摘要

A ruthenium(II) complex coordinated by cordycepin, [Cor-Ru(II)], was synthesized for investigation as a potential novel candidate for cancer therapy. The antitumor activity of Cor-Ru(II) was investigated by MTT and flow cytometry (FCM) assays. The results showed that Cor-Ru(II) significantly inhibited the proliferation of Bel-7402 human hepatoma cells and delayed cell cycle progression. Subsequent experiments using FCM and western blot analysis indicated that Cor-Ru(II) induced cell apoptosis via suppression of bcl-2 expression and stimulation of p53 expression. Cor-Ru(II) was shown to interfere with the synthesis of DNA. This was confirmed by the in vitro binding to DNA in the groove binding mode (K-b=4.22(+/- 0.2)x10(5) M-1). Thus, Cor-Ru(II) appears to act as an effective antitumor agent in vitro.