Dong Chunmin, Wang Yue
Traditional Chinese Medicine Department, Daqing Oilfield General Hospital, Daqing, Heilongjiang, China.
Department of Pharmacology and Toxicology, Wright State University, Fairborn, OH, 45435, USA.
J Fluoresc. 2025 Sep 3. doi: 10.1007/s10895-025-04548-9.
Non-small cell lung cancer (NSCLC) remains one of the most lethal malignancies worldwide, highlighting the urgent need for the development of novel multifunctional therapeutic strategies. In this study, a bioinspired nanocomposite drug delivery system was designed and constructed by covalently modifying propylene glycol alginate (PGA) with a microbial-derived coumarin compound (Compound 1) and a fluorinated small molecule (Compound 2), followed by assembly with the silane-based crosslinker ATPMS. The system was subsequently loaded with Dendrobium extract to produce the final nanocomposite material, 2-PGA-1-ATPMS@Dendrobium. This platform exhibited excellent biocompatibility, enhanced cellular uptake, and significant anti-proliferative effects against NSCLC cells. Mechanistic investigations revealed that the nanomaterial induced tumor cell pyroptosis by upregulating the expression of Caspase-1 and GSDMD and promoting the transcription of pro-inflammatory cytokines. Moreover, the nanocomposite demonstrated ultra-sensitive ratiometric fluorescence detection of Cu²⁺ ions, with a detection limit as low as 0.068 nM. Given the critical role of copper ions in inducing cuproptosis and their involvement in tumor progression, this dual-functional nanoplatform presents promising potential for both early diagnosis and targeted treatment of NSCLC.
非小细胞肺癌(NSCLC)仍然是全球最致命的恶性肿瘤之一,这凸显了开发新型多功能治疗策略的迫切需求。在本研究中,通过将微生物来源的香豆素化合物(化合物1)和氟化小分子(化合物2)共价修饰丙二醇藻酸盐(PGA),随后与硅烷基交联剂ATPMS组装,设计并构建了一种仿生纳米复合药物递送系统。该系统随后负载石斛提取物以制备最终的纳米复合材料2-PGA-1-ATPMS@石斛。该平台表现出优异的生物相容性、增强的细胞摄取以及对NSCLC细胞显著的抗增殖作用。机制研究表明,该纳米材料通过上调Caspase-1和GSDMD的表达并促进促炎细胞因子的转录来诱导肿瘤细胞焦亡。此外,该纳米复合材料对Cu²⁺离子表现出超灵敏的比率荧光检测,检测限低至0.068 nM。鉴于铜离子在诱导铜死亡中的关键作用及其参与肿瘤进展,这种双功能纳米平台在NSCLC的早期诊断和靶向治疗方面具有广阔的前景。