高等学校化学学报 ›› 2001, Vol. 22 ›› Issue (9): 1446.

• 研究论文 • 上一篇    下一篇

水溶性卟啉及其系列金属化合物的合成、抗癌活性及其作用机制研究

刘杰1, 许东晖2, 梅文杰1, 蒲含林2, 黄锦汪1, 计亮年1   

  1. 1. 超快速激光光谱国家重点实验室, 中山大学化学化工学院;
    2. 中山大学药学院药物药理研究室, 广州 510275
  • 收稿日期:2000-07-13 出版日期:2001-09-24 发布日期:2001-09-24
  • 通讯作者: 计亮年(1934年出生),男,教授,博士生导师,从事生物无机化学研究.
  • 基金资助:

    广东省博士后基金(批准号:021424435)资助

Synthesis, Anticancer Activity and Mechanism of Water-soluble Porphyrin and Metalloporphyins

LIU Jie1, XU Dong-Hui2, MEI Wen-Jie1, PU Han-Lin2, HUANG Jin-Wang1, JI Liang-Nian1   

  1. 1. State Key Laboratory of Ultrafast Laser Spectroscopy, Department of Chemistry;
    2. Department of Pharmacy, Zhongshan University, Guangzhou 510275, China
  • Received:2000-07-13 Online:2001-09-24 Published:2001-09-24

摘要: 合成了水溶性四-[(4-三甲铵基)苯基]卟啉TAPP及其金属卟啉化合物MTAPP,其中M=Zn(),Cu(),Fe(),Co(),Ni(),Mn().通过元素分析、紫外-可见光谱确定了化合物的组成和结构.以紫外-可见光谱、荧光光谱及粘度法等手段研究了卟啉化合物TAPP和金属卟啉化合物ZnTAPP与小牛胸腺DNA的相互作用,结果表明,TAPP,ZnTAPP与DNA相互作用使紫外-可见光谱发生了8~12nm的红移,并出现了明显的减色效应.荧光光谱强度明显增大,吸收峰位发生变化.以艾氏腹水癌(Ac)和肝癌(Hept)细胞为靶细胞,采用MTT染色法评价了化合物的抗癌活性,部分化合物表现出较高的抗癌活性

关键词: 水溶性卟啉, DNA反应, 抗癌活性, 作用机制

Abstract: A water-soluble porphyrin tetrakis[4-(trimethylammoniumly)phenyl]porpyrin (TAPP) and its metalloporphyrin derivatives MTAPP with M=Zn(Ê),Cu(Ê),Fe(Ë),Co(Ë),Ni(Ê),Mn(Ë), containing various functional groups within the porphyrin have been synthesized and characterized by elemental analysis, and UV-Vis spectra. Binding of TAPP and Zn-TAPP with calf thymus DNAwas investigated by absorption spectra, fluorescence spectra and viscosity measurements. Addition of CT DNAresulted in obvious hypochromism and bathochromic of 12 nm in absorption spectra, and an enhancement in fluorescence spectra were also observed. The anticancer activities of these complexes were also tested by MTTon two mice tumor cells of Ac and Hept, the results indicated that Co(Ë)-TAPPshowed a high inhibitory action and high anticancer activity in cell.

Key words: Water soluble porphyrins, Calf thymus DNA, Anticancer activity, Function mechanism

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