A ruthenium(II) complex inhibits tumor growth in vivo with fewer side-effects compared with cisplatin

• The antitumor activity of Δ-Ru1 was evaluated.
• The antitumor activity of Δ-Ru1 was comparable with cisplatin in vivo.
• Δ-Ru1 exerts its cytotoxicity through the mitochondria-mediated apoptotic pathway.
• Δ-Ru1 inhibits tumor growth in vivo with fewer side-effects than cisplatin.

The antitumor activity of a ruthenium(II) polypyridyl complex, Δ-[Ru(bpy)2(HPIP)](ClO4)2 (Δ-Ru1, where bpy = 2,2′-bipyridine, HPIP = 2-(2-hydroxyphenyl)imidazo[4,5-f][1,10]phenanthroline), was evaluated. The in vivo experiments showed that Δ-Ru1 inhibited the growth of a human cervical carcinoma cell line (HeLa) xenotransplanted into nude mice with efficiency similar to that of cisplatin. Histopathology examination of the tumors from treated xenograft models was consistent with apoptosis in tumor cells. Importantly, in striking contrast with cisplatin, Δ-Ru1 did not cause any detectable side effects on the kidney, liver, peripheral neuronal system, or the hematological system at the pharmacologically effective dose. The preclinical studies reported here provide support for the clinical use of Δ-Ru1 as an exciting new drug candidate with lower toxicity than cisplatin, endowed with proapoptotic properties.

A ruthenium(II) polypyridyl complex, Δ-[Ru(bpy)2(HPIP)](ClO4)2 (Δ-Ru1), was found to inhibit tumor growth in vivo without causing any detectable side effects on the kidney, liver, peripheral neuronal system, or the hematological system at the pharmacologically effective dose.Figure optionsDownload as PowerPoint slide