Ruthenium polypyridyl complexes that induce mitochondria-mediated apoptosis in cancer cells.
The limitations of cisplatin-based chemotherapy, including high toxicity, undesirable side effects, and drug resistance, have motivated extensive investigations into alternative metal-based cancer therapies. Ruthenium (Ru) possesses several favorable properties suited to rational anticancer drug design and biological applications. In the present study, we synthesized a series of ruthenium polypyridyl complexes containing N,N-chelating ligands, examined their anticancer activities, and elucidated the molecular mechanisms through which they caused the cancer cell death. The results demonstrated that [Ru(phen)(2)-p-MOPIP](PF(6))(2).2H(2)O (RuPOP), a complex with potent antiproliferative activity, is able to induce mitochondria-mediated and caspase-dependent apoptosis in human cancer cells. On the basis of these results, we suggest that RuPOP may be a candidate for further evaluation as a chemopreventive and chemotherapeutic agent for human cancers, especially for melanoma.
Department of Chemistry, Jinan University, Guangzhou 510632, People's Republic of China.
Tianfeng
T
Chen
Yanan
Y
Liu
Wen-Jie
WJ
Zheng
Jie
J
Liu
Yum-Shing
YS
Wong
D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis; D002460:Cell Line; D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008928:Mitochondria / Q000187:drug effects*; D009942:Organometallic Compounds / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D012428:Ruthenium / Q000494:pharmacology*
D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D011725:Pyridines; D012428:Ruthenium