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Chlorogenic acid activates ERK1/2 and inhibits proliferation of osteosarcoma cells
Luigi Sapio1, Alessia Salzillo1, Michela Illiano1
1Department of Precision Medicine, University of Campania "Luigi Vanvitelli", Naples, Italy.
Abstract:
Osteosarcoma (OS) is a very aggressive metastatic pediatric and adolescent tumor. Due to its recurrent development of chemotherapy resistance, clinical outcome for OS patients remains poor. Therefore, discovering more effective anticancer agents is needed. Chlorogenic acid (CGA) is a phenolic compound contained in plant-related products that modulates many cellular functions and inhibits cell proliferation in several cancer types. However, few evidence is available in OS. Here, we investigate the effects of CGA in U2OS, Saos-2, and MG-63 OS cells. By multiple approaches, we demonstrate that CGA acts as anticancer molecule affecting the cell cycle and provoking cell growth inhibition mainly by apoptosis induction. We also provide evidence that CGA strongly activates extracellular-signal-regulated kinase1/2 (ERK1/2). Strikingly, ERK1/2 inhibitor PD98059 sensitizes the cells to CGA. Altogether, our data enforce the evidence of the anticancer activity mediated by CGA and provide the rationale for the development of innovative therapeutic strategies in OS cure.
Insights
Chlorogenic acid (CGA) shows anticancer effects against osteosarcoma (OS) by inducing apoptosis and inhibiting cell growth. CGA also activates ERK1/2, suggesting potential for new therapeutic strategies in OS treatment.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Osteosarcoma (OS) is an aggressive pediatric cancer with poor outcomes due to chemotherapy resistance.
- Novel therapeutic agents are crucial for improving clinical results in OS patients.
- Chlorogenic acid (CGA), a plant-derived phenolic compound, exhibits anticancer properties in various cancer types, but its role in OS is underexplored.
Purpose of the Study:
- To investigate the anticancer effects of Chlorogenic acid (CGA) on osteosarcoma (OS) cell lines.
- To elucidate the mechanisms underlying CGA's anti-OS activity, including cell cycle, apoptosis, and signaling pathways.
- To explore the potential synergistic effects of CGA with ERK1/2 inhibition in OS treatment.
Main Methods:
- In vitro studies using U2OS, Saos-2, and MG-63 osteosarcoma cell lines.
- Assessment of cell cycle progression, apoptosis induction, and cell growth inhibition.
- Analysis of extracellular-signal-regulated kinase 1/2 (ERK1/2) pathway activation.
- Evaluation of the effects of an ERK1/2 inhibitor (PD98059) in combination with CGA.
Main Results:
- Chlorogenic acid (CGA) demonstrated significant inhibition of osteosarcoma cell proliferation.
- CGA treatment led to cell cycle arrest and induced apoptosis in OS cells.
- CGA was found to strongly activate the extracellular-signal-regulated kinase 1/2 (ERK1/2) pathway.
- Inhibition of ERK1/2 with PD98059 sensitized osteosarcoma cells to CGA, enhancing its cytotoxic effects.
Conclusions:
- Chlorogenic acid (CGA) possesses potent anticancer properties against osteosarcoma (OS) through apoptosis induction and cell growth inhibition.
- The activation of the ERK1/2 pathway by CGA is a key mechanism in its anti-OS activity.
- CGA represents a promising candidate for developing novel therapeutic strategies against osteosarcoma, potentially in combination with targeted therapies.
