Colon cancer is one of the most common
cancers with high mortality in humans. Early diagnosis and treatment of
colon cancer is of great significance for
cancer therapy. Numerous
theranostic agents have been developed to detect and kill
cancer cells. However, few reports have focused on how these agents control and affect the gene expression of
cancer cells in vivo. Herein, three pyridinium-functionalized
tetraphenylethylene derivatives, namely, TPE-OM, TPE-H, and TPE-NO2, with electron-donating and electron-withdrawing groups were facilely synthesized as
theranostic agents for cell imaging and anticolon
cancer therapy. Among these AIE luminogens (AIEgens), TPE-OM with donor and acceptor structure showed the best treatment efficacy for
colon cancer through systematic biological evaluation and comparison. Both in vitro cell imaging and in vivo
tumor treatment experiments demonstrated that TPE-OM can be utilized as an efficient
theranostic agent to diagnose and kill
colon cancer cells. Flow cytometric analysis revealed that the cell cycle process was disturbed by TPE-OM in
colon cancer cells. Deep insight into the gene level revealed that the expressions of cell-cycle-promoting genes was inhibited upon addition of TPE-OM. This study may open a new venue for unraveling the mechanisms of
cancer metastasis.