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Antitumor Activity and Mechanism Study of Riluzole and Its Derivatives.
- Source :
- Iranian Journal of Pharmaceutical Research; Summer2020, Vol. 19 Issue 3, p217-230, 14p
- Publication Year :
- 2020
-
Abstract
- To explore novel antitumor agents with high efficiency and low toxicity, riluzole alkyl derivatives (4a-4i) were synthesized. Their anti-proliferative activities against HeLa, HepG2, SP2/0, and MCF-7 cancer cell lines were assessed by the CCK-8 assay and compared with human normal liver (LO2) cells. Most of them showed potent cytotoxic effects against four human tumor cell lines and low toxic to LO2 cells. In particular, 2-(N-ethylamine)-6-trifluoromethoxybenzothiazole (4a) showed a IC50 value of 7.76 μmol/L in HeLa cells and was found to be nontoxic to LO2 cells up to 65 μmol/L. Furthermore, flow cytometry indicated that 4a could induce remarkable early apoptosis and G2/M cell cycle arrest in HeLa cells. It also impaired the migration ability of HeLa cells in wound healing assays. Western blot results demonstrated that 4a suppressed Bcl-2 protein expression but increased the level of Bax in HeLa cells, and elevated the Bax/Bcl-2 expression ratio. These new findings suggest that 4a exhibited beneficially anticervical cancer effect on HeLa cells by inducing HeLa cell apoptosis. [ABSTRACT FROM AUTHOR]
- Subjects :
- HELA cells
RILUZOLE
CELL cycle
BCL-2 proteins
CANCER cells
ANTINEOPLASTIC agents
Subjects
Details
- Language :
- English
- ISSN :
- 17350328
- Volume :
- 19
- Issue :
- 3
- Database :
- Complementary Index
- Journal :
- Iranian Journal of Pharmaceutical Research
- Publication Type :
- Academic Journal
- Accession number :
- 147796730
- Full Text :
- https://doi.org/10.22037/ijpr.2020.1101149