锌（II）金属卟啉作为光热致光敏剂，用于癌症光动力/光热协同治疗,ACS Applied Materials & Interfaces

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锌（II）金属卟啉作为光热致光敏剂，用于癌症光动力/光热协同治疗
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2017-12-26 00:00:00 , DOI: 10.1021/acsami.7b15583
Kaikai Ding ₁ , Yewei Zhang ₂ , Weili Si ₁ , Xiangmin Zhong ₃ , Yu Cai ₁ , Jianhua Zou ₁ , Jinjun Shao ₁ , Zhou Yang ₃ , Xiaochen Dong ₁

Affiliation

卟啉衍生物是第一代光敏剂，因此迫切需要设计一种具有良好水溶性的强吸收性近红外（NIR）吸收性卟啉，以更好地治疗肿瘤。在此，三种新的卟啉衍生物：5,10,15,20-四（3,4-二甲氧基苯基）卟啉（P1），5,10,15,20-四（3,4-二甲氧基苯基）卟啉锌（ZnP1），合成了5,15-双（3,4-二甲氧基苯基）-10,20-双（（4-甲氧基苯基）乙炔基）锌卟啉（ZnP2）。其中，ZnP2由于具有最强的光采集能力和最深的肿瘤组织穿透力，它在近红外（NIR）区域中显示出最长和最密集的Q波段。通过纳米沉淀法将这三种卟啉衍生物制备成纳米颗粒（NPs），并通过增强的通透性和保留效果，表现出良好的水分散性和被动的靶向肿瘤特性。此外，这些纳米粒子展示了光动力和光热效应。通过对Hela细胞上P1，ZnP1和ZnP2 NPs的单线态氧量子产率和细胞毒性的系统研究，发现ZnP2显示出最高的单线态氧量子产率（79％），其NP在体外显示出最佳的治疗功效。体内实验表明，ZnP2 NPs具有高的光毒性，低的暗毒性和优异的生物相容性，可作为有前景的光致热光敏剂用于癌症治疗。

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Zinc(II) Metalated Porphyrins as Photothermogenic Photosensitizers for Cancer Photodynamic/Photothermal Synergistic Therapy

Porphyrin derivatives are the first-generation photosensitizers, and to design a strong near-infrared (NIR)-absorbing porphyrin with good water solubility is highly desired for better therapeutic effect to treat tumors. Herein, three new porphyrin derivatives, 5,10,15,20-tetrakis(3,4-dimethoxyphenyl) porphyrin (P1), 5,10,15,20-tetrakis(3,4-dimethoxyphenyl) zinc porphyrin (ZnP1), and 5,15-bis(3,4-dimethoxyphenyl)-10,20-bis((4-methoxyphenyl)ethynyl) zinc porphyrin (ZnP2) have been synthesized. Among them, ZnP2 shows the longest and most intensive Q-bands in the near-infrared (NIR) region, as it endows the strongest light-harvesting capability and deepest tumor tissue penetration. The three porphyrin derivatives were prepared into nanoparticles (NPs) via nanoprecipitation method, and the NPs exhibit good water dispersibility and passive tumor-targeting property through enhanced permeability and retention effect. Furthermore, these NPs demonstrate both photodynamic and photothermal effects. Through a systematic study of the singlet oxygen quantum yield and cytotoxicity of P1, ZnP1, and ZnP2 NPs in vitro on Hela cells, it is found that ZnP2 shows the highest singlet oxygen quantum yield (79%), and its NPs show the best therapeutic efficacy in vitro. In vivo experiments disclosed that ZnP2 NPs present high phototoxicity, low dark toxicity, and excellent biocompatibility, and could be used as promising photothermogenic photosensitizer for cancer treatment.

更新日期：2017-12-26

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