高等学校化学学报

高等学校化学学报

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乏氧激活化疗药物AQ4N与碳点自组装用于化疗联合声动力治疗肿瘤

庞娥1,唐垣钰1,赵少静1,程强1,王晨1,陈健敏2,蓝敏焕1   

  1. 1. 中南大学
    2. 莆田学院
  • 收稿日期:2024-10-31 修回日期:2024-12-05 出版日期:2024-12-09 发布日期:2024-12-09
  • 通讯作者: 蓝敏焕 E-mail:minhuanlan@csu.edu.cn
  • 基金资助:
    国家重点研发计划(批准号：2022YFA1207600)、国家自然科学基金(批准号：62375289，62175262)、湖南省重点研发计划(批准号：2022SK2101，2023NK2029)和福建省高校药物分析与检验医学重点实验室(莆田学院)开放课题(批准号：PALM 202201)的资助

Hypoxia activated chemotherapy drug AQ4N and carbon dots self-assembly for chemotherapy combined with sonodynamic therapy of tumors

PANG E1, TANG Yuanyu1, ZHAO Shaojing1, CHENG Qiang1, WANG Chen1, CHEN Jianmin2, LAN Minhuan1   

  1. 1. Central South University
    2. Putian University
  • Received:2024-10-31 Revised:2024-12-05 Online:2024-12-09 Published:2024-12-09
  • Contact: Min-Huan LAN E-mail:minhuanlan@csu.edu.cn
  • Supported by:
    Supported by the National Key Research and Development Program of China (No. 2022YFA1207600), the National Natural Science Foundation of China (Nos. 62375289, 62175262), and the Key Laboratory of Pharmaceutical Analysis and Laboratory Medicine (Putian University), Fujian Province University (No. PALM 202201)

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摘要： 本文合成了一种具有声敏活性的红色荧光发射碳点(CDs)，将乏氧激活化疗药物AQ4N与CDs通过静电相互作用，氢键和π-π相互作用组装制备了CDs@AQ4N纳米组装体. CDs@AQ4N在超声辐照下可有效产生单线态氧(1O2)用于声动力治疗(SDT)；SDT过程消耗肿瘤内氧气进一步加剧了肿瘤乏氧，从而激活AQ4N，将其转化为具有细胞毒性的AQ4，在小鼠肿瘤模型下实现了荧光成像指导下的SDT联合化疗. 小鼠主要器官切片、血常规和血液生化分析均证实CDs@AQ4N具有优异的生物安全性.

关键词: 碳点, 乏氧激活, 声动力治疗, 化疗, 协同治疗

Abstract: A red fluorescent emitting carbon dots (CDs) with sonodynamic activity were synthesized, and the CDs@AQ4N nano-assemblies were prepared by assembling the hypoxia-activating drug AQ4N, with CDs via electrostatic interaction, hydrogen bonding, and π-π interactions. CDs@AQ4N could effectively generate singlet oxygen (1O2) for sonodynamic therapy (SDT) of cancer cells. Moreover, the depletion of intra-tumor oxygen during SDT further exacerbated the tumor hypoxia, which activated AQ4N and converted it into cytotoxic AQ4, enabling fluorescence-imaging-guided combination of SDT and chemotherapy for the treatment of mice tumors. The excellent biosafety of CDs@AQ4N was confirmed by mouse major organ sections, blood routine and blood biochemical analyses.

Key words: Carbon dots, Hypoxic activation, Sonodynamic therapy, Chemotherapy, Synergistic therapy

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