Tuning Push-Pull Electronic Effects of AIEgens to Boost the Theranostic Efficacy for Colon Cancer

Area of Science:

• Materials Science
• Oncology
• Biomedical Engineering

Background:

• Colon cancer presents a significant global health challenge due to its high mortality rate.
• Early diagnosis and effective treatment are crucial for improving patient outcomes.
• Existing theranostic agents lack comprehensive understanding of their in vivo gene expression modulation in cancer cells.

Purpose of the Study:

• To synthesize novel pyridinium-functionalized tetraphenylethylene derivatives as theranostic agents for colon cancer.
• To evaluate the efficacy of these agents in cell imaging and in vivo tumor treatment.
• To investigate the mechanism of action at the gene expression level.

Main Methods:

• Facile synthesis of three pyridinium-functionalized tetraphenylethylene derivatives (TPE-OM, TPE-H, TPE-NO2).
• In vitro cell imaging and in vivo tumor treatment experiments.
• Flow cytometry analysis and gene expression profiling.

Main Results:

• TPE-OM, featuring a donor-acceptor structure, demonstrated superior colon cancer treatment efficacy.
• TPE-OM effectively performed both in vitro cell diagnosis and in vivo tumor eradication.
• Flow cytometry revealed TPE-OM disrupts the cell cycle, inhibiting cell-cycle-promoting genes.

Conclusions:

• Pyridinium-functionalized tetraphenylethylene derivatives, particularly TPE-OM, are promising theranostic agents for colon cancer.
• TPE-OM's mechanism involves the inhibition of cell-cycle-promoting genes, offering new insights into cancer therapy.
• This research opens avenues for understanding and targeting cancer metastasis mechanisms.