The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo

doi:10.1007/s00343-009-9119-x

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	The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo
	Shi Dayong; Li Jing; Guo Shuju; Su Hua; Fan Xiao
	2009-06-01
发表期刊	CHINESE JOURNAL OF OCEANOLOGY AND LIMNOLOGY
ISSN	0254-4059
卷号	27 期号:2 页码:277-282
文章类型	Article
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 S(180)-bearing mice. All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC(50) below 10 mu g/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.; 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 S-180-bearing mice. All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC50 below 10 mu g/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.
关键词	Leathesia Nana Bromophenol Derivatives Antitumor In Vitro In Vivo
学科领域	Limnology ; Oceanography
DOI	10.1007/s00343-009-9119-x
URL	查看原文
收录类别	SCI
语种	英语
WOS记录号	WOS:000267970300011
引用统计	被引频次：45[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.qdio.ac.cn/handle/337002/3484
专题	海洋生物技术研发中心实验海洋生物学重点实验室
作者单位	Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China
第一作者单位	中国科学院海洋研究所
推荐引用方式 GB/T 7714	Shi Dayong,Li Jing,Guo Shuju,et al. The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo[J]. CHINESE JOURNAL OF OCEANOLOGY AND LIMNOLOGY,2009,27(2):277-282.
APA	Shi Dayong,Li Jing,Guo Shuju,Su Hua,&Fan Xiao.(2009).The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo.CHINESE JOURNAL OF OCEANOLOGY AND LIMNOLOGY,27(2),277-282.
MLA	Shi Dayong,et al."The antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo".CHINESE JOURNAL OF OCEANOLOGY AND LIMNOLOGY 27.2(2009):277-282.

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