CHENG Rumei,BU Yexu.. Synthesis of triethylenetetramine-starch and its antitumor effects#br#[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2016, 46(1): 19-23.
Abstract:Objective: To design and synthesize the potential antitumor drug, CTS (triethylenetetraminestarch). Its interactions with the human telomere DNA (d[g3(T2Ag3)3 series]) and cytotoxicity to oCM-1 tumor cells are investigated. As a consequence, it provides a new strategy to develop targeted antitumor drugs. Methods: The triethylenetetramine reacted with the epichlorohydrin crosslinked-starch (CS) to produce the CTS. It was characterized by various methods. The circular dichroism (CD) spectra were used to clarify the interaction mechanism between the CTS and human telomere DNA. Its cytotoxity to oCM-1 cells was determined by CCK-8 method. Results: The antiparallel g-quadruplex could be induced and stabilized by CTS. This may be the reason that CTS inhibited the growth of oCM-1 cells, and moreover it showed very low cytotoxicity to ARPE-19 human cells. Such observations indicated that CTS was a promising antitumor drug. Conclusion: The CTS can stabilize the g-quadruplex and has higher cytotoxicity to oCM-1 cells. It has insignificant effects on the growth of normal human cells.