A lipophilic AIEgen for lipid droplet imaging and evaluation of the efficacy of HIF-1 targeting drugs. Issue 7 (31st January 2020)

• Record Type: Journal Article
• Authors: Shi, Xiujuan; Sung, Simon H. P.; Lee, Michelle M. S.; Kwok, Ryan T. K.; Sung, Herman H. Y.; Liu, Haixiang; Lam, Jacky W. Y.; Williams, Ian D.; Liu, Bin; Tang, Ben Zhong
• Is Part Of: Journal of materials chemistry. Volume 8:Issue 7(2020)
• Page Start: 1516
• Page End: 1523
• Publication Date: 2020-01-31
• Subjects: Materials -- Periodicals; Chemistry, Analytic -- Periodicals; Biomedical materials -- Research -- Periodicals; 543.0284
• DOI: 10.1039/c9tb02848j
• Languages: English
• ISSNs: 2050-750X

Abstract

Abstract : A lipid-droplet-specific AIEgen was used to evaluate the inhibitory efficacy of HIF-1-targeting drugs by assessing lipid-droplet levels. 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.