聚集诱导发光活性天然产物及其衍生物的生物医学应用

Biomedical applications of AIE-active natural products and derivatives

摘要

大自然所孕育的天然产物以其结构多样性与良好生物相容性著称。天然产物在应用于生物成像时，仍面临灵敏度低、可视化能力弱、实时监测效果不足及生物相容性差等方面的挑战。此外，在应用于治疗过程中，实时成像和动态监测仍存在背景噪声高和低灵敏度等诸多问题，而聚集诱导发光（aggregation-induced emission，AIE）现象的发现为解决这一困境提供了崭新视角。近年来，研究者发现诸多天然产物自身便具备内在的AIE特性，或可被巧妙改造为高效的AIE发光基元（AIEgens）。这类天然AIEgens像被点亮的“多彩”探针，不仅为阐释传统药效机制提供了独特窗口，更在细胞器成像、癌症诊疗、抗菌抗炎等生物医学领域展现出一体化诊疗的巨大潜力。本文系统梳理该领域研究进展，旨在为相关研究绘制一幅清晰的“导航图”。

Abstract

Natural products, endowed by nature, are renowned for their structural diversity and favorable biocompatibility. However, their application in bioimaging still faces challenges such as low sensitivity, poor visualization capability, inadequate real-time monitoring performance, and compromised biocompatibility. Furthermore, in therapeutic applications, real-time imaging and dynamic monitoring remain plagued by high background noise and low sensitivity. Fortunately, the discovery of aggregation-induced emission (AIE) provides a novel perspective for addressing these limitations. In recent years, researchers have identified numerous natural products that either inherently exhibit AIE characteristics or can be judiciously engineered into efficient AIE luminogens (AIEgens). These natural AIEgens function as illuminated "colorful" fluorescent probes, not only providing a unique window for elucidating traditional pharmacological mechanisms but also demonstrating great potential in integrated diagnostics and therapeutics across various biomedical fields, including organelle imaging, cancer theranostics, and antibacterial/anti-inflammatory applications. This review systematically summarizes the recent advances of AIE-active natural products, aiming to provide a "navigation map" for natural AIE research.

关键词

聚集诱导发光 / AIE发光基元 / 天然产物 / 天然产物衍生物 / 生物医学应用 / 生物成像 / 细胞器成像 / 癌症诊疗 / 诊疗一体化

Key words

aggregation-induced emission / AIEgens / natural products / natural product derivatives / biomedical application / bioimaging / organelle imaging / cancer theranostics / theranostics

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基金资助

国家自然科学基金重大项目(22595401)

广东省基础与应用基础研究基金资助项目(2024A1515010855)

广西青年人才托举工程项目(GXYESS2025006)