半乳糖修饰的酞菁锌用于结肠癌光动力治疗。

IF 2.6 3区医学 Q2 ONCOLOGY

Photodiagnosis and Photodynamic Therapy Pub Date : 2025-08-15 DOI:10.1016/j.pdpdt.2025.104765

Weiying Ge , Yuetong Liu , Haiying Ji , Haoyan Chen , Tianjun Liu , Ge Hong , Zhanjuan Zhao

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引用次数: 0

摘要

在先前的研究中，将半乳糖基团引入到酞菁锌（ZnPc）的结构中，以增强其水溶性和肿瘤靶向能力，用于体内荧光成像。半乳糖修饰的ZnPcs （T1-4）作为近红外光学探针在癌症诊断中具有很大的潜力。然而，目前还不确定它们是否也可以作为光动力治疗（PDT）的抗肿瘤候选物。本研究对T1-4体外抗结肠癌的细胞摄取、光动力活性及抗肿瘤机制进行了研究。结果表明，T1-4在结肠癌和成纤维细胞系中的细胞摄取具有浓度依赖性和时间依赖性，其中含1半乳糖组（T1）的ZnPc的细胞摄取效果最佳。在650 nm激光照射20 min （6 J/cm2）下，T1-3（1.25 ~ 40µM）对结肠癌细胞表现出明显的细胞毒性。T1主要定位于CT-26的溶酶体，T1- pdt破坏细胞的膜结构。T1-PDT在CT-26细胞中的抗肿瘤机制主要与诱导自噬有关，并伴随自噬生物标志物beclin-1和LC3-II的上调，同时下调自噬相关蛋白P62。这些发现加强了半乳糖修饰的ZnPcs （T1-4）作为结肠癌PDT光敏药物的潜力，其抗肿瘤机制与结肠癌细胞自噬的激活有关。

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Galactose-modified zinc phthalocyanines for colon cancer photodynamic therapy

In a previous research, galactose groups were introduced into the structure of zinc phthalocyanine (ZnPc) to enhance water solubility and tumor-targeting ability for in vivo fluorescence imaging. Galactose-modified ZnPcs (T1-4) showed great potential as near-infrared optical probes in the diagnose of cancer. However, it had not yet been determined whether they could also serve as antitumor candidates for photodynamic therapy (PDT). In this study, the cellular uptake, photodynamic activity and anti-tumor mechanisms of T1-4 against colon cancer in vitro were investigated. The results showed that the cellular uptake of T1-4 in colon cancer and fibroblast cell lines was both concentration- and time-dependent, and ZnPc with one galactose group (T1) exhibited the optimal cellular uptake. Under 650 nm laser irradiation for 20 min (6 J/cm²), T1-3 (1.25-40 µM) displayed significant cytotoxicity against colon cancer cells. T1 mainly localized in lysosomes of CT-26, and T1-PDT destroyed the membrane structure of cells. The anti-tumor mechanism of T1-PDT in CT-26 cells was mainly related to the induction of autophagy, which was accompanied by upregulation of the autophagy biomarkers beclin-1 and LC3-II, and meanwhile downregulation of the autophagy-related protein P62. These findings reinforced the potential of galactose-modified ZnPcs (T1-4) as photosensitive agents for colon cancer PDT and their anti-tumor mechanism was related to the activation of autophagy in colon cancer cells.

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来源期刊

Photodiagnosis and Photodynamic Therapy ONCOLOGY-

CiteScore

5.80

自引率

24.20%

发文量

509

审稿时长

50 days

期刊介绍： Photodiagnosis and Photodynamic Therapy is an international journal for the dissemination of scientific knowledge and clinical developments of Photodiagnosis and Photodynamic Therapy in all medical specialties. The journal publishes original articles, review articles, case presentations, "how-to-do-it" articles, Letters to the Editor, short communications and relevant images with short descriptions. All submitted material is subject to a strict peer-review process.