共价有机笼在药物递送、生物成像和生物传感中的研究进展OA
Research Progress of Covalent Organic Cages in Drug Delivery,Bioimaging,and Biosensing
共价有机笼(COCs)是一类由有机小分子通过共价键构筑的离散笼状功能材料,具有空腔尺寸可调、结构明确、化学稳定性高及溶液可加工性优良等核心特征.近年来,COCs在生物医学领域展现出巨大应用潜力,尤其在药物递送、生物成像和生物传感3大方向取得显著进展.在药物递送方面,通过精准结构设计与功能化修饰,COCs可实现对芳香族、疏水性等不同类型药物的高选择性包载,结合pH、氧化还原、酶响应等刺激机制,实现药物的靶向可控释放,显著提升治疗效果并降低毒副作用.在生物成像领域,COCs可通过嵌入荧光模块、配合顺磁金属离子或负载放射性核素,构建荧光、磁共振、PET等单模态及多模态成像探针,兼具高灵敏度、低生物蓄积风险及良好生物相容性.在生物传感领域,依托其精确定义的分子空腔与可控表面化学,COCs可实现对ATP、活性氧、金属离子及生物标志物的高特异性识别与信号转导,展现出优异的传感性能.系统综述了COCs的结构设计、合成策略及生物功能化修饰方法,重点探讨其在上述3大领域的作用机制与代表性应用,并分析了COCs在生物稳定性、体内代谢、规模化制备等方面面临的关键挑战,最后对其在精准医学、疾病早筛等领域的未来发展方向进行展望,为相关研究提供参考.
Covalent organic cages(COCs)are a class of discrete cage-like functional materials constructed from small organic molecules via covalent bonding and feature tunable cavity sizes,well-defined structures,high chemical stability,and excellent solution processability.In recent years,COCs have demonstrated enormous application potential in the biomedical field,achieving remarkable progress in three key areas in particular:Drug delivery,bioimaging,and biosensing.For drug delivery,COCs that achieve the highly selective encapsulation of various drugs,such as aromatic and hydrophobic agents,have been developed through precise structural design and functional modification.Combined with stimulus-responsive mechanisms,including pH,redox,and enzyme responsiveness,these COCs enable targeted and controlled drug release,significantly enhancing therapeutic efficacy while reducing side effects.For bioimaging,COCs can be engineered into single-modal and multimodal imaging probes(e.g.,fluorescence,magnetic resonance,and PET)that exhibit high sensitivity,low bioaccumulation risk,and favorable biocompatibility by incorporating fluorescent modules,chelating paramagnetic metal ions,or loading radionuclides.Further,owing to their precisely defined molecular cavities and controllable surface chemistry,COCs can realize the highly specific recognition and signal transduction of ATP,reactive oxygen species,metal ions,and biomarkers,thereby exhibiting outstanding performance in biosensing.This review systematically summarized the structural design,synthetic strategies,and biological functionalization methods of COCs,focusing on their mechanisms of action and representative applications in the above three areas.It also analyzed the key challenges faced by COCs in terms of their biological stability,in vivo metabolism,and large-scale production.Finally,the future development directions of COCs in precision medicine,early disease screening,and other fields were discussed,providing references for related research.
王满江;于江;魏会强;侯文彬;李祎亮
中国医学科学院北京协和医学院放射医学研究所,天津 300192中国医学科学院北京协和医学院放射医学研究所,天津 300192中国医学科学院北京协和医学院放射医学研究所,天津 300192中国医学科学院北京协和医学院放射医学研究所,天津 300192中国医学科学院北京协和医学院放射医学研究所,天津 300192
化学化工
共价有机笼动态共价化学药物递送生物成像生物传感
covalent organic cagesdynamic covalent chemistrydrug deliverybioimagingbiosensing
《化学试剂》 2026 (3)
27-41,15
国家自然科学基金项目(82404449).
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