一种亲脂性的聚集诱导发光探针，用于脂滴成像和评估 HIF-1 靶向药物的疗效。
A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs.
机构信息
HKUST Shenzhen Research Institute, No. 9 Yuexing 1st RD, South Area, Hi-tech Park, Nanshan, Shenzhen 518057, China.
Department of Chemistry, Department of Chemical and Biological Engineering, Hong Kong Branch of Chinese National Engineering Research Center for Tissue Restoration and Reconstruction, and Institute of Advanced Study, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.
出版信息
J Mater Chem B. 2020 Feb 19;8(7):1516-1523. doi: 10.1039/c9tb02848j.
Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that mediates the cellular response to hypoxia. The upregulation of HIF-1 expression in hypoxic cells can induce the accumulation of lipid droplets (LDs), and the LD levels can in turn reflect the expression level of HIF-1. Herein, we report a LD-specific luminogen with aggregation-induced emission characteristics (AIEgen), and have explored its potential applications in the evaluation of the inhibitory efficacy of HIF-1 targeting drugs. Compared to Nile red, this AIEgen shows a larger Stokes shift, better photostability, a more sensitive response to changes in dye concentration and a broader quantitative range. We found that the AIEgen can be used for semi-quantifying LD levels in cancer cells under hypoxic conditions, and for evaluating the inhibitory efficacy of HIF-1 targeting drugs. This work provides a simple and cost-effective strategy for screening HIF-1-targeted drugs, which may also be an alternative for evaluating the drug efficacy of other LD-related diseases.
缺氧诱导因子 1（HIF-1）是一种转录因子，介导细胞对缺氧的反应。在缺氧细胞中，HIF-1 表达的上调可以诱导脂滴（LD）的积累，而 LD 水平反过来又可以反映 HIF-1 的表达水平。在此，我们报道了一种具有聚集诱导发射特性（AIEgen）的 LD 特异性发光团，并探讨了其在评估 HIF-1 靶向药物抑制效果中的潜在应用。与尼罗红相比，该 AIEgen 具有更大的斯托克斯位移、更好的光稳定性、对染料浓度变化更敏感的响应以及更宽的定量范围。我们发现，该 AIEgen 可用于半定量检测缺氧条件下癌细胞中的 LD 水平，并评估 HIF-1 靶向药物的抑制效果。这项工作为筛选 HIF-1 靶向药物提供了一种简单且经济有效的策略，也可能是评估其他与 LD 相关疾病药物疗效的一种替代方法。
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