期刊
BIOCHEMICAL PHARMACOLOGY
卷 75, 期 4, 页码 826-835出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2007.10.014
关键词
2-styrylchromone; antimitotic drugs; tubulin; mitosis; cell cycle; cancer chemotherapy
4 '-Methoxy-2-styrylchromone, a new synthetic chromone was identified as a selective proliferation inhibitor of human tumor (MCF-7 and NCI-H460) cell lines than to non-tumor cells (MRC-5). The antiproliferative activity of this chromone was also extensive to peripheral human lymphocytes. 4 '-Methoxy-2-styrylchromone was found to block tumor cells in the G(2)/M phase of the cell cycle. The G(2)/M arrest of NCI-H460 cells was dose- and time-dependent, reaching a maximum after 12-h treatment while MCF-7 cells reached the maximum value of G2/M accumulation only after a 24-h treatment. Chromone-treated cells evidenced a high frequency of cells in prometaphase, indicating progression beyond G(2) and arrest early in mitosis. This mitotic arrest was associated with abnormal mitotic spindles characterized by the formation of a monopolar structure, suggesting that the chromone interferes with microtubules. The results of an in vitro tubulin polymerization assay showed that this chromone stabilizes microtubules in a manner similar to paclitaxel. (c) 2007 Elsevier Inc. All rights reserved.
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