色谱

色谱

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色谱指纹谱用于中药大黄抗肿瘤活性成分的筛选

孔亮1,包永明2,于志远1,李伟1,陈学国1,胡良海1,邹汉法1

  

  1. 1. Dalian Institute of Chemical Physics, The Chinese Academy of Sciences, Dalian 116023, China; 2. School of Environmental and Biological Science and Technology, Dalian University of Technology, Dalian 116024, China
  • 收稿日期:2005-04-10 修回日期:1900-01-01 出版日期:2005-09-30 发布日期:1988-03-25
  • 通讯作者: 邹汉法

Screening of Antineoplastic Components in Radix et Rhizoma Rhei Using Chromatographic Fingerprints

KONG Liang1, BAO Yongming2, YU Zhiyuan1, LI Wei1, CHEN Xueguo1, HU Lianghai1, ZOU Hanfa1
  

  1. 1. Dalian Institute of Chemical Physics, The Chinese Academy of Sciences, Dalian 116023, China; 2. School of Environmental and Biological Science and Technology, Dalian University of Technology, Dalian 116024, China
  • Received:2005-04-10 Revised:1900-01-01 Online:2005-09-30 Published:1988-03-25

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摘要：

采用液相色谱-质谱联用方法分析了中药大黄经过SD大鼠肝匀浆体外代谢前后的指纹谱中色谱峰面积、保留值的差异。指出5种游离型蒽醌化合物在SD大鼠肝匀浆体外代谢体系中只有大黄酚发生代谢反应转化为芦荟大黄素。考察了体外代谢条件下,肝匀浆浓度与代谢时间对大黄酚转化及其代谢产物的影响。SD大鼠体外抗肿瘤试验表明,大黄代谢物对于人宫颈癌(HeLa)细胞的抑制活性略高于其提取物。通过比较芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚的活性,并结合大黄酚的体外代谢反应的考察,解释了大黄代谢物对肿瘤细胞活性的抑制率的提高是由大黄酚的代谢产物芦荟大黄素浓度的增加引起的。

关键词: SD大鼠, 大黄, 肝匀浆 , 高效液相色谱-质谱, 色谱指纹谱, 体外代谢, 中药

Abstract:

A new strategy for screening of antineoplastic components in the traditional Chinese medicine of Radix et Rhizoma Rhei has been developed using chromatographic fingerprints before and after metabolism by high performance liquid chromatography-mass spectrometry. The metabolizing method was established based on the in vitro metabolism by Sprague-Dawley (SD) rat liver homogenate. By means of the metabolism methods in vitro, the antineoplastic activity of the extracts, metabolites and components of Radix et Rhizoma Rhei were determined by microculture tetrazolium （MTT） assays in vitro. It was observed that the inhibition rate of the crude extract for HeLa cell was increased from 26.7% to 36.2% after 60 min of metabolism. The changes of activities resulted from the changes of components’ structures and the bioactive components were discovered simultaneously in view of metabolism by inhibiting rate assay for the components in Radix et Rhizoma Rhei. It is concluded that the antineoplastic activity of the crude extract from Radix et Rhizoma Rhei was increased after in vitro metabolism because the antineoplastic activity of aloe-emodin, the metabolite of chrysophanol, is higher than its parent compounds.

Key words: traditional Chinese medicine, chromatographic fingerprints, liver homogenate , metabolism in vitro, Radix et Rrhizoma Rhei, SD rat, high performance liquid chromatography-mass spectrometry