This study was aimed to investigate the growth inhibition effect of diimide G-quadruplex ligand on leukemia cells and to explore its molecular mechanisms. K562 leukemia cell lines were treated with various concentrations of the diimide G-quadruples ligand small molecule (0.1 - 10 micromol/L). Trypan blue exclusion assay was used to evaluate the proliferation inhibition. Cell apoptosis was observed using terminal deoxynucleotide transferase-mediated dUTP nick end labeling (TUNEL). Telomerase activity was analyzed by telomere repeat amplification protocol. Gene expression was detected by microarray and confirmed by RT-PCR assay. The results showed that diimide small molecule inhibited the proliferation of K562 cells and induced apoptosis of these cells. After treating with diimide G-quadruplex ligand, telomerase activity of K562 cells was reduced and the transcriptional levels of some important genes were changed significantly. These genes were involved in cell apoptosis, cell signaling pathway and other key functions. In conclusion, the diimide G-quadruplex ligand is a small molecule that inhibits the proliferation and induces apoptosis in leukemia cells, and these functions may be related to telomerase inhibition and regulation of some important gene transcription.
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