The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo
文献类型：CNKI期刊论文
| 作者 | Shi DY(史大永); Li J(李敬); Guo SJ(郭书举); Su H(苏华); Fan X(范晓) |
| 发表日期 | 2009-05-15 |
| 出处 | Chinese Journal of Oceanology and Limnology
 |
| 关键词 | Leathesia nana bromophenol derivatives antitumor in vitro in vivo |
| 英文摘要 | To investigate the antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo, six bromophenol derivatives 6-(2,3-dibromo-4,5-dihydroxybenzyl)-2,3-dibromo-4,5-dihydroxy benzyl methyl ether (1), (+)-3-(2,3-dibromo-4,5-dihydroxyphenyl)-4-bromo-5,6-dihydroxy-1,3- dihydroisobenzofuran (2), 3-bromo-4-(2,3-dibromo-4,5-dihydroxybenzyl)-5-methoxymethyl-pyrocatechol (3), 2,2′,3,3′-tetrabromo-4,4′,5,5′-tetrahydroxy-diphenylmethane (4), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (5), 2,2′,3-tribromo-3′,4,4′,5-tetrahydroxy-6′-ethyloxymethyldiphenylmethane (6) were isolated from brown alga Leathesia nana, and their cytotoxicity were tested by MTT assays in human cancer cell lines A549, BGC-823, MCF-7, B16-BL6, HT-1080, A2780, Bel7402 and HCT-8. Their inhibitory activity against protein tyrosine kinase (PTK) with over-expression of c-kit was analyzed also by ELISA. The antitumor activity of ethanolic extraction of Leathesia nana (EELN) was evaluated on S180-bearing mice. All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC50 below 10 μg/mL. In PTK inhibition study, all bromophenol derivatives showed moderate inhibitory activity and compounds 2, 5 and 6 showed significant bioactivity with the inhibition ratio of 77.5%, 80.1% and 71.4%, respectively. Pharmacological studies reveal that EELN could inhibit the growth of Sarcoma 180 tumor and increase the indices of thymus and spleen to improve the immune system remarkably in vivo. Results indicated that the bromophenol derivatives and EELN can be used as potent antitumor agents for PTK over-expression of c-kit and considered in a new therapeutic strategy for treatment of cancer. |
| 文献子类 | CNKI期刊论文 |
| 资助机构 | Supported by the National High Technology Research and Development Program of China (863 Program, No. 2007AA09Z410) ; Knowledge Innovation Program of Chinese Academy of Sciences (No. KZCX2-YW-209) |
| 卷 | v.27期:02页:95-100 |
| 语种 | 英文; |
| 分类号 | R285 |
| ISSN号 | 0254-4059 |
| 源URL | [http://ir.qdio.ac.cn/handle/337002/192598]  |
| 专题 | 中国科学院海洋研究所 |
| 作者单位 | InstituteofOceanology,ChineseAcademyofSciences |
| 推荐引用方式 GB/T 7714 | Shi DY,Li J,Guo SJ,et al. The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo. 2009. |
入库方式： OAI收割
来源：海洋研究所
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