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Developing a novel binuclear copper complex for enhanced cellular copper uptake and cancer treatment
Haoran Liu1, Jingyi Zhang1, Yanping Li2
1Guangxi Key Laboratory of Tumor Immunology and Microenvironmental Regulation, Guangxi Health Commission Key Laboratory of Tumor Immunology and Receptor-Targeted Drug Basic Research, Guilin Medical University, Huan Cheng North 2nd Road 109, Guilin 541004, PR China.
A novel copper complex, C1, shows enhanced anticancer efficacy by improving copper uptake and inducing cuproptosis, mitochondrial damage, and apoptosis. This new agent significantly inhibits tumor growth, outperforming existing copper-based therapies.
Area of Science:
- Medicinal Chemistry
- Cancer Biology
- Pharmacology
Background:
- Elesclomol (Es) is a copper ionophore with limited anticancer efficacy due to inefficient copper transport.
- Existing copper-based therapies require improved mechanisms of action for enhanced antitumor activity.
Purpose of the Study:
- To design and synthesize a novel copper chelator, L1, forming a binuclear copper complex C1.
- To evaluate the therapeutic potential and anticancer mechanisms of C1 compared to Elesclomol-Cu (EsCu).
Main Methods:
- Synthesis of L1 and its binuclear copper complex C1.
- Assessment of cellular copper uptake in gastric cancer cells.
- Evaluation of anticancer mechanisms including cuproptosis, reactive oxygen species generation, DNA damage, and apoptosis.
- In vivo tumor inhibition studies in animal models.
Main Results:
- C1 demonstrated superior copper uptake and multiple anticancer mechanisms compared to EsCu.
- C1 potently induced cuproptosis, mitochondrial superoxide, ROS, autophagic lysosome accumulation, DNA damage, and apoptosis.
- In vivo studies showed C1 achieved an 80.3% tumor inhibition rate, significantly higher than EsCu's 45%.
Conclusions:
- C1 represents a next-generation copper-based anticancer agent with enhanced therapeutic potential.
- The improved efficacy of C1 is attributed to its efficient copper transport and multifaceted anticancer mechanisms.
