Self-Assembly versus Coassembly: An Amphiphilic NIR-II Aggregation-Induced Emission Luminogen for Phototheranostics of Orthotopic Glioblastoma

IF 6.8 1区医学 Q1 CHEMISTRY, MEDICINAL

Journal of Medicinal Chemistry Pub Date : 2025-05-13 DOI:10.1021/acs.jmedchem.5c0059010.1021/acs.jmedchem.5c00590

Yan Sun, Xueke Yan, Dong Wang, Jun Zhu, Huifang Su*, Dongxia Zhu*, Dingyuan Yan* and Ben Zhong Tang*,

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Abstract

Glioblastoma (GBM) is the most lethal form of malignant brain tumor, known for its high infiltration, aggressiveness, and poor prognosis. Second near-infrared (NIR-II, 1000–1700 nm) phototheranostic agents bring intriguing opportunities for GBM management owing to their noninvasive nature, controllability, and deeper tissue penetration. Herein, an amphiphilic NIR-II luminogen (PEG-TD) with aggregation-induced emission (AIE) characteristics, along with its hydrophobic counterpart (C6-TD), was meticulously synthesized. Specifically, PEG-TD nanoparticles (NPs), formed through straightforward self-assembly, exhibited superior stability, simplicity, robust reactive oxygen species production efficiency, and excellent photothermal conversion compared to C6-TD NPs, which were fabricated via coassembly with DSPE-mPEG, primarily attributed to the distinct molecular arrangements within the forming aggregates. The inherent advantages of PEG-TD NPs led to significant therapeutic efficacy against GL261 cells under 808 nm laser irradiation. Eventually, NIR-II fluorescence/photothermal duplex imaging-guided combined photodynamic/photothermal therapy was successfully performed in an orthotopic glioblastoma mouse model with minimal adverse effects.

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自组装与共组装：用于原位胶质母细胞瘤光疗的两亲性NIR-II聚集诱导发射发光剂

胶质母细胞瘤（GBM）是恶性脑肿瘤中最致命的一种，以其高浸润性、侵袭性和预后差而闻名。第二种近红外（NIR-II, 1000-1700 nm）光治疗药物由于其非侵入性、可控性和更深的组织穿透性，为GBM的治疗带来了有趣的机会。本文精心合成了具有聚集诱导发射（AIE）特性的两亲性NIR-II发光材料（PEG-TD）及其疏水性对应物（C6-TD）。具体来说，通过直接自组装形成的PEG-TD纳米颗粒（NPs），与通过与DSPE-mPEG共组装制备的C6-TD纳米颗粒相比，表现出优越的稳定性、简单性、强大的活性氧生产效率和出色的光热转化，这主要归功于形成聚集体内独特的分子排列。PEG-TD NPs的固有优势导致其在808 nm激光照射下对GL261细胞有显著的治疗效果。最终，NIR-II荧光/光热双成像引导下的光动力/光热联合治疗成功地在原位胶质母细胞瘤小鼠模型中进行，副作用最小。

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来源期刊

Journal of Medicinal Chemistry 医学-医药化学

CiteScore

4.00

自引率

11.00%

发文量

804

审稿时长

1.9 months

期刊介绍： The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents. The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.