Professor Xia Xuefeng and Associate Professor Zhang Jinqiang of the Pharmacological Research Team of the School of Pharmaceutical Sciences, Chongqing University, published a research paper titled “Novel Stapling by Lysine Tethering Provides Stable and Low Hemolytic Cationic Antimicrobial Peptides” in Journal of Medicinal Chemistry (2020, 63, 8, 4081–4089), a top international journal on medicinal chemistry in April 2020, with Chongqing University as the only corresponding organization. Journal of Medicinal Chemistry is run by American Chemical Society and covers the latest original research findings in the area of medicinal chemistry. It is one of the most influential journals on medicinal chemistry in the world and its factor of influence now stands at 6.189. This paper is the first one published by Chongqing University in the journal and marks the progress made by School of Pharmaceutical Sciences in the area.
This paper introduces the design, synthesis and application of a novel type of cationic bridging antimicrobial peptide analogues. It is the first time in the world to bridge the hydrophilic surface of amphiphilic cationic antimicrobial peptides. It was found that this novel type of antimicrobial peptide had high protease stability, excellent broad-spectrum antibacterial activity, low hemolytic toxicity and promising application in clinical field. In this paper, the design, synthesis and antibacterial activity screening of the novel cationic bridging antimicrobial peptide were described in detail, and the antibacterial mechanism of the novel cationic bridging stapling peptide was explained in terms of the bactericidal kinetics and the change of bacterial cell membrane after administration. This study is of great scientific significance to overcome the challenge of bacterial multidrug resistance in clinical treatment and promote the research and development of new antibiotics based on antimicrobial peptides. At the same time, this novel type of cationic antimicrobial peptides also has broad clinical application prospects.