Bacterial drug resistance is becoming
increasingly serious, and
it is urgent to develop effective antibacterial drugs. Antimicrobial
peptides (AMPs), as potential candidates against bacteria, have a
broad prospect for development. Herein, a series of AMPs with biological
characteristics (net positive charge, amphiphilicity, and α-helix),
an AXA motif recognized by membrane bound serine protease type I signal
peptidases (SPase I), an FLPII motif to reduce hemolysis, and a monosaccharide
motif to improve the stability and activity were designed and synthesized,
and among which, the glycolipidpeptide GLP6 (glycosylated LP6 lipopeptide)
had excellent antibacterial and immunomodulatory activity, good stability
and biocompatibility, and excellent biofilm eradication and membrane
penetrating activity. The positively charged spherical aggregates
formed by self-assembly of GLP6 could encapsulate tetracycline (TC)
to form GLP6@TC with a sustained-release effect, which could enhance
the sensitivity of bacteria to the antibiotic and realize combined
sterilization. The results of acute peritonitis and bacterial keratitis
showed that GLP6@TC had a good combined antibacterial effect and the
ability to inhibit interleukin-2 (IL-2), which could significantly
reduce the inflammatory response while treating bacterial infection,
and it had great potential for application. The results of computer
molecular docking showed the AXA motif could effectively bind to SPase
I, which was consistent with the results of biological experiments.
In general, the study could provide a perspective for the design of
AMPs and combined antibacterial therapy.
It is urgent to develop new antimicrobial drugs to overcome bacterial resistance which is a serious threat to human health. Antimicrobial peptides (AMPs) which are ideal substitutes for traditional antibiotics...
Herein, an amphiphilic cationic α-helical anticancer lipopeptide P10 with the low toxicity and high penetrating membrane activity was developed. The lipopeptide could self-assemble into stable spherical aggregates in aqueous solution,...
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