Related Experiment Video
Updated: Jul 4, 2025
Characterization of the Effects of Migrastatic Inhibitors on 3D Tumor Spheroid Invasion by High-resolution Confocal Microscopy
Published on: September 16, 2019
Anti-migratory and cytotoxic effect of indole derivative in C6 glioma cells
Ana Karolina de Souza Andrade1, Mariana Nobre Farias de Franca2, Jileno Ferreira Santos1
1Physiological Sciences Graduate Program, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil; Morphology Department, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
Abstract:
Gliomas are among the most common primary malignant brain tumors. Despite advances in cancer treatment, survival is very low, so the discovery of new therapeutic agents is essential. In this context, indole is an important source for the development of new bioactive molecules. A pharmacological screening of ten indole derivatives was carried out to evaluate the cytotoxic capacity against three tumor cell lines. After pharmacological screening, three compounds were selected, based on their high capacity to reduce cell proliferation, and their IC50 values were determined. Compound 9 exhibited the highest cytotoxic activity (IC50 = 0.4 μg/mL) in gliomas (C6 cell line), and were selected for further experiments. C6 cells were treated with compound 9 to evaluate cellular mechanisms such as colony formation and cell migration capacity and morphological alterations. Compound 9 decreased clone formation (0.4 and 0.8 μg/mL), and inhibited migration (0.2-0.8 μg/mL) in C6 cells. Morphological changes in cells treated with the compound 9 were also observed, such as chromatin condensation, and disorganization in cellular stress beams. Indole derivatives had a cytotoxic effect on tumor cells, and compound 9 showed the best anti-proliferative and anti-migratory activity in glioma cells.
Insights
New indole derivatives show promise as anti-cancer agents. Compound 9 effectively reduced glioma cell proliferation and migration, offering a potential new therapeutic avenue for brain tumors.
Area of Science:
- Oncology
- Medicinal Chemistry
- Pharmacology
Background:
- Gliomas are aggressive primary malignant brain tumors with poor patient survival rates.
- Developing novel therapeutic agents is crucial for improving glioma treatment outcomes.
- Indole derivatives represent a promising scaffold for discovering new bioactive molecules.
Purpose of the Study:
- To screen indole derivatives for cytotoxic activity against tumor cell lines.
- To identify and characterize potent indole-based compounds for glioma therapy.
- To investigate the anti-proliferative and anti-migratory mechanisms of active compounds in glioma cells.
Main Methods:
- Pharmacological screening of ten indole derivatives against three tumor cell lines.
- Determination of IC50 values for selected compounds.
- In vitro evaluation of compound 9's effects on glioma (C6) cell colony formation, migration, and morphology.
Main Results:
- Three indole derivatives demonstrated significant cytotoxic capacity.
- Compound 9 exhibited the highest cytotoxic activity against C6 glioma cells with an IC50 of 0.4 μg/mL.
- Compound 9 significantly inhibited C6 cell colony formation and migration, and induced morphological changes indicative of cell death.
Conclusions:
- Indole derivatives possess cytotoxic effects against tumor cells.
- Compound 9 displays potent anti-proliferative and anti-migratory activity in glioma cells.
- Compound 9 warrants further investigation as a potential therapeutic agent for glioma treatment.
