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Evaluating the Angiogenetic Properties of Ovarian Cancer Stem-Like Cells using the Three-Dimensional Co-Culture System, NICO-1
Published on: December 5, 2020
In Vitro and In Vivo Effect of Palladacycles: Targeting A2780 Ovarian Carcinoma Cells and Modulation of Angiogenesis
Francisco Reigosa-Chamorro1, Luís R Raposo2, Paula Munín-Cruz1
1Departamento de Química Inorgánica, Universidade de Santiago de Compostela, Avenida das Ciencias s/n, 15782 Santiago de Compostela, Spain.
Abstract:
Palladacycles are versatile organometallic compounds that show potential for therapeutic use. Here are described the synthesis and characterization of mono- and dinuclear palladacycles bearing diphosphines. Their biological effect was investigated in A2780, an ovarian-derived cancer line, and in normal dermal fibroblasts. The compounds displayed selective cytotoxicity toward the A2780 cell line. Compound 3 decreased the cell viability through cell cycle retention in G0/G1, triggered apoptosis through the intrinsic pathway, and induced autophagy in A2780 cells. Compound 9 also induced cell cycle retention, apoptosis, and cellular detachment. Notably, compound 9 induced the production of intracellular reactive oxygen species (ROS). Our work demonstrated that compound 3 enters A2780 cells via active transport, which requires energy, while compound 9 enters A2780 cells mostly passively. The potential effect of palladacycles in angiogenesis was investigated for the first time in an in vivo chorioallantoic membrane model, showing that while compound 3 displayed an antiangiogenic effect crucial to fighting cancer progression, compound 9 promoted angiogenesis. These results show that palladacycles may be used in different clinical applications where pro- or antiangiogenic effects may be desirable.
Insights
New palladacycles show selective cancer cell killing. Compound 3 inhibits tumor growth via anti-angiogenesis, while compound 9 promotes it, offering diverse therapeutic potential.
Area of Science:
- Organometallic Chemistry
- Cancer Biology
- Pharmacology
Background:
- Palladacycles are organometallic compounds with demonstrated therapeutic potential.
- Understanding their biological effects is crucial for developing novel cancer treatments.
Purpose of the Study:
- To synthesize and characterize novel mono- and dinuclear palladacycles containing diphosphines.
- To evaluate the biological activity and therapeutic potential of these compounds against ovarian cancer cells and normal fibroblasts.
- To investigate the impact of palladacycles on angiogenesis.
Main Methods:
- Synthesis and characterization of mono- and dinuclear palladacycles.
- Cytotoxicity assays using A2780 ovarian cancer cells and normal dermal fibroblasts.
- Cell cycle analysis, apoptosis assays, and reactive oxygen species (ROS) detection.
- In vivo chorioallantoic membrane assay to assess angiogenesis.
Main Results:
- Palladacycles exhibited selective cytotoxicity towards A2780 ovarian cancer cells.
- Compound 3 induced G0/G1 cell cycle arrest, apoptosis, and autophagy, entering cells via active transport.
- Compound 9 induced cell cycle arrest, apoptosis, and ROS production, entering cells passively. Compound 3 showed anti-angiogenic effects, while compound 9 promoted angiogenesis.
Conclusions:
- Palladacycles demonstrate selective anti-cancer properties and distinct mechanisms of action.
- The differential effects on angiogenesis suggest potential for tailored clinical applications.
- These findings highlight palladacycles as promising candidates for cancer therapy, with tunable pro- or anti-angiogenic activities.
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