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Updated: Jul 30, 2025
A 3D Spheroid Model for Glioblastoma
Published on: April 9, 2020
Effect of sunitinib derivatives on glioblastoma single-cell migration and 3D cell cultures
Girstaute Dabkeviciute1,2, Ellias Maccioni3, Vilma Petrikaite1,2
1Institute of Biotechnology, Life Sciences Center, Vilnius University Sauletekio al. 7, LT-10257, Vilnius, Lithuania.
Abstract:
This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The effect on cell viability was determined by the MTT assay. Single-cell migration assay was performed to examine the effect of selected compounds on individual cell migration. The activity of compounds in 3D cell cultures was examined by measuring the size change of spheroids formed using the Hanging drop method. The viability of brain cancer (U-87MG and A-172) cells was most reduced by compound EMAC4001. EMAC4001 showed the strongest effect on U-87MG cell migration, and EMAC4007 was the most active in the A-172 cell line. Only sunitinib had a statistically significant impact on spheroid growth at 100 nM and 500 nM concentrations in the U87-MG cell line and EMAC4007 had a statistically significant impact on A-172 spheroid growth at 100 nM and 500 nM concentrations, similarly to sunitinib.
Insights
Researchers explored new sunitinib derivatives for brain cancer treatment. Compound EMAC4001 showed significant anticancer activity in cell viability and migration assays, while EMAC4007 impacted spheroid growth.
Area of Science:
- Oncology
- Medicinal Chemistry
- Cancer Cell Biology
Background:
- Brain cancer poses significant treatment challenges.
- Sunitinib is a known tyrosine kinase inhibitor with anticancer properties.
- Developing novel derivatives with improved efficacy is crucial.
Purpose of the Study:
- To evaluate the anticancer potential of 16 novel sunitinib derivatives.
- To assess their activity against brain cancer cells in 2D and 3D models.
- To identify lead compounds for further development.
Main Methods:
- Cell viability assessed using MTT assay.
- Single-cell migration analyzed via migration assay.
- Spheroid growth inhibition measured using Hanging drop method.
- Tested on U-87MG and A-172 brain cancer cell lines.
Main Results:
- Compound EMAC4001 demonstrated the highest reduction in brain cancer cell viability.
- EMAC4001 significantly inhibited U-87MG cell migration.
- EMAC4007 showed potent activity against A-172 cell migration.
- Sunitinib and EMAC4007 significantly impacted spheroid growth in respective cell lines.
Conclusions:
- Novel sunitinib derivatives, particularly EMAC4001 and EMAC4007, exhibit promising anticancer activity against brain cancer cells.
- These compounds show potential in both 2D and 3D cell culture models.
- Further investigation is warranted to explore their therapeutic applications.
