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    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.


    Xiujuan Shi, Simon H P Sung, Michelle M S Lee, Ryan T K Kwok, Herman H Y Sung, Haixiang Liu, Jacky W Y Lam, Ian D Williams, Bin Liu, Ben Zhong Tang. A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs. Journal of materials chemistry. B. 2020 Feb 19;8(7):1516-1523

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    PMID: 32003399

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