Antitumor Activity and Mechanism Study of Riluzole and Its Derivatives
| Author | Xiang-Long Wu | en |
| Author | Liu Liu | en |
| Author | Qing-Chuan Wang | en |
| Author | Hai-Fang Wang | en |
| Author | Xiang-Rong Zhao | en |
| Author | Xu-Bin Lin | en |
| Author | Wen-Jun Lv | en |
| Author | Yin-Bo Niu | en |
| Author | Ting-Li Lu | en |
| Author | Qi-Bing Mei | en |
| Issued Date | 2020-07-31 | en |
| 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-trifluoromethoxy- benzothiazole (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 anti-cervical cancer effect on HeLa cells by inducing HeLa cell apoptosis. | en |
| DOI | https://doi.org/10.22037/ijpr.2020.1101149 | en |
| Keyword | Riluzole | en |
| Keyword | Benzothiazole derivatives | en |
| Keyword | Antitumour activity | en |
| Keyword | Synthesis | en |
| Keyword | Mechanism | en |
| Publisher | Brieflands | en |
| Title | Antitumor Activity and Mechanism Study of Riluzole and Its Derivatives | en |
| Type | Original Article | en |
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