Log P analyzation-based discovery of GSH activated biotin-tagged fluorescence probe for selective colorectal cancer imaging

Eur J Med Chem. 2022 Sep 5:239:114555. doi: 10.1016/j.ejmech.2022.114555. Epub 2022 Jun 22.

Abstract

Targeted activatable fluorescent probes could provide an effective approach for colorectal cancer imaging. In this study, F1 was found as an effective targeted activatable fluorescent probe based on log P analysis. In vitro experiments demonstrated that the initial fluorescence of the developed probe F1 was initially well quenched, and the fluorescence increased after the probe interacted with glutathione. Cell imaging results showed that the probe had good cell permeability and selectivity. Remarkably, F1 displayed enhanced tumor tissue fluorescence in MC-38 tumor-bearing mice. Notably, it showed selectivity in imaging clinical specimens of human colorectal cancer tissues. Accordingly, this study shows that log P analysis can facilitate the developing efficient of biotin-tagged activatable probes, and the identified F1 has a good potential in clinical colorectal cancer diagnosis.

Keywords: Activatable probe; Colorectal cancer; Fluorescent probe; Glutathione; Tumor-specific imaging.

MeSH terms

  • Animals
  • Biotin
  • Colorectal Neoplasms* / diagnostic imaging
  • Fluorescence
  • Fluorescent Dyes*
  • Glutathione
  • Mice
  • Optical Imaging / methods

Substances

  • Fluorescent Dyes
  • Biotin
  • Glutathione