Abstract

The efficacy and safety of photodynamic therapy (PDT) have drawn much attention from clinicians and researchers in the field of anticancer treatments since the last century. Despite the numerous positive outcomes, the works on PDT have brought to light over the last decades, much room remains for improvements in PDT tools, mainly on the photosensitizer molecules. This work reports the first experiments evidencing the photosensitizing activity of DHX-1, a xanthene derivative-based near-infrared probe recently described in the literature, both as a free molecule and associated to a nanostructured lipid carrier. The results show that the DHX-1 presents a broad band of light absorption within the optical window of biological tissues (600–800 nm), generates reactive oxygen species when photoactivated, and is phototoxic against murine breast adenocarcinoma 4T1 cells and murine fibroblast NIH-3T3 in vitro. Moreover, the association of DHX-1 to a nanostructured lipid carrier strongly reduced its phototoxicity against the normal cell line.

摘要

自上个世纪以来，光动力疗法（PDT）的有效性和安全性引起了抗癌治疗领域临床医生和研究人员的广泛关注。尽管取得了许多积极成果，但在过去的几十年中，PDT 的工作已经显露出来，但 PDT 工具仍有很大的改进空间，主要是在光敏剂分子上。这项工作报告了第一个证明 DHX-1 光敏活性的实验，DHX-1 是一种最近在文献中描述的基于呫吨衍生物的近红外探针，既作为游离分子又与纳米结构的脂质载体相关联。结果表明，DHX-1在生物组织的光学窗口（600-800 nm）内呈现出较宽的光吸收带，在光活化时产生活性氧，体外。此外，DHX-1 与纳米结构脂质载体的结合大大降低了其对正常细胞系的光毒性。