The invention belongs to the technical field of biological medicines, and provides a
ciprofloxacin derivative as well as a preparation method and application thereof. The
ciprofloxacin derivative provided by the invention has a structure as shown in a formula I, an electrostatic effect sequence (
amino acid part) with positive charges is connected to a lipid part, and then a series of amphiphilic
ciprofloxacin derivatives are formed through conjugation of
Linker and ciprofloxacin. The electrostatic effect sequence with positive charges can enhance the interaction with a bacterial
cell membrane with negative charges through
electrostatic interaction, then the lipid part can be inserted into a
phospholipid bilayer of the bacterial
cell membrane, so that the integrity of the bacterial
cell membrane is damaged, the ciprofloxacin derivative enters the cell, and the ciprofloxacin derivative is degraded. Finally, bacterial cell content leakage, bacterial
chromosome breakage and bacterial cell death are caused. According to the amphiphilic ciprofloxacin derivative disclosed by the invention, the amphiphilic structure and the membrane destruction mechanism of the
antibacterial peptide are simulated, so that the ciprofloxacin derivative shows the unique
advantage that the
drug resistance is not easy to generate. # imgabs0 #