Title:Synthesis, Characterization, and Inducing Tumor Cell Apoptosis of Two Ru(II) Complexes Containing Guanidinium as Ligands
VOLUME: 18 ISSUE: 1
Author(s):Jing Sun*, Wen-Xiu Chen, Xing-Dong Song, Shu-Fen He, Jia-Xi Chen, Jun Mei, Xiao-Xian Zhu and Tie Wu
Affiliation:School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, School of Pharmacy, Guangdong Medical University, Dongguan, 523808
Keywords:Synthesis, Ru(II) complexes, cytotoxicity, apoptosis, protein, tumor cell.
Abstract:Description: Two new ruthenium(II) complexes containing guanidinium as ligands, [Ru(dip)2
(L1)]3+ (Ru1) and [Ru(dip)2(L2)]3+ (Ru2) (dip=4,7-diphenyl-1,10-phenanthroline; L1=1-(4-(1H-imidazo[4,5-
f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation; L2 = 1-(3-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl)
phenyl)guanidine cation) have been synthesized and characterized. Both complexes display higher cytotoxicity
against several cancer cell lines compared to cisplatin and are less cytotoxic on the nontumorigenic cell
line LO2. Intracellular distribution studies show that these complexes are selectively localized in the
cytoplasm.
Findings: Further analysis revealed that Ru1 and Ru2 had no obvious effects on the cell cycle and induced
apoptosis in HeLa cells via the mitochondrial pathway, which involved reactive oxygen species (ROS) accumulation,
mitochondrial dysfunction, and Bcl-2 family member activation. Taken together, the two complexes have
the potential to be utilized as anticancer agents.
