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Issue 7, 2020
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A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs

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Abstract

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.

Graphical abstract: A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs

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Supplementary files

Article information


Submitted
16 Dec 2019
Accepted
21 Jan 2020
First published
23 Jan 2020

J. Mater. Chem. B, 2020,8, 1516-1523
Article type
Paper

A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs

X. Shi, S. H. P. Sung, M. M. S. Lee, R. T. K. Kwok, H. H. Y. Sung, H. Liu, J. W. Y. Lam, I. D. Williams, B. Liu and B. Z. Tang, J. Mater. Chem. B, 2020, 8, 1516
DOI: 10.1039/C9TB02848J

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