高等学校化学学报 ›› 2009, Vol. 30 ›› Issue (10): 1976.

• 研究论文 • 上一篇    下一篇

鱼藤中抗肿瘤活性化合物的追踪分离及与DNA的相互作用

方玉春, 邵长伦, 李静, 李延团, 姜曼, 王长云   

  1. 海洋药物教育部重点实验室, 中国海洋大学医药学院, 青岛 266003
  • 收稿日期:2009-01-25 出版日期:2009-10-10 发布日期:2009-10-10
  • 通讯作者: 王长云, 男, 博士, 教授, 博士生导师, 主要从事海洋天然产物化学和海洋药物研究. E-mail: changyun@ouc.edu.cn
  • 基金资助:

    国家自然科学基金(批准号: 30572314)、国家教育部新世纪优秀人才支持计划(批准号: NCET-05-0600)、国家科技基础性工作专项基金(批准号: 2007FY210500)和山东省优秀中青年科学家科研奖励基金(批准号: 03BS109)资助.

Bioassay-guided Isolation of Antitumor Compounds from Derris trifoliate Lour and Their Interaction with DNA

FANG Yu-Chun, SHAO Chang-Lun, LI Jing, LI Yan-Tuan, JIANG Man, WANG Chang-Yun*   

  1. Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
  • Received:2009-01-25 Online:2009-10-10 Published:2009-10-10
  • Contact: WANG Chang-Yun
  • Supported by:

    国家自然科学基金(批准号: 30572314)、国家教育部新世纪优秀人才支持计划(批准号: NCET-05-0600)、国家科技基础性工作专项基金(批准号: 2007FY210500)和山东省优秀中青年科学家科研奖励基金(批准号: 03BS109)资助.

摘要:

采用活性追踪分离的方法, 从鱼藤中分离鉴定出了2个抗肿瘤活性化合物, 即羟基鱼藤素(1)和鱼藤酮(2). 用丽丝胺罗丹明B(SRB)法评价其抗肿瘤活性, 用紫外光谱和荧光光谱等方法探讨了化合物与DNA的相互作用. 结果发现, 羟基鱼藤素(1)与鱼藤酮(2)为鱼藤的抗肿瘤活性成分, 对人大肠癌细胞HCT8、人肝癌细胞BEL7402、人胃癌细胞BGC823、人肺癌细胞A549和人卵巢癌细胞A2780的半数抑制浓度(IC50) 在0.1~90.0 μmol/L之间. 这两种化合物的紫外吸收强度随着HS-DNA的加入均呈现减色效应, 并使EB-HS-DNA复合体系荧光强度减弱, 表明化合物的抗肿瘤活性与DNA以插入方式作用有关.

关键词: 鱼藤; 抗肿瘤化合物; 追踪分离; DNA作用

Abstract:

Two antitumor compounds, tephrosin(1) and rotenone(2), were acquied by bioassay-guided isolation from Derris trifoliate Lour. Compounds 1 and 2, assayed by SRB(Sulforhodamine B) methods, showed antitumor activities against cell lines of HCT8, BEL7402, BGC823, A549 and A2780 in vitro with IC50 values from 0.1 to 90.0 μmol/L. The interaction of the compounds with HS-DNA was investigated using UV spectra and fluorescent spectra. The absorbance values at the UV max peaks of compounds 1 and 2 were reduced by adding HS-DNA while the intensity of fluorescent spectra of EB-HS-DNA were gradually weaken following the increased amounts of compounds 1 and 2. It indicated that the mode of antitumor activities of compounds 1 and 2 was relative to binding with DNA through intercalation mode.

Key words: Derris trifoliate Lour; Antitumor compound; Bioassay-guided isolation; DNA interaction

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