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

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.

• Authors: 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
• Journal: Journal of materials chemistry. B (J Mater Chem B) Vol. 8 Issue 7 Pg. 1516-1523 (02 19 2020) ISSN: 2050-7518 [Electronic] England
• PMID: 32003399 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Hypoxia-Inducible Factor 1
• Pyridines

Topics

• HeLa Cells
• Humans
• Hypoxia-Inducible Factor 1 (antagonists & inhibitors, metabolism)
• Lipid Droplets (chemistry, metabolism)
• Molecular Structure
• Optical Imaging
• Particle Size
• Pyridines (chemistry, pharmacology)
• Surface Properties