应用化学 ›› 2019, Vol. 36 ›› Issue (12): 1376-1386.DOI: 10.11944/j.issn.1000-0518.2019.12.190066

• 研究论文 • 上一篇    下一篇

咔咯铁(Ⅲ)配合物与DNA的作用及其抗肿瘤活性

史蕾a*(),杨文聪a,沈淇a,尹伟a,霍朝晖a,司利平b,刘海洋c   

  1. a广东第二师范学院化学系 广州 510303
    b佛山科学技术学院材料科学与能源工程学院 广东 佛山 528000
    c华南理工大学化学与化工学院 广州 510640
  • 收稿日期:2019-03-14 接受日期:2019-06-25 出版日期:2019-12-01 发布日期:2019-12-10
  • 通讯作者: 史蕾
  • 基金资助:
    广东省高等教育教学改革项目(2018),佛山科学技术学院材料科学与能源工程学院科技开放基金项目(2018),广东大学生攀登计划专项资金,大学生创新创业训练计划项目,广东第二师范学院教学质量与教学改革工程项目(2018), 广东省教育厅“创新强校工程”青年创新人才类项目;(2016KQNCX112)资助

Iron Corrole Complexes: DNA-Binding and Anti-tumor Activity

SHI Leia*(),YANG Wenconga,SHEN Qia,YIN Weia,HUO Zhaohuia,SI Lipingb,LIU Haiyangc   

  1. aDepartment of Chemistry,Guangdong University of Education,Guangzhou 510303,China
    bSchool of Materials Science and Energy Engineering,Foshan University,Guangdong Foshan 528000,China
    cKey Laboratory of Functional Molecular Engineering of Guangdong Province,South China University of Technology,Guangzhou 510640,China
  • Received:2019-03-14 Accepted:2019-06-25 Published:2019-12-01 Online:2019-12-10
  • Contact: SHI Lei
  • Supported by:
    Supported by the Higher Education Teaching Reform Project in Guangdong Province(2018), the Open Fund Project of Foshan University(2018), the Special Funds for Guangdong University Students' Climbing Plan, College Students Innovation and Entrepreneurship Training Program, the Teaching Quality and Teaching Reform in Guangdong Second Normal University(2018), and the Innovation and Strong School Funding from Guangdong University of Education-Foundation for Distinguished Young Talents in Higher Education of Guangdong(No.2016KQNCX112)

摘要:

本文合成了10-(4-吩噻嗪苯基)-5,15-二(五氟苯基)铁咔咯配合物(2-Fe)。 在H2O2存在下,配合物2-Fe能有效抑制人肺癌细胞(A549)增殖。 流式细胞术检测结果显示在H2O2和2-Fe共同作用下,A549细胞生长被阻滞在S期和G2期,且有63.76%发生细胞凋亡。 Hoechst-33342细胞核染色实验观察到A549细胞核呈典型的凋亡形态学变化,同时细胞线粒体膜电势发生明显下降。 2-Fe与小牛胸腺DNA(ct-DNA)以外部模式相结合,且能有效催化氧化断裂DNA,此过程中涉及的活性氧物种可能是单线态氧。

关键词: 咔咯, 吩噻嗪, DNA, 细胞毒性, 铁, 细胞凋亡

Abstract:

10-(4-Phenothiazine)-5,15-bis(pentafluorophenyl)corrolatoiron (2-Fe) was synthesized. Complex 2-Fe displays high cytotoxic activity against human lung adenocarcinoma (A549) cell lines. Flow cytometry detected 2-Fe arrested the cell cycle in the S and G2 phase in the presence of H2O2 and apoptotic rate was 63.76%. Hoechst-33342 staining showed considerable morphological changes in nuclear chromatin and mitochondrial transmembrane potential dropped respectively. Complex 2-Fe could interact with DNA via an outside binding mode and trigger 1O2 generation.

Key words: corrole, phenothiazine, DNA, cytotoxicity, iron, apoptosis