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Updated: Feb 2, 2026

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
Ruthenium complex delivery using liposomes to improve bioactivity against HeLa cells via the mitochondrial pathway
Bohong Guo1,2,3,4, Cancheng Liao1,2,3,4, Yuqi Fang1,2,3,4
1Department of Pharmaceutics, School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China.
Aim:
The aim of this study was to encapsulate a ruthenium complex [Ru(ttbpy)2PIP](ClO4)2 (Ru) in liposomes to enhance their antitumor effect on human cervical cancer.
Methods:
The Ru-loaded PEGylated liposomes (Ru-Lip) were prepared using thin-film hydration method. The mechanism of action was studied.
Results:
A novel Ru was successfully synthesized. Ru-Lip showed stronger cytotoxic activity against HeLa cells than Ru. Ru-Lip demonstrated a more significant increase in apoptosis, reactive oxygen species production and apoptosis-associated processes (intracellular calcium concentration, cytochrome c release and activation of Bax and caspase-3) than Ru. Ru-Lip exhibited greater blockade efficacy in the cell cycle G1 phase and greater DNA damage than Ru.
Conclusion:
Ru-Lip significantly elevates the anticancer effect via reactive oxygen species-mediated mitochondrial dysfunctional pathway.
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