Anti-migratory and cytotoxic effect of indole derivative in C6 glioma cells

• Published in: Toxicology in vitro 2024-04, Vol.96, p.105786-105786, Article 105786
• Main Authors: Andrade, Ana Karolina de Souza, de Franca, Mariana Nobre Farias, Santos, Jileno Ferreira, Macêdo, Nathália Araújo, de Lucca Junior, Waldecy, Scher, Ricardo, Cavalcanti, Socrates Cabral de Holanda, Corrêa, Cristiane Bani
• Format: Article
• Language: English
• Subjects: Cancer; Cell death; Cytotoxic effect; Indole derivatives; Tumor cells
• ISSN: 0887-2333; 1879-3177
• DOI: 10.1016/j.tiv.2024.105786

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 [Display omitted] •Indole derivatives had higher cytotoxicity than indole.•The viability of glioma, melanoma and lung adenocarcinoma cells decreased after treatment with indole derivatives.•The indole derivatives had anti-proliferative and anti-migratory effects on glioma cells.•Indole derivatives were cytotoxic against glioma cells and not cytotoxic against erythrocytes.