纳米颗粒 (NP)。所获得的纳米粒子不仅表现出高光毒性，而且对 HeLa 细胞的暗毒性可以忽略不计，证明了其优异的光动力治疗功效。体内荧光成像显示，DPPBDPI NPs可以通过增强的渗透性和保留（EPR）效应快速靶向肿瘤部位，并且即使在低剂量（0.5 mg kg ^-1 ）下也可以使用光动力疗法有效抑制肿瘤生长。 DPPBDPI增强的成像和光动力性能表明DPP和BODIPY的协同作用为癌症诊断和光动力治疗提供了一个新的治疗诊断平台。

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Photosensitizer synergistic effects: D–A–D structured organic molecule with enhanced fluorescence and singlet oxygen quantum yield for photodynamic therapy†

The development of photosensitizers with high fluorescence intensity and singlet oxygen (¹O₂) quantum yields (QYs) is of great importance for cancer diagnosis and photodynamic therapy (PDT). Diketopyrrolopyrrole (DPP) and boron dipyrromethene (BODIPY) are two kinds of building block with great potential for PDT. Herein, a novel donor–acceptor–donor (D–A–D) structured organic photosensitizer DPPBDPI with a benzene ring as a π bridge linking DPP and BODIPY has been designed and synthesized. The results indicate that the combination of DPP with BODIPY can simultaneously increase the fluorescence QY (5.0%) and the ¹O₂ QY (up to 80%) significantly by the synergistic effect of the two photosensitizers. By nanoprecipitation, DPPBDPI can form uniform nanoparticles (NPs) with a diameter of less than 100 nm. The obtained NPs not only exhibit high photo-toxicity, but also present negligible dark toxicity towards HeLa cells, demonstrating their excellent photodynamic therapeutic efficacy. In vivo fluorescence imaging shows that DPPBDPI NPs can target the tumor site quickly with the enhanced permeability and retention (EPR) effect and can effectively inhibit tumor growth using photodynamic therapy even with low doses (0.5 mg kg⁻¹). The enhanced imaging and photodynamic performance of DPPBDPI suggest that the synergistic effect of DPP and BODIPY provides a novel theranostic platform for cancer diagnosis and photodynamic therapy.

更新日期：2018-01-18

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