ABSTRACT
Aim To evaluate the antitumor activity of ruthenium polypyridyl complexes and the underlying mechanism. Methods The right complexes 2b were filtered with highest activity and lowest toxicity by MTT assay. The change of cell cycle was detected by flow cytometry . The expression of p53 and p21 was detected by Western blot. The in vivo antitumor activity of 2b was evaluated by the assay of tumor bearing nude mice. Results 2b potentially inhibited proliferation of a variety of hepatoma cell lines, among which Hep 3B cell was the most significant ( IC50 was 12. 1 μmol · L-1 ) . The apoptosis of Hep 3 B cell was induced by 2b, as evidenced by DNA fragmentation, chromatin condensation and appearance of subG1 peak. The ac-tivities of caspase-9 and caspase-3 were activated by 2b. The phosphorylation of p53 was induced by 2b. The expression of p53 and p21 was also up-regulated by 2b. The growth of tumor of nude mice was signifi-cantly inhibited by 2b in vivo experiment. Conclusion 2b has good in vitro and vivo antitumor activities, and it can inhibite growth of Hep 3 B cells by inducing apoptosis.