Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (1): 148-155.DOI: 10.6023/cjoc201708042 Previous Articles     Next Articles

Special Issue: 庆祝吴养洁院士九十华诞专辑


基于Tat (49-57)抗菌肽的设计、合成与性质研究

吕名秀a,b, 买文鹏b, 卢奎b,c, 段冰潮a, 赵玉芬a   

  1. a 郑州大学化学与分子工程学院 郑州 450001;
    b 河南工程学院材料与化学工程学院 郑州 450007;
    c 郑州工程技术学院化工食品学院 郑州 450044
  • 收稿日期:2017-08-21 修回日期:2017-10-23 发布日期:2017-10-31
  • 通讯作者: 卢奎, 赵玉芬;
  • 基金资助:


Design, Synthesis and Properties of the Antibacterial Peptides Based on Tat(49-57)

Lü Mingxiua,b, Mai Wenpengb, Lu Kuib,c, Duan Bingchaoa, Zhao Yufena   

  1. a College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001;
    b School of Material and Chemical Engineering, Henan University of Engineering, Zhengzhou 450007;
    c School of Chemical Engineering and Food Science, Zhengzhou Institute of Technology, Zhengzhou 450044
  • Received:2017-08-21 Revised:2017-10-23 Published:2017-10-31
  • Contact: 10.6023/cjoc201708042;
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21572046, 21172054).

Four novel cationic antibacterial peptide analogs were modified at the N-terminus of the cell-penetrating peptide transacting activator of transcription TAT(49-57) by attaching dipeptides. Peptides were synthesized through standard Fmoc solid-phase peptide synthesis procedures, purified by reversed-phase high performance liquid chromatography (RP-HPLC), and characterized by 1H NMR, ESI-MS and elemental analysis. Tat(YY), Tat(FF), Tat(FF) and Tat(YY), Tat(FF) demonstrated better antibacterial activities against E. coli, S. typhimurium, B. subtilis and S. aureus with low hemolysis. respectively, but had no inhibitory effect on fungus growth. The Tat(49-57) analogs inhibited the bacteria more effectively than Tat(49-57). The interactions between peptides and calf thymus DNA (ct-DNA) were investigated with multi-spectroscopic techniques. The results showed that both peptides could interact with DNA via the groove binding mode. Compared to TAT(49-57), antibacterial peptide analogs combined with DNA much closer via binding constants, which has the value to become an excellent antibacterial agent with further improved and designed.

Key words: cell-penetrating peptide, solid-phase synthesis, antibacterial activity, non-covalent binding