Cholic-Acid Derived, Guanidine-Functionalized Polymers as Broad-Spectrum Antimicrobial Agents

Area of Science:

• Biomaterials Science
• Polymer Chemistry
• Antimicrobial Research

Background:

• Antimicrobial resistance is a growing global health threat.
• Cholic acid's amphiphilicity and guanidine's phosphate affinity are key for antimicrobial action.
• Developing novel antimicrobial agents is crucial.

Purpose of the Study:

• To design and synthesize a new guanylated, cholic-acid-based monomer (GM).
• To investigate the antimicrobial activity of GM monomers, homopolymers, and copolymers.
• To explore structure-activity relationships for antimicrobial material development.

Main Methods:

• Synthesis of a guanylated, cholic-acid-based monomer (GM).
• Photoiniferter reversible addition-fragmentation chain-transfer (RAFT) polymerization for homopolymer and copolymer synthesis.
• Antimicrobial activity assays and hemolysis testing.

Main Results:

• The GM monomer exhibited significant antimicrobial activity.
• GM homopolymers lost antimicrobial activity, attributed to polymer conformation.
• GM copolymers with PEGMA or HEMA restored antimicrobial efficacy.
• Hemolysis was dependent on GM content due to cholesterol interactions.

Conclusions:

• Novel amphiphilic GM monomer shows promise for antimicrobial applications.
• Polymer architecture significantly impacts the antimicrobial activity of GM-based materials.
• GM copolymers offer a viable strategy for developing potent antimicrobial materials.