Antibacterial polypeptide and application thereof in pharmacy

By replacing amino acids in the template peptide raniseptinPL to form a staple peptide, the problem of its resistance to enterococci was solved, and the antibacterial performance against a variety of bacteria, especially enterococci, was significantly improved, achieving more efficient antibacterial activity.

CN122255241APending Publication Date: 2026-06-23SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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Patent Information

Application Number
CN202610404926.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-01-29
Publication Date
2026-06-23

AI Technical Summary

Technical Problem

The problem of resistance to Enterococcus by existing antimicrobial peptides such as raniseptin PL has not been effectively solved, and they are easily hydrolyzed by enzymes, resulting in limited antimicrobial activity, which hinders their development into new antibiotics.

Method used

By replacing amino acid residues in the template peptide raniseptinPL, and using Rink amide MBHA amino resin as a solid support, the original amino acids were replaced with S5 and R8 at positions i, i+4 and i, i+7, respectively, to form a stapling peptide, which improves conformational stability and anti-drug-resistant bacterial activity.

Benefits of technology

It significantly improved the antibacterial properties of staple peptides against a variety of bacteria, especially against enterococci. The antibacterial properties of some staple peptides against enterococci were increased by 3-31 times, and the antibacterial effects against Staphylococcus aureus, Enterococcus faecium and Enterococcus faecalis were enhanced.

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Abstract

The invention belongs to the field of polypeptide drugs, and particularly relates to an antibacterial polypeptide and application thereof in pharmacy. According to the invention, Rink amide MBHA amino resin is used as a solid phase carrier, modification and transformation are carried out according to an amino acid sequence of a template polypeptide ranseptinPL: Ac-GVFDTVKKIGKAVGKFALGVAKNYLNS-NH2, amino acid residues 19G and 26N are replaced by R8 and S5, and a target stapled peptide PL-16 is obtained. Compared with a template polypeptide PL-0, the obtained stapled peptide PL-16 has the advantage that the antibacterial activity on staphylococcus aureus, enterococcus faecium, enterococcus faecalis and staphylococcus epidermidis can be obviously improved.
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