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Published on: December 7, 2014
Effectiveness and Mechanism of Resibufogenin on Human Renal Cancer Cell Caki-1
Yuqi Wu1, Yue Yang1, Run Huang1
1School of Life Science and Technology, Mudanjiang Normal University, Mudanjiang 157011, China.
Abstract:
In this study, we investigated the effect and mechanism of Resibufogenin on renal cell carcinoma based on network pharmacology, molecular docking, and in vitro experiments. The results showed that there were 35 cross-targets between Resibufogenin and renal cell carcinoma. GO and KEGG pathway analyses indicated that Resibufogenin inhibited renal cancer cells through the vascular smooth muscle contraction signalling pathway and EGFR tyrosine kinase inhibitor resistance signaling pathway, and MAPK1, PRKCB, and Resibufogenin had strong associative activities. After different concentrations of Resibufogenin were applied to human renal cancer cells, it was found that the IC50 value was 408.2 nM, 10 nM resibufogenin could significantly inhibit cell migration (p < 0.0001), the percentage of apoptosis and necrosis increased dose-dependently, and the expression of genes of MAPK1 and PRKCB in the cells was significantly reduced (p < 0.001) in a dose-dependent manner. The above results indicate that Resibufogenin can inhibit human renal cell carcinoma through multi-targets and multi-methods, which provides a theoretical basis for the application of Resibufogenin in the treatment of renal cell carcinoma and the development of novel drugs in the future.
Insights
Resibufogenin effectively inhibits renal cell carcinoma by targeting multiple pathways, including vascular smooth muscle contraction and EGFR resistance. This natural compound significantly reduces cancer cell migration and increases apoptosis, offering a promising basis for new renal cancer treatments.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Renal cell carcinoma (RCC) remains a significant health concern with limited treatment options.
- Identifying novel therapeutic agents with multi-target mechanisms is crucial for improving patient outcomes.
Purpose of the Study:
- To investigate the anti-cancer effects and underlying mechanisms of Resibufogenin on renal cell carcinoma.
- To explore Resibufogenin's potential as a therapeutic agent for RCC.
Main Methods:
- Network pharmacology was employed to identify potential targets of Resibufogenin in RCC.
- Molecular docking was used to assess binding affinities.
- In vitro experiments were conducted on human renal cancer cells to evaluate Resibufogenin's efficacy.
Main Results:
- 35 overlapping targets were identified between Resibufogenin and RCC.
- Resibufogenin demonstrated significant inhibition of renal cancer cell migration (IC50 = 408.2 nM).
- Apoptosis and necrosis increased dose-dependently, with reduced expression of MAPK1 and PRKCB genes.
Conclusions:
- Resibufogenin exhibits multi-target and multi-modal inhibitory effects on human renal cell carcinoma.
- These findings provide a theoretical foundation for developing Resibufogenin-based therapies for RCC.
