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| 远志活性成分优呫吨酮铜（Ⅱ）配合物的抗肿瘤活性研究 |
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宋路路1, 于俏1, 齐学洁1, 杨爱红1, 张昕阳2, 申蕊1, 寇晓娣1, 赵利花2
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1.天津中医药大学中药学院, 天津 301617;2.天津大学仁爱学院化工系, 天津 301636
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| 摘要: |
| [目的] 研究优呫吨酮铜（Ⅱ）配合物的细胞毒性以及与DNA的相互作用。[方法] 利用噻唑蓝（MTT）法研究优呫吨酮铜（Ⅱ）配合物对食管鳞癌细胞（ECA109）、胃癌细胞（SGC7901）和宫颈癌细胞（Hela）的体外抑制活性；利用荧光光谱法、紫外光谱法和圆二色谱法研究铜（Ⅱ）配合物与小牛胸腺DNA的相互作用。[结果] 优呫吨酮铜（Ⅱ）配合物对ECA109、SGC-7901和Hela细胞的抑制活性明显高于优呫吨酮，并且与DNA发生插入作用。[结论] 优呫吨酮铜（Ⅱ）配合物以插入方式与DNA结合，可能引起肿瘤细胞的DNA损伤，进而抑制细胞生长。 |
| 关键词: 优呫吨酮 中药配位化学 细胞毒性 DNA结合 |
| DOI：10.11656/j.issn.1672-1519.2019.07.19 |
| 分类号: |
| 基金项目:天津市应用基础与前沿技术研究计划一般项目（16JCYBJC28000）；天津市大学生创新训练计划项目（201814038009）。 |
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| Antitumor activity of Cu(Ⅱ) complex with bioactive constituent Euxanthone from polygala |
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SONG Lulu1, YU Qiao1, QI Xuejie1, YANG Aihong1, ZHANG Xinyang2, SHEN Rui1, KOU Xiaodi1, ZHAO Lihua2
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1.School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China;2.Department of Chemical Engineering, Tianjin University Renai College, Tianjin 301636, China
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| Abstract: |
| [Objective] To study of cytotoxic activity and DNA-binding properties of Euxanthone Cu(Ⅱ) complex. [Methods] Three tumor cell lines including esophagus cancer (ECA109),stomach cancer (SGC7901) and cervical cancer (Hela) are used to evaluate the cytotoxic activities of Euxanthone Cu(Ⅱ) complex by MTT. The interactions of Euxanthone Cu(Ⅱ) complex with calf thymus DNA are investigated by fluorescence emission,ultraviolet absorption and circular dichroic spectra. [Results] Euxanthone Cu(Ⅱ) complex exhibits more effective inhibition activity against three cancer cells than Euxanthone and can intercalate into the DNA base pairs. [Conclusion] Euxanthone Cu(Ⅱ) complex could intercalate between DNA base pairs and cause DNA damage in cancer cells,thus inhibiting the division of cancer cells. |
| Key words: euxanthone coordination chemistry of traditional Chinese medicine cytotoxicity DNA binding |
