Related Experiment Video
Updated: Oct 2, 2025
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and Biological Evaluation of Novel Cinnamic Acid-Based Antimicrobials
Marina Mingoia1, Carmela Conte2, Annalisa Di Rienzo3
1Department of Biomedical Sciences and Public Health, Medical School, Polytechnic University of Marche, 60121 Ancona, Italy.
Abstract:
The main antimicrobial resistance (AMR) nosocomial strains (ESKAPE pathogens such as Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) are the most widespread bacteria in cutaneous infections. In this work we report the synthesis, in silico skin permeability prediction, antimicrobial, antibiofilm, and wound healing properties of novel cinnamic acid-based antimicrobials (DM1-11) as novel antibacterial drugs for the treatment of ESKAPE-related skin infections. Antimicrobial and wound healing scratch assays were performed to evaluate the antibacterial properties of DM1-11. In silico skin permeability capabilities of DM1-11 were evaluated using Swiss-ADME online database. Cytotoxicity assays were performed on keratinocytes and fibroblasts. DM2, bearing a catechol group on the aromatic ring of the cinnamic portion of the molecule, possesses a significant antibacterial activity against S. aureus (MIC range 16-64 mg/L) and contrasts the biofilm-mediated S. epidermidis infection at low concentrations. Wound healing assays showed that wound closure in 48 h was observed in DM2-treated keratinocytes with a better healing pattern at all the used concentrations (0.1, 1.0, and 10 µM). A potential good skin permeation for DM2, that could guarantee its effectiveness at the target site, was also observed. Cytotoxicity studies revealed that DM2 may be a safe compound for topical use. Taking together all these data confirm that DM2 could represent a safe wound-healing topical agent for the treatment of skin wound infections caused by two of main Gram-positive bacteria belonging to ESKAPE microorganisms.
Insights
Researchers developed novel cinnamic acid-based antimicrobials (DM1-11) to combat ESKAPE pathogens in skin infections. Compound DM2 demonstrated significant antibacterial, antibiofilm, and wound healing properties, showing potential as a safe topical treatment for Gram-positive bacterial skin infections.
Area of Science:
- Medicinal Chemistry
- Microbiology
- Dermatology
Background:
- Antimicrobial resistance (AMR) is a growing threat, with ESKAPE pathogens causing widespread nosocomial infections.
- Cutaneous infections frequently involve ESKAPE pathogens, necessitating novel therapeutic strategies.
- Current treatments face challenges due to rising AMR, driving the search for new antimicrobial agents.
Purpose of the Study:
- To synthesize and evaluate novel cinnamic acid-based compounds (DM1-11) for treating ESKAPE pathogen-related skin infections.
- To assess the antimicrobial, antibiofilm, and wound healing properties of these compounds.
- To predict skin permeability and evaluate cytotoxicity for potential topical application.
Main Methods:
- Synthesis of novel cinnamic acid derivatives (DM1-11).
- In silico skin permeability prediction using Swiss-ADME.
- Antimicrobial assays (MIC), antibiofilm assays, and wound healing scratch assays.
- Cytotoxicity assays on keratinocytes and fibroblasts.
Main Results:
- Compound DM2 exhibited significant antibacterial activity against Staphylococcus aureus (MIC 16-64 mg/L) and inhibited Staphylococcus epidermidis biofilms.
- DM2 demonstrated effective wound healing in keratinocytes across tested concentrations (0.1-10 µM) within 48 hours.
- In silico analysis suggested good skin permeation for DM2, and cytotoxicity studies indicated its safety for topical use.
Conclusions:
- DM2, a cinnamic acid derivative, shows promising antibacterial and wound healing potential against Gram-positive ESKAPE bacteria.
- Its favorable in silico skin permeability and low cytotoxicity suggest suitability as a topical agent for skin wound infections.
- DM2 represents a potential new therapeutic option for managing skin infections caused by specific ESKAPE microorganisms.
More Related Videos
08:20Systematic Approach to Identify Novel Antimicrobial and Antibiofilm Molecules from Plants' Extracts and Fractions to Prevent Dental Caries
Published on: March 31, 2021
09:39A Platform of Anti-biofilm Assays Suited to the Exploration of Natural Compound Libraries
Published on: December 27, 2016
