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- Title
Antitumor Activity and Mechanism Study of Riluzole and Its Derivatives.
- Authors
Xiang-Long Wu; Liu Liu; Qing-Chuan Wang; Hai-Fang Wang; Xiang-Rong Zhao; Xu-Bin Lin; Wen-Jun Lv; Yin-Bo Niu; Ting-Li Lu; Qi-Bing Mei
- 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.
- Subjects
HELA cells; RILUZOLE; CELL cycle; BCL-2 proteins; CANCER cells; ANTINEOPLASTIC agents
- Publication
Iranian Journal of Pharmaceutical Research, 2020, Vol 19, Issue 3, p217
- ISSN
1735-0328
- Publication type
Article
- DOI
10.22037/ijpr.2020.1101149