A Mitochondria-targeted AIEgen Labelled with 18 F for Breast Cancer Cell Imaging and Therapy

Chem Asian J. 2021 Dec 1;16(23):3963-3969. doi: 10.1002/asia.202101029. Epub 2021 Oct 20.

Abstract

A lack of efficient diagnostic tools for early and noninvasive diagnosis of breast cancer has restricted the clinical treatment effect. This problem might be addressed by the combination of aggregation-induced emission (AIE) fluorescence imaging and positron emission tomography (PET) with the dual advantages of high resolution and easy operation, and unlimited penetration and high sensitivity. Here, a mitochondria-targeted AIE luminogen (AIEgen) radiolabeled with 18 F was developed through a two-step radiochemical reaction by virtue of a prosthetic group. The obtained 18/19 F-Bz-CP imaging probe was examined by in vitro cell uptake and cell proliferation inhibition in two breast cancer cell lines, showing that the probe can efficiently target and locate in the mitochondria through the analysis of fluorescence imaging and PET simultaneously. Additionally, the probe can induce cancer cell apoptosis with the half maximal inhibitory concentration (IC50) of 4.8 μM for MCF-7 cells and 7.2 μM for T47D cells, indicating its potential application for breast cancer therapy.

Keywords: aggregation-induced emission; breast cancer; imaging and therapy; mitochondria; positron emission tomography.

MeSH terms

  • Apoptosis / drug effects
  • Breast Neoplasms / diagnostic imaging
  • Breast Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Fluorine Radioisotopes
  • Humans
  • Mitochondria
  • Optical Imaging
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacology*

Substances

  • Fluorescent Dyes
  • Fluorine Radioisotopes
  • Radiopharmaceuticals