高效 PBS/聚山梨醇酯可溶性顺铂衍生的基于卟啉的光动力治疗光敏剂。
Potent PBS/Polysorbate-Soluble Transplatin-Derived Porphyrin-Based Photosensitizers for Photodynamic Therapy.
机构信息
Department of Chemistry, University of Zurich, CH-8057 Zurich, Switzerland.
出版信息
Inorg Chem. 2021 Jul 5;60(13):9416-9426. doi: 10.1021/acs.inorgchem.1c00415. Epub 2021 Jun 11.
In this study, we addressed an important drawback of our previously reported tetraplatinated (metallo)porphyrin-based photosensitizers (PSs) for photodynamic therapy (PDT), namely, the poor solubility in aqueous media. We aimed to create tetraplatinated porphyrin-based PSs that are soluble in aqueous media modified with polysorbate (Tween) and do not need to be pre-dissolved in organic solvents. A structural optimization of the previously reported PSs resulted in the synthesis of an extremely potent novel porphyrin-based PS. The novel PS displays effective phototoxicity upon light irradiation against multicellular tumor spheroids and has a phototoxic index (PI) of 6030 in HeLa cells. This PI value is, to the best of our knowledge, the highest value reported for any porphyrin so far.
在这项研究中，我们解决了我们之前报道的基于四铂（金属）卟啉的光动力治疗（PDT）光敏剂（PS）的一个重要缺点，即其在水介质中的溶解度差。我们的目标是创建基于四铂卟啉的 PS，其在经过聚山梨酯（吐温）修饰的水介质中具有良好的溶解性，并且不需要预先溶解在有机溶剂中。对之前报道的 PS 进行结构优化，合成了一种非常有效的新型基于卟啉的 PS。新型 PS 在光照下对多细胞肿瘤球体表现出有效的光毒性，在 HeLa 细胞中的光毒性指数（PI）为 6030。就我们所知，这个 PI 值是迄今为止报道的任何卟啉中最高的值。
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