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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. 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.
AuthorsHai-Tao Feng, Shaomin Zou, Ming Chen, Feng Xiong, Mong-Hong Lee, Lekun Fang, Ben Zhong Tang
JournalJournal of the American Chemical Society (J Am Chem Soc) Vol. 142 Issue 26 Pg. 11442-11450 (07 01 2020) ISSN: 1520-5126 [Electronic] United States
PMID32479068 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Fluorescent Dyes
  • Stilbenes
  • tetraphenylethylene
Topics
  • Animals
  • Colonic Neoplasms (diagnostic imaging, drug therapy)
  • Density Functional Theory
  • Electrons
  • Fluorescent Dyes (chemistry)
  • HCT116 Cells
  • Humans
  • Mice
  • Mice, Nude
  • Molecular Structure
  • Neoplasms, Experimental (diagnostic imaging, drug therapy)
  • Optical Imaging
  • Stilbenes (chemistry)
  • Theranostic Nanomedicine

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