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

Abstract

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. Up until now, numerous theranostic agents have been developed to detect and kill cancer cells. However, few reports have focused on how these agents control and affect 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 anti-colon 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 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 were inhibited upon addition of TPE-OM. This study may open a new venue for unraveling the mechanisms of cancer metastasis.