Global Advanced Research Journal of Medicine and Medical Sciences (GARJMMS) ISSN: 2315-5159
September 2014 Vol. 3(9), pp. 240-250
Copyright © 2014 Global Advanced Research Journals

 

Full Length Research Paper

Cytotoxic effect of three novel thiochromanone derivatives on tumor cell in vitro and underlying mechanism

Yuemin Zhao1, Chunna Li1, Haitao Suo1, Yanping Wang1, Chunliu Yang1,2, Zhengyue Ma1,2 and Yuxin Liu1,2

1College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei Province, 071002, P. R. China;
2Drug Quality Control Key Laboratory of Hebei Province, Baoding, Hebei Province, 071002, P. R. China

*Corresponding Author E-mail: yuxinliu@hbu.edu.cn; Tel: (86)186-3026-2196; Fax: (86)0312-597-1107

Accepted 09 September, 2014

Abstract

Thiochromanone derivatives have received extensive attention for their biological activities, but their anti-tumor activities were seldom reported. In this paper, in vitro anti-proliferative activities of three novel thiochromanone derivatives, (z)-3-(chloromethylene)-6-fluorothiochroman-4-one (CMFT), (z)-3-(bromomethylene)-6-fluorothiochroman-4-one (BMFT) and (z)-3-(chloromethylene)-6-chlorothiochroman-4-one (CMCT) were investigated by the method of MTT assay. All the tested chemicals showed cell toxicity to 13 human cell lines (A549, SGC-7901, BGC-823, U937, K562, Hela, MCF-7, HepG-2, A375, LS174T, HT1080, C4-2B and MRC-5), and half maximal inhibitory concentration (IC50) values were between 2.3-36.3 μM. CMFT was chosen as a representative to invested the underlying mechanism. Cell apoptotic ratio was measured by flow cytometry analysis. The results showed that CMFT induced tumor cell apoptosis. Cysteinyl aspartate-specific proteases detection confirmed CMFT increased activity of caspase-8, caspase-9 and caspase-3. Moreover, CMFT could enhance the level of death receptor 3 (DR3). In conclusion, current results suggested novel thiochromanone derivative CMFT could kill tumor cells by inducing tumor cell apoptosis via increasing apoptosis-related factors.

Keywords Thiochromanones; antiproliferation; apoptosis; caspases; tubulin.

 

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