Ru(II) complexes bearing guanidinium ligands as potent anticancer agents.
Two ruthenium(II) complexes containing guanidinium ligands have been synthesized and characterized for the first time. It was found that the two complexes exhibit moderate antitumor activity in Hela, A549, CNE-2, MCF-7, and HepG2 human tumor cells. Flow cytometric analysis showed that both complexes arrested the cell cycle in the G2/M phase and induced apoptosis in Hela cells. Mechanism studies indicate that both complexes induced apoptosis through caspase- and reactive oxygen species (ROS)-dependent pathways. Additionally, the two complexes displayed higher phototoxicity to tumor cells and almost no influence on normal liver LO2 cells upon irradiation at 450nm.
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Wen-Xiu
WX
Chen
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Xing-Dong
XD
Song
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Shu-Fen
SF
He
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China. Electronic address: sunjing03@foxmail.com.
Jing
J
Sun
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Jia-Xi
JX
Chen
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Tie
T
Wu
MOE Key laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, China. Electronic address: cesmzw@mail.sysu.edu.cn.
Zong-Wan
ZW
Mao
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D016195:G2 Phase / Q000187:drug effects; D019791:Guanidine / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D056831:Coordination Complexes; D012428:Ruthenium; D019791:Guanidine
Apoptosis; CT-DNA; Cytotoxicity; Guanidinium; Phototoxicity; Ru(II) complex